β
Explore 18 research publications tagged with this keyword
Publications Tagged with "β"
18 publications found (showing 1-10)
2017
2 publicationsDevelopment and validation of a method for densitometric analysis of umbelliferone, β-sitosterol and methoxsalen in polyherbal formulation
Herbal medicines are generally available as a mixture of more than one plant constituent. It is important to quantify the maximum possible number of markers in such herbal formulations by which the quality of the formulations may be assessed. TLC densitometric methods were developed using High performance thin layer chromatography for the quantification of the three marker compounds, umbelliferone, β-sitosterol and methoxsalen, from the polyherbal tablet formulation. Solvent systems were optimized to achieve best resolution of the marker compounds from the other components of the sample. From the various solvent systems tried, the one containing toluene: ethyl acetate: methanol: formic acid (3: 3: 0.2: 0.8) gave best resolution of umbelliferone (Rf=0.35), β-sitosterol (Rf=0.47) and methoxsalen (Rf=0.6) in the presence of the other compounds in the polyherbal tablet sample and enabled the quantification of the marker compounds. The methods were validated in terms of precision, repeatability and accuracy. The method was found to be suitable for the quantification of these marker compounds in polyherbal formulation.
Novel Synthetic Unnatural β3 aminoacids via acid hydrolysis of diazepinones as Synthons for Antibiotics
A convenient two-step method for the preparation of β3-amino acids is described.  This paper describes an efficient and straightforward two-step synthetic sequence leading in excellent yields to a relatively inaccessible lipophilic β3-amino acids with antimicrobial potential  from easily available starting materials. Schmidt reaction of substituted piperidin-4-ones with HN3 generated in situ afforded the corresponding diazapinones. Acid hydrolysis of chosen diazapinones yielded β3-amino acids. Selective cleavage of only the lactam bond is achieved using 4N HCl-MeOH (1:1) mixture  leading to the formation of N-alkyl β3-amino acids in quantitative yields. synthesized aminoacids are subjected to antimicrobial activity for gram positive, gram negative bacteria, fungi. compounds 3e & 3h possess excellent antimicrobial and antifungal activity comparable to standard streptomycin and ketoconazole. Therefore obtained β3-amino acids serves as a scaffold for synthetic antibiotics as they have desired structural moieties necessary for antibiotic action. Further refinement of the β3-amino acids  using either conjugation or structural modification or incorporation of these aminoacids into synthetic peptides would bring about excellent antimicrobial activity.
2016
3 publicationsMicrobial Enzymatic Activity in some Marine Sites of the North Mediterranean sea Coast of Egypt
Microbial enzymatic activities of α- Amylase and β- Galactosidase enzymes were measured seasonally in marine water samples that were collected from two sites located at the south Levantine Sea basin of the Mediterranean Sea of Egypt, Port Fouad city in the east and Alexandria city in the west during four successive seasons from autumn 2014 to summer 2015. Determination of microbial enzymatic activities were carried out by determining reducing sugars using DNS reagent. This research provided a newly applied method for the determination of microbial enzymatic activities in natural open water system, the Mediterranean Sea. The applied methodology involved using marine water samples as the source of crude enzyme , eliminating the difficulties of extracting an enzyme from specific microorganism as well as avoiding the adjustment of aseptically required conditions for the inoculation and incubation of the desired microorganism in culture media tube under the laboratory conditions while providing almost natural conditions for the microbial community represented in water samples. The water samples were chemically analyzed to determine the effect of certain metal ions concentrations on the enzymatic activities of the microbial α- Amylase and β- Galactosidase enzymes. The results showed that though water samples were collected from the same marine source yet, spatial variations occurred between the two sampling sites and seasonal variations at the same sampling sites which were attributed to the naturally occurring environmental variations during the different seasons of the year.
Wnt/β-Catenin As Anticancer Drug Target
Wnt /β-catenin signaling plays an important role in tumor cell dedifferentiation and proliferation. Wnt proteins are a family of secreted glycoproteins. Abnormal activation of wnt signaling results in tumor progression. Wnt proteins binds to the frizzled receptors and LRP5/6 co-receptors and through the stabilization of β-catenin a critical mediator, initiates a complex signaling cascade that plays an important role in regulating cell proliferation and differentiations. The elevated levels of oncogenic protein-β-catenin have been observed in many of the human cancers, indicating that this pathway plays an important role in tumor development. The wnt signaling can be inhibited at the extracellular level, at regulatory protein level and also by targeting the expressions of β-catenin by protein knockdown and by targeting the downstream mediators of β-catenin signaling such as c-myc, cyclin D1, PPARS and COX-2. In this review we discuss the effects of NSAIDS and flavanoids that are being used or explored to target the β-catenin signaling in the treatment of cancers.
