Estrogenic Activity of Sanguiin H-6 through Activation of Estrogen Receptor α Coactivator-binding Site
10.20307/nps.2019.25.1.28
- Author:
Tuy An TRINH
1
;
Eun Ji PARK
;
Dahae LEE
;
Ji Hoon SONG
;
Hye Lim LEE
;
Ki Hyun KIM
;
Younghoon KIM
;
Kiwon JUNG
;
Ki Sung KANG
;
Jeong Eun YOO
Author Information
1. College of Korean Medicine, Gachon University, Seongnam 13120, Korea. kkang@gachon.ac.kr
- Publication Type:Original Article
- Keywords:
Rubus coreanus;
Sanguiin H-6;
Estrogen receptor α;
Coactivator-binding site;
MCF-7 human breast cancer cells
- MeSH:
Breast Neoplasms;
Cell Line;
Cell Proliferation;
Estrogens;
Humans;
Molecular Docking Simulation;
Phytochemicals;
Rubus
- From:Natural Product Sciences
2019;25(1):28-33
- CountryRepublic of Korea
- Language:English
-
Abstract:
A popular approach for the study of estrogen receptor α inhibition is to investigate the protein-protein interaction between the estrogen receptor (ER) and the coactivator surface. In our study, we investigated phytochemicals from Rubus coreanus that were able to disrupt ERα and coactivator interaction with an ERα antagonist. The E-screen assay and molecular docking analysis were performed to evaluate the effects of the estrogenic activity of R. coreanus extract and its constituents on the MCF-7 human breast cancer cell line. At 100 µg/mL, R. coreanus extract significantly stimulated cell proliferation (574.57 ± 8.56%). Sanguiin H6, which was isolated from R. coreanus, demonstrated the strongest affinity for the ERα coactivator-binding site in molecular docking analysis, with a binding energy of
