Sargassum fusiforme fraction is a potent and specific inhibitor of HIV-1 fusion and reverse transcriptase

doi:10.1186/1743-422X-5-8

Virology Journal

Volume 5

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Paskaleva EE
Lin X
Duus K
McSharry JJ
Veille JCL
Thornber C
Liu Y
Lee DY
Canki M

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Paskaleva EE
Lin X
Duus K
McSharry JJ
Veille JCL
Thornber C
Liu Y
Lee DY
Canki M
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Research

Sargassum fusiforme fraction is a potent and specific inhibitor of HIV-1 fusion and reverse transcriptase

Elena E Paskaleva¹ , Xudong Lin¹ , Karen Duus¹ , James J McSharry² , Jean-Claude L Veille¹^,3 , Carol Thornber⁴ , Yanze Liu⁵ , David Yu-Wei Lee⁵ and Mario Canki¹

¹Center for Immunology and Microbial Disease, Albany Medical College, Albany, NY, USA

²Ordway Research Institute, Inc., Albany, NY, USA

³Department of Ob/Gyn, Albany Medical College, Albany, NY, USA

⁴Department of Biological Sciences, University of Rhode Island, Kingston, USA

⁵Mailman Research Center, McLean Hospital, Harvard Medical School, Belmont, MA, USA

author email corresponding author email

Virology Journal 2008, 5:8doi:10.1186/1743-422X-5-8


Published:	15 January 2008

Abstract

Sargassum fusiforme (Harvey) Setchell has been shown to be a highly effective inhibitor of HIV-1 infection. To identify its mechanism of action, we performed bioactivity-guided fractionation on Sargassum fusiforme mixture. Here, we report isolation of a bioactive fraction SP4-2 (S. fusiforme), which at 8 μg/ml inhibited HIV-1 infection by 86.9%, with IC₅₀value of 3.7 μg. That represents 230-fold enhancement of antiretroviral potency as compared to the whole extract. Inhibition was mediated against both CXCR4 (X4) and CCR5 (R5) tropic HIV-1. Specifically, 10 μg/ml SP4-2 blocked HIV-1 fusion and entry by 53%. This effect was reversed by interaction of SP4-2 with sCD4, suggesting that S. fusiforme inhibits HIV-1 infection by blocking CD4 receptor, which also explained observed inhibition of both X4 and R5-tropic HIV-1. SP4-2 also inhibited HIV-1 replication after virus entry, by directly inhibiting HIV-1 reverse transcriptase (RT) in a dose dependent manner by up to 79%. We conclude that the SP4-2 fraction contains at least two distinct and biologically active molecules, one that inhibits HIV-1 fusion by interacting with CD4 receptor, and another that directly inhibits HIV-1 RT. We propose that S. fusiforme is a lead candidate for anti-HIV-1 drug development.