1. Determination of Gymnemic Acid I as a Protein Biosynthesis Inhibitor Using Chemical Proteomics
- Author
-
Raffaele Riccio, Alessandra Tosco, Angela Capolupo, Angela Zampella, Carmen Festa, Roberta Esposito, Agostino Casapullo, Maria Chiara Monti, Capolupo, Angela, Esposito, Roberta, Zampella, Angela, Festa, Carmen, Riccio, Raffaele, Casapullo, Agostino, Tosco, Alessandra, and Monti, Maria Chiara
- Subjects
Proteomics ,0301 basic medicine ,Pharmaceutical Science ,interactome ,Interactome ,Ribosome ,Analytical Chemistry ,chemistry.chemical_compound ,0302 clinical medicine ,Triterpene ,Drug Discovery ,Protein Synthesis Inhibitors ,chemistry.chemical_classification ,Molecular Structure ,biology ,A protein ,Complementary and Alternative Medicine2708 Dermatology ,Biochemistry ,030220 oncology & carcinogenesis ,Gymnemic acid ,Molecular Medicine ,Gymnema sylvestre ,Cell Survival ,03 medical and health sciences ,Biosynthesis ,Animals ,Humans ,Hypoglycemic Agents ,Nuclear Magnetic Resonance, Biomolecular ,Pharmacology ,protein biosynthesis inhibitor ,Drug Discovery3003 Pharmaceutical Science ,Organic Chemistry ,Plant ,Plant Components, Aerial ,Saponins ,biology.organism_classification ,chemical proteomic ,Triterpenes ,Plant Leaves ,030104 developmental biology ,Complementary and alternative medicine ,chemistry ,Protein Biosynthesis ,3003 ,HeLa Cells - 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.
- Published
- 2017
- Full Text
- View/download PDF