Synthesis and Biological Studies of 4-(4-chloro-1-hydroxynaphthalen-2-YL)-6- aryl-5,6-dihydropyrimidin-2(1H)-one

V.M.Sherekar; S.E.Bhandarkar; Mrinmoy Basak; Biplab Kr. Dey; Somayeh Afsah Vakili; Ajay George; Syed Fayazuddin; Nandkishor Chandan; Daniel Attard; Claire Shoemake; John Vella; Paweł Żmudzki; Grażyna Chłoń-Rzepa; Elżbieta Wyska; S. Jyothi Sri; D.V.R.N.Bhikshapathi; Ghulam Mohammad Jan; Shakeel Ahmad Khanday1 Samina Akthar; Bhavsar Ankita; Bhavsar Ayushi; A.Thirupathaiah; R. Shyam Sunder; Sonaa Elango; Usha Subbiah; Shahnaz Usman1 ⃰; khawla Al Awad; Muaadh Al Saeedi; Hamam Al Naemi; Huma Zaidi; Mohammad Idrees*1 Roshan D. Nasare; Naqui J. Siddiqui; V. Abhishiktha; M. Sudhakar; Vinay Umesh Rao; Prajapati PR; Desai N; Modi VS; Tarasankar Basuri; M. O. Malpani; P. R. Rajput; P. S. Pande; M. M. Sapkal; Md Aklakur; N. P. Sahu; S. Dasgupta; M.M. Gatne2 and A. K. Pal; Nandhakumar Loganathan; Mohan Sellappan; Shakeel Ahmad Khanday; Samina Akthar2 M.Y.Peerzada; Abhishek Pathak; Sadhana J Rajput; Abhimanyu Sharma1* and Amla Batra

📢 Latest Update: New special issue call for papers on "Emerging Technologies in Research" - Submit by March 31, 2025

October 2016 Issue 5

Volume 6, Issue 5 - $2016

Issue Details:

Volume 6 Issue 5

Published:Invalid Date

Editorial: October 2016 Issue 5

Welcome to the 2016 issue of American Journal of PharmTech Research. This issue showcases the remarkable breadth and depth of contemporary research across multiple disciplines. From cutting-edge applications of machine learning in climate science to the revolutionary potential of quantum computing in drug discovery, our featured articles demonstrate the power of interdisciplinary collaboration in addressing global challenges.

We are particularly excited to present research that bridges traditional academic boundaries, reflecting our journal's commitment to fostering innovation through cross-disciplinary dialogue. The integration of artificial intelligence with environmental science, the application of blockchain technology to supply chain management, and the convergence of urban planning with smart city technologies exemplify the transformative potential of collaborative research.

As we continue to navigate an era of rapid technological advancement and global challenges, the research presented in this issue offers both insights and solutions that will shape our future. We thank our authors, reviewers, and editorial board members for their continued dedication to advancing knowledge and promoting scientific excellence.

Dr Hemangi J Patel
Editor-in-Chief
American Journal of PharmTech Research

Articles in This Issue

Showing 67 of 67 articles

Research PaperID: AJPTR65001

Approaches of Nanomedicine in Cancer Therapy

Kola Prasanna Yadav, Bojedla Naveena, Nemarugommula Prunvitha, Thirungiri Praveenkumar

Cancer is the leading cause of mortality worldwide. Treating the cancer is one of the major challenges in modern science as the drug delivery to solid tumors is a seminal challenge to develop more effective cancer therapies. A well-designed drug delivery system can potentially enhance the efficacy of a treatment by improving drug accumulation in the tumor. Application of nanotechnology to prevent and treat the cancer disease is known as nanomedicine. Cancer diagnosis and treatment can be achieved to a greater extent by the application of nanotechnology principles to biomedicine. Over these years targeted treatment for cancer has been greatly improved by the approaches based on nanotechnology. Nanoparticles have the potential to increase the specificity in treating cancer cells while leaving the healthy cells. The goal of this review is to discuss the current state of nanomedicine in the field of cancer detection and the subsequent application of nanotechnology to treat cancer by using nanoparticles such as dendrimers, quantum dots, nanocells, nanocrystals, and nanoshells for the detection and treatment of cancer.

CancerDrug deliveryQuantum dotsNanomedicineNanotechnologyDrug Therapy.

232,369 views

69,774 downloads

Contributors:

Kola Prasanna Yadav

Bojedla Naveena

Nemarugommula Prunvitha

Thirungiri Praveenkumar

Research PaperID: AJPTR65002

Zika Virus Disease-Epidemiology, Diagnosis, Prevention and Treatments

CM Jamkhandi, Kambli MR, Hirave PA, JI Disouza

Zika virus is a member of the Flavivirus family which was discovered in Uganda in 1947. Zika virus was widely spread in areas of Africa & Asia in 2007. The first Zika virus infection is confirmed in Brazil. This virus transmitted via infected mosquito belonging to Aedes mainly of type Aedes aegypti. It may be suspected from symptoms of the patient but detection of Zika virus disease can only be done by laboratory testing for presence of Zika virus RNA in the blood or other body fluids such as urine or saliva. This disease shows symptoms like Yellow fever, joint pain, and headache & skin rashes. ZVD (Zika Virus Disease) is usually mild but don’t have specific treatment. The ZVD patient should take rest, drink enough fluid & treat pain & fever with common medicines. As there is no vaccine on this disease the person should take prevention to stay away from ZVD.

Zika Virus DiseaseEndemicEpidemicFlavivirusMicrocephaly.

232,750 views

69,786 downloads

Contributors:

CM Jamkhandi

Kambli MR

Hirave PA

JI Disouza

Research PaperID: AJPTR65003

Comparative evaluation of postoperative pain with different intracanal medicaments – A Systematic Review

Sanu N, Sindhu Ramesh

Patients as well as clinicians have been apprehensive of pain of endodontic origin for many years1. Pain during root canal treatment can be attributed to inflammation in the periapical tissues due to exudation of irritants from the root canal2. The persistence of microorganism due to improper disinfection of root canal is the most important cause of pain 1. The eradication of microorganism from the root canals is therefore vital during root canal treatment . Thus, an antimicrobial dressing in root canals is advocated after root canal preparation 1. To evaluate the effectiveness of different intra canal medication in reducing the post operative pain in nonsurgical root canal treatment. The following databases were searched: PubMed CENTRAL, MEDLINE and Cochrane Databases of Systemic Reviews, Bibliographies of Clinical Studies and Reviews identified in the electronic search were analysed for studies published outside the electronically searched journals. Trials were selected if they met the following criteria: Clinical trials or in-vivo studies that evaluated the post operative pain after using different intracanal medicament in patients undergoing root canal treatment. All the studies included, were based on the data extraction and analysis of the studies for quality and publication bias. The primary outcome measure was to evaluate the reduction in post operative pain after using different intra canal medicaments in patients undergoing root canal treatment. The reviews some clinical evidence that use of intra canal medicaments can reduce postoperative pain. There is no enough evidence to prove that calcium hydroxide is effective in reduction of pain. Corticosteroids antibiotic combination and calcium hydroxide combination with chlorhexidine and camphorated paramonochlorophenol were effective in reducing pain. From this systematic review it can be concluded that, certain intra canal medicaments can be used to reduce postoperative pain during root canal treatment. Most of the studies proved that, corticosteroid antibiotic solution or combination of calcium hydroxide with other medicine like camphorated paramonochlorophenol or chlorhexidine is effective in reducing post operative pain. There is no evidence that, use of calcium hydroxide is effective in relieving pain. Further clinical trials are required to evaluate the efficacy of intra canal medicaments in reducing postoperative pain.

Post operative paincalcium hydroxideintracanal medicamentantimicrobial

232,929 views

69,887 downloads

Contributors:

Sanu N

Sindhu Ramesh

Research PaperID: AJPTR65004

Catalytic Oxidation of Schiff Base metal Complexes: A Review

Ab. Rashid Wani, Haroon Rashid Boked, Ghulam Mohammad Jan, Mukhtar Ahmad Wani, Nazir Ahmad Wani

Catalysis is an area of research which still continues to be a premier area of chemistry. It plays a key role in modern chemical technology. There are a large number of important organic transformations such as oxidation, hydrogenation, hydroformylation, carbonylation, polymerization and various coupling reactions. The majority of these novel catalysts are based on silica, primarily since silica displays many advantageous properties excellent stability (chemical and thermal), high surface area, good accessibility, and organic groups can be robustly anchored to the surface, to provide catalytic centers. However, it does have drawbacks it has limited stability in aqueous especially basic conditions, and it cannot easily be formed into membranes or into other forms which could be attached to novel reactors for use in intensive processing applications.

Schiff baseOxidationCatalysisPolymerizationSynthesis.

232,715 views

69,797 downloads

Contributors:

Ab. Rashid Wani

Haroon Rashid Boked

Ghulam Mohammad Jan

Mukhtar Ahmad Wani

Nazir Ahmad Wani

Research PaperID: AJPTR65005

Prickly Amaranth (Amaranthus spinosus Linn.): a Review on Phytochemistry and Pharmacological Activities

Sangita Boro, Bhriganka Bharadwaj, B.G. Unni

This paper reviews the traditional, clinical potential, ethnopharmacology, phytoconstituent studies and safety profile of Prickly Amaranth (Amaranthus spinosus Linn.) with a view to explore the potentiality of the plant and proclaim it to the nature product researchers throughout the world. Phytochemical investigations prove its importance as valuable medicinal plant. It is known as a rich source of alkaloids, flavonoids, glycosides, phenolic acids, steroids, amino acids, terpenoids, lipids, saponin, betalain, b-sitosterol, stigmasterol, linoleic acid, rutin, catechuic tannins and carotenoids. Various researchers have carried out wide spectrum studies on its pharmacological actions and preliminary work has been reported on antidiabetic, antitumour, analgesic, antimicrobial, anti-inflammatory, spasmolytic, bronchodilator, hepato-protective, antifertility, antimalarial, antioxidant properties etc. Hence Prickly Amaranth holds a great potential for in depth biological evaluation.

Prickly AmaranthAmaranthus spinosusTraditional medicinePhytochemistryPharmacological activitiesEthnopharmacology+1 more

232,953 views

69,970 downloads

Contributors:

Sangita Boro

Bhriganka Bharadwaj

B.G. Unni

Research PaperID: AJPTR65006

GC-MS Study and Pharmacognostic Study of Pithecellobium Dulce Leaves

Anil F.Bobade

Pithecellobium dulce is a species of flowering plant in the pea family Fabaveae, that is native to the Pacific Coast and adjacent highlands of Maxico, Central Amerca, and northern South America. Pithecellobium dulce. It is used as medicinal plant. An extract of the leaves is used for gall ailments and to prevent miscarriage. The methanolic extract of leaves was obtained by Soxhelt extractor followed by concentration in rotary evaporator. Separation of bioactive chemicals was carried out by column chromatography while studies by GC-MS which shows presence of following bioactive chemicals Phytol, Anthracene, 9(3butenyl), mm Diisooctyl phthalate, 13Docosenamide,, 3,6,9triethyl3,6,9trimethyl Formic acid, Cyclotetrasiloxane, octamethyl, l(+) Ascorbic acid 2,6dihexadecanoate. The leaf extract of Pithecellobium dulce showed good inhibition against gram positive Organisms. The highest inhibition was noted S.epidermidis (24mm), P. acne(14mm) and s. aur(11mm).

GC-MSSoxhletChemical CompositionAntimicrobial.

232,944 views

69,886 downloads

Contributors:

Anil F.Bobade

Research PaperID: AJPTR65007

Synthesis and evaluation of quinolone derivatives as potential antibacterial agents

Mohammad Shoeb, Rahimullah Shaikh

A series of 1-(substituted -2-oxoquinolin-1(2H)-yl) urea and thiourea have been synthesized by using coumarin derivatives and semicarbazide in presence of ethanol as a solvent. Coumarin derivatives were prepared via pechmann condensation by adding a mixture of substituted phenol and ethyl acetoacetate in concentrated sulfuric acid. Coumarin derivatives then subjected to condensation with semicarbazide and thiosemicarbazide. The structure of all these synthesized compounds has been established on the basis of chemical transformation, IR and 1HNMR spectral studies. Synthesized compounds are showing amazing antibacterial activity for common food borne pathogens such as Escherichia coli, Shigella flexneri, Staphylococcus aureus, and Bacillus cereus.

