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Abstract Title:

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

Abstract Source:

Virol J. 2008;5:8. Epub 2008 Jan 15. PMID: 18197976

Abstract Author(s):

Elena E Paskaleva, Xudong Lin, Karen Duus, James J McSharry, Jean-Claude L Veille, Carol Thornber, Yanze Liu, David Yu-Wei Lee, Mario Canki

Article Affiliation:

Center for Immunology and Microbial Disease, Albany Medical College, Albany, NY, USA. paskale@mail.amc.edu

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 mug/ml inhibited HIV-1 infection by 86.9%, with IC50 value of 3.7 mug. 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 mug/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.

Study Type : In Vitro Study
Additional Links
Pharmacological Actions : Enzyme Inhibitors : CK(602) : AC(312)

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Sayer Ji
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