Baicalein, 7,8-Dihydroxyflavone and Myricetin as Potent Inhibitors of Human Ornithine Decarboxylase.

ABSTRACT:

Background

Human ornithine decarboxylase (ODC) is a well-known oncogene, and the discovery of ODC enzyme inhibitors is a beneficial strategy for cancer therapy and prevention.

Methods

We examined the inhibitory effects of a variety of flavone and flavonol derivatives on ODC enzymatic activity, and performed in silico molecular docking of baicalein, 7,8-dihydroxyflavone and myricetin to the whole dimer of human ODC to investigate the possible binding site of these compounds on ODC. We also examined the cytotoxic effects of these compounds with cell-based studies.

Results

Baicalein, 7,8-dihydroxyflavone and myricetin exhibited significant ODC suppression activity with IC₅₀ values of 0.88 µM, 2.54 µM, and 7.3 µM, respectively, which were much lower than that o

SUBMITTER: Liu YC 

PROVIDER: S-EPMC7765794 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature