2. Academic Validation
  3. Discovery and characterization of flavonoids in vine tea as catechol-O-methyltransferase inhibitors

Discovery and characterization of flavonoids in vine tea as catechol-O-methyltransferase inhibitors

  • Fitoterapia. 2021 Jul:152:104913. doi: 10.1016/j.fitote.2021.104913.
Dong-Fang Zhao 1,  Yu-Fan Fan 1,  Hao-Nan Yu 1,  Fan-Bin Hou 1,  Yan-Wei Xiang 2,  Ping Wang 3,  Guang-Bo Ge 4,  Ling Yang 1,  Jian-Guang Xu 2
Affiliations

Affiliations

  • 1 Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China.
  • 2 School of Rehabilitation Science, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China.
  • 3 Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China. Electronic address: pwang@shutcm.edu.cn.
  • 4 Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai, 201203, China. Electronic address: geguangbo@shutcm.edu.cn.
PMID: 33932529 DOI: 10.1016/j.fitote.2021.104913
Abstract

Vine tea has been used as a traditionally functional herbal tea in China for centuries, which exhibits paramount potential for chronic metabolic diseases. Herein, the inhibitory potential of vine tea toward human catechol-O-methyltransferase (hCOMT) was investigated. A practical bioactivity-guided fractionation combined with chemical profiling strategy was developed to identify the naturally occurring hCOMT inhibitors. Five Flavonoids in vine tea displayed moderate to strong inhibition on hCOMT with IC50 values ranging from 0.96 μM to 42.47 μM, in which myricetin was the critically potent constituent against hCOMT. Inhibition kinetics assays and molecular docking simulations showed that myricetin could bind to the active site of COMT and inhibited COMT-catalyzed 3-BTD methylation in a mixed manner. Collectively, our findings not only suggested that the strong hCOMT inhibition of vine tea has guiding significance in the drug exposure of catechol drugs, but also identified a promising lead compound for developing more efficacious hCOMT inhibitors.

Keywords

Catechol-O-methyltransferase; Flavonoids; Inhibitors; Vine tea.

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