Pharmaceutical Sciences and Natural Products - Research Publications
Permanent URI for this collectionhttps://kr.cup.edu.in/handle/32116/56
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Item Cucumis melo Var. agrestis Naudin as a potent antidiabetic: Investigation via experimental methods(Elsevier B.V., 2022-09-06T00:00:00) Yadav, Jagat Pal; Singh, Ankit Kumar; Grishina, Maria; Pathak, Prateek; Patel, Dinesh KumarBackground: The present study reveals that the ethanolic extract of Cucumis melo var. agrestis (CMVA), can influence the activity of blood glucose level, insulin level, oxidative stress, and lipid profile in Alloxan monohydrate induced diabetic rats. Methods: Wistar albino rats were randomly divided into five groups (n=6), viz. Normal control (non-diabetic), diabetic control (alloxan induced), diabetic treated group (infused with doses 250 and 500 mg/kg b.w) of CMVA ethanolic extract, and standard treated diabetes (infused with pioglitazone 1 mg/kg b.w). Diabetes was induced by administration of alloxan monohydrate (150 mg/kg i.p). The ethanolic extract of CMVA was supplemented orally in different doses for 45 days. Biochemical investigations as well as histopathological examination were carried out accordingly. Results: The diabetic rats supplemented with CMVA significantly decreased blood glucose levels in a dose dependent manner (#p < 0.001). The plasma insulin level was found significantly increased in rats treated with CMVA. However, in CMVA treated group, the oxidative stress parameters (such as SOD, CAT, GSHpx and GSH) and lipid parameters were restored up to normal level (#p < 0.001). Histopathological studies showed that the microscopic architecture of pancreatic cells were improved in CMVA treated groups. Conclusion: The research illustrated that CMVA has potent antidiabetic as well as antioxidant activity along with hypolipidemic effect. Therefore, active phyto-compounds of the selected plants can be isolated and further formulation can be develop in near future. � 2022Item Synthesis, biological evaluation and in-silico ADME studies of novel series of thiazolidin-2,4-dione derivatives as antimicrobial, antioxidant and anticancer agents(BioMed Central Ltd, 2022-09-15T00:00:00) Kumar, Harsh; Kumar, Davinder; Kumar, Pradeep; Thareja, Suresh; Marwaha, Minakshi Gupta; Navik, Umashanker; Marwaha, Rakesh KumarBackground: A novel series of thiazolidine-2,4-dione molecules was derived and their chemical structures were established using physiochemical parameters and spectral techniques (1H-NMR, IR, MS etc.). The synthesized molecule were then evaluated for their antioxidant, anticancer and antimicrobial potential. Results and discussion: Serial tube dilution method was employed to evaluate the antimicrobial potential against selected fungal and bacterial strains by taking fluconazole and cefadroxil as reference antifungal and antibacterial drugs respectively. 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity was used to assess the antioxidant potential of the synthesized analogues. Further, the anticancer potential of the selected molecules was assessed against DU-145 cancer cell lines using MTT assay. The drug-likeness was also evaluated by studying in-silico ADME parameters of the synthesized analogues. Conclusion: In antioxidant evaluation studies, the analogue H5 with IC50 = 14.85�?g/mL was found to be the most active molecule. The antimicrobial evaluation outcomes suggested that the molecules H5, H13, H15 and H18 possessed moderate to promising activity against the selected species of microbial strains having MIC range 7.3��M to 26.3��M. The results of anticancer evaluation revealed that all the screened derivatives possess mild anticancer potential. The in-silico ADME studies revealed that all the compounds were found to be drug-like. � 2022, The Author(s).Item Synthesis and xanthine oxidase inhibitory activity of 5,6 dihydropyrazolo/pyrazolo[1,5-c]quinazoline derivatives(Elsevier, 2014) Kumar, Deependra; Kaur, Gagandeep; Negi, Arvind; Kumar, Sanjeev; Singh, Sandeep; Kumar, RajSome 5,6-dihydropyrazolo/pyrazolo[1,5-c]quinazoline derivatives were rationally designed, synthesized and evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Some notions about structure activity relationships are presented. The compounds 6g, 6h and 6e were found to be significantly active against XO. The compound 6g emerged as the most potent XO inhibitor as compared to allopurinol and free radical scavenger. The molecular docking of 6g into the XO active site highlighted its mode of binding and important interactions such as hydrogen bonding, π–π stacking with amino acid residues like Ser876, Thr1010, Phen914, Phe1009 and Phe649 and its close proximity to dioxothiomolybdenum (MOS).Item Photoprotective, antioxidant screening and new ester from dry root extracts of Potentilla atrosanguinea (Himalayan cinquefoil)(Elsevier, 2016) Kaur, Rajbir; Singla, Ramit; Jaitak, Vikas; Gupta, Vinay KumarIn vitro photoprotective and antioxidant activities of dried aqueous-methanolic (H2O/MeOH) crude extract and ethyl acetate (EtOAc), n-butanol (n-BuOH) as well as aqueous (H2O) fractions of roots of western Himalayan plant Potentilla atrosanguinea (Himalayan cinquefoil) were evaluated. The ability of protection against UVB region followed the trend EtOAc>n-BuOH>H2O/MeOH>H2O. Total phenol content of crude H2O/MeOH extract was found to be 429.808mg GAE/g. The H2O/MeOH crude extract showed highest antioxidant of DPPH radical scavenging, superoxide anion radical scavenging and cupric ion reducing of 90.04, 78.86 and 88.64% respectively at 200?g/mL. One new compound methyl pentatetraconta-30,32,34,36,38,40,42-heptaenoate (PA-1) along with a known pentadecylbutyrate (PA-2) was isolated by column chromatography. Results indicated the importance of root extracts as photoprotective agents in sunscreen preparation in the pharmaceutical industry and considered as a natural source of antioxidants. ? 2015 South African Association of Botanists.