Inhibition of human carboxylesterases by ginsenosides: structure-activity relationships and inhibitory mechanism.

ABSTRACT:

Background

Human carboxylesterases (hCES) are key serine hydrolases responsible for the hydrolysis of a wide range of endogenous and xenobiotic esters. Although it has been reported that some ginsenosides can modulate the activities of various enzymes, the inhibitory effects of ginsenosides on hCES have not been well-investigated.

Methods

In this study, more than 20 ginsenosides were collected and their inhibitory effects on hCES1A and hCES2A were assayed using the highly specific fluorescent probe substrates for each isoenzyme. Molecular docking simulations were also performed to investigate the interactions between ginsenosides and hCES.

Results

Among all tested ginsenosides, Dammarenediol II (DM) and 20S-O-β-(d-glucosyl)-dammarenediol II (DMG) displayed pote

SUBMITTER: Sun ZH 

PROVIDER: S-EPMC6915887 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature