Phytomedicine
Volume 17, Issue 1 , Pages 69-74, January 2010

Ellagitannins from Tuberaria lignosa as entry inhibitors of HIV

  • L.M. Bedoya

      Affiliations

    • Centro Nacional de Microbiología, Instituto de Salud Carlos III, Crt. Majadahonda a Pozuelo, 28220 Majadahonda, Madrid, Spain
    • Departamento de Farmacología, Facultad de Farmacia, Universidad Complutense, Avda. Complutense, s/n, 28040 Madrid, Spain
    • ,
  • M.J. Abad

      Affiliations

    • Departamento de Farmacología, Facultad de Farmacia, Universidad Complutense, Avda. Complutense, s/n, 28040 Madrid, Spain
    • Corresponding Author InformationCorresponding author. Tel.: +34913942276; fax: +34913941726.
    • ,
  • S. Sánchez-Palomino

      Affiliations

    • Centro Nacional de Microbiología, Instituto de Salud Carlos III, Crt. Majadahonda a Pozuelo, 28220 Majadahonda, Madrid, Spain
    • ,
  • J. Alcami

      Affiliations

    • Centro Nacional de Microbiología, Instituto de Salud Carlos III, Crt. Majadahonda a Pozuelo, 28220 Majadahonda, Madrid, Spain
    • ,
  • P. Bermejo

      Affiliations

    • Departamento de Farmacología, Facultad de Farmacia, Universidad Complutense, Avda. Complutense, s/n, 28040 Madrid, Spain

published online 14 September 2009.

Abstract 

Screening of plants from the Iberian Peninsula for anti-human immunodeficiency virus (-HIV) activity revealed that aqueous extract of Tuberaria lignosa gave positive results. Following an activity-guided procedure, the crude extract was counterextracted, and the subsequent fractions obtained tested for their anti-HIV activity in vitro. The bioassay-guided fractionation of the extract afforded an ellagitannin enriched fraction (EEF) isolated for the first time from this species. This EEF exhibited antiviral activity against HIV in MT-2 infected cells, with an IC50 value of 2.33μg/ml (selectivity index greater than 21). Inhibition of HIV infection by EEF appears to be mediated by CD4 down-regulation, the main receptor for HIV entry. CXCR4 and CCR5 receptors were not affected by EEF, explaining why EEF is able to inhibit R5 and X4 infections.

Keywords: Tuberaria lignosa, Cistaceae, Ellagitannin, Human immunodeficiency virus

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PII: S0944-7113(09)00209-8

doi:10.1016/j.phymed.2009.08.008

Phytomedicine
Volume 17, Issue 1 , Pages 69-74, January 2010

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