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Article Dans Une Revue Phytochemistry Letters Année : 2020

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

Résumé

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

hal-03021823 , version 1 (24-11-2020)

Identifiants

  • HAL Id : hal-03021823 , version 1

Citer

Clément Huguet, Eleonore Real, Wei-Min Zhao, Aurelie Urbain. Secretion of glucagon-like peptide-1 induced by Cynanchum pregnane derivatives: preliminary hypotheses regarding key structural elements. Phytochemistry Letters, 2020. ⟨hal-03021823⟩
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