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以黄芩黄素作对照,研究了车前草属植物中黄酮类化台物对HIV逆转录酶的抑制作用及其结构与抑制活性的关系。 实验材料与方法:从车前(Plantago asiatica)分离出芹黄素、木犀草素、大波斯菊甙、木犀草素-7-葡糖甙、黄芩素、6-羟基木犀草素、车前甙和6-羟基木犀草素-7-葡糖甙,从大车前(Plantago major)分离出高车前甙。 实验结果:黄芩素和6-羟基木犀草素是作用较强的HIV逆转录酶抑制剂。抑制作用的强弱顺序为6-羟基木犀草素>黄芩素>黄芩黄素>木犀草素。芹黄素无抑制作用。车前甙和6-羟基木犀草素-7-葡糖甙对HIV逆转录酶具有较强的抑制作用,与黄芩黄素的作用相当。但是,黄酮骨架中与7位羟基进行O-葡萄糖基化及6位羟基进行O-甲基化都能够增强抑制作用。
Astragaloside was used as a control to study the inhibitory effect of flavonoids from Plantago asiatica on HIV reverse transcriptase and its relationship with its inhibitory activity. Experimental materials and methods: isolation of apigenin, luteolin, cosmos, luteolin-7-glucoside, baicalein, 6-hydroxy luteolin, psyllium from the plantago (Plantago asiatica) With 6-hydroxy luteolin-7-glucoside, we separated the front caravan from Plantago major. Experimental results: Baicalein and 6-hydroxyluteolin are potent HIV reverse transcriptase inhibitors. The order of inhibition was 6-hydroxy luteolin> safrole> baicalein> luteolin. Apigenin has no inhibitory effect. Psyllium and 6-hydroxyluteolin-7-glucoside have a strong inhibitory effect on HIV reverse transcriptase, which is equivalent to that of astragaloside. However, O-glucosylation of the 7-position hydroxyl group in the flavonoid skeleton and O-methylation of the 6-position hydroxyl group enhance the inhibitory effect.