Next Article in Journal
A Screening of a Library of T7 Phage-Displayed Peptide Identifies E2F-4 as an Etoposide-Binding Protein
Next Article in Special Issue
Echinacea—A Source of Potent Antivirals for Respiratory Virus Infections
Previous Article in Journal
Cytotoxicity and Pro-Apoptotic Activity of 2,2´-Bis[4,5-bis(4-hydroxybenzyl)-2-(4-hydroxyphenyl)cyclopent-4-en-1,3-dione], a Phenolic Cyclopentenedione Isolated from the Cyanobacterium Strain Nostoc sp. str. Lukešová 27/97
Previous Article in Special Issue
Identification and Characterization of Three Novel Small Interference RNAs That Effectively Down-Regulate the Isolated Nucleocapsid Gene Expression of SARS Coronavirus
Molecules 2011, 16(5), 4264-4277; doi:10.3390/molecules16054264

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

1,†, 2,3,†, 4, 1,3, 4,* , 2,*  and 1,*
1 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 2 State Key Laboratory of Genetic Resources and Evolution, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China 3 Graduate School of Chinese Academy of Sciences, Beijing 100039, China 4 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)
Download PDF [468 KB, uploaded 18 June 2014]


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.
Keywords: mangiferin; HIV-1; protease; anti-HIV agents; drug resistance mangiferin; HIV-1; protease; anti-HIV agents; drug resistance
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote |
MDPI and ACS Style

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.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here


Cited By

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert