title: Determination of Gymnemic Acid I as a Protein Biosynthesis Inhibitor Using Chemical Proteomics.
abstract: 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 validation of the proteomics results was achieved by orthogonal approaches. Further biochemical and biological investigations revealed an inhibitory effect of 1 on the ribosome machinery.
authors.forename: Angela
authors.initials: A
authors.lastname: Capolupo
authors.forename: Roberta
authors.initials: R
authors.lastname: Esposito
authors.affiliation: Department of Pharmacy, University of Napoli "Federico II" , 80131, Naples, Italy.
authors.forename: Angela
authors.initials: A
authors.lastname: Zampella
authors.affiliation: Department of Pharmacy, University of Napoli "Federico II" , 80131, Naples, Italy.
authors.forename: Carmen
authors.initials: C
authors.lastname: Festa
authors.forename: Raffaele
authors.initials: R
authors.lastname: Riccio
authors.forename: Agostino
authors.initials: A
authors.lastname: Casapullo
authors.forename: Alessandra
authors.initials: A
authors.lastname: Tosco
authors.forename: Maria Chiara
authors.identifier: 0000-0002-1337-2909
authors.initials: MC
authors.lastname: Monti
mesh_terms: D000818:Animals; D002470:Cell Survival / Q000187:drug effects; D031104:Gymnema sylvestre / Q000737:chemistry*; D006367:HeLa Cells; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry; D015394:Molecular Structure; D019906:Nuclear Magnetic Resonance, Biomolecular; D035261:Plant Components, Aerial / Q000737:chemistry; D018515:Plant Leaves / Q000737:chemistry; D014176:Protein Biosynthesis / Q000187:drug effects; D011500:Protein Synthesis Inhibitors / Q000032:analysis*; D040901:Proteomics; D012503:Saponins / Q000032:analysis / Q000737:chemistry / Q000494:pharmacology*; D014315:Triterpenes / Q000032:analysis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D007004:Hypoglycemic Agents; D011500:Protein Synthesis Inhibitors; D012503:Saponins; D014315:Triterpenes; C007898:gymnemic acid