Inhibitory kinetics and mechanism of pentacyclic triterpenoid from endophytic Colletotrichum gigasporum against pancreatic lipase
作者： Ravindra Patil , Samadhan Patil , Vijay Maheshwari , Mohini Patil
DOI: 10.1016/J.IJBIOMAC.2021.02.036
关键词:
摘要: Abstract The burden of obesity is increasing all over the world. Except for Orlistat, no effective anti-obesity drug currently available. Therefore, a search new compound need time. This study demonstrates macromolecular interaction and inhibitory effect pentacyclic triterpenoids (PTT) on pancreatic lipase (PL). In present PTTs from endophytic Colletotrichum gigasporum were found to show significant activity against PL with IC50 16.62 ± 1.43 μg/mL. PTT isolated through bioassay-guided isolation showed dose-dependent (R2 = 0.915) inhibition porcine results comparable standard (Orlistat). Based kinetic data, gradual increase in Km (app) concentration indicated that mode was competitive type, it directly competed substrate (pNPB) active site PL. vivo studies Wistar rats at oral dose (100 mg/kg body weight) significantly decreased (p
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