伪-Mangostin and Gambogic Acid as Potential Inhibitors of the p53鈥揗DM2 Interaction Revealed by a Yeast Approach

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• 作者：Mariana Le茫o ; Sara Gomes ; Jos茅 Pedraza-Chaverri ; Neuza Machado ; Em铆lia Sousa ; Madalena Pinto ; Alberto Inga ; Clara Pereira ; Luc铆lia Saraiva
• 刊名：Journal of Natural Products
• 出版年：2013
• 出版时间：April 26, 2013
• 年：2013
• 卷：76
• 期：4
• 页码：774-778
• 全文大小：289K
• 年卷期：v.76,no.4(April 26, 2013)
• ISSN：1520-6025

文摘

伪-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鈥揗DM2 interaction. This activity on p53鈥揗DM2 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.