CoumarinQuinoloneOxoquinoloneAnti-bacterial activity.

232,988 views

70,008 downloads

Contributors:

Mohammad Shoeb

Rahimullah Shaikh

Research PaperID: AJPTR65008

The role of FSH, LH, and Prolactin Hormones in Female Infertility

Ali A. Al-Fahham, Hisham Q. Al-Nowainy

Recently, a great attention has been paid to the role of hormones as a diagnostic too in the evaluation of female infertility . The purpose of this study was to identify the association between female infertility and hormonal imbalance (FSH, LH and Prolactin) and what is the relationship between these hormones and the woman's socio- demographic and clinical characteristics. The study was carried out at the Fertility Center in Al-Sadr Medical City, which is located in Najaf province, Iraq, during the period from Dec, 2014 to Apr, 2015. The study involved (44) infertile women who attended the Fertility Center. In accordance to the socio-demographic data, the majority of the studies women were from urban regions (81.18%), while all them were housewives. The clinical history revealed a relatively high percentage (56.82%) of vaginitis, and UTI (50%) among the studies women, while most of them were either overweight (40.91%) or obese (22.73%). The results showed that the majority of studies women had normal hormonal levels according to the standard reference limits for FSH, LH and Prolactin. The study also showed that there was a significant positive correlation between the level of FSH and the age of the studies infertile women. It was concluded that hormonal imbalance for (LH, FSH and prolactin) is just a minor suspected etiologic factor in causing infertility in the studies women the level of FSH increases with age, while the level of prolactin slightly decreases with age. It was recommended to achieve a comprehensive case-control study for evaluating hormonal imbalance of (FSH, LH, prolactin, estrogens, progesterone, thyroid and inhibit) hormones in the infertile women.

FSHLHand Prolactin Hormones

233,190 views

70,119 downloads

Contributors:

Ali A. Al-Fahham

Hisham Q. Al-Nowainy

Research PaperID: AJPTR65009

The Effects Parabens on the Estrogenic Receptors Behavior in Human Breast Adenocarcinoma MCF-7 Cell Line.

Maryam Nakhjavani, Nastaran Nikounezhad, Farshad H. Shirazi

Parabens are a group of preservatives that have vast indications in pharmaceuticals, cosmetics and food industries. Recently, there have been reports about the estrogenic effects of these compounds which raised concerns about the possibility of involvement of parabens in estrogen-responsive cancers. In the current study, the effect of methylparaben (MP) and propylparaben (PP) was assessed on the growth pattern of human breast adenocarcinoma cell line, MCF-7. 17-ß-estradiol (EST) and tamoxifen (TAM) were used as estrogenic and anti-estrogenic compounds. EC50 of EST and IC50 of TAM were calculated to be 1.206 and 7.017 µg/ml, respectively, based on trypan blue dye exclusion assay in a 5-day exposure. Proliferation kinetics of MCF-7 cells in a 10 day exposure to these compounds showed that EST (1.206 µg/ml) could induce cell proliferation, while exposure of MP or PP (at the same dose) did not change the growth curve of MCF-7. TAM, on the other hand could decrease the proliferation rate of MCF-7. This inhibition was more exacerbated when MP and PP were added to the culture media, suggesting a competitive binding of these compounds to receptors. In conclusion, the data propose the probable estrogenic effect of MP and PP with less potency compared to EST and less competitive binding to ERs compared to TAM.

MFC-7MethylparabenPropylparaben17-ß-estradiolTamoxifen

233,631 views

70,075 downloads

Contributors:

Maryam Nakhjavani

Nastaran Nikounezhad

Farshad H. Shirazi

Research PaperID: AJPTR65010

Synthesis, Characterization and Biological Evaluation of New Glycosyl Thiocarbamides Derived from Glycosylamines

Sneha U. Jadhao, Shirish P. Deshmukh

Thiourea and urea are important functional groups in various natural products and drug intermediates. They are used as neutral receptor for various anions (anion complexation) and building blocks for various heterocycles. Sugar-based thioureas are a new class of molecules promising for many biological applications. Here, we have synthesized a new range of 1-β-D-glycosyl-3-aryl thiocarbamides by the interaction of various glycosylamines with aryl isothiocyanates. The structure of title compounds were confirmed by their IR, NMR mass spectral data and elemental analysis. The newly synthesized compounds were screened for their in vitro antimicrobial activities using standard cup plate method against bacteria E. coli, P. aeruginosa, S. aureus and fungi A. niger, T. viride. The title compounds exhibited mild to moderate antimicrobial activities.

1-&#946-D-glycosyl-3-aryl thiocarbamidesglycosylaminesaryl isothiocyanatesdrug intermediates.

233,389 views

70,021 downloads

Contributors:

Sneha U. Jadhao

Shirish P. Deshmukh

Research PaperID: AJPTR65011

Formulation and Evaluation of Lornoxicam Topical Gel

Shereen A. Eladawy, Amal S. M. Abu El-Enin, Soha A. Ismail, Eman R. Mishrif

The aim of this work is to improve the anti-inflammatory activity of Lornoxicam through incorporating it in a topical gel using different polymers as Carbopol 934, Sodium carboxy methylcellulose or Sodium alginate. Various penetration enhancers (Glycerin, Polyethylene glycol or Sorbitol) were used with objective of enhancement in the percutaneous permeation of the drug. Formulations were evaluated for pH, drug content, rheological properties, spreadability, in-vitro drug release in phosphate buffer (pH 6.5) and permeation study through cellulose membrane. Anti-inflammatory activity of Lornoxicam gel was studied in rats by carrageenan induced paw edema method and compared with the commercial formulation (Feldene® gel). Considering physical properties, in-vitro release and in-vitro permeation studies, FS1 (Lornoxicam gel containing 1% Carbopol with 10% Sorbitol as penetration enhancer) was the best formula among the studied formulations, this formula also exhibited significantly higher anti-inflammatory activity in rats compared to Feldene® gel.

LornoxicamTopical gelPenetration enhancersIn-vitro drug diffusion studyAnti-inflammatory activity.

233,535 views

70,162 downloads

Contributors:

Shereen A. Eladawy

Amal S. M. Abu El-Enin

Soha A. Ismail

Eman R. Mishrif

Research PaperID: AJPTR65012

Simultaneous Determination of Triamterene and Hydrochlorothiazide In Human Plasma by Liquid Chromatography-Mass Spectrometry

Dhananjay Sable, Abhas Tiwari, Milind Bagul, Sailendra Goswami

Triamterene is a potassium-sparing diuretic which is commonly used in combination with Hydrochlorothiazide, a thiazide-type diuretic in clinical management of edema and moderate hypertension. In this study, a rapid and sensitive LC–MS/MS method was developed and validated for determination of Triamterene and Hydrochlorothiazide from K3EDTA based Human Plasma. Triamterene D5 and Hydrochlorothiazide 13C6 were used as an Internal Standards for analysis of Plasma Samples. The analytes and internal standards, were extracted by liquid–liquid extraction method using Se Quant®ZIC-HILIC, (5um,200A 150 X 4.6 mm) column with Acetonitrile and 2 mM Ammonium formate containing 0.1% formic acid (80:20 v/v) as the mobile phase. Linearity was assessed from 3.10ng/mL to 229.72 ng/mL for Triamterene and 5.47 ng/mL to 405.27 ng/mL for Hydrochlorothiazide in plasma. No significant matrix effects were observed by analysing the plasma samples on LC–MS/MS. The accuracy was in the range of 98.32 % to 102.86 % for both compounds. Triamterene and Hydrochlorothiazide were found to be stable up to 120 days in K3EDTA based Human Plasma at -20ºC. The stability of Triamterene and Hydrochlorothiazide in plasma was confirmed up to five freeze-thaw cycles (−20°C) and on bench up to 25 hours. The proposed bioanalytical method for the quantitation of Triamterene and Hydrochlorothiazide from K3EDTA based human plasma samples was satisfactorily validated. It can be used to include study data for quantitation of Triamterene and Hydrochlorothiazide from K3EDTA based human plasma in bioequivalence and bioavailability study.

TriamtereneHydrochlorothiazideEdemaHypertensionLiquid ChromatographyMass Spectroscopy

233,995 views

70,088 downloads

Contributors:

Dhananjay Sable

Abhas Tiwari

Milind Bagul

Sailendra Goswami

Research PaperID: AJPTR65013

Comparative Study of Antihypertensive Drugs At Tertiary Care Hospital

R.Sivasakthi, W.D.Sam Solomon, Nousheen shafi, Mohammed Aslam1. Nithiyan.P

Hypertension is the most important risk factor for cardio vascular disease. But, the key question remains: which of the many available types of blood pressure lowering drugs is the better choice as first line medication. Hence, the prospective, randomized, single blind , Comparative study was conducted at tertiary care Hospital to assess the beneficial outcomes of drugs by comparative method. The study concludes that the physicians were prescribed the ACEIs for hypertension with various co morbidities as per JNC-7 guidelines. The study conclude that the A+E+N is the most effective combination therapy for better control of hypertension. The study indicates that the combination therapy can be individualized according to the presence of co morbidities with HTN.

HypertensionComparative studyco morbiditiescombination therapy.

234,092 views

70,177 downloads

Contributors:

R.Sivasakthi

W.D.Sam Solomon

Nousheen shafi

Mohammed Aslam1. Nithiyan.P

Research PaperID: AJPTR65014

Lifesaving effect of lidocaine on Odontobuthos Doriae scorpion envenomation in mice.

Maryam Nakhjavani, Hossein Vatanpour, Fatemeh Shahriari, Baharak Mohamadzadehasl

Odontobuthos doriae, a native scorpion in southern tropical parts of Iran, can cause serious health threats and wide ranges of pharmacological disturbances. α-toxins in its venom cause prolongation of Na+ channels activity. In this study, reversing effects of lidocaine, as a Na+-channel blocker, was studied on mice following exposure to venom. Lidocaine (up to 500 mg/kg) and O. doriae crude venom (up to 12 µg/mice) was used in a 14-day acute toxicity test, to yield LD50s of 110mg/kg and 10µg/mice, respectively. Afterward, different sub-acute amounts of lidocaine (25%, 50% and 80% of LD50) were used in the presence of venom (80%, 100% and 120% of LD50). Our results show 80% LD50 of lidocaine, and not higher concentrations, could cause 50% reduction in lethality rate induced by O. doriae venom at LD50 concentration, showing the Na+-channel function in this event. Reducing the amount of lidocaine to safer doses show no significant effect in this aspect. Finally, lidocaine (80% LD50) can partially decrease the O. doriae venom mortality. However, due to some other systemic dangerous lidocaine adverse effects, it is doubtful that it can be a relevant life-saving agent in this case. Further to lidocaine failure in reversing the complete venom toxicity, it would be explained that high Na+ current induced by venom might prevent lidocaine effect at above doses, while higher concentrations also can cause lidocaine toxicity, which restricts our further investigation. Preferably, it would be suggested to use other medical approaches and medication to save the envenomed victim’s life.

LidocaineOdontobuthus doriaeScorpionVenomsSodium Channel.

233,927 views

70,285 downloads

Contributors:

Maryam Nakhjavani

Hossein Vatanpour

Fatemeh Shahriari

Baharak Mohamadzadehasl

Research PaperID: AJPTR65015

Synthesis and pharmacological evaluation of 2-substituted 1,3,4-oxadiazole derivatives as antimicrobial agents

Shivi Bhatia, Amandeep Kaur1 and Monika Gupta

The present communication deals with the synthesis of some N´-alkylidene/arylidene-2-(4-substituted-5-phenyl-1,3,4-oxadiazol-2-ylthio) aceto/arylhydrazides, their characterization and antimicrobial activity against medically important microbes. The final compounds were synthesized by reaction of 2-(4-substituted-5-phenyl-1,3,4-oxadiazol-2-ylthio) acetohydrazide with various aliphatic and aromatic aldehydes in presence of glacial acetic acid in ethanol. The structures of the synthesized compounds were established by IR, NMR and Mass spectral studies. The antimicrobial activity was studied against Staphylococcus aureus (MTCC 87), Bacillus subtilis (MTCC 121), Pseudomonas aeruginosa (MTCC 424), Escherichia coli (MTCC 40), Candida albicans (MTCC 183), Fusarium solani (MTCC 2935) using agar well diffusion method. Some of the tested compounds exhibited activity against all the microorganisms. In particular, compounds 12, 19 and 22 were found to be active against all the tested bacterial strains and fungal strain Candida albicans. It was concluded that number and position of electron withdrawing substituents affects the activity.

