Kang, Kyungsu Lee, Saet Byoul Jung, Sang Hoon Cha, Kwang Hyun Park, Woo Dong Sohn, Young Chang Nho, Chu Won 2024-01-20T21:36:05Z 2024-01-20T21:36:05Z 2021-09-03 2009-03 1016-8478 https://pubs.kist.re.kr/handle/201004/132682 Phytoestrogens are the natural compounds isolated from plants, which are structurally similar to animal estrogen, 17 beta-estradiol. Tectoridin, a major isoflavone isolated from the rhizome of Belamcanda chinensis. Tectoridin is known as a phytoestrogen, however, the molecular mechanisms underlying its estrogenic effect are remained unclear. In this study we investigated the estrogenic signaling triggered by tectoridin as compared to a famous phytoestrogen, genistein in MCF-7 human breast cancer cells. Tectoridin scarcely binds to ER alpha as compared to 17 beta-estradiol and genistein. Despite poor binding to ER alpha, tectoridin induced potent estrogenic effects, namely recovery of the population of cells in the S-phase after serum starvation, transactivation of the estrogen response element, and induction of MCF-7 cell proliferation. The tectoridin-induced estrogenic effect was severely abrogated by treatment with U0126, a specific MEK1/2 inhibitor. Tectoridin promoted phosphorylation of ERK1/2, but did not affect phosphorylation of ER alpha at Ser(118). It also increased cellular accumulation of cAMP, a hallmark of GPR30-mediated estrogen signaling. These data imply that tectoridin exerts its estrogenic effect mainly via the GPR30 and ERK-mediated rapid nongenomic estrogen signaling pathway. This property of tectoridin sets it aside from genistein where it exerts the estrogenic effects via both an ER-dependent genomic pathway and a GPR30-dependent nongenomic pathway. English KOREAN SOC MOLECULAR & CELLULAR BIOLOGY PROTEIN-COUPLED RECEPTOR BREAST-CANCER CELLS PROSTAGLANDIN E-2 PRODUCTION GROWTH-FACTOR RECEPTOR INDUCED LIVER-INJURY BELAMCANDA-CHINENSIS TECTORIGENIN PHOSPHORYLATION PHYTOESTROGENS RHIZOMES Tectoridin, a poor ligand of estrogen receptor alpha, exerts its estrogenic effects via an ERK-dependent pathway Article 10.1007/s10059-009-0045-8 1 MOLECULES AND CELLS, v.27, no.3, pp.351 - 357 MOLECULES AND CELLS 27 3 351 357 scie scopus kci ART001328602 000264623400012 2-s2.0-69849105847 Biochemistry & Molecular Biology Cell Biology Biochemistry & Molecular Biology Cell Biology Article PROTEIN-COUPLED RECEPTOR BREAST-CANCER CELLS PROSTAGLANDIN E-2 PRODUCTION GROWTH-FACTOR RECEPTOR INDUCED LIVER-INJURY BELAMCANDA-CHINENSIS TECTORIGENIN PHOSPHORYLATION PHYTOESTROGENS RHIZOMES ERK genistein GPR30 nongenomic estrogen signaling tectoridin