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Griffithsin, a potent HIV entry inhibitor, is an excellent candidate for anti-HIV microbicide

  1. Author:
    Emau, P.
    Tian, B.
    O'Keefa, B. R.
    Mori, T.
    McMahon, J. B.
    Palmer, K. E.
    Jiang, Y.
    Bekele, G.
    Tsai, C. C.

  2. Author Address

    Univ Washington, Washington Natl Primate Res Ctr, Seattle, WA 98195 USA. NCI, Canc Res Ctr, Mol Targets Dev Program, Frederick, MD 21702 USA. Univ Louisville, James Graham Brown Canc Ctr, Owensboro, KY 42303 USA.;Tsai, CC, Univ Washington, Washington Natl Primate Res Ctr, Box 357330,HSB, Seattle, WA 98195 USA.;cctsai@u.washington.edu
    1. Year: 2007
    2. Date: Aug
  2. Journal: Journal of Medical Primatology
    1. 36
    2. 4-5
    3. Pages: 244-253
  4. Type of Article: Article
  5. ISSN: 0047-2565
  1. Abstract:

    Background The predominant mode of HIV-1 transmission is by heterosexual contact. The cervical/vaginal mucosa is the main port of HIV entry in women. A safe and effective topical microbicide against HIV is urgently needed to prevent sexual transmission. Hence, we evaluated griffithsin (GRFT), a 12.7 kDa carbohydrate-binding protein, both native and recombinant GRFT, potently inhibited both CXCR4-and CCR5-tropic HIV infection and transmission in vitro. Methods The antiviral efficacy of native and recombinant GRFT against CXCR4-and CCR5-tropic HIV and SHIV strains and SIVmac251 was evaluated by in vitro assays. We also evaluated the time course of antiviral activity and stability of GRFT in cervical/vaginal lavage as a function of pH 4-8. Results Griffithsin blocked CXCR4-and CCR5-tropic viruses at less than 1 nm concentrations and exhibited a high potency. GRFT was stable in cervical/vaginal lavage fluid and maintained a similar potency of anti-HIV activity. GRFT is not only a highly potent HIV entry inhibitor, but also prevents cell fusion and cell-to-cell transmission of HIV. Conclusions The in vitro efficacy of GRFT revealed low cytotoxicity, high potency, rapid onset of antiviral activity and long-term stability in cervical/ vaginal lavage. GRFT is an excellent candidate for anti-HIV microbicide development.

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External Sources

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  2. DOI: 10.1111/j.1600-0684.2007.00242.x
  3. View record in Web of Science®
  4. WOS: 000248482700009

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