Studies On The Anti-HIV Principles Of Ilex Pubescens Hook.et Arn

The traditional Chinese medicine (TCM), Maodongqing, dry roots of Ilex pubescens Hook.et Arn. of Aquifoliaceae, has been used against such diseases caused by virus and fungi, even other usages in China. Flavones, coumarins, terpenes, amino acids, sterols, polysaccharides and some other types of components have been found in Maodongqing, and over 10 compounds were determined clearly. But the true principles to its anti-virus are not elucidated yet.The crude extract of Maodongqing exhibited remarkable anti-HIV activity among the 40 kinds of TCM screened previously by MT4 cell model. The minimal effective concentration is 40ug/mL. In this project, isolation and purification were performed guiding by anti-HIV activities. The 90%EtOH extract of Maodongqing was re-extracted with petroleum ether, ethyl acetate, n-butanol, and water successively to give four fractions, among of which, fraction ethyl acetate was the most effective one.Fifteen compounds were separated and determined from fraction ethyl acetate, including emodin (I), chrysophanol(II), aloe-emodin(III), p-sitosterol (IV), isovanillin(V), physcion(VI), syringaldehyde(VII), tyrosol(VIII), olivil(IX), emodin 8-O-β-D-glucopyranoside(X), chrysophanol 8-O-β-D-glucopyranoside (XI), desoxyrhaponticin (XII), oleuropein (XIII), ligustroside (XIV) and daucosterol (XV). And all compounds were found from Maodongqing for the first time.Compounds I, II, III, VIII, IX, and XI were screened by MT4 cell model, three of which (I, IX, XI) showed remarkable anti-HIV activities. The anti-HIV activities of compound IX and XI were indicated firstly. Compound IX was obtained in large quantities, exhibited good effect, and may be the major anti-HIV principle of Maodongqing. Furthermore, compound IX belongs to the tetrahydrofuran-type lignan, and its anti-HIV activity was reported firstly in this type of lignan.