Naturally-occurring TGR5 agonists modulating glucagon-like peptide-1 biosynthesis and secretion.
作者： Laila Jafri , Samreen Saleem , Danielle Calderwood , Anna Gillespie , Bushra Mirza
DOI: 10.1016/J.PEPTIDES.2016.01.015
关键词:
摘要: Selective GLP-1 secretagogues represent a novel potential therapy for type 2 diabetes mellitus. This study examined the secretory activity of ethnomedicinal plant, Fagonia cretica, which is postulated to possess anti-diabetic activity. After extraction and fractionation extracts purified compounds were tested GIP in pGIP/neo STC-1 cells. Intracellular levels incretin hormones their gene expression also determined. Crude F. cretica stimulated both secretion, increased cellular hormone content, upregulated proglucagon, prohormone convertase. However, ethyl acetate partitioning significantly enriched this fraction underwent bioactivity-guided fractionation. Three isolated potent selective secretagogues: quinovic acid (QA) two QA derivatives, QA-3β-O-β-D-glycopyranoside QA-3β-O-β-D-glucopyranosyl-(28→1)-β-D-glucopyranosyl ester. All activated TGR5 receptor intracellular expression. derivatives more than QA. first time that its naturally-occurring have been shown activate stimulate secretion. These data provide plausible mechanism use may assist ongoing development agonists.
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