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为了评价黄芩甙中糖的存在和糖的种类对抗ＨＩＶ活性的影响，由天然黄芩甙出发制备了黄芩甙元和５，６Ｏ二苄基黄芩甙元，并合成了５羟基６Ｏ苄基黄酮７βＤ葡萄糖甙（１２），５羟基６Ｏ苄基黄酮７βＤ半乳糖甙（１３），５羟基６Ｏ苄基黄酮７αＤ甘露糖甙（１４），５羟基６Ｏ苄基黄酮７αＤ阿拉伯糖甙（１５）。以上化合物及部分中间体的生物活性试验表明：黄芩甙及黄芩甙元均抑制免疫缺陷病毒逆转录酶（ＨＩＶ１ＲＴ）及在细胞培养中抑制ＨＩＶ１；黄芩甙及黄芩甙元的６位羟基被遮蔽则丧失抑制ＨＩＶ１ＲＴ活性，说明６羟基为抑制ＨＩＶＲＴ活性所必需；黄芩甙元抑制ＨＩＶ１活性及细胞毒性均强于黄芩甙，两种化合物治疗指数相近。
In order to evaluate the presence of carbohydrates in baicalin and the type of sugar on the anti-HIV activity, baicalin and 5,6-O-dibenzyl baicalin were prepared from natural baicalin and 5-hydroxy-6 O benzyl flavonoids 7 β D glucoside (12), 5 hydroxy 6 O benzyl flavonoids 7 β D galactoside (13), 5 hydroxy 6 O benzyl flavonoids 7 α D mannoside (14), 5 hydroxy 6 O benzyl flavonoids 7 α Arabinoside (15). The above compounds and some of the biological activity of intermediate tests showed that: baicalin and baicalin glycosides inhibit immunodeficiency virus reverse transcriptase (HIV 1RT) and in cell culture inhibit HIV 1; baicalin and baicalin 6 Hydroxylation was lost to inhibit HIV 1RT activity, indicating that 6 hydroxylation is necessary for the inhibition of HIV RT activity; baicalin inhibition of HIV 1 activity and cytotoxicity were stronger than baicalin, two compounds similar therapeutic index.