Ravi

To establish a comparative account within the taxa by assessing its anti-oxidative property and mapping it with the morphometric characters. The methanolic leaf extracts of 12 Cassia L. species were screened for their antioxidant activity using 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging assay and reducing power capability with reference to standard Ascorbic acid. Chamaecrista kleinii exhibited strong antioxidant activity with IC50 2.17 µg mL-1, followed with Senna auriculata (IC50 11.51 µg mL-1) and Senna polyphylla (15.17 µg mL-1). Highest reducing ability was observed in Senna auriculata extract with 0.676 nm absorbance. The correlation observed between the reducing power and DPPH radical scavenging assay supports the contribution of the phytoconstitutents like phenolics and flavonoids towards managing oxidative stress. The present study reveals the beneficiary effects of the selected plants by virtue of their antioxidant activity that can be harnessed in drug formulations. Keywords: Antioxidant, 1, 1-diphenyl-2-picryl hydrazyl, reducing power, Cassia.

Bortezomib is formulated as the solid lipid nanoparticle (SLN) system with the use of a 3-factor, 3-level Box–Behnken design, by hot homogenization followed by an ultra sonication method. Trimyristin (Dynasan-114), tripalmitin (Dynasan116) and tristearin (Dynasan-118) were used as lipids and based on the results from the initial studies tripalmitin (Dynasan116) was selected as the lipid for the further studies along with phosphate dylcholine as surfactant and Poloxamer 188 as stabilizer. The optimized formulation (F1) was obtained with minimum particle size (204 nm), maximum entrapment efficiency (70.24) and drug loading (21.24). In vitro release studies showed that maximum cumulative drug release was obtained for F1 (99.74%). The optimized formulation Bortezomib followed zero-order release kinetics with a strong correlation coefficient (R2= 0.9994). The pharmacokinetic studies in rabbits demonstrated that SLN formulation could be used for increasing the oral bioavailability of the drug for more than 2 fold when compared with pure drug. SLNs of Bortezomib were successfully developed to yield an optimized formulation with lowest particle size and highest entrapment efficiency that could sustain the release of drug. Key words: Bortezomib, SLN, Cancer, Tripalmitin, Box-Behnken design, Pharmacokinetic studies.

Atorvastatin calcium is a HMG-CoA reductase inhibitor used in the treatment of hyperlipidaemia. It has oral bioavailability of less than 12%. It also undergoes high first pass metabolism. The objective of the present work was to formulate, optimize and in vivo evaluation of the potential novel proniosomal gel containing atorvastatin for transdermal delivery. On the basis of the preliminary trials a 3-factor, 3-level Box–Behnken design was employed to study the effect of Cholesterol, soya lecithin and Span 60 independent variable on dependent variables (particle size and % entrapment efficiency). Atorvastatin optimized proniosomal formulation F2 shown better particle size and % entrapment efficiency and also the drug release was 99.72% within 24h in slow and controlled manner when compared with control. The particle size and Zeta potential of the optimized atorvastatin proniosomal gel was found to be 65.72 and -10.5 respectively. Optimized batch of Proniosomes was used for the preparation of Atorvastatin - based proniosomal hydrogel by incorporating hydrated Proniosomes to Carbopol matrix to enhance the stability and viscosity of the system. The enhanced skin permeation for prolonged period of time, may lead to improved efficacy and better patient compliance. From in vivo studies the maximal concentrations (Cmax) of drug was significantly reduced while the areas under the plasma concentration–time curve (AUC) and t1/2 were evidently increased and extended. This study suggests that proniosomal gel of atorvastatin would be a promising alternative to improve the bioavailability problems of atorvastatin.

Cefixime, cefpodoxime and cefepime are cephalosphrin antibiotics used widely in the different infectious diseases. Newer HPTLC methods were developed for their estimation from individual dosage forms due to versatile applications and advantages. The HPTLC chromatogram of cefixime was developed by using a mobile phase ethylene acetate: methanol: water (4.5:5:0.5%v/v) and scanning wavelength was 292nm. The Rf value was 0.58±0.02. The mobile phase optimized for cepodoxime was methanol: ethyl acetate: toluene (1.5:3:5.5% v/v), with the Rf value 0.53±0.02. The cefixime was retained using methanol :water : chloroform (6:3:1%v/v), on a  silica gel G60 F254 aluminium sheet and  scanning wavelength kept at 285nm. The Rf value was 0.44. The methods were optimized validated as per guidelines and successfully applied for individual dosage form containing  of each of cephalosporin.

