The Flavonoid Apigenin Is a Progesterone Receptor Modulator with In Vivo Activity in the Uterus.

ABSTRACT: Apigenin is a flavonoid with well-documented anti-cancer properties; however, its mechanisms of action are still unclear. We previously identified apigenin as a potential phytoprogestin, a natural product with a chemical scaffold that interacts with the progesterone receptor (PR). Our objective was to characterize the ability of apigenin to interact with PR through molecular docking studies, in vitro activity assays, and the ability of apigenin to elicit progestin-like effects in vivo. Molecular docking confirmed that apigenin could interact with PR, though with lower affinity than progesterone due to fewer van der Waals interactions. In Ishikawa cells stably expressing PR-B, apigenin significantly increased progesterone response element/luciferase (PRE/Luc) activity at 5 and 10 μM, but no

SUBMITTER: Dean M 

PROVIDER: S-EPMC6222006 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature