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Molecules 2011, 16(5), 4264-4277;

Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains

Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
State Key Laboratory of Genetic Resources and Evolution, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
Graduate School of Chinese Academy of Sciences, Beijing 100039, China
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
These authors contributed equally to this work.
Authors to whom correspondence should be addressed.
Received: 25 February 2011 / Revised: 6 May 2011 / Accepted: 13 May 2011 / Published: 24 May 2011
(This article belongs to the Special Issue Antivirals)
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The anti-HIV-1 activity of mangiferin was evaluated. Mangiferin can inhibit HIV-1B induced syncytium formation at non-cytotoxic concentrations, with a 50% effective concentration (EC50) at 16.90 μM and a therapeutic index (TI) above 140. Mangiferin also showed good activities in other laboratory-derived strains, clinically isolated strains and resistant HIV-1 strains. Mechanism studies revealed that mangiferin might inhibit the HIV-1 protease, but is still effective against HIV peptidic protease inhibitor resistant strains. A combination of docking and pharmacophore methods clarified possible binding modes of mangiferin in the HIV-1 protease. The pharmacophore model of mangiferin consists of two hydrogen bond donors and two hydrogen bond acceptors. Compared to pharmacophore features found in commercially available drugs, three pharmacophoric elements matched well and one novel pharmacophore element was observed. Moreover, molecular docking analysis demonstrated that the pharmacophoric elements play important roles in binding HIV-1 protease. Mangiferin is a novel nonpeptidic protease inhibitor with an original structure that represents an effective drug development strategy for combating drug resistance. View Full-Text
Keywords: mangiferin; HIV-1; protease; anti-HIV agents; drug resistance mangiferin; HIV-1; protease; anti-HIV agents; drug resistance

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Wang, R.-R.; Gao, Y.-D.; Ma, C.-H.; Zhang, X.-J.; Huang, C.-G.; Huang, J.-F.; Zheng, Y.-T. Mangiferin, an Anti-HIV-1 Agent Targeting Protease and Effective against Resistant Strains. Molecules 2011, 16, 4264-4277.

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