Study on estrogenic effect of genistein and apigenin in vitro.

Ruiqing Zhu; Baofeng GE; Bin Yang; Keming Chen; Yimin Wen; Jian Zhou; Guiqiu Han; Guozheng Cheng; Yuankun Zhai

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Study on estrogenic effect of genistein and apigenin in vitro.

Author: Ruiqing ZHU ¹ ; Baofeng GE ; Bin YANG ; Keming CHEN ; Yimin WEN ; Jian ZHOU ; Guiqiu HAN ; Guozheng CHENG ; Yuankun ZHAI
Author Information

1. School of Life Science and Engineering, Lanzhou University of Technology, Lanzhou 730050, China. darqing_zhu@yahoo.com.cn
Publication Type:Journal Article
MeSH: Apigenin; pharmacology; Cell Proliferation; drug effects; Estrogen Receptor alpha; genetics; metabolism; Estrogen Receptor beta; genetics; metabolism; Female; Gene Expression; drug effects; Genistein; pharmacology; Humans; MCF-7 Cells; Phytoestrogens; pharmacology; Presenilin-2; genetics; metabolism
From: China Journal of Chinese Materia Medica 2012;37(15):2317-2322
CountryChina
Language:Chinese
Abstract:
OBJECTIVETo detect the estrogenic activity of genistein and apigenin with ER-positive cell line MCF-7 human breast cancer cells.
METHODMTT method was adopted to study the impact of genistein and apigenin on MCF-7 proliferation in vitro. Real-time RT-PCR method was used to detect their impact on ERalpha, ERbeta, PR and PS2 mRNA expression levels.
RESULTGenistein and apigenin promoted the proliferation of MCF-7. Genistein 1 x 10(-10) mol x L(-1) group showed a significant increase in the expression of ERa mRNA levels or a 17. 76 times more than the control group and a 1.75 times more than the E2 group. Apigenin notably promoted the PR mRNA expression or a 4. 57 times more than the control group and a 1.11 times more than the E2 group. Both of them had different effect in promoting ERalpha, ERbeta, PR or PS2 mRNA.
CONCLUSIONBoth genistein and apigenin have a strong estrogen-like effect. Although they have different effect in promoting estrogenic response genes (such as ERa, ERbeta, PR and PS2 mRNA), genistein shows a stronger activity than apigenin. It also suggests that the signaling pathways of phytoestrogens showing estrogen-like effect are not completely identical with estrogen pathways. The B-cycle position of flavonoids is one of the key sites to estrogen-like activity, and isoflavones (cycle B on site 3) show stronger estrogen-like activity than flavones (B-cycle lies in site 2).