[Study on Estrogenic Effect of Genistein and Apigenin in Vitro]

Zhongguo Zhong Yao Za Zhi. 2012 Aug;37(15):2317-22.
[Article in Chinese]

Abstract

Objective: To detect the estrogenic activity of genistein and apigenin with ER-positive cell line MCF-7 human breast cancer cells.

Method: MTT 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.

Result: Genistein 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.

Conclusion: Both 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).

Publication types

  • English Abstract
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apigenin / pharmacology*
  • Cell Proliferation / drug effects
  • Estrogen Receptor alpha / genetics
  • Estrogen Receptor alpha / metabolism
  • Estrogen Receptor beta / genetics
  • Estrogen Receptor beta / metabolism
  • Female
  • Gene Expression / drug effects
  • Genistein / pharmacology*
  • Humans
  • MCF-7 Cells
  • Phytoestrogens / pharmacology*
  • Presenilin-2 / genetics
  • Presenilin-2 / metabolism

Substances

  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • PSEN2 protein, human
  • Phytoestrogens
  • Presenilin-2
  • Apigenin
  • Genistein