Chalcones afford a facile route of access to many of the heterocyclic systems containing oxygen and nitrogen. An attempt is therefore made to synthesize chalcones from 3-acetylpyridine by reaction with either aromatic or heteroaromatic aldehyde using Claisen-Schmidt condensation. The resulting chalcones after purification and characterization by physical and spectral methods have been successfully converted into substituted pyrimidines by reaction with guanidine hydrochloride. All these compounds were characterized by means of their IR, 1 H NMR, 13 C NMR and mass spectral data. These compounds were evaluated for antimicrobial activities by cup plate method.

Purpose: The purpose of the study was to develop and optimize rosiglitazone maleate mucoadhesive extended-release tablets by quality by design (QbD) approach. Based on QTPP (quality target product profile) CQAs (critical quality attributes) were identified. Methods: Failure mode and effects analysis (FMEA) method were adopted for risk assessment. Risk analysis by the evaluation of formulation and process parameters showed that the optimizing the levels of polymers could reduce high risk to achieve target profile. Drug-excipient compatibility studies by Fourier transforms infra-red and DSC studies showed that the drug was compatible with the polymers used. Design of experiment (DoE) performed by Sigma tech software, Carbopol 934P and sodium carboxymethyl cellulose (SCMC) were identified as independent variables and hardness, drug release at 12 hours and ex vivo mucoadhesion time were adopted as responses. Contour plots generated from the software were used for identification of design space. Results: Carbopol 934P and SCMC had positive and negative effects respectively on the selected responses. Higher the concentration of Carbopol 934P and lower the concentration of SCMC mucoadhesive extended release criteria could be achieved. Drug release kinetics followed first order release with Higuchi diffusion and Fickian diffusion. Ex vivo mucoadhesion test on goat stomach mucosa indicated that adhesion time increased at higher concentrations of Carbopol 934P. Optimized formula satisfying all the required parameters was selected and evaluated. The predicted response values were in close agreement with experimental response values, confirmed by calculating standard error. Conclusion: It has been concluded that the application of QbD in the optimization reduced the number of trials to produce a cost-effective formula.

No abstract

No abstract

No abstract

Introduction: Caralluma adscendens var. attenuata (Wight) Grav. and Mayur., a member of Apocynaceae, is a perennial stem succulent plant with wide distribution in tropics and subtropics of the world. This plant is reported for the presence of steroids, flavonoids, saponins, triterpenes, and pregnane glycosides, and is known to have antidiabetic and antiulcerogenic properties. Materials and Methods: In this study, an attempt was made to identify antioxidant capacity and cytotoxic potential of n-hexane and aqueous methanolic extracts of total stem part of C. adscendens var. attenuata . Antioxidant activity was evaluated by total phenolic content assay, total flavonoid content assay, free radical scavenging activity, and reducing ability methods. Cytotoxic activity was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) assay and nuclear staining methods for colorectal cancer cell lines HT29 and liver cancer cell lines HepG2. Results: MTT assay method has proven that the IC50 value was 10 μg/mL for both extracts, whereas for cisplatin standard, it was 2 μg/mL. By nuclear staining, the apoptotic cells were identified as oval masses with dark cytoplasm and dense green nuclear chromatin fragments indicating the programmed cell death for both n-hexane and aqueous methanolic extracts at the same concentration (10μg/mL). Conclusion: However, aqueous methanolic extract showed prominent cytotoxic potential against both cancer cell lines.

Objectives: Alzheimer's disease is a leading neurodegenerative disorders having serious effect on an individual's occupational potential and quality of life. The natural and nutritional based remedy is continuing interest for neurological disorders; hence an attempt was made to reveal memory enhancing potential of commonly available fruits, by applying the molecular docking studies. Methods: The study was conducted in aluminium chloride induced Alzheimer's Wistar albino rats for the period of 28 days. The oral administered animal groups with ethanolic extracts of peels of ripped banana and papaya (200 and 400 mg/ kg, p.o) is comparatively evaluated with positive control rats (donepezil, 1mg/kg. p.o) by behavioural studies like pole climbing test and elevated plus maze test, biochemical and histopathological parameters. Further, interaction of selected leads of banana and papaya peel with selected targets were analysed by Schrodinger Glide software. Results: Memory enhancing effects of peels was supported by shortening of transfer latency (elevated plus maze), increased number of escapes (cooks pole climbing), enhancement of brain tissue antioxidant defensive enzymes such as SOD, Catalase, GSH, reduction of activity of acetylcholine esterase and improvement of histopathological changes. Memory enhancement effect further observed by best docking score and glide energy of selected leads with targets of Alzheimer's disease such as beta secretase and acetylcholine esterase. Conclusion:On the basis of the present study, the results revealed that peel extracts of papaya and banana and used as adjuvant which shows anti-Alzheimer's disease.

Objectives: Atherosclerosis is caused by vascular inflammation and oxidative stress. Pro-atherogenic effect of hypercholesterolemia caused by impairment of nitric oxide generation due to activated arginase. The current study was wanted to explore the atheroprotective effect of polyphenolic fraction of Rivea ornata by using lipid emulsion induced atherosclerosis in rat model. Materials and Methods:The study carried out by studying atherogenic markers in the serum (lipid profiles, C-reactive protein), vascular tissue (myeloperoxidase, arginase, hydroxyproline, lipid peroxidation) and atheroprotective factors in the serum (paraoxonase, nitric oxide,) and in the vascular tissue (thiol levels, endogenous antioxidants) after feeding the rats with lipid emulsion for 12 weeks. Results: Treatment of polyphenolic rich butanol fraction is able to correct the imbalance of atherogenic and antiatherogenic factors induced by lipid emulsion feeding. Butanol fraction at the dose of 400 mg/kg significantly increases HDL, paraoxonase, nitric oxide, tissue thiol levels, endogenous antioxidants and decreases TG, TC, VLDL, LDL myeloperoxidase, arginase, hydroxyproline, lipid peroxidation. And atheroprotection reflected in histopathology studies also. Lipid emulsion associated foam cells formation is inhibited by butanol fraction. Conclusion: This is all due to presence of gallic acid in polyphenol rich butanol fraction is responsible for the underlying mechanism of atheroprotection.