134-oxadiazoledisc diffusion methodacetohydrazides and imines.

234,162 views

70,243 downloads

Contributors:

Shivi Bhatia

Amandeep Kaur1 and Monika Gupta

Research PaperID: AJPTR65016

Changes in Anti-Oxidative Enzyme and Hematological Parameters of Rohu (Labeo Rohita) Fingerlings Exposed To Ivermectin

Md Aklakur, N. P. Sahu, S. Dasgupta, M.M. Gatne2 and A. K. Pal

Argulosis is the sever problem in carp culture and its severity turns to be panic in case of unregulated treatment with ivermectin, when the post treatment mortality of the fish or subsequent slow growth becomes common. Therefore, present study was aimed to study the effect of acute ivermectin exposure (96 hr) of different concentration on antioxidative enzymes (catalase, superoxide dismutase, glutathione S-transferase), acetyl choline enzyme activity and hematological parameters like platelets, white blood cell (WBC), red blood cell (RBC), haemoglobin content, haematocrit (HCT), mean corpuscular haemoglobin concentration (MCHC), mean corpuscular volume (MCV), mean corpuscular haemoglobin (MCH) and Nitro-blue tetrazolium (NBT) of a tropical freshwater fish, rohu (Labeo rohita) fingerlings (5.5 g). The estimated LC50 value of 7.89 µg/L was found at 96 h of exposure by probit analysis. Activities of anti-oxidative enzymes, immune hematological profile and neurotransmitter activity were significantly altered (P < 0.05) in a dose dependent manner. The early gross sign like sluggishness and dark body were, followed by disorientation and imbalance in swimming, finally mortality during acute toxicity.

IvermectinArgulusRohuHematological parametersAnti-oxidative enzymes

234,292 views

70,323 downloads

Contributors:

Md Aklakur

N. P. Sahu

S. Dasgupta

M.M. Gatne2 and A. K. Pal

Research PaperID: AJPTR65017

Development and Validation of Stability-Indicating RP-HPLC Method for Determination of Fluindione

Mrinalini C. Damle, Mahesh G. Thakare

Fluindione is an oral anticoagulant drug. A simple and rapid and was validated stability indicating HPLC method for Fluindione was successfully developed and was validated. This method is based on HPLC separation followed by UV detection at 285 nm. HPLC method was developed on a Symmetry thermo C18 (4.6 x 250 mm) column with a mobile phase consisting of 10mM di-sodium hydrogen phosphate buffer pH 3.5: methanol 15:85 v/v, pumped at 1.0 ml min-1 flow rate. The pH of buffer was adjusted to 3.5 with ortho phosphoric acid. The column was maintained at ambient temperature and 20μl of solutions were injected. The eluted compound was detected by using PDA detector. Fluindione was eluted at 2.4 ± 0.2 min. Stress degradation study shows that sample degraded with acid and base hydrolysis, under oxidation, thermal and photolytic stress conditions. The method was validated in accordance with requirement of ICH guidelines.

FluindioneStability indicating RP-HPLCForced degradationvalidation

234,411 views

70,381 downloads

Contributors:

Mrinalini C. Damle

Mahesh G. Thakare

Research PaperID: AJPTR65018

Seasonal Food Security Through Edible Leafy Weeds to Local Inhabitants of A Village In Ranchi District of Jharkhand During Rainy Season

Lal Ratnakar Singh

Jharkhand state is blessed with a very rich diversity of wild leafy vegetables as nature’s gift to the local inhabitants of in and around forest areas. These are main source of food and nutrition to the poor tribal and other forest dwelling communities. The wild leafy vegetables are available in marshy border habitat of ponds, watersides of crop fields, its border areas, waste land, cultivated land and forest land. These wild leafy vegetables are available in plenty during the rainy season in particular. The present study was undertaken to explore the seasonal food security through wild leafy vegetables in a village having predominantly Oraon tribal community specifically with respect to seasonal availability, use, and traditional knowledge of wild leafy indigenous foods.

Food securityWild Leafy vegetabletraditional knowledgenutrition.

234,800 views

70,323 downloads

Contributors:

Lal Ratnakar Singh

Research PaperID: AJPTR65019

Anticancer and antiviral potential of folic acid conjugated with silver and gold Nanoparticles produced by Thermoduric Bacillus alcalophilus subsp halodurans

Rawhia Arafa

Fifteen bacterial isolates were purified from Wady El Natrun loam salty calcareous sand soil textures and subjected to screen for their ability to produce folic acid. Bacterial isolate number WN12 was highly producer of folic acid (Vitamin 9) and it was selected tentatively to be identified physiologically and phylogeny. The strain grows at 15-50°C, pH 6.0-12.5 and at salinities of 3.0-27.5 % NaCl (w/v). It was Gram positive , translucent brownish smooth color colony, long rods; non spore forming, motile by peritrichous numerous flagella.WN12 isolate identify as Bacillus alcalophilus subsp halodurans .The TLC Rf values for crude folic acid was 0.7 by using solvent system n-butanol, glacial acetic acid, water, methanol (20:10:20:5 v/v). The UV analysis of the fractions to the purified bacterial folic acid peak at 270 nm .Also, TEM images estimated the average size nearly around 0.1µm. While HPLC chromatograms of free folic acid maximum absorption wavelength was selected at 280 nm .And the FTIR spectra show absorption bands for pure folic acid infrared spectrum showed several identical absorption bands including OH, band at 3500 cm−1, C-H, band at 2900 cm−1 C=O band at 1100 cm−1. Comparison of the two synthesis conjugates Nano gold (AuNPs) and Nano silver(AgNPs) with folic acid (FA) characterization were done . Six treatment were tested for measuring infected dose 50 (IC50) on four cancer cell lines,. Cytotoxic effect of folic acid alone and Ag NP showed a variable pattern of reactivity to cell lines arranged ion in the order of MCF7> HCT> CaCO2> HEPG2 (P CacO2 >HCT >HEPG2 (P

Folic acidBacillus alcalophilus subsp. halodurans bacteriaantitumor'sAntivirusnanosilver and nanogol

234,790 views

70,376 downloads

Contributors:

Rawhia Arafa

Research PaperID: AJPTR65020

Characterization of antioxidant property and Chemical compositions of Lagenaria Siceraria stand. Fruit extract

Sarang Sunil Mahamuni, Vishal Sanjay Savant

Last few decades, research data has prompted a passionate debate as to whether oxidation, or specifically, oxidative stress mediated by free radicals/reactive oxygen species (ROS)/reactive nitrogen species (RNS), is a primary or secondary cause of many chronic diseases. Lagenaria siceraria is fair source of ascorbic acid, beta carotene and different phytochemicals to heal many disorders. It shows ribonucleolytic, antihyperlipidemic, hepatoprotective, antioxidant, immunomodulatory, cardiotonic activity. The collection and identification of juice of Lgenaria siceraria and preparation of four fractions of concentrated juice were carried out and preliminary phytochemical and pharmacological screening of same fractions was done. Preliminary pharmacological screening of each fraction was investigated to find out desired in-vitro antioxidant activity. Aqueous fraction showed better yield because of polarity of compound. Preliminary phytochemical screening of four different fractions had various phytochemicals like steroids, flavonids, glycosides, saponins, etc. As we had followed the biological activity guided isolation of active constituents, the fractions were evaluated for antioxidant activity. Isolated aliphatic and saponins moiety may be responsible for the antioxidant activity.

Lagenaria sicerariaantioxidant activityphytochemical and pharmacological screening.

234,933 views

70,397 downloads

Contributors:

Sarang Sunil Mahamuni

Vishal Sanjay Savant

Research PaperID: AJPTR65021

A Development and Validation of RP-HPLC Method For Simultaneous Estimation of Nadifloxacin and Clobetasol Propionate In Its Pharmaceutical Dosage Form

Nidhi Patel, Pooja Patel, Dhananjay Meshram

A novel, simple, precise, rapid, reproducible and cost effective RP-HPLC method was developed and validated for the simultaneous estimation of Nadifloxacin and Clobetasol propionate in its pharmaceutical dosage form. The chromatographic separation was carried out using C18 Shim pack XR ODS II (250 mm × 4.6 mm, 5µm) column with mobile phase comprising of Acetonitrile : Water (50:50)(%v/v). Flow rate was maintained 1.0 mL/min and quantitation was carried out using UV detection at 242nm. Retention time of Nadifloxacin and Clobetasol propionate were found to be 2.64 min and 6.19 min respectively. The method was validated by assessing different parameters such as specificity, linearity, precision, accuracy, robustness, LOD and LOQ for the developed method. The linearity range 20-240 µg/mL and 1-12 µg/mL were selected for Nadifloxacin and Clobetasol propionate respectively. The correlation coefficient (r2) for Nadifloxacin and Clobetasol propionate were found to be 0.9995 and 0.9999 respectively. The limit of detection for Nadifloxacin and Clobetasol propionate were found to be 0.029 µg/mL and 0.21 µg/mL. The limit of quantitation for Nadifloxacin and Clobetasol propionate were found to be 0.089 µg/mL and 0.64 µg/ml respectively. Percentage recovery was found to be 99% to 100.56% for Nadifloxacin and 99.37% to 99.79% for Clobetasol propionate. All the validation parameters were with-in the acceptance limit. The relative standard deviation (%RSD) was found to beless than 2% in all the assessed parameters. The developed HPLC method can successfully used for the quantitative estimation of both the drugs in its formulation.

NadifloxacinClobetasol propionateRP-HPLCSimultaneous determinationValidation

234,936 views

70,418 downloads

Contributors:

Nidhi Patel

Pooja Patel

Dhananjay Meshram

Research PaperID: AJPTR65022

Evaluation of antioxidant potential of grains of Paspalum scrobiculatum Linn.

Swati Sharma, Jyoti Saxena

Antioxidants play a vital role in protection against various diseases and disorders. In search for new antioxidants, nutraceuticals are extensively studied for their preventive effects. Paspalum scrobiculatum Linn., commonly known as Kodo millet, is a minor millet found in India having pharmacological importance. Whole grains of kodo millet were evaluated for its antioxidant potential. Five different extracts of kodo millet, i.e. 70% ethanol, 70% methanol, ethyl acetate, chloroform and petroleum ether extracts were screened for their reducing capacity and free radical scavenging capacity. 1, 1-diphenyl-2-picrylhydrazyl (DPPH) Assay was performed using ascorbic acid as standard at 515 nm. The reducing capacity was measured at 700 nm with ascorbic acid as reference standard. Highest radical quenching was observed in ethanol extract, 64.609 ± 0.131µg/ml Ascorbic Acid Equivalent (AAE). The reducing capacity was found maximum in ethanol extract, followed by methanol. All the extracts showed antioxidant potential and the hydro-alcoholic extracts, i.e. methanol and ethanol showed high reducing and radical scavenging capacity respectively. The results of preliminary study indicate that the grains of Paspalum scrobiculatum have good antioxidant potential and these can be used as potent Nutraceutical against target diseases which can be studied further.

DPPHKodo milletNutraceuticalPaspalum scrobiculatumReducing Power.

234,828 views

70,532 downloads

Contributors:

Swati Sharma

Jyoti Saxena

Research PaperID: AJPTR65023

RP-HPLC Method Development for Determination of Vasopressin From Nanoparticles

Dipti Desai, Dushyant Shah

Vasopressin, nonapeptide, used as an antidiuretic hormone. Very few method has been reported for analysis of Vasopressin from pharmaceutical dosage form. A simple and rapid high performance liquid chromatography (HPLC) method was developed for the quantitative analysis of arginine vasopressin released from polymeric nanoparticles. Chromatographic analysis was performed on an RP C18 column with a mobile phase consisting of acetonitrile and phosphate buffer (13:87 v/v) at a flow rate of 1.6 ml/min at a wavelength of 220 nm, with a retention time 4.1 min. The method was shown to be specific and linear in the range of 1-50 IU/ml (r2 = 0.9997). Developed method was validated for various evaluation parameters as per ICH guidelines. The method showed no peak interference in presence of formulation excipients. The limit of detection and quantitation were 0.32 and 1.06 IU/ml, respectively. The method was applied to the quantitative analysis of drug to study in vitro drug release from polymeric nanoparticles.

