Discovery and characterization of naturally occurring potent inhibitors of catechol-O-methyltransferase from herbal medicines.

ABSTRACT: Human catechol-O-methyltransferase (hCOMT) is considered a therapeutic target due to its crucial roles in the metabolic inactivation of endogenous neurotransmitters and xenobiotic drugs. There are nevertheless few safe and effective COMT inhibitors and there lacks a diversity in structure. To discover novel safe and effective hCOMT inhibitors from herbal products, in this study, 53 herbal products were collected and their inhibitory effects against hCOMT were investigated. Among them, Scutellariae radix (SR) displayed the most potent inhibitory effect on hCOMT with an IC₅₀ value of 0.75 μg mL^-1. To further determine specific chemicals as COMT inhibitors, an affinity ultrafiltration coupled with liquid chromatography-mass spectrometry method was developed

SUBMITTER: Zhao DF 

PROVIDER: S-EPMC8695704 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature