Ellagitannins from Tuberaria lignosa as entry inhibitors of HIV

Phytomedicine. 2010 Jan;17(1):69-74. doi: 10.1016/j.phymed.2009.08.008. Epub 2009 Sep 11.


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 IC(50) value of 2.33mug/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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / isolation & purification
  • Anti-HIV Agents / pharmacology
  • Anti-HIV Agents / therapeutic use*
  • CD4-Positive T-Lymphocytes / metabolism
  • Cistaceae / chemistry*
  • Down-Regulation
  • HIV / drug effects*
  • HIV Infections / prevention & control*
  • Humans
  • Hydrolyzable Tannins / isolation & purification
  • Hydrolyzable Tannins / pharmacology
  • Hydrolyzable Tannins / therapeutic use*
  • Inhibitory Concentration 50
  • Jurkat Cells
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology
  • Plant Extracts / therapeutic use*
  • Receptors, CCR5
  • Receptors, CXCR4
  • Virus Integration / drug effects*


  • Anti-HIV Agents
  • Hydrolyzable Tannins
  • Plant Extracts
  • Receptors, CCR5
  • Receptors, CXCR4