A comparison of HIV-1 integrase inhibition by aqueous and methanol extracts of Chinese medicinal herbs.
The aqueous and methanol extracts of twenty herbs traditionally used in Chinese medicine were screened for anti-HIV-1 integrase activity in a non-radioactive ELISA-based HIV-1 integrase assay. The screening was performed at an herb extract concentration of 50 microg/ml. It was found that most of the aqueous and methanol herb extracts could elicit strong inhibition of HIV-I integrase activity. The inhibition was most likely due to tannins or polyphenolics in the herb extracts. In most of the herb extracts, 40-80% of the anti-HIV-1 integrase activity could be removed after passing through a minicolumn of polyamide resin. After removal of polyphenolic compounds, the methanol extract of Paeonia suffruticosa still exerted potent inhibition of HIV-1 integrase (EC50 = 15 microg/ml) and the aqueous extract of Prunella vulgaris caused moderate inhibition (EC50 = 45 microg/ml). The results support the view that herbs represent a rich source of anti-HIV compounds.
Au
T K
TK
Department of Biochemistry, The Chinese University of Hong Kong, Shatin, NT.
Lam
T L
TL
Ng
T B
TB
Fong
W P
WP
Wan
D C
DC
D004365:Drugs, Chinese Herbal / Q000494:pharmacology*; D004797:Enzyme-Linked Immunosorbent Assay; D019427:HIV Integrase / Q000378:metabolism*; D019428:HIV Integrase Inhibitors / Q000494:pharmacology*; D006801:Humans; D000432:Methanol; D010636:Phenols / Q000494:pharmacology; D010936:Plant Extracts / Q000494:pharmacology; D012997:Solvents; D014867:Water
D004365:Drugs, Chinese Herbal; D019428:HIV Integrase Inhibitors; D010636:Phenols; D010936:Plant Extracts; D012997:Solvents; D014867:Water; D019427:HIV Integrase; D000432:Methanol