A comparison of human immunodeficiency virus type-1 protease inhibition activities by the aqueous and methanol extracts of Chinese medicinal herbs

The aqueous and methanol extracts of thirty-one herbs traditionally used as anti-fever remedies in China were screened for their in vitro inhibition o n human immunodeficiency virus type-1 protease (HIV-1 PR). The activity of recombinant HIV-1 protease was determined by sequence-specific cleavage at the Tyr-Pro bond of the fluorogenic substrate (Arg-Glu(EDANS)-Ser-Gln-Asn-T yr-Pro-Ile-Val-Gln-Lys(DABCYL)-Arg) or by HPLC anaylsis of the cleavage pro ducts after incubation of the enzyme with a synthetic peptide substrate (Ac etyl-Ser-Gln-Asn-Tyr-Pro-Val-Val-amide) Among the herbal extracts examined, the aqueous extracts of Prunella vulgaris and Scutellaria baicalensis and the methanol extracts of Woodwardia unigemmata, Paeonica suffruticosa and S patholobus suberectus elicited significant inhibition (>90%) at a concentra tion of 200 mug/ml. (C) 2000 Elsevier Science Inc. All rights reserved.