Determination of Gymnemic Acid I as a Protein Biosynthesis Inhibitor Using Chemical Proteomics

作者:Capolupo Angela; Esposito Roberta; Zampella Angela; Festa Carmen; Riccio Raffaele; Casapullo Agostino; Tosco Alessandra*; Monti Maria Chiara*
来源:Journal of Natural Products, 2017, 80(4): 909-915.
DOI:10.1021/acs.jnatprod.6b00793

摘要

The plant Gymnema sylvestre has been used widely in traditional medicine as a remedy for several diseases, and its leaf extract is known to contain a group of bioactive triterpene saponins belonging to the gymnemic acid class. Gymnemic acid I (1) is one of the main components among this group of secondary metabolites and is endowed with an interesting bioactivity profile. Since there is-a lack of information about its specific biological targets, the full interactome of 1 was investigated through a :quantitative chemical proteomic approach, based on stable-isotope dimethyl labeling. The ribosome complex was found to be the main partner of compound 1, and a full valiolation of the proteomics results was achieved by orthogonal-approaches. Further biochemical and biological investigations revealed-an inhibitory effect of 1 on the ribosome machinery.

  • 出版日期2017-4