The Studies On Chemical Modification Of Two Anti-HIV Natural Products

Acquired Immune Deficiency Syndrome (AIDS) caused by human immuno dificiency virus (HIV) has brought to the people's great attention in a global scale for it's quick spread and high mortality. Many countries have been working for the studies on exploiting and developing anti-HIV agents and devoted great attention to searching anti-HIV compounds from medicinal plants and other natural products. Professor Chen Hong Shan and her co-workers in our institute first discovered the experimental anti-HIV activity of Baicalin, a natral flavonoid compound in 1988. Hypericin extracted from the fresh flowers of genus Hypericum has been conducting clinical trial on thetreatment of AIDS. Our studies were focused on the partial structure modification of the above-mentioned two natural products in the searching for anti-HIV agents.The aglycone Baicalien, the key intermediate 5,6-O-di-benzyl-baicalien(B5) were prepared from Baicalin in order to evaluate the influence on anti-HIV activity of different glycosyls linked to Baicalien. Baicalin is a glycuronoide which is difficult to be hydrolized. Reported methods are enzyme hydrolysis with baicalinase which exists in the fresh plant. It is unconvenient for quantity preperation. We have tried out acidic hydrolysis and employed to prepare Baicalien from Baicalin. Benzyl and acetyl blocked...