Secretion of glucagon-like peptide-1 induced by Cynanchum pregnane derivatives: Preliminary hypotheses regarding key structural elements

In our continued efforts to explore the antidiabetic potential of pregnanes from Apocynaceae, especially Asclepiadoideae subfamily, sixteen derivatives 1-16 previously isolated various Cynanchum species, have been evaluated for their ability increase glucagon-like peptide-1 (GLP-1) release in a cell assay. As result, otophylloside A (2), wilfoside C1N (13), and C3N (16) were found stimulate significantly secretion GLP-1, doubling extracellular content this incretin. Caudatin 3-O-β-D-glucopyranosyl-(1→4)-β-D-oleandropyranosyl-(1→4)-β-D-cymaropyranosyl-(1→4)-β-D-cymaropyranoside (6) was also bioactive, but lesser extent (133 % compared control cells). This study confirms certain pregnane subfamily reduced patients with type 2 diabetes. addition, outlines some putative structure-activity relationships: nature sugar chain at C-3, as well ester moiety C-12 position appear be key elements GLP-1 secretion.