Ellagitannins from Tuberaria lignosa as entry inhibitors of HIV

• Published in: Phytomedicine (Stuttgart) 2010, Vol.17 (1), p.69-74
• Main Authors: Bedoya, L.M., Abad, M.J., Sánchez-Palomino, S., Alcami, J., Bermejo, P.
• Format: Article
• Language: English
• Subjects: Anti-HIV Agents - isolation & purification; Anti-HIV Agents - pharmacology; Anti-HIV Agents - therapeutic use; Care and treatment; CD4-Positive T-Lymphocytes - metabolism; Cistaceae; Cistaceae - chemistry; Down-Regulation; Ellagitannin; Frostwort; Health aspects; HIV - drug effects; HIV infection; HIV Infections - prevention & control; Human immunodeficiency virus; Humans; Hydrolyzable Tannins - isolation & purification; Hydrolyzable Tannins - pharmacology; Hydrolyzable Tannins - therapeutic use; Inhibitory Concentration 50; Jurkat Cells; Materia medica, Vegetable; Plant extracts; Plant Extracts - chemistry; Plant Extracts - pharmacology; Plant Extracts - therapeutic use; Receptors, CCR5; Receptors, CXCR4; Tuberaria lignosa; Virus Integration - drug effects
• ISSN: 0944-7113; 1618-095X
• DOI: 10.1016/j.phymed.2009.08.008

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 2.33 μg/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.