The African cactiform Hoodia gordonii exhibits anorexant properties, but the active components and molecular targets remain unclear. Here, a screen of 4,400 natural products identified Gordonoside F — a pregnane steroidal glycoside isolated from Hoodia gordonii — to activate GPR119, a GPCR highly expressed in pancreatic β cells and intestinal L cells which can stimulate both insulin and GLP-1 release. Synthesized Gordonoside F improved glucose tolerance, enhanced glucose-stimulated insulin secretion and reduced food intake in mice.
References
Zhang, S. et al. Molecular matchmaking between the popular weight-loss herb Hoodia gordonii and GPR119, a potential drug target for metabolic disorder. Proc. Natl Acad. Sci. USA 111, 14571–14576 (2014)
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Crunkhorn, S. Weight loss herb targets GPCR. Nat Rev Drug Discov 13, 888 (2014). https://doi.org/10.1038/nrd4498
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DOI: https://doi.org/10.1038/nrd4498