Novel Validated HPLC Method Development for Simultaneous Analysis of Curcumin and β-Boswellic Acid
A simple, rapid and specific High performance liquid chromatography (HPLC) method has been developed for simultaneous analysis of Curcumin and β-Boswellic acid in a prepared polyherbal gel formulation containing turmeric and boswellia extracts. High performance liquid chromatography analysis was performed on a C18 column using 90:10 (v/v) mixture of acetonitrile and water as isocratic mobile phase at a flow rate of 1 ml/min. Ultra violet detection was set at 425 nm for Curcumin and 242 for β-Boswellic acid. The method was validated for accuracy, precision, linearity, specificity and sensitivity in accordance with International Conference on Harmonization guidelines. Validation data reveals that the method is specific, accurate, precise, reliable and reproducible. Good linear correlation coefficients (r2>0.9993) were obtained for calibration plots in the range tested. Limit of detection for Curcumin was 0.16 µg/ml and limit of quantification was 0.50 µg/ml while for β-Boswellic acid limit of detection (LOD) and limit of quantification (LOQ) were found to be 3.3 and 9.9 µg/ml respectively. Recovery was found to be between 98.75 to 99.01 % for Curcumin and from 98.72 to 100.01 % for β-Boswellic acid. The established HPLC method is appropriate and the two selected markers are well resolved, enabling efficient quantitative analysis of Curcumin and β-Boswellic acid. The method was successfully used for quantitative analysis of these two marker constituents in an in-house prepared polyherbal gel formulation. Key word: HPLC, Simultaneous analysis, Polyherbal gel formulation, Curcumin, β-Boswellic acid
2015
1 publicationAntipyretic Activity of β -Sitosterol Isolated from Leaves of Oxalis Corniculata LINN.
Oxalis corniculata Linn. (Oxalidaceae) is one of the important medicinal plants used traditionally for the treatment of fever, pain and inflammation. The present study was aimed to screen antipyretic activity of petroleum ether, chloroform, ethyl acetate, methanol extracts and β-sitosterol isolated from petroleum ether extract of Oxalis corniculata Linn. The leaves of Oxalis corniculata Linn. was used for successive extraction with increasing polarity solvents. Petroleum ether extract was selected for activity-guided fractionation to isolate β-sitosterol due to its better efficacy than other extracts. Antipyretic activity was done by yeast induced pyrexia method. All the extracts were screened at the dose of 100 mg/kg, i.p. and isolated β-sitosterol was screened at the dose of 10 and 20 mg/kg. The result showed that after five hour of petroleum ether extract (100 mg/kg) administration significant inhibition of pyrexia up to 89.5% was observed. Isolated β-sitosterol 10 and 20 mg/kg, i.p. showed promising antipyretic activity with inhibition of pyrexia by 91.23 and 94.41% respectively. Results are compared with standard drug paracetamol (50 mg/kg i.p.). Thus the present pharmacological screening provides support for the folklore claim of antipyretic activity of Oxalis corniculata Linn.
2014
2 publicationsPreparation and Evaluation of Cyclodextrin based Atorvastatin Nanopsonges
Cyclodextrin nanosponges are solid, porous, bio-compatible, nano-particulate three dimensional structures which form inclusion complexes with different types of lipophilic or hydrophilic drug molecules and have been used as drug carrier for different drugs. In this present work, new cyclodextrin-based nanosponges of atorvastatin were prepared by condensation polymerization and interfacial polymerization to release Atorvastatin in expected manner in the treatment of dyslipidaemia as novel carriers. Results of encapsulation efficiencies of all formulation trials revealed that condensation polymerization is the best method for nanosponges formation and that is considered as best selected method for preparation. For the selected condensation polymerization, encapsulation efficiencies of atorvastatin in nanosponge formulations were found to be 72 to 86%. SEM images revealed their porous nature and cavity was of β-cyclodextrin. The mean particle size of nanosponges was about 328 nm and Zeta potentials of the nanosponges were sufficient enough (-10 to -15mv) due to presence of carboxylic group and inclusion complex formation which assured stability of formulations. The results of FTIR and DSC confirmed that atorvastatin was compatible with β-cyclodextrin and completely encapsulated in nanosponges structure respectively. The selected formulation produces good dissolution profile (release more than 75% atorvastatin within 60 mins in 0.1 N HCL) which indicated that the solubility of atorvastatin was improved by forming nanosponges. In accelerated stability studies, no significant changes occurred in physical appearance and drug content of atorvastatin nanopsonges formulation during 3 months stability studies. Atorvastatin nanosponges confirmed by insolubility in water and organic solvents like dimethyl formamide, dichloromethane.