VasopressinNanoparticlesRP-HPLCmethod validation.

235,378 views

70,584 downloads

Contributors:

Dipti Desai

Dushyant Shah

Research PaperID: AJPTR65024

Evaluation and Determination of Antifungal Potentials of Sap of Azadirachta Indica

Tribhuvan Singh, Syed Imran Ul Haq, K. Rajeshwar Dutt, Ibrahim Makintami Ibrahim

The present research was conducted to determine in vitro Antifungal activity of Sap of Azadirachta indica. The Fungal strain like C. Albicans and A. Niger cause wide range of health complications to most people worldwide. From various studies we found the different parts of plant of Azadirachta indica exhibiting significant Antifungal activity. We conducted research to determine Antifungal activity of Sap of Azadirachta indica in four different volumes (0.25, 0.5, 1, 1.5 ml) and zone of inhibition of 10 to 22mm of the fungal strain were determined after 36hrs. By this research we found the Sap of Azadirachta indica exhibited significant Antifungal activity.

Azadirachta IndicaAntifungal ActivityZone of Inhibition.

235,149 views

70,691 downloads

Contributors:

Tribhuvan Singh

Syed Imran Ul Haq

K. Rajeshwar Dutt

Ibrahim Makintami Ibrahim

Research PaperID: AJPTR65025

Synthesis, Characterization and Antimicrobial Studies of Schiff Base Complexes of 1-(5-Chloro-2-Hydroxy-4-Methylphenyl)Ethanone

Jaishri N. Bavane*1 and Rahul B. Mohod

The chemistry of metal complexes has fascinated and inspired the chemist all over the world. Among the chelating ligand, Schiff base have attracted the attention of the chemist due to the ease of the preparation and complexation. Schiff base complexes have remained an important and popular area of research due to their simple synthesis versatility and diverse range of applications. Schiff bases are able to stabilize many different metals in various oxidation states. In the present study the Schiff base of 1-(5-chloro-2-hydroxy-4-methylphenyl) ethanone with 4-(2-aminoethyl)phenol has been synthesized. The complexes of this Schiff base ligand have been synthesized by using Mn(II), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) ions under refluxed in ethanol. These compounds have been investigated by elemental analysis, infra-red, 1H nuclear magnetic resonance, diffuse reflectance spectroscopic techniques and magnetic susceptibility measurements. The free ligand and their metal complexes have been screened in vitro for their antimicrobial activity against gram-positive bacteria S. aureus, gram negative bacteria, E. coli, S. typhi and fungi P. notatum and R. oligosporus.

4-(2-aminoethyl) phenolinfra-redmagnetic susceptibility measurementsantimicrobial activity etc.

235,507 views

70,558 downloads

Contributors:

Jaishri N. Bavane*1 and Rahul B. Mohod

Research PaperID: AJPTR65026

Effect of d-Limonene on behavior and brain oxidative stress in cerebral-ischemia reperfusion injury of mice

Harpreet Kaur, Nitin Bansal

The present study explored the neuroprotective role of d-Limonene in the cerebral ischemia-reperfusion injury in mice. Swiss Albino mice (either sex), weighing between 20-30 g were divided in different groups (n≥6). The animals were anaesthetized using Chloral hydrate (400 mg/kg; i.p.) and cerebral blood supply was occluded for 10 min and afterwards reperfusion for 24 h. d-Limonene has been administered in 3 doses (50, 100 and 200 mg/kg; p.o.) successively to mice for 30 days before surgery. Edaravone (3 mg/kg, i.p.) was used as standard drug. The effect of surgery on memory, anxiety, muscle relaxant and locomotor was estimated by using passive avoidance paradigm, elevated zero maze, rota rod apparatus, and actophotometer. After behavioural evaluation, the animals were sacrificed and brains were isolated, homogenized and centrifuged for TBARS, GSH, catalase and brain nitrite estimations. Ishemia-reperfusion injury caused decrease in locomotor, motor-co-ordination, decreased the time spent in open arm, no. of entries and increased in latency time in elevated zero maze and memory of mice. Ischemic mice showed higher brain TBARS and nitrite levels and lower GSH and catalase levels. However, d-Limonene administration significantly attenuated (p

d-Limoneneischemia-reperfusion injurybilateral carotid artery occlusionoxidative stress.

235,581 views

70,669 downloads

Contributors:

Harpreet Kaur

Nitin Bansal

Research PaperID: AJPTR65027

Benzimidazole – A Potent Antimicrobial Agent

Pullagura M Krishna Prasad1 Avdhut Kanvinde S1 and Raja S

The use of heterocyclic compounds in field of medicinal chemistry is increasing day by day due to various reasons like heterocyclic compounds are included in the structure of many biochemical materials, which are essential for life. Nucleic acid, many naturally occurring pigments like chlorophyll, vitamins and antibiotics contains heterocyclic nucleus. Modern society is also dependent on synthetic heterocycles for use as drugs, pesticides and dyes. The work embodied in this article relates to benzimidazole as it is a versatile heterocycle which exhibit broad range of biological activities. Benzimidazoles (known as o-phenylenediamine derivatives) are mostly synthesized from o-phenylenediamines. This ring system is present in numerous anti-protozoal, anti-helmintics, anti-HIV, anti-convulsant, anti-inflammatory, anti-neoplastic, and anti-ulcer agents. Several benzimidazoles such as albendazole, mebendazole, flubendazole, fenbendazole, omeprazole, lansoprazole, and clofazone are used in therapy. In this review, various antimicrobial benzimidazoles were summarized & reported. In addition this review highlights the antimicrobialpotency of benzimidazole to medicinal world.

Benzimidazoleo-Phenylenediamine derivativeAntimicrobialAntibacterialAntifungal.

235,579 views

70,665 downloads

Contributors:

Pullagura M Krishna Prasad1 Avdhut Kanvinde S1 and Raja S

Research PaperID: AJPTR65028

Formulation and Evaluation of In Vitro Blood-Brain Barrier Penetration of Emtricitabine Niosomes Using Immobilized Artificial Membrane Phosphatidyl Choline Column Chromatography

Santha Sheela Natarajan Bhargavi, Nappinnai Mohanavelu, Panneer Selvam Perumal, Sundhararajan Ranganathan

The main objective of the study is to formulate emtricitabine, a nucleoside reverse transcriptase inhibitor used in the treatment of Human Immuno deficiency Virus (HIV) infections as a niosomal formulation to improve the Central Nervous System (CNS) penetration of the drug and evaluate its CNS penetration using in vitro blood-brain barrier penetration study using immobilized artificial membrane phosphatidylcholine column chromatography. Emtricitabine encapsulated niosomes were prepared by thin layer evaporation (TLE)-paddle stirring method with Span 60 as main surfactant. Cholesterol (CHL), Solulan C24 (SOL) and N-palmitoyl glucosamine (NPG) were also included in the niosomal formulations. The ratio of Span 60:CHL:SOL:NPG was 50:40:10:10 with total concentration of components as 38 mM. The hydration temperature was maintained at 65 0C. Sonication method was employed for size reduction of the niosomes. The formulation was evaluated for CNS penetration by in vitro blood-brain barrier penetration study using immobilized artificial membrane phosphatidylcholine column chromatography. The Scanning electron microscopic images showed good formation of the niosomal vesicles. The mean particle size and encapsulation efficiency were found to be 154±4 nm and 64.45±1.14% respectively. In vitro blood-brain barrier (BBB) penetration of emtricitabine from drug loaded NPG niosomes using immobilized artificial membrane phosphatidylcholine column chromatography showed an improved CNS penetration of the drug with (kIAM/MW4) X 1010 values of 2.79±0.05 at pH 5.5 and 8.48±0.18 at pH 7.0. The results showed an increased CNS penetration when the drug was encapsulated in niosomes and may be considered as a potential alternative to improve brain targeting of emtricitabine and thus minimize HIV Associated Neurocognitive Disorders (HAND).

NiosomesEmtricitabineCNS penetrationBrain targeted drug delivery.

236,017 views

70,680 downloads

Contributors:

Santha Sheela Natarajan Bhargavi

Nappinnai Mohanavelu

Panneer Selvam Perumal

Sundhararajan Ranganathan

Research PaperID: AJPTR65029

Development and Validation of RP-HPLC Method for the Quantitation of Ticagrelor Using Box-Behnken Experimental Design

Rahul P. Chilbule1 and Rajendra B. Kakde

For determination of ticagrelor, a high performance stability indicating liquid chromatographic method was developed, validated and optimized for the determination of quality in any quality control laboratory. The drug was subjected to stress alkaline, acidic, oxidative, thermal, Neutral and photo-degradation and was found to hydrolyze in acidic, alkaline conditions as well as under oxidative stress. Ticagrelor with the interferents are separated on a reversed phase Cosmosil (R) 5C8-MS (5 μm, 250 mm × 4.6 id) column using acetonitrile: 35 mM ammonium acetate buffer (pH 3.8) in the ratio of 40:60 as mobile phase at a flow rate of 1 ml min-1. The drug was detected at 254 nm over a concentration range of 5–140 μg ml−1 with mean percentage recovery 100.08% using a PDA detector. The method was validated and a 32 factorial was employed by using Box–Behnken experimental design for the validation of robustness. These designs have three factors such as mobile phase composition, flow rate and pH while peak area and retention time were taken as a response. This showed that little changes in the mobile phase and flow rate affect the response while pH has no effect. The compilation of precision result shows % RSD for system precision, and method precision is 0.4. The developed method was found to be precise, accurate, linear, robust and rugged. This method was successfully applied for the assay of commercially market tablet formulation; hence it can be adopted for the determination of quality in any quality control laboratory.

TicagrelorStability-indication methodsLinear regression analysisDesign of experiment

235,988 views

70,866 downloads

Contributors:

Rahul P. Chilbule1 and Rajendra B. Kakde

Research PaperID: AJPTR65030

Development and Evaluation of Olmesartan Medoxomil Solid SEDDS: In Vivo Bioavailability Studies

B. Usha sri, Y. Indiramuzib, D.V.R.N. Bhikshapathi, P. Varalaxmi

The objective of present study was to develop solid self micro emulsifying drug delivery system (S-SEDDS) with Neusilin for enhancement of dissolution rate of model drug Olmesartan medoxomil. Olmesartan medoxomil SEDDS was prepared using oils - Captex 35, Capryol 90, Castor oil, Olive oil, surfactants - Gelucire 44/14, Kolliphor HS 15, Kolliphor RH 40, Labrasol, Tween 80, Lauroglycol, co-surfactants - PEG 400, PEG 600, Propylene glycol. Solid SEDDS were prepared using adsorbing agent Neusilin US2. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. Further, the resultant formulations were investigated for clarity, phase separation, globule size, effect of pH and dilutions and freeze-thaw stability and found to be within the limits. The optimized SMEDDS (F6) formulation of Olmesartan contained Castor oil (Oil), Kolliphor RH 40 (Surfactant) and PEG 400 (Co-surfactant). The prepared liquid SEDDS was thermodynamically stable with good self emulsification efficiency and having globule size in nanometric range which may be physiologically stable. On the basis of different evaluation parameters F6 was found to be optimized formulation. S-SEDDS of Olmesartan medoxomil prepared with optimized SEDDS (F6) using adsorbing agent Neusilin US2 by adsorption technique have good flow property and drug content. This optimized formulation (F6) was converted in to solid SEDDS by adding required quantity of Neusilin US2 as adsorbing agent used for in vitro dissolution and bioavailability assessment. Results of SEM demonstrate that spherical S-SEDDS can be obtained without agglomeration. In vivo studies revealed that the oral bioavailability of Olmesartan medoxomil from solid SEDDS was 2.3-fold higher compared to that of Olmesartan suspension in rats, suggesting a significant increase (p < 0.05) in oral bioavailability of Olmesartan medoxomil from solid SEDDS. Hence it was concluded that S-SEDDS can be efficiently formulated by adsorption technique using Neusilin US2 as solid carrier to enhance dissolution rate of poorly soluble drug such as Olmesartan medoxomil.

