The natural estrogenic compound diarylheptanoid (D3): in vitro mechanisms of action and in vivo uterine responses via estrogen receptor α.

ABSTRACT:

Background

Diarylheptanoid (D3) isolated from the medicinal plant, Curcuma comosa, has estrogenic activity.

Objective

We aimed to elucidate the mechanism(s) of D3 action and compare it with that of 17β-estradiol (E2) using both in vitro and in vivo uterine models.

Methods

We used human uterine (Ishikawa) cells to determine the estrogenic action of D3 on the activation and nuclear translocation of estrogen receptor α (ERα). In addition, we further characterized the uterine response to D3 treatment in vivo.

Results

D3 activated an estrogen responsive element (ERE) luciferase reporter through ERα, and molecular modeling suggested that D3 could be accommodated in the ERα binding pocket. Using modified ERα to assay ligand-dependent nuclear translocation, we observed

SUBMITTER: Winuthayanon W 

PROVIDER: S-EPMC3620745 | biostudies-literature | 2013 Apr

REPOSITORIES: biostudies-literature