Synthesis of phenyl (5-substituted phenyl-1,3,4-thiadiazol-2-yl) methanediamine (TDZ-A to TDZ-C), reaction between aryl aldehydes and Thiosemicarbazide yielded thiosemicarbazone. Thiosemicarbazone in the presence of citric acid and sodium acetate gives 2-amino-5-aryl -1,3,4-thiadiazole, which is treated with aniline in the presence of formaldehyde to obtained targeted compounds phenyl(5-substituted phenyl-1,3,4-thiadiazol-2-yl)methanediamine. The synthesized Thiadiazoles have been characterized on the basis of analytical spectral data. The resulted compounds were screened for their antibacterial, antifungal and antioxidant activities.

Present report is the successful synthesis, spectral characterization and in-vitro antimicrobial evaluation of a series of azomethine and novel 2-azetidinone derivatives. Two cyanoethylated tertiaryaminobezaldehydes A and B were prepared by cyanoethylation of the corresponding aromatic primary amines followed by formylation in presence of POCl3 and DMF. These cyanoethylated tertiaryaminobenzaldehydes on condensation with different aromatic primary amines afforded azomethines SB1-SB14, which on cyclization with chloroacetylchloride and triethylamines in 1,4-dioxan gave new 2-azetidinone BL1-BL14. All compounds were prepared by reported methodology and characterized by elemental analysis, FT-IR and 1HNMR data. Further screened in-vitro for antimicrobial activity against S. aureus, B. subtilis, P. vulgaris, E. coli, A. niger and A. fumigatus. Most of the compounds showed significant activity against tested pathogens. The work shows the emergence of a new series of compounds in the field of antimicrobials.

Alzheimer’s disease is a degenerative brain disease and the most common cause of dementia. Dementia is also caused by other diseases and conditions. it is characterized by decline in memory , language , problem solving and other cognitive skills that effects a person’s ability to perform everyday activities. This decline occurs because nerve cells (neurons) in parts of the brain involved in cognitive function have been damaged and no longer function normally , In Alzheimer’s neuronal damage eventually affects parts of the brain that enable a person to carry out basic bodily functions such as walking and swallowing . People in the final stages of the disease are bed-bound and required around  the-clock care .Alzheimer’s disease is ultimately fatal.1

Arbutin and quercetin are anti-cancer agents, extracted from leaves and flowers of Origanum majorana L which can be simultaneously estimated using a rapid, specific and sensitive high – performance thin layer chromatographic technique using silica gel G60F254 as the stationary phase and butyl acetate: methanol: formic acid: toluene (8: 1.5: 5: 0.5) as mobile phase for the separation. The method was validated for linearity, precision and recovery. Linearity was established in the range 300-900 ng/spot for arbutin and 150-450 ng/spot for quercetin, respectively. The % RSD values of repeatability of application, repeatability of measurement, intra-day and inter day precision studies of arbutin and quercetin were found to be below 1 for 500 and 250 ng/spot of arbutin and quercetin, respectively. The recovery of the drugs were found to be 99.8 and 100.2%, proves that the developed method was highly accurate. Hence the proposed validated method could be applied for the simultaneous analysis of arbutin and quercetin in methanolic extract of Origanum majorana L as well as for its marketed formulation.

The substituted chalcones (C1-5) was prepared by reaction of acetophenone (a) and aromatic aldehydes (b1-5). One series of N-phenyl pyrazoline analogues (K1-K5) were synthesized by reaction of the substituted chalcones (C1-5) with phenyl hydrazine in acidic medium. Another series of 3, 4-dihydropyrimidine-2-one analogues (K6-K10) were synthesized by reaction of substituted chalcones (C1-5) with ethanolic urea in alkali medium. The yield of the synthesized analogues ranged from 62-76%. The structures of the synthesized analogues were verified by FTIR,1H-NMR, mass spectral data and physical analysis. The structures of the synthesized heterocyclics are correlated with the spectral analysis and the synthesized heterocyclics structures are well agreed with the proposed structure.

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.