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Beneficial effect of phospholipase A2 group IIA inhibitors from Acacia suma in obesity: an in silico and in vitro study

Oriental Pharmacy and Experimental Medicine 2020년 20권 4호 p.599 ~ 608
Kanbarkar Nikita, Mishra Sanjay, Khanal Pukar,
소속 상세정보
 ( Kanbarkar Nikita ) - KLE Academy of Higher Education and Research V. K. Institute of Dental Sciences
 ( Mishra Sanjay ) - KLE Academy of Higher Education and Research V. K. Institute of Dental Sciences
 ( Khanal Pukar ) - KLE Academy of Higher Education and Research KLE College of Pharmacy

Abstract


Acacia suma Roxb. (Fabaceae) is Ayurvedic medicine distributed in Karnataka, Bengal and Bihar region. Phytoconstituents of A. suma were retrieved from ChEIB databases and queried for phospholipase A2 group IIA inhibitors. The present study is an effort to find out a novel therapeutic solution for the management of obesity disorders. Out of 29 reported compounds three were identified in modulating phospholipase A2 group IIA inhibitor their drug likeness score andprobable gene expression was identified. Docking study was performed using autodock4.0 to predict binding affinity of phytoconstituents with phospholipase A2 group IIA inhibitor and compared with clinically proven drug ‘Orlistat’ as lipase inhibitor. The respected pathway to show networking between phytochemicals and target were analyse by kyoto encyclopedia of genes and genomes pathway analysis for regulated genes. Further, in silico findings were validated for hydroalcoholic extract of A. suma by in vitro lipase inhibition assay. Molecular docking result revealed the presence of three flavonoid compounds for lipase inhibition activity namely: (1) (5S,7R,8R,9R,10S)-(?)-7,8?seco-7,8?oxacassa-13,15-diene-7,17-diol (2) Fisetinidol-(4α,6)-gallocatechin and (3) Quercetin4′-O-α-L-rhamnopyranosyl-3-O-β-D-allopyranoside. However, Quercetin4′-O-α-L-rhamnopyranosyl-3-O-β-D-allopyranoside was predicted to possess the highest docking score i.e. ? 7.6 kcal/mol with phospholipase A2 group IIA. The in vitro findings revealed significant anti-lipase activity with IC50 value ? 46.07 μg/ml. Hence, the in silico and in vitro approaches has presented strong binding affinity and significant lipase inhibition activity respectively which supports anti-obesity potential of heart wood hydroalcoholic extract of A. suma.

키워드

Acacia suma; Catechin; Lipase inhibition; In silico study; Obesity

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