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Article Publish Status: FREE
Abstract Title:

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

Abstract Source:

Nutrients. 2020 Dec 17 ;12(12). Epub 2020 Dec 17. PMID: 33348871

Abstract Author(s):

Yun-Chin Liu, Yi-Liang Liu, Ju-Yi Hsieh, Chang-Hsu Wang, Chi-Li Lin, Guang-Yaw Liu, Hui-Chih Hung

Article Affiliation:

Yun-Chin Liu

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 ICvalues of 0.88µM, 2.54 µM, and 7.3 µM, respectively, which were much lower than that of the active-site irreversible inhibitor α-DL-difluoromethylornithine (IC, the half maximal inhibitory concentration, of approximately 100µM). Kinetic studies and molecular docking simulations suggested that baicalein, and 7,8-dihydroxyflavone act as noncompetitive inhibitors that are hydrogen-bonded to the region near the active site pocket in the dimer interface of the enzyme. Baicalein and myricetin suppress cell growth and inducecellular apoptosis, and both of these compounds suppress the ODC-evoked anti-apoptosis of cells.

CONCLUSIONS: Therefore, we suggest that the flavone or flavonol derivatives baicalein, 7,8-dihydroxyflavone, and myricetin are potent chemopreventive and chemotherapeutic agents that target ODC.

Study Type : In Vitro Study

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