Olmesartan medoxomilsolid SEDDSneusilin US2Castor oilbioavailability studies

235,913 views

70,893 downloads

Contributors:

B. Usha sri

Y. Indiramuzib

D.V.R.N. Bhikshapathi

P. Varalaxmi

Research PaperID: AJPTR65031

In Vivo Antianaphylactic Activity of Different Extracts of Glycyrrhiza Glabra on Mesenteric Mast Cells of Rats

C.Girish, Y. Narsimha reddy

Antianaphylactic activity of Glycyrrhiza glabra was evaluated with the help of mesenteric mast cells of rats. The study was carried out by sensitization of the rat mesenteries by using sheep serum and tripple antigen to induce degranulation of mast cells. The mesenteries which are pretreated with prednisolone (10 mg), petroleum ether, methanol and aqueous extract of Glycyrrhiza glabra (250mg, 500mg and 750mg) were analyzed for the mast cell degranulation during the anaphylactic reactions. Treatment with aqueous extract of Glycyrrhiza glabra (500mg) showed beneficial effect on degranulation of mast cells in actively sensitized rats. The activity was comparable with that of standard drug, Prednisolone. Antianaphylactic activity of aqueous extract of Glycyrrhiza glabra on the mesenteric mast cells of the rat may be possibly due to the membrane stabilizing potential.

Antianaphylactic activityMast cell degranulationGlycyrrhiza glabraMembrane stabilizationAnaphylaxis.

236,066 views

70,818 downloads

Contributors:

C.Girish

Y. Narsimha reddy

Research PaperID: AJPTR65032

An Effective Novel Strategy of Combined Plants Extract for the Treatment of Parkinson's Disease

Parwez Alam, Jyoti Gupta, Seema Firdouse

The aim of present study was an effective novel strategy of combined plants extract for the treatment of Parkinson’s disease, using Amla Withania and Tulsi extract in different ratio. The extracts were prepared by using solvents like 60% ethanol for Amla fruit, 50% ethanol for Withania root and pure ethanol for Tulsi aerial part. Haloperidol was used to induce catalepsy and Akinesia. The ability of these combined extracts in inhibition of haloperidol-induced catalepsy and Akinesia in rodent models of Parkinsonian symptoms also Motor co-ordination test was conducted using a rota rod apparatus. It was found that treatment with the extract signiﬁcantly reduced catalepsy according to dose. In the second experiment haloperidol was used to suppress locomotor activity in test. Treatment with extract signiﬁcantly increased locomotion reduced by haloperidol according to dose.

Amla fruitsWithania rootsTulsi aerial partsExtractsParkinson’s disease.

236,539 views

70,991 downloads

Contributors:

Parwez Alam

Jyoti Gupta

Seema Firdouse

Research PaperID: AJPTR65033

Atorvastatin Calcium Solid Dispersion in Floating Tablets for Hypolipedmic Effect.

Al Zahraa G. Al Ashmawy, Marwa H. Abdallah, Hanan M. El Nahas

The aim of this study was increasing the bioavailability of poorly water soluble, atorvastatin calcium (ATC) via preparation of solid dispersion then incorporating it in floating tablets for oral use. Physical mixtures of ATC were prepared by mixing the appropriate amounts of ATC and carriers (PVP k-2000, PEG 6000 and skimmed milk) in geometric proportions using a mortar and pestle, until a homogeneous mixture was obtained. Solid dispersions of ATC with all carriers were prepared at ratios of (1:1, 1:3, 1:5, 1:7 and 1:9 drug to carrier ratio w/w) by three methods, kneading method, solvent evaporation and melting method. Evaluation of solid dispersion was done by studying the phase solubility, in-vitro dissolution, FTIR spectroscopy, DSC and X-ray powder diffractometry. The selected solid dispersion formulation was incorporated in floating tablets which were prepared by melting granulation method. Evaluation of floating tablets was done by determination of tablet thickness, diameter, weight uniformity, content uniformity, hardness, friability, in-vitro dissolution, in-vitro buoyancy in addition to bioavailability studies. PEG 6000, PVP k-2000 and skimmed milk increased the solubility of ATC by 180, 290 and 1200 folds, respectively. Solid dispersion prepared using PEG 6000 (S2, 1:3 drug: polymer ratio) gave the highest % drug released than PVP k-2000 and skimmed milk. Floating tablet formulation (T1) showed the best drug dissolution rate which is 102.18% after 24 h. Bioavailability results showed that floating tablets containing ATC solid dispersion is effectively used for treatment of hyperlipedmia. Floating tablets contained PEG 6000 solid dispersion reduced the % of TC, TGS and LDL by 58.46, 32.00 and 91.21 %, respectively while the percent of HDL was raised by 11.11%.

Atorvastatin calciumPEG 6000PVPskimmed milkfloating tablets and cholesterol.

236,244 views

70,873 downloads

Contributors:

Al Zahraa G. Al Ashmawy

Marwa H. Abdallah

Hanan M. El Nahas

Research PaperID: AJPTR65034

Development of Pulsatile System of Nabumetone for Effective Management of Colonic Spasms

Bhargavi ganiwada, Suresh moka, Raju Venkata Krishna, Manogna.K

In the present study, an attempt was made to develop pulsatile system of Nabumetone for effective management of colonic spasms. We tried to explore the feasibility of time dependent pulsatile drug delivery system of nabumentone to treat colon spasms. And also to prepare enteric coated tablets consisting of super disintegrates by direct compression method and to evaluate for their quick release properties and disintegration. Literature review has proved that Nabumetone , which undergoes hepatic biotransformation, 6- methoxy -2-naptthylacetic acid a protein inhibitor of prostaglandin synthesis through binding COX-1 and COX-2 receptors. Explosol used as super disintegrant and hydroxy propyl methyl cellulose (HPMC K100M), Eudragit as film former. Drug and excipients are studied for pulsatile release of precompressional tablets by using FT-IR spectrophotometry. Tablets were prepared by direct compression method. Evaluation of tablets by pre-compression parameters like angle of repose, bulk density, tapped density, compressibility index, Hausner’s ratio and post compressional parameters namely thickness, weight variation , Hardness, friability, dissolution studies, assement of kinetics of dissolution, zero order model, first order model, Higuci model, Korsmeyer-peppas model and stability studies were determined. All the obtained results from the tests were found to be within permissible limit. From the overall results, we can conclude that pulsatile tablets of nabumetone would deliver the drug according to the need of the patient for control of sever colon spasms.

Colon drug delivery systemNabumetonecolonic spasms

236,614 views

71,025 downloads

Contributors:

Bhargavi ganiwada

Suresh moka

Raju Venkata Krishna

Manogna.K

Research PaperID: AJPTR65035

Flavonoids insulinogeneic action” may be “A promising alternative for diabetes” management

Nandhakumar Loganathan, Mohan Sellappan

Flavonoids (polyphenols) do have their entire sort of insulin inception like action genetically on β- cells of islets of langerhans, and then decline blood glucose level to an optimum. Researches over few flavonoids like diosmin, fisetin, morin, hesperidin, naringenin etc., perceived to have insulin secreting and utilizing action in pancreatic cells and peripheral tissues glucose respectively. For this reason only, exploitation of these polyphenols in treating diabetes is highly beneficial, and it is rarely pronounced on its experimental front in recent times. Though vincristine (vincristine tablets) a natural alkaloid obtained from periwinkle plant has been contemporary, in place for treating Hodgkin’s lymphoma clinically, and found to be the most successful modern medicine. Similarly, may be flavonoids do have a very huge potential, for treating diabetes clinically with therapeutic significance, if the area of interest of flavonoids focused on diabetic management. At the same time as, fundamental research performed on these flavonoids suggests that, the flavonoids mechanisms of action are manifold. Typically mechanisms of flavonoids on glucose metabolisms are insulin uptake in skeletal muscles, regulating rate-limiting enzymes in carbohydrate metabolic pathways, insulin mimetic and secretagogue action. Hence, in this hypothesis we suggest that, managing diabetes and its complications with one or more flavonoids as a novel dosage form, having various facets of glucose metabolism regulation with regards to insulin secretion, mimic and utilization, as it would be a novel approach in treating diabetes.

Flavonoidsinsulinogenic actiondiabetestreatment for diabetes and dosages.

236,441 views

71,045 downloads

Contributors:

Nandhakumar Loganathan

Mohan Sellappan

Research PaperID: AJPTR65036

Effects of intraperitoneal administration of ivermectin on antioxidative enzymes and blood parameters in Rohu (Labeo rohita)

Md Aklakur, N. P. Sahu, S. Dasgupta, M.M. Gatne2 and A. K. Pal

Ivermection is widely being use for treatment of ectoprarastic infestation in fishes globally in carp farming. The post treatment mortality of the fish or subsequent slow growth becomes common due to unregulated dose. Therefore, present study was aimed to study the effect of acute sub- lethal ivermectin administration (96 hr) on antioxidative enzymes (catalase, superoxide dismutase, glutathione S-transferase) and hematological parameters like platelets, white blood cell (WBC), red blood cell (RBC), haemoglobin content, blood glucose and Nitro-blue tetrazolium (NBT) of a tropical freshwater fish, rohu (Labeo rohita). The calculated LD50 value was found to be 1.81 mg/Kg at 96 h by probit analysis. The three sub lethal doses like 125 125 µg/Kg, 250 µg/Kg , 500 µg/Kg and one control (0.00 µg/Kg ) were intraperitoneally administered. After 96 hours it showed significantly altered (P < 0.05) activities of anti-oxidative enzymes and hematological profile, in a dose dependent manner. The early gross sign like sluggishness and dark body were recorded during acute toxicity study. The result indicates ivermectin can impact negatively at higher doses to host rohu (Labeo rohita )

IvermectinIntraperitonealL rohitaHematological parametersAnti-oxidative enzymes

236,926 views

71,118 downloads

Contributors:

Md Aklakur

N. P. Sahu

S. Dasgupta

M.M. Gatne2 and A. K. Pal

Research PaperID: AJPTR65037

Phytochemical screening, Antimicrobial and Antioxidant activity of whole extract of Cardiospermum halicacabum Linn. (Sapindaceae)

M. O. Malpani, P. R. Rajput, P. S. Pande, M. M. Sapkal

Man’s existence on this earth has been made possible only because of the vital role played by the plant kingdom in sustaining his life. The three important necessities of life – food, clothing and shelter and a host of other useful products are supplied to a great extent by the plant kingdom. Cardiospermum halicacabum is one of the medicinally potential plants which is used in the treatment of rheumatism, lumbago, cough, hyperthermia, and nervous diseases. The present investigation was undertaken to screen the phytochemical analysis, antimicrobial and antioxidant activity of Cardiospermum halicacabum whole extract.

AntimicrobialantioxidantCardiospermum halicacabumwhole extract.

236,875 views

71,006 downloads

Contributors:

M. O. Malpani

P. R. Rajput

P. S. Pande

M. M. Sapkal

Research PaperID: AJPTR65038

Process Validation of Extra Power Pain Control Caplets

Prajapati PR, Desai N, Modi VS, Tarasankar Basuri

Process validation is an important step to maintain the quality of final product. This work presents the process validation of Extra Power Pain Control caplets at manufacturing plant Wockhardt ltd. Daman. Revalidation was performed to ensure corrective actions to deliver finished product that meet at intermediate stage, finished product stage and possess laid down specification till claimed shelf life. Three consecutive batches were taken for the validation study. It provides a documented evidence for manufacturing process, critical process parameter and sampling plans.

Process ValidationRevalidationCapletsQuality.

236,867 views

71,174 downloads

Contributors:

Prajapati PR

Desai N

Modi VS

Tarasankar Basuri

Research PaperID: AJPTR65039

Enhancement of Solubility and Bioavailability of Glimepiride Using Solid Dispersion Technique

V. Abhishiktha, M. Sudhakar, Vinay Umesh Rao

The poor aqueous solubility of Glimepiride is the major factor limiting its oral bioavailability. The objective of the work is to enhance the solubility of Glimepiride, there by its bioavailability by using solid dispersion technique. Solid dispersions of Glimepiride were prepared by using Poly vinyl Pyrrolidone (PVP K30), by solvent evaporation method in different ratios of 1:0.5, 1:1, 1:3, 1:5 respectively and evaluated for its in vitro & in vivo release along with Mdsc & FTIR. The equilibrium solubility of solid dispersions was determined in water to study the effect of PVP K30 on solubility of Glimepiride. In Vitro dissolution studies were conducted in water from solid dispersions equivalent to 4 mg of Glimepiride. Protocol bound in vivo studies were conducted in non diabetic rats with the best formulation. Two groups of rats (6 rats in each group) were orally fed Glimepiride as plain drug dispersion (control group) & as drug: PVP K30 solid dispersion (test group). The fall in blood glucose level was monitored over 24 hours. Successful conversion of the crystalline Glimepiride to amorphous solid dispersion was achieved at 1:5 level of drug to PVP K30 (F4). The solid dispersion prepared with PVP K30 at 1:5 level (F4) showed a 4 folds enhancement in aqueous solubility of the drug. So the in vivo studies conducted with 1:5 drug to PVP K30 (F4) solid dispersion, the best formulation, it was observed that the fall in the test group is significantly faster and more intense as compared to the control group. The above study shows that solid dispersion of Glimepiride offers an simple and attractive solution to increase the solubility of the poorly water soluble drug and thereby improve its oral bioavailability. Key words: Glimepiride, Poly vinyl Pyrrolidone (PVP K30), Solid dispersions (SD)

GlimepiridePoly vinyl Pyrrolidone (PVP K30)Solid dispersions (SD)

237,059 views

71,140 downloads

Contributors:

V. Abhishiktha

M. Sudhakar

Vinay Umesh Rao

Research PaperID: AJPTR65040

Synthesis of 2,3,5-Trisubstituted 1,3,4-Oxadiazole Via Cyclization of 5-Fused Heteryl Pyrazole-3-Carbohydrazone having Quinolin-3-yl Moiety and their Antibacterial Activity

Mohammad Idrees*1 Roshan D. Nasare, Naqui J. Siddiqui

In the undertaken research, 5-(5-H/Br benzofuran-2-yl)-N'-((-2-(p-tolyloxy) substituted quinolin-3-yl)methylene)-1-phenyl-1H-pyrazole-3-carbohydrazide (3a-h) on treatment with acetic anhydride afforded novel 1-(5-(5-(5-H/Br benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl)-2-(-2-(p-tolyloxy)substitutedquinolin-3-yl)-1,3,4-oxadiazol-3(2H)-yl)ethanone derivatives (4a-h). 5-fused heteryl pyrazole-3-carbohydrazone (3a-h) needed for the synthesis of 4a-h were synthesized by reaction of 2-(p-tolyloxy) substituted quinoline-3-carbaldehyde (2a-h) with 5-(5-H/Br benzofuran-2-yl)-1-phenyl-1H-pyrazole-3-carbohydrazides (1a-b) in ethanol as solvent. The structures of the newly synthesized compounds were identified on the basis of elemental analysis and spectral studies like IR, 1H NMR and Mass spectra. The in-vitro antibacterial screening of these synthesized compounds against E. coli, S. aureus, E. areogenes and B. thurengienesis relative to the reference standard Chloramphenicol have been found to possesses good to moderate inhibitory activity.

134-OxadiazoleQuinoline carbaldehydefused heteryl pyrazole-3-carbohydrazone

237,372 views

71,199 downloads

Contributors:

Mohammad Idrees*1 Roshan D. Nasare

Naqui J. Siddiqui

Research PaperID: AJPTR65041

Trend of Smoking In Students of Ras Al Khaimah, UAE

Shahnaz Usman1 ⃰, khawla Al Awad, Muaadh Al Saeedi, Hamam Al Naemi, Huma Zaidi

The present study aims to find the incidence of smoking among the youth of Ras Al Khaimah (UAE). It is assumed that adolescence and young adulthood are the most susceptible stages to start tobacco use. This study mainly focuses on analyzing the age patterns in which the youth is mostly inclined towards smoking, finding the major causes and factors that influence this inclination, and creating awareness about the harmful effects of smoking on their health. A structured questionnaire consisting of 15 questions was administered among 116 randomly selected participants. The main parameters of the study were prevalence of smoking, age, category of responder, number of cigarette /day, reason, whether they tried to stop smoking, methods used to stop smoking, awareness about passive killer and whether they got any advice from parents/guardians regarding smoking etc. The results shows that many sociodemographic, environmental, behavioral and personal factors are responsible for smoking. More than 88.37% of young adults get this habit at the age below 18 years either directly or indirectly and family/friends play a significant role in this habit. Only an insignificant 9% benefitted from the awareness programs. This emphasizes the importance of creating more awareness programs for the youth. The study comes to the conclusion that more longitudinal and cohort analyses with a large number of volunteers is necessary to examine these trends more closely. The findings demonstrate considerable heterogeneity in smoking among young adults. So it is the time to warrant immediate attention from the public health community.

Smoking and youthfactors influence smokingsmoking in RAKsocial norms attitudes to smoking.

237,362 views

71,221 downloads

Contributors:

Shahnaz Usman1 ⃰

khawla Al Awad

Muaadh Al Saeedi

Hamam Al Naemi

Huma Zaidi

Research PaperID: AJPTR65042

Synthesis and Biological Studies of 4-(4-chloro-1-hydroxynaphthalen-2-YL)-6- aryl-5,6-dihydropyrimidin-2(1H)-one

V.M.Sherekar, S.E.Bhandarkar

1-(4- chloro -1-hydroxynaphthalen-2-yl)-ethanone were prepared by refluxing 4- chloro -naphthalen-1-ol with glacial acetic acid in presence of fused ZnCl2 then 1-(4- chloro -1-hydroxynaphthalen-2yl)-2-aryl-prop-2-en-1-one were synthesized from 1-(4- chloro -1-hydroxynaphthalen-2-yl)-ethanones by condensing it with aromatic aldehydes. 1-(4- chloro -1-hydroxy-naphthalen-2-yl)-3-aryl-prop-2-en-1-ones, urea and concentrated HCl in DMF were added and refluxed. Cool & pour in crushed ice, it was then treated with cold NH4OH solution to get titled compounds. The structure assignment of the new compounds is based on chemical and spectroscopic evidence. All of these titled synthesized compounds are found to posses excellent antimicrobial activities.

SynthesisBiological Studiesantimicrobial study4-(Chloro-Naphthalene-2-Yl)-6-Aryl-56- Dihydropyrimidin-2(1h)-One.

237,391 views

71,332 downloads

Contributors:

V.M.Sherekar

S.E.Bhandarkar

Research PaperID: AJPTR65043

Preparation and In Vivo Evaluation of Extended Release Trilayer Matrix Tablets Containing Simvastatin Solid Dispersions

A.Thirupathaiah, R. Shyam Sunder

The solid dispersion method was originally used to improve the dissolution properties and the bioavailability of poorly water soluble drugs by dispersing them into water soluble carriers. In addition to the above, dissolution retardation through solid dispersion technique using water insoluble and water swellable polymer for the development of controlled release dosage forms has become a field of interest in recent years. The objective of this present investigation was to develop extended release (ER) trilayer matrix tablets containing simvastatin solid dispersion prepared by direct compression and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), guar gum, ethyl cellulose. Upper and lower layers are prepared with Carnauba wax, guar gum and carbopol 934P. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF14) was described by the Zero-order and Higuchi model. In-vivo bioavailability studies were carried out with the optimized formulation (HF14) and reference standard. A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a trilayer extended release formulation up to 24h. These results also demonstrated that the Simvastatin solid dispersion incorporated trilayer tablets shown more bioavailability because of its conversion from crystalline to amorphous form.

Simvastatinrelease order kineticsGeomatrixIn-vivo bioavailability studies

237,683 views

71,296 downloads

Contributors:

A.Thirupathaiah

R. Shyam Sunder

Research PaperID: AJPTR65044

Analytical Approach to Develop and Validate Stability Indicating HPLC Method for Simultaneous Estimation of Tolperisone Hydrochloride and Diclofenac Sodium In Combined Pharmaceutical Dosage Form

Bhavsar Ankita, Bhavsar Ayushi

A simple and precise stability-indicating high performance liquid chromatography method was developed and validated for the simultaneous estimation of Tolperisone Hydrochloride and Diclofenac Sodium in commercial tablet dosage form. Separation was achieved by using C18 (250mm × 4.6 mm, 5µm) column and mobile phase comprising of potassium dihydrogen phosphate buffer (pH: 6.0): acetonitrile (70:30% v/v) at a flow rate of 1.0ml/min. The detection wavelength was 275 nm. The retention times for Tolperisone Hydrochloride and Diclofenac Sodium were 5.26min and 3.59min, respectively. Linearity of Tolperisone Hydrochloride and Diclofenac Sodium were found in range of 15-52.5µg/ml and 5-17.5µg/ml. The % recovery of Tolperisone Hydrochloride was found to be 99.58%-100.88% and 100.75%-101.33% for Diclofenac Sodium. The values of Limit of detection and limit of quantification were found to be 0.203µg/ml and 0.616µg/ml for Tolperisone Hydrochloride and 0.003µg/ml and 0.010µg/ml for Diclofenac Sodium, respectively. The linear regression coefficient for both drugs was found to be 0.999. The method was found to be robust since the retention times and areas were within the limits even after little deliberate variations in pH, flow rate, mobile phase ratio. Stress studies were conducted on the drug substance and product under the ICH prescribed stress condition viz. hydrolysis, oxidation, photolysis and thermal stress. The drugs showed sufficient decomposition under acidic hydrolysis, alkaline hydrolysis, and oxidation. The drug was found to be moderately sensitive to thermal studies and sunlight studies. This method can be successfully employed for simultaneous quantitative analysis of Tolperisone Hydrochloride and Diclofenac Sodium in pharmaceutical dosage form.

Tolperisone HydrochlorideDiclofenac SodiumStress degradationStability IndicatingValidation.

237,728 views

71,300 downloads

Contributors:

Bhavsar Ankita

Bhavsar Ayushi

Research PaperID: AJPTR65045

Preparation, Spectrachemical Characterization and Antimicrobial Activity of Some New Acredinediones Derivatives

Ghulam Mohammad Jan, Shakeel Ahmad Khanday1 Samina Akthar

In this study we prepare different types of acredinediones derivatives. The derivatives were characterized by using different types of spectra chemical techniques like IR, NMR CHN and mass spectra. The anti-microbial activity was done using diffusion method technique. The antibiotic Streptomycin and Amphotericin was used as a standard for comparative study. All the derivatives were found active and show good antimicrobial activity.

AcredonesAntimicrobialdiffusion methodstreptomycinamphotericin.

237,940 views

71,417 downloads

Contributors:

Ghulam Mohammad Jan

Shakeel Ahmad Khanday1 Samina Akthar

Research PaperID: AJPTR65046

Design, Optimization and In Vivo Evaluation of Granisetron HCl Mouth Dissolving Films

S. Jyothi Sri, D.V.R.N.Bhikshapathi

Present work aimed at preparing quick onset of action of Granisetron HCl which is beneficial in emesis, aiding in the enhancement of bioavailability and is very convenient for administration without the problem of swallowing and using water. The films were prepared by using different grades of HPMC E3, E6 and E15, maltodextrin DE6 and other polymers by solvent casting method. They were evaluated for physical characteristics such as thickness, uniformity of weight, folding endurance, drug content, surface pH, percentage elongation and tensile strength and results were found to be satisfactory. The formulations were subjected to disintegration and in-vitro drug release test. The in vitro disintegration time of the optimized formulation F9 was 9 sec and drug release was found to be very fast i.e. 97.8% of within 8 min when compared with innovator product i.e 70.8%. In vivo studies confirmed that their potential as an innovative dosage form to improve the bioavailability and considered to be potentially useful for the treatment of emesis where quick onset of action is desirable. DSC and FTIR data revealed that no interactions takes place between the drug and polymers used in the optimized formulation. From the above results, it can be a good alternative to conventional Granisetron Hydrochloride tablets in the treatment of emesis. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Granisetron Hydrochloride.

Granisetron Hydrochloridefast dissolving oral filmsemesisHPMCbioavailability studies.

238,102 views

71,508 downloads

Contributors:

S. Jyothi Sri

D.V.R.N.Bhikshapathi

Research PaperID: AJPTR65047

Evaluation and Optimization of In Silico Designed PDE4B Modulators

Daniel Attard, Claire Shoemake, John Vella, Paweł Żmudzki, Grażyna Chłoń-Rzepa, Elżbieta Wyska

Cyclic nucleotide phosphodiesterase 4 (PDE4) catalyses the hydrolysis of 3’,5’-cyclic AMP to 5’-AMP. Inhibition of this enzyme preserves high intracellular levels of cAMP which in turn causes suppression of TNF-α and other pro-inflammatory cytokines. It also promotes the expression of anti-inflammatory mediators. The design of small molecule inhibitors selective for PDE4B subtype is considered relevant owing to the fact that this could lead to the identification of potent anti-inflammatory agents with a low side effect profile. In vitro evidence was indicative of the fact that a synthesized analog series of xanthine derivatives were PDE4B inhibitors. This in silico study consequently sought to model the xanthine scaffold within the PDE4B Ligand Binding Pocket (PDE4B_LBP) in order to understand the critical interactions forged by this scaffold and the amino acids lining the PDE4B_LBP and to use this information to model novel high affinity selective PDE4B inhibitors. The results obtained from the study were structurally insightful. The xanthine scaffold was deemed suitable for the design of PDE4B modulators. It was however determined that slight modifications of this scaffold could impart greater selectivity for the 4B cyclic nucleotide phosphodiesterase subtype. The modified xanthine scaffold was consequently further optimized and a series of high affinity molecules with varying physiochemical properties was identified.

PhosphodiesteraseXanthine derivativescAMP signallingPDE4B Ligand Binding PocketSelective inhibition.

237,962 views

71,420 downloads

Contributors:

Daniel Attard

Claire Shoemake

John Vella

Paweł Żmudzki

Grażyna Chłoń-Rzepa

Elżbieta Wyska

Research PaperID: AJPTR65048

Synthesis of Highly Substituted Pyrrolidines via Double Michael Addition Reaction and its Anti-Microbial Activity

Nandkishor Chandan

The synthesis of Nitrogen base heterocycles particularly highly substituted pyrrolidines are very important skeleton of many biologically active molecules1 including natural and non-natural substances. The synthesis of functionalized pyrrolidines persists to attract interest, both for their synthetic challenges,2 and also their value in synthetic chemistry3 and their diverse biological activity.4 The present work includes the synthesis of highly substituted pyrrolidines through double Michael addition reaction of acetylene carboxylate with substituted malonate and amine in one pot results into the cyclisation. This methodology gives substitution pattern on 2, 2, 3,3,5-position of the pyrrolidines Scheme 1 and 3. This strategy is very simple and efficient to have highly substituted nitrogen containing heterocycle as pyrrolidines.

PyrrolidineHeterocyclic compoundamino acid.

238,320 views

71,592 downloads

Contributors:

Nandkishor Chandan

Research PaperID: AJPTR65049

Appraisal of the Anticancer Activity of Various Formulations of Triphala Against Ehrlich Ascites Carcinoma In Mice

Somayeh Afsah Vakili, Ajay George, Syed Fayazuddin

The current investigation was delineated to find out the anticancer activity of three different formulations of Triphala and to find the best Triphala formulation for anticancer activity among the three. Aqueous extracts of Terminalia chebula, Termialia bellerica and Phyllanthus emblica were obtained from Amruta herbals, Indore was dissolved in purified water to make Triphala 1:1:1, 1:2:3, 1:2:4 (F1, F2, F3 respectively) formulation. The number of 1x106 Ehrlich ascites carcinoma (EAC) cell was inoculated in mice. Group I served as untreated negative control while group II was considered as positive control. Group III cancerous animals received standard drug cyclophosphamide 25 mg/kg b.w., whereas group IV to VI cancerous animals were treated with F1 150, 300 and 600mg/kg b.w., group VIII to IX with F2 150, 300 and 600 mg/kg b.w and group X to XII with F3 150, 300 and 600mg/kg b.w., respectively. Different parameter such as change in body weight, determination of survival time, total ascites fluid volume, packed cell volume and haematological parameters were perceived. At the end of investigation, 6 animals from each group were immolated, blood samples were collected and WBC, RBC, Hb content was reckoned. The effect of all three formulations on reduction in body weight, tumor volume, packed cell volume, percentage increase in life span (%ILS) and haematological parameters were compared. The data revealed were suggested that all the three Triphala formulation possessed significant anticancer activity and Triphala 1:2:3 formulation at 600 mg/kg b. w., possessed maximum anticancer activity among the 9 groups compared. Key words: Triphala, Antitumor activity; Ehrlich ascites carcinoma.

TriphalaAntitumor activityEhrlich ascites carcinoma.

238,384 views

71,584 downloads

Contributors:

Somayeh Afsah Vakili

Ajay George

Syed Fayazuddin

Research PaperID: AJPTR65050

Phytochemical and antiulcer potential of ethanolic leaf extract of houttuynia cordta, thumb.

Mrinmoy Basak, Biplab Kr. Dey

Gastric ulcer is one of the most prevalent gastrointestinal disorders, which affects approximately 5-10% of people during their life. In recent years, abundant work has been carried out on herbal medicine to clarify their potential efficacy in gastric ulcer prevention or management. Here, present study was carried out to investigate antiulcer activity of ethanol extract of Houttuynia cordata Thumb. (Family: Saururaceae) leaves in aspirin plus pylorus ligated ulceration in the albino rats. Preliminary ethanol extract of H. cordata was subjected to the phytochemical study. Two dose levels i.e. 250 and 500 mg/kg were selected for the further study. In Aspirin plus pylorus ligation induced ulcer model, various parameters were studied viz. gastric volume, pH, total acidity, free acidity, and ulcer index. Ranitidine at 50 mg/kg was used as the standard drug. Pretreatment of ethanol extract of H. cordata leaves showed significant (P

Antiulcer activityAspirin plus Pylorus ligationUlcer indexPhytochemical screeningHouttuynia cordata.Thumb

238,740 views

71,514 downloads

Contributors:

Mrinmoy Basak

Biplab Kr. Dey

Research PaperID: AJPTR65051

Radiosensitization effect of Selenium on the ''Warburg effect'', Metabolism of hypoxic Oral Squamous cell Carcinoma

Sonaa Elango, Usha Subbiah

One of the hallmarks of oral cancer is its inherent insensitivity to Radiotherapy. We have analysed the tumor metabolites and quantization of biochemical and bioenergetic metabolites by NMR spectroscopic analysis. In this study, trace element selenium exhibit dual nature in oxic and hypoxic conditions as an antioxidant and anticarcinogen respectively, indexing its radiosensitising effect, denoting a remarkable decrease in tumor mass with the gradual disappearance of tumor characteristics and oxidative stress in oral cancer cases undergoing radiotherapy. Dual role of selenium as a radio sensitizer and radio-protector could warrant a significant progress in the cancer patients, as an adjuvant to the conventional therapies in oral cancer management. Key words: Selenium, Free radicals, Oral cancer, Radiosensitisation, Radiotherapy.

SeleniumFree radicalsOral cancerRadiosensitisationRadiotherapy.

238,708 views

71,698 downloads

Contributors:

Sonaa Elango

Usha Subbiah

Research PaperID: AJPTR65052

Anti-Angiogenic Activity of L-Type Voltage Gated Calcium Channel Blocker, Nifedipine: An In-Vitro and In-Vivo Study

Chandana Kamili, K. Ravi Shankar, Uma Maheshwararao Vattikutti

Angiogenesis is the development of new blood vessels. A wealthy number of ion channels are found on the endothelial cells. These ion channels play a vital action in cell proliferation and in related angiogenesis. We aimed to investigate the effects of Nifedipine (L-Type voltage gated calcium channel blocker). The anti-angiogenic activities of Nifedipine was investigated by measuring its effects on number of branches formed, angiogenic score, number of sprouts formed, weight of sponge implanted, Hemoglobin content and histopathological studies by in-vitro (aortic ring assay) and in-vivo (sponge implantation method) methods. The test and standard drug (Bevacizumab) groups were compared with the control group using One-way ANOVA, followed by post hoc test, the Dennett’s test to compare mean of all the groups with the control mean. The results revealed that Nifedipine treatment led to significant inhibition of proliferation and related angiogenesis in the dose dependent manner and were quite comparable with the standard antiangiogenic drug Bevacizumab. These scientific findings indicate the clinical benefits of Nifedipine in pathological situations involving excessive angiogenesis. Negative regulation of cell cycle progression at various checkpoints and cell migration may be the underlying molecular mechanisms for antiangiogenic action.

Angiogenesisaortic ring assaysponge implantation method.

238,851 views

71,674 downloads

Contributors:

Chandana Kamili

K. Ravi Shankar

Uma Maheshwararao Vattikutti

Research PaperID: AJPTR65053

Isocratic RP-HPLC Method Development, Validation and Stability Indicating Studies for Simultaneous Determination of Escitalopram and Clonazepam In the Combined Dosage Form

G.V.Adilakshmi, P.V.V. Satyanarayana

A new rapid, sensitive and precise stability indicating HPLC method was developed on kromasil RP-C18 column (250mm X 4.6mm, 5µm), for the simultaneous analysis of Escitalopram and Clonazepam. Chromatographic separation was achieved at 229nm by using a mobile phase composed of methanol, acetonitrile and phosphate buffer (70: 28: 2, v/v). Retention time of escitalopram and clonazepam were found to be 2.67min and 3.46min respectively. Method validation was done as per the ICH guidelines. Good linearity was established in the concentration range of 50-300µg/ml and 2.5-15µg/ml by escitalopram and clonazepam respectively. Resolution of escitalopram and clonazepam was found to be 5.25. Percentage RSD of precision was found to be less than 2. The percentage assay of escitalopram and clonazepam in commercial formulation was found to be 99.18 and 99.22 respectively. Stability of the molecule was measured by inducing different stress conditions like acidic, basic, peroxide, thermal, light and UV light.

EscitalopramclonazepamHPLC method and stability indicating studies.

238,927 views

71,709 downloads

Contributors:

G.V.Adilakshmi

P.V.V. Satyanarayana

Research PaperID: AJPTR65054

Nephroprotective Activity of Poly Herbal Methanolic Extract Against Gentamicin-Induced Nephrotoxicity and Renal Dysfunction In Experimental Rodents

V.V. Rajesham, Balusu Haarika, DVRN Bikshapathi, T. Rama Mohan Reddy, M.Srinivasa Chandramouli

To evaluate Nephrpotective potential of Polyherbal methanolic extraction (Terminalia chebula, tinospora cordifolia, Phyllanthus emblica, Portulaca oleracea) against gentamicin (GM) induced Nephrotoxicity and renal dysfunction. It was observed that the GM treatment induced significant elevation (P

NephroprotectiveTerminalia chebulatinospora cordifoliaPhyllanthus emblicaPortulaca oleracea.

238,942 views

71,728 downloads

Contributors:

V.V. Rajesham

Balusu Haarika

DVRN Bikshapathi

T. Rama Mohan Reddy

M.Srinivasa Chandramouli

Research PaperID: AJPTR65055

Development of Validated HPTLC Method for the Standardization of Euphorbia Hirta using Gallic Acid, Rutin and Quercetin as Phytochemical Markers

A.Suganthi, N. Ramu, K. Arthi, T.K. Ravi

Euphorbia Hirta belonging to the Euphorbiaceae family contains more amounts of phenolic compounds and flavonoids which are responsible for the main pharmacological actions like anti-oxidant, anti-inflammatory, anti-dengue and anti-cancer. Considering the current importance of these ingredients, an attempt has been made for the simultaneous estimation of gallic acid, rutin and quercetin from euphorbia hirta by successive extraction involves the use of solvents in an order of increasing polarity in soxhlet extractor at 30-45 °C using 800 ml solvents for 5 hours in increasing polarity to isolate the active constituents without other interferences. Hence we proposed to develop easy, rapid, accurate, precise and reliable analytical HPTLC method for the standardization of Euphorbia hirta(L) using gallic acid, rutin and quercetin as phytochemical markers from its methanolic extract and herbal capsule formulation. The separation was performed on TLC aluminum Plates precoated with silica gel 60F254, good separation was achieved in the mobile phase of butyl acetate: 1,4-dioxane (5:5% v/v) and densitometric determination of gallic acid, rutin and quercetin was carried out at 266nm.The linear regression data showed a good linearity in the concentration range of 136-748ng/spot of gallic acid, rutin and quercetin with a good correlation coefficient of 0.9989. Limit of detection was found to be 102 ng/spot of gallic acid,17ng/spot of rutin and 68ng/spot of quercetin. The limit of quantification for the estimation of gallic acid, rutin and quercetin was found to be 136ng/spot.

Euphorbia Hirtagallic acidrutinquercetinmethanolphytochemical markers.