The Analysis of Virulence Factors and Β-LACTAMASE Production In Clinical Isolates of Staphylococcus Aureus
Staphylococcus aureus is associate with variety of clinical infections in various communities and healthcare institutions both in developed and developing countries. It produces extracellular enzymes like lipase, protease and lecithinase that degrade lipid, proteins present in the skin environment. Study was conducted to associated virulence factors in clinical isolates of S. aureus and to evaluate the incidence of β lactamase production. It comprised 271 clinical samples (pus from surgical, burn, ulcer, abscess and sputum from hospitals of Allahabad. S. aureus was isolated and identified by conventional culture followed by biochemical tests including coagulase test. β-lactamase test and antibiotic susceptibility tests were performed for all isolates. Among 59 isolates of S. aureus, coagulase, carotenoid pigment, haemolysis, lipase, lecithinase and protease activity was examined to be in 59 (100%), 55(93.22%), 51 (86.44%), 23 (39.98%), 25 (42.37%) and 19 (32.2%) respectively. Secretion of lipase, protease and lecithinase were insignificantly related to each other as well as bacterial isolates from different sample type. Regarding 43 (72.89%) penicillin resistant isolates, 31(72.09%) were β-lactamase producers and of 20 (33.89%) methicillin resistant S. aureus (MRSA), 14 (70%) were β-lactamase producer. β-lactamase production was analyzed to be statistically significant for penicillin but not quite significant for methicillin resistant S. aureus (χ2=24.30, P>0.05 for penicillin and χ2=3.7, P=0.054 for methicillin). Positive correlation occurs between β-lactamase production and resistance to other antibiotics included in the study (R=0.97).It seems no variation in the liberation of virulence detecting enzymes among S. aureus. Even if penicillin resistance majorly results due to β-lactamase, methicillin resistance shares some other mechanism of resistance.
2013
2 publicationsDesign and Characterization of Sublingual Tablets of Prochlorperazine Maleate by Natural and Synthetic Superdisintegrants
Sublingual administration of the drug is known as placement of the drug under the tongue and drug reaches directly in to the blood stream. The concept of formulating sublingual tablets of Prochlorperazine maleate offers suitable and practical approach in serving the desired objective of faster disintegration and dissolution characteristic. Bitter taste of Prochlorperazine maleate was masked by inclusion complex with β-cyclodextrin and then sublingual tablets were prepared using various natural superdisintegrants such as hibiscus-rosa and fenugreek and synthetic superdisintegrants like Indion 414 and kyron T-314 in different concentrations by direct compression method. Prepared tablets were subjected to different evaluation parameters such as hardness, thickness, friability, weight variation, drug content uniformity, in-vitro disintegration time, water absorption ratio, wetting time, in vitro dissolution studies and stability studies are carried out by using best formulation. Overall, formulation F3 (10 mg of Indion 414) and F9 (10 mg of Hibiscus-rosa) based on disintegration time, wetting time and drug release were found to be an excellent formulations. Hence It was found that there was no significant difference between F3 and F9, which shows that natural superdisintegrants (10 mg of Hibiscus rosa) is as good as synthetic superdisintegrants (10 mg of Indion 414). Hence it proves that synthetic disintegrant can be replaced by natural disintegrants due to easy availability and compatibility.
Characterization of Marine streptomyces sp. T1027 Producing β-Carotene Under Light Induction
Marine Streptomyces sp.T1027 obtained from South coast of India was discovered to produce and accumulate β-carotene under the influence of light in liquid shake flask culture. The accumulation of β-carotene was growth associated and controlled by light, aeration, carbon and substrate solubility. Starch was the ideal substrate for maximum growth (4.5-6.1 g l-1) and β-carotene accumulation (92-130 μg g-1). Rapid extraction was done in Dimethylsulphoxide, Methanol (1:1) Solvent mixture. The organism was sensitive to a variety of antibiotics; in turn it was able to inhibit the human pathogen Corynebacterium diphtheria. Commercial substrates with high soluble starch content were found to produce maximum biomass and β-carotene production.
