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J Med Virol. 2015 Dec;87(12):2054-60. doi: 10.1002/jmv.24271. Epub 2015 Jun 9.

A resveratrol analog termed 3,3',4,4',5,5'-hexahydroxy-trans-stilbene is a potent HIV-1 inhibitor.

Author information

1
McGill University AIDS Centre, Lady Davis Institute for Medical Research, Jewish General Hospital, Montreal, Quebec, Canada.
2
Department of Clinical Pharmacy and Diagnostics, University of Vienna, Vienna, Austria.
3
Clinical Institute for Medical and Chemical Laboratory Diagnostics, Medical University of Vienna, Vienna, Austria.

Abstract

HIV resistance to current anti-HIV drugs and drug toxicity have created a need for new anti-HIV agents. We have examined and characterized a synthetic resveratrol analog, termed 3,3',4,4',5,5'-hexahydroxy-trans-stilbene (M8), for potential anti-HIV activity. Here, we demonstrate that M8 possesses potent anti-HIV activity against several HIV variants with EC50 values in the low μM range. M8 was shown to act at a very early step of HIV entry prior to fusion to host cells. These results demonstrate that this novel resveratrol derivative possesses potent anti-HIV-1 activity and may have a mechanism of action that is different from current anti-HIV-1 drugs including entry inhibitors. Further structure-guided design might lead to the development of newer improved resveratrol derivatives that could have value either in therapy or as microbicides to prevent the sexual transmission of HIV-1.

KEYWORDS:

HIV-1; entry inhibitors; resveratrol

PMID:
25989218
DOI:
10.1002/jmv.24271
[Indexed for MEDLINE]

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