Requirement of Metabolic Activation for Estrogenic Activity of Pueraria mirifica

Lee, Y.-S.;Park, J.-S.;Cho, S.-D.;Son, J.-K.;Cherdshewasart, W.;Kang, Kyung-Sun

  • Published : 20020000

Abstract

A wide range of chemicals derived from plant and human-made xenobiotics are reported to have hormonal activities. The present study was performed to examine the estrogenic effect of Kwao Keur, Pueraria mirifica (PM), that has been used as a rejuvenating folk medicine in Thailand. using recombinant yeast, MCF-7 cell proliferation and HepG2 cell transient transfection assay. In recombinant yeast assay, 0.025, 0.25, 2.5, 25, $2.5{\times}10^2$ $2.5{\times}10^3$, $2.5{\times}10^4$mg/mI concentrations of PM did not show any estrogenic activities, while $10^{-9}$ of 17 ${\beta}$-estradiol (positive control) showed high estrogenic activity. Estrogenic activities were induced at 2.5ng/mI to 25${\mu}g$ml concentrations of PM in a dose-dependent manner on MCF-7 cells and the estrogenic effect of PM was blocked by tamoxifen treatment, a well-known anti-estrogen, PM also showed estrogenic effect on human hepatoma cell line, HepG2 cells, containing estrogen receptor and luciferase reporter gene. Taken together, PM in itself may have no estrogtenicity in yeast system, but it has estrogenicity in MCF-7 & HepG2 cells that have human metabolic enzymes. The results indicated that PM may require metabolic activation for estrogenic activity.

Keywords

pueraria mirifica (PM);endocrine disrupter;metabolic activation

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