Sasmita Dash, Nityananda Sahoo, G. Pattnaik, Chandan Das, Sovan Pattnaik, Goutam Ghosh, Goutam Rath, B. Kar
{"title":"In vitro and in-silico Anti-diabetic Evaluation of the Combination of\u0000Annona squamosa Linn., Leaf Extract and Oleanolic Acid","authors":"Sasmita Dash, Nityananda Sahoo, G. Pattnaik, Chandan Das, Sovan Pattnaik, Goutam Ghosh, Goutam Rath, B. Kar","doi":"10.2174/0115734072294929240206060527","DOIUrl":"https://doi.org/10.2174/0115734072294929240206060527","url":null,"abstract":"\u0000\u0000Diabetes mellitus (DM) is a metabolic disorder caused by insufficient\u0000insulin production from pancreatic β-cells or insulin resistance; its prevalence rapidly increases\u0000worldwide. Increasing reports indicate that most plant bioactive agents exhibited alternative and\u0000safe effects in managing DM.\u0000\u0000\u0000\u0000The study aims to evaluate the in vitro antioxidant and anti-diabetic efficacy of the\u0000combination of Annona squamosa Linn. (AS) leaf extract and Oleanolic acid (OA) using in vitro\u0000and in-silico approaches.\u0000\u0000\u0000\u0000The leaf of AS was extracted by soxhlet extraction using n-hexane and methanol. The\u0000methanol extract of AS (MEAS) was subjected to GC-MS analysis. Quantification of total phenolic\u0000and flavonoid content and OA were carried out by HPLC and HPTLC analysis, respectively.\u0000In vitro antioxidant (DPPH, NO, and H2O2) and anti-diabetic (α-amylase and α-glucosidase)\u0000potentials of MEAS, OA, and a combination of MEAS and OA (MEAS + OA) were studied at\u0000different concentrations using ascorbic acid and acarbose as standard, respectively. An in-silico\u0000study determined their binding interactions with α-amylase (PDB ID-1B2Y) and α-glucosidase\u0000(PDB ID-3W37).\u0000\u0000\u0000\u0000We found that the combination of MEAS + OA exhibited the highest in vitro antioxidant\u0000and anti-diabetic activities compared to MEAS and OA. It concluded that OA has a significant\u0000role in potentiating the anti-diabetic effect of A. squamosa.\u0000\u0000\u0000\u0000GC-MS analysis of MEAS revealed three major bioactives like bicyclo[7.2.0]undec-4-\u0000ene, 4,11,11-trimethyl-8-methylene-,[1R-(1R*,4Z,9S*)]-, germacrene D and undecane. The highest\u0000amount of phenolic (tannic acid and gallic acid) (150 μg/ml) and flavonoid (rutin and quercetin)\u0000(40 μg/ml) compounds were found in MEAS. OA was quantified as 356.74 ng/ml in MEAS\u0000by HPTLC. The significant inhibitory effects of MEAS, OA, and (MEAS + OA) on free radicals\u0000and α-amylase and α-glucosidase were observed concentration-dependent. However, MEAS +\u0000OA exhibited a greater percentage of inhibition than MEAS and OA alone. The in-silico analysis\u0000revealed highest docking-score of OA (-9.8 & -8.8), Germacrene D (-7.5 & -6.5) and Bicyclo[\u00007.2.0]undec-4-ene, 4,11,11-trimethyl-8-methylene-,[1R-(1R*,4Z,9S*)]-, (-7.0 & -6.4) against\u0000IB2Y and 3W37 proteins, respectively.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"9 8","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-02-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139962957","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}