Lee, R. Choi, S.-H. Cho, H.-S. Hwang, H. Rhim, H. Kim, H.-C. Hwang, S.-H. Nah, S.-Y. 2024-01-19T13:33:17Z 2024-01-19T13:33:17Z 2022-01-10 2021-10 1420-3049 https://pubs.kist.re.kr/handle/201004/116292 Ginseng-derived gintonin reportedly contains functional lysophosphatidic acids (LPAs) as LPA receptor ligands. The effect of the gintonin-enriched fraction (GEF) on in vitro and in vivo glucagon-like protein-1 (GLP-1) secretion, which is known to stimulate insulin secretion, via LPA receptor(s) remains unclear. Accordingly, we examined the effects of GEF on GLP-1 secretion using human enteroendocrine NCI-H716 cells. The expression of several of LPA receptor subtypes in NCIH716 cells using qPCR and Western blotting was examined. LPA receptor subtype expression was in the following order: LPA6 > LPA2 > LPA4 > LPA5 > LPA1 (qPCR), and LPA6 > LPA4 > LPA2 > LPA1 > LPA3 > LPA5 (Western blotting). GEF-stimulated GLP-1 secretion occurred in a dose-and time-dependent manner, which was suppressed by cAMP-Rp, a cAMP antagonist, but not by U73122, a phospholipase C inhibitor. Furthermore, silencing the human LPA6 receptor attenuated GEF-mediated GLP-1 secretion. In mice, low-dose GEF (50 mg/kg, peroral) increased serum GLP-1 levels; this effect was not blocked by Ki16425 co-treatment. Our findings indicate that GEF-induced GLP-1 secretion could be achieved via LPA6 receptor activation through the cAMP pathway. Hence, GEF-induced GLP secretion via LPA6 receptor regulation might be responsible for its beneficial effects on human endocrine physiology. ？ 2021 by the authors. Licensee MDPI, Basel, Switzerland. English Multidisciplinary Digital Publishing Institute (MDPI) Effect of the gintonin-enriched fraction on glucagon-like-protein-1 release Article 10.3390/molecules26206298 1 Molecules, v.26, no.20 Molecules 26 20 Y scie scopus 000716356300001 2-s2.0-85117802618 Biochemistry & Molecular Biology Chemistry, Multidisciplinary Biochemistry & Molecular Biology Chemistry Article LYSOPHOSPHATIDIC ACID RECEPTOR PEPTIDE-1 SECRETION GINSENG INVOLVEMENT ACTIVATION MANAGEMENT AGONIST INSULIN BIOLOGY LIGAND Ginseng Gintonin Gintonin-enriched fraction GLP-1 secretion NCI-H716 cell