Flavans from Desmos cochinchinensis as potent aromatase inhibitors

Flavans from Desmos cochinchinensis as potent aromatase inhibitors

Flavans from the roots of Desmos cochinchinensis exhibited potent aromatase inhibitory activity at nanomolar levels, and could be leads for the development of anti-aromatase drugs. In addition, these aromatase inhibitors did not show pronounced cytotoxic activity. Flavans exert their inhibitory acti...

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Bibliographic Details
Main Authors: Vilailak Prachyawarakorn, Suwannee Sangpetsiripan, Panida Surawatanawong, Chulabhorn Mahidol, Somsak Ruchirawat, Prasat Kittakoop
Other Authors: Chulabhorn Research Institute
Format: Article
Published: 2018
Subjects:
Biochemistry, Genetics and Molecular Biology
Pharmacology, Toxicology and Pharmaceutics
Online Access:https://repository.li.mahidol.ac.th/handle/123456789/31151
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Institution: Mahidol University
Description
Summary:Flavans from the roots of Desmos cochinchinensis exhibited potent aromatase inhibitory activity at nanomolar levels, and could be leads for the development of anti-aromatase drugs. In addition, these aromatase inhibitors did not show pronounced cytotoxic activity. Flavans exert their inhibitory activity through binding, as revealed by molecular docking studies, with aromatase at Arg115, Met374, and Leu477; the C-7 hydroxyl (or methoxyl) forms hydrogen bonds with Met374 and Arg115 of aromatase. © 2013 The Royal Society of Chemistry.

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