α-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach

Mariana Leão, Sara Gomes, José Pedraza-Chaverri, Neuza MacHado, Emília Sousa, Madalena Pinto, Alberto Inga, Clara Pereira, Lucília Saraiva (Lead / Corresponding author)

Research output: Contribution to journalArticlepeer-review

26 Citations (Scopus)

Abstract

α-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.

Original languageEnglish
Pages (from-to)774-778
Number of pages5
JournalJournal of Natural Products
Volume76
Issue number4
DOIs
Publication statusPublished - 29 Mar 2013

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