Molecules, Vol. 25, Pages 1102: Ginseng Gintonin Contains Ligands for GPR40 and GPR55

Molecules, Vol. 25, Pages 1102: Ginseng Gintonin Contains Ligands for GPR40 and GPR55 Molecules doi: 10.3390/molecules25051102 Authors: Yeon-Jin Cho Sun-Hye Choi Rami Lee Hongik Hwang Hyewhon Rhim Ik-Hyun Cho Hyoung-Chun Kim Jeong-Ik Lee Sung-Hee Hwang Seung-Yeol Nah Gintonin, a novel ginseng-derived glycolipoprotein complex, has an exogenous ligand for lysophosphatidic acid (LPA) receptors. However, recent lipid analysis of gintonin has shown that gintonin also contains other bioactive lipids besides LPAs, including linoleic acid and lysophosphatidylinositol (LPI). Linoleic acid, a free fatty acid, and LPI are known as ligands for the G-protein coupled receptors (GPCR), GPR40, and GPR55, respectively. We, herein, investigated whether gintonin could serve as a ligand for GPR40 and GPR55, using the insulin-secreting beta cell-derived cell line INS-1 and the human prostate cancer cell line PC-3, respectively. Gintonin dose-dependently enhanced insulin secretion from INS-1 cells. Gintonin-stimulated insulin secretion was partially inhibited by a GPR40 receptor antagonist but not an LPA1/3 receptor antagonist and was down-regulated by small interfering RNA (siRNA) against GPR40. Gintonin dose-dependently induced [Ca2+]i transients and Ca2+-dependent cell migration in PC-3 cells. Gintonin actions in PC-3 cells were attenuated by pretreatment with a GPR55 antagonist and an LPA1/3 receptor antagonist or by down-regulating GPR55 with siRNA. Taken together, t...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research