Isolation And Extraction Of Anti-HIV Oligosaccharide And Active Components From Salvia Miltiorrhiza Bunge And Methods For Evaluating Anti-HIV/AIDS Agents

AIDS increasingly threatens the whole world including China. Though there are many active drugs against AIDS, it is still one of the most austere challenge in the 21st century.HIV reverse transcriptase, integrase and protease are 3 essential targets for virus replication. There are 20 drugs approved for clinical usage, involving inhibitors of reverse transcriptase, protease and membrane fusion. Although the HAART has succeeded in reducing the mortality and morbidity of the disease, the current drugs have many problems that can not be overcome easily. HIV vaccine for preventing the infection has not yet been made. It is urgently needed to develop low toxic, highly active and cheap drugs for AIDS patients and HIV victims.Salvia miltiorrhiza Bunge, a plant of Salvia of the Labiatae, is one of important traditional plants used in clinic for treatment of cerebrovascular and hepatic disease. Salvia miltiorrhiza Bunge have been found with multiple pharmacological activities. During the latest decade, looking for the water-soluble active components is mostly interested, and many phenic acids, such as danshensu, caffeic acid, Salvianolic acid A^H, lithospermic acid, rosmarinic acid and so on have been found.The water extracts of Salvia miltiorrhiza Bunge has been found inhibited HIV both in vitro and in vivo in our laboratory. But only the rosmarinic acid, rosmarinic acid glycoside, lithospermic acid and lithospermic acid B have been identified to inhibit HIV-IN in vitro.By using detection of the inhibitory activities on HIV RT and IN in vitro as indicators, The roots were soaked by non-ion water, the water-soluble part passed through resin and eluted with 50% ethanol, the eluents were condensed and lyophilizated to obtain the total active part T6. T6 was detected to have several depsidones and glycosides in it, and the concentration of lithospermic acid B was the main ingredient. T6 inhibited HIV-1 RT and IN with the IC₅₀ of (26.94±4.92)μg/ml and (2.86±1.99)μg/ml respectively in vitro, but was inactive on HIV-1 PR. In MT-4 cell culture, T6 inhibited HIV-1 IIIB virus with the EC₅₀ of...