239,361 views

71,788 downloads

Contributors:

A.Suganthi

N. Ramu

K. Arthi

T.K. Ravi

Research PaperID: AJPTR65056

A Review On Isatin and Its Pharmacological Profile

Rekha Pharswan, Meenu Chaudhary

Isatin is an endogeneous and an important class of heterocyclic compound. It possess indole nucleus having both keto and lactam moiety with a diverse pharmacological properties like antimicrobial, antitubercular, anticonvulsant activity etc. Isatin derivatives are synthetically important substrates, which can be used for the synthesis of a large variety of heterocyclic compounds, and as raw material for drug synthesis. Recently, isatin derivatives have attracted strong interest in organic and medicinal chemistry due to their potent biological and pharmacological activities. The purpose of this review is to provide information on the pharmacological activities of isatin and its derivative.

IsatinAntimicrobialAnticonvulsantAnticancerAntitubercularAnti-inflammatory.

239,076 views

71,792 downloads

Contributors:

Rekha Pharswan

Meenu Chaudhary

Research PaperID: AJPTR65057

Antilithiatic activity of Grewia asiatica by Sodium oxalate induced Urolithiatic model

P. Veeresh Babu, M. Vamsi krishna, M. Ganga Raju, P. Venkanna

Grewia asiatica is a plant commonly used as a traditional herbal medicine and possesses the wide range of pharmacological applications. The present study investigated the antilithiatic activity of an ethanolic leaf extract of Grewia asiatica Linn (EEGA). Sodium oxalate (7 mg/100 gm i.p) administration resulted in hyperoxaluria as well as increased urinary volume and its pH. EEGA (200 & 400 mg/kg) was given orally in curative and preventive regimens over a period of 14 days. Supplementation with EEGA significantly (p

Grewia asiaticaSodium oxalateCystoneHyperoxaluria

239,285 views

71,934 downloads

Contributors:

P. Veeresh Babu

M. Vamsi krishna

M. Ganga Raju

P. Venkanna

Research PaperID: AJPTR65058

Preparation and Photochemical Studies of Schiff Base Metal Complexes

Haroon Rashid Boked, Ghulam Mohammad Jan

Fe (III) and Cu (II) metal complexes of Schiff base derived from ethylenediamine, succinic acid and formaldehyd. The newly synthesized Schiff base complexes were characterized by elemental analysis, Melting point, conductivity, IR and UV-VIS spectral methods. The absorption spectrum of CrL displayed only one low energy transition centered at 488 nm, which was attributed to 2A1g→2Eg transition indicating its square planer geometry.

Schiff baseelement analysis

239,660 views

71,891 downloads

Contributors:

Haroon Rashid Boked

Ghulam Mohammad Jan

Research PaperID: AJPTR65059

Synthesis, Surface Morphological Studies and Biological Application of Polymer Supported Metal Complex

Shakeel Ahmad Khanday, Samina Akthar2 M.Y.Peerzada

The polymer supported Cu metal Complex was characterized by some physicochemical and spectroscopic methods like elemental analysis Scanning electron micrographs (SEM) and Energy dispersion spectra (EDS). The complex was tested for their antimicrobial activity against bacteria and fungi. The anti- microbial activity was determined in Mueller Hinton media (M H Media).

Chloromethylated polystyreneenergy dispersion spectraAntimicrobial activity.

239,696 views

71,856 downloads

Contributors:

Shakeel Ahmad Khanday

Samina Akthar2 M.Y.Peerzada

Research PaperID: AJPTR65060

Chemical and Biological Properties of vanadium and Iron compounds in relation to cancer treatment and other Biological Applications- A review

Ab. Rashid Wani, Ghulam Mohammad Jan

Overall, we are convinced that in the future the field of medicinal inorganic chemistry will be a key part of drug development for personalized medicine, allowing also considerable advances in predictive medicine. However, we should also fight against the prejudice associated to metal-based drugs, mostly in terms of in vivo toxicity. Thus, as bioinorganic chemists, we should be able to address the difference between the toxicity related to the “naked”, non-coordinated metal ion, and that of the corresponding metal stabilized by the coordinating ligand(s). Moreover, the toxicity of metal complexes is a multifaceted subject during the development of metal-based drugs as it primarily depends on the type of selected application. In the case of metal-based radiopharmaceuticals for diagnosis or therapy toxicity is not the main matter of concern due to the low concentrations of metal-complexes administered to the patients. In order to exert pharmacological effects (e.g. cisplatin is activated by hydrolysis inside cancer cells), however, further studies are necessary to “fine tune” the stability metal complexes while maintaining their biological activity and reduce their side-effects.

Coordinated metal complexCisplatinToxicityCancer cells.

239,573 views

72,027 downloads

Contributors:

Ab. Rashid Wani

Ghulam Mohammad Jan

Research PaperID: AJPTR65061

Synthesis, Characterization and Mechanism of Catalytic Oxidation of Dendrimer metal Complex

Mir Shabeer Ahmad, Ghulam Mohammad Jan

The unique properties associated with these dendrimers such as uniform size, high degree of branching, water solubility, multivalency, well-defined molecular weight and available internal cavities make them attractive for biological and drug-delivery applications. Commercialization of dendrimers is now forthcoming. A new dendrimeric ligand (L) was synthesized by the Michael addition of ethylenediamine to methyl methacrylate. The prepared ligand was complexed Cu (II) ions, the ligand and its complex were characterized by elemental analysis and spectroscopic studies (FT-IR, UV-Vis, 1H NMR and ESI-MS). Square pyramidal geometry was proposed for copper complexes, on the basis of UV-Vis spectroscopic data and molar conductance measurements. The dendrimer metal complex is active towards the oxidation of alcoholic substrates using molecular oxygen as substrate. The effect of various parameters on the rate of reaction is also explained.

DendrimersMichael additionSquare pyramidalCatalystOxidation

239,900 views

71,948 downloads

Contributors:

Mir Shabeer Ahmad

Ghulam Mohammad Jan

Research PaperID: AJPTR65062

Preparation Characterization and Antifungal Activity of Chitosan Thiozole Metal Complex

Mir Shabeer Ahmad, Ghulam Mohammad Jan, G.M.Mir

In this paper we synthesized a natural polymer based metal complex. The complex were characterize using different spectrochemical techniques like FT-IR, Mass spectroscopy and X-ray diffraction etc. The complex was found to be active towards different fungal, MIC80 was determined in vitro in liquid medium by the macro broth dilution method as per the guidelines of CLSI reference document M27-A3 for fungi, document NCCLS/CLSI M11-A6 for gram negative bacteria, and document CLSI M100-S15 for gram positive bacteria. The order of sensitivity to these compounds was C. albicans > E. coli > S. aureus.

MIC80in vitroX-ray diffractiongram positive bacteria.

239,826 views

71,933 downloads

Contributors:

Mir Shabeer Ahmad

Ghulam Mohammad Jan

G.M.Mir

Research PaperID: AJPTR65063

Drugs Contain Metals – A short Review on the Application of drug Contains Gold

Ab. Rashid Wani, Ghulam Mohammad Jan

Pharmaceutical Chemistry combines knowledge of the biological, medical, and physical sciences in the study of the scientific aspect of drug therapy. The emphasis is on the chemical nature of the reactions and interactions involved in drug therapy. The students will receive a solid background in the aspects of chemistry the most relevant to drugs: physical, organic, and analytical chemistry. They will also learn the fundamental aspects of the synthesis, manufacture, use, and mode of action of drugs. Pharmaceutical drug, also referred to as a medicine or medication, can be loosely defined as any chemical substance - or product comprising such - intended for use in the medical diagnosis, cure, treatment or prevention of disease.

Biological MedicalPhysical ScienceDrugsDisease

240,108 views

72,035 downloads

Contributors:

Ab. Rashid Wani

Ghulam Mohammad Jan

Research PaperID: AJPTR65064

Preparation, Morphological and Thermal Study of Cysteine Amino acid Metal Complexes

Ghulam Mohammad Jan, Fayaz Ahmad Bhat, Haroon Rashid Boked

The Complexes of Mn (II) and Cr (II) with amino acid cysteine were synthesized and Characterized by elemental analysis, SEM, TGA. In these complexes the amino acid coordinated to 1:2 with metal and they exhibits octahedral geometry. The catalytic activity of these complexes was studied in olefins using eco-friendly nontoxic molecular oxygen as oxidant.

Amino acidMetal complexescysteineMolecular Oxygen.

240,091 views

72,051 downloads

Contributors:

Ghulam Mohammad Jan

Fayaz Ahmad Bhat

Haroon Rashid Boked

Research PaperID: AJPTR65065

Catalytic Oxidation of Phenols, Benzyl alcohols and Olefins using Schiff Base Metal Complexes- A review

Fayaz Ahmad Bhat, Ghulam Mohammad Jan, Haroon Rashid Boked

There are a large number of important organic transformations such as oxidation, hydrogenation, hydroformylation, carbonylation, polymerization and various coupling reactions. The majority of these novel catalysts are based on silica, primarily since silica displays many advantageous properties excellent stability (chemical and thermal), high surface area, good accessibility, and organic groups can be robustly anchored to the surface, to provide catalytic centers. In this study we only discuss the catalytic application of schiff base metal complexes in the field of oxidation of phenol, benzyl alcohol, olefin etc

High surface areagood accessibilityexcellent stabilitycatalytic centersbenzyl alcohololefin

240,479 views

72,057 downloads

Contributors:

Fayaz Ahmad Bhat

Ghulam Mohammad Jan

Haroon Rashid Boked

Research PaperID: AJPTR65066

Ingestion Effect of pathogens on Primary Metabolites of Tinospora cordifolia.

Abhimanyu Sharma1* and Amla Batra

Plants play many important roles in the environment. Not only do they provide us with food and useful products, but also they play a main role in maintaining the ecological balance of nature, the food chain and the natural cycles and also have medicinal value. Laboratory evaluations were made to assess the study of primary metabolites of Tinospora cordifolia, belongs to the family menispemeacae. It contains chlorophyll, sugars, starch, protein, ascorbic acid and phenols in, leaves, stem, root and callus of the plant. Levels of plant metabolites are strongly affected via genetic and environmental factors. Different types of pests’ are causing changes in plant metabolite production. The results revealed the evidence of different infestation of the plant by common herbivores. In this manuscript we report primary metabolites of the Tinospora cordifolia along with the quantification after the pests’ effect.

Tinospora cordifoliamenispemeacae ChlorophyllProteinAscorbic acidsugarstarch and callus.

240,704 views

72,083 downloads

Contributors:

Abhimanyu Sharma1* and Amla Batra

Research PaperID: AJPTR65067

Inclusion of Diacerein with cyclodextrin carriers: Preparation, physicochemical characterization, cytotoxicity assessment and pharmacological evaluation

Abhishek Pathak, Sadhana J Rajput

The present investigation aims on the preparation and in-vitro/in-vivo examination of inclusion complex of Diacerein (DAR) an anthraquinone derivative indicated for treatment of osteoarthritis by inhibiting interlukin-1 and hydroxypropyl-β-cyclodextrin (HP-β-CD). In this study, the inclusion complexes of DAR with β-cyclodextrin (β-CD), HP-β-CD, methyl-β-cyclodextrin (M-β-CD) and γ-cyclodextrin (γ-CD) were prepared and characterized for phase solubility study and inclusion efficiency. On the basis of results obtained, HP-β-CD was selected to prepare inclusion complexes with DAR by physical mixing, kneading method and freeze drying method and subjected to solid state characterizations. Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD) and Infra-red spectroscopy (IR) analysis confirmed the formation of perfect inclusion complex of DAR with HP-β-CD in solids. In-vitro dissolution and % drug content of DAR in freeze dried inclusion complex showed its superiority over plain drug and commercial formulation. . In-vitro cell cytotoxicity studies (MTT Assay) using Caco-2 cell line model confirmed the bio-tolerability of DAR-inclusion complex. . The relative oral bioavailability of DAR in Albino rabbits resulted from Freeze dried inclusion complex was found 3.32 fold and 2.03 fold greater than plain DAR and marketed formulation, respectively which ultimately demonstrated the enhancement of oral bioavailability of DAR in freeze dried inclusion complex with HP-β-CD.

Inclusion complexDiacereincyclodextrincytotoxicitybioavailability

240,525 views

72,113 downloads

Contributors:

Abhishek Pathak

Sadhana J Rajput

Volume 16, Issue 1Current

2026 • 6 articles

Volume 15, Issue 6

2025 • 17 articles

Volume 15, Issue 5

2025 • 15 articles

Volume 15, Issue 4

2025 • 10 articles

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Editorial: October 2016 Issue 5

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