alpha-Mangostin and Gambogic Acid as Potential Inhibitors of the p53-MDM2 Interaction Revealed by a Yeast Approach

• Type: Article in International Scientific Journal
• Date: 2013

Authors

Mariana Leao (Author) Other; Sara Gomes (Author) Other; Jose Pedraza Chaverri (Author) Other; Neuza Machado (Author) Other; Emilia Sousa (Author) FFUP; Madalena Pinto (Author) FFUP; Alberto Inga (Author) Other; Clara Pereira (Author) Other; Lucilia Saraiva (Author) FFUP

Journal

Title: Journal of Natural Products

Vol. 76

Pages: 774-778

ISSN: 0163-3864

Publisher: American Chemical Society

Indexing

ISI Proceedings

ISI Web of Knowledge - 31 Citations

Scopus - 32 Citations

Scientific classification

FOS: Medical and Health sciences > Basic medicine

Other information

Authenticus ID: P-005-1S0

DOI: 10.1021/np400049j

Abstract (EN): alpha-Mangostin (1) and gambogic acid (2) are natural products with potent cytotoxic activity against several human tumor cells. However, their molecular mechanisms of action remain controversial. In this work, using yeast-based assays, it was shown that both xanthones are potential inhibitors of the p53-MDM2 interaction. This activity on p53-MDM2 interaction was confirmed by a gene reporter assay in a human tumor cell. Additionally, computational docking studies supported the potential of these xanthones to bind to MDM2 and therefore act as putative MDM2 inhibitors. Altogether, this work provides a new insight concerning the molecular basis of activity for these compounds.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 5