GPCR6A Is a Molecular Target for the Natural Products Gallate and EGCG in Green Tea.

ABSTRACT:

Scope

The molecular mechanisms whereby gallates in green tea exert metabolic effects are poorly understood.

Methods and results

We found that GPRC6A, a multi-ligand-sensing G-protein-coupled receptor that regulates energy metabolism, sex hormone production, and prostate cancer progression, is a target for gallates. Sodium gallate (SG), gallic acid (GA) > ethyl gallate (EG) > octyl gallate (OG) dose dependently activated ERK in HEK-293 cells transfected with GPRC6A but not in non-transfected controls. SG also stimulated insulin secretion in β-cells isolated from wild-type mice similar to the endogenous GPRC6A ligands, osteocalcin (Ocn) and testosterone (T). Side-chain additions to create OG resulted in loss of GPRC6A agonist activity. Another component of green tea, epigalloc

SUBMITTER: Pi M 

PROVIDER: S-EPMC6296227 | biostudies-literature | 2018 Apr

REPOSITORIES: biostudies-literature