Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

G-protein-coupled estrogen receptor agonist G-1 inhibits the proliferation of breast cancer cells through induction of apoptosis and cycle arrest

Hancheng Liu, Minghui Wang, Chunyu Tian, Jie Zhang, Hongxu Zhang, Lihui Ma

Department of Breast Surgery, Affiliated Hospital of Chengde Medical College, Chengde 067000, Hebei Province, China;

For correspondence:- Lihui Ma Email: hanchengssdd@163.com

Accepted: 6 January 2022 Published: 31 January 2022

Citation: Liu H, Wang M, Tian C, Zhang J, Zhang H, Ma L. G-protein-coupled estrogen receptor agonist G-1 inhibits the proliferation of breast cancer cells through induction of apoptosis and cycle arrest. Trop J Pharm Res 2022; 21(1):25-30 doi: 10.4314/tjpr.v21i1.5

© 2022 The authors.
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Abstract

Purpose: To determine the effect of G-1, a G-protein-linked estrogen receptor (GPER) agonist on apoptosis, cell cycle, and proliferative potential of mammary tumor cells, and the associated mechanisms of action.
Methods: Three groups of human breast cancer cell line MDA-MB-231 were used: control group, estradiol (E2) group and G-1 group. Control group was not treated. The effects of treatment (10 ?M G-1) on cell proliferation were determined and compared amongst the groups. Cell cycle distribution and apoptosis were determined while expression levels of proteins related to pi3k/AKT/MAPK were assessed by western blotting.
Results: Apoptosis was significantly reduced in E2 group relative to control, but was enhanced in G-1 group, when compared to the other 2 groups (p < 0.05). There were marked down-regulations in protein levels of cylinb1, p21, caspase 6, p53, p-ERK in E2 group, relative to the corresponding expression levels in the control group.
Conclusion: GPER agonist G-1 suppresses the proliferation of mammary tumor cells and induces apoptotic changes and cycle blockage in the cells via inhibition of pi3k/AKT pathway and activation of MAPKs pathway. Thus, GPER is a potential target in breast tumor treatment, and G-1 is a potential new anti-tumor drug.

Keywords: GPER agonist G-1, Breast cancer, Apoptosis, Cycle block, Cell proliferation