江南卷柏中的雙黃酮化合物於HIV-1蛋白酵素的抑制活性

Test of the Biflavones from Selaginella Moellendorffii on the in Vitro Inhibition of HIV-1 Protease

從中樂江南卷柏中分出的五個雙黃酮化合物，分別測定對於HIV-1蛋白酵素之抑制活性。結果顯示其中之穗花衫雙黃酮具有抑制作用，而其他四個雙黃酮未顯出抑制作用。不過，穗花衫雙黃酮的抑制活性比天門冬酸蛋白酵素抑制劑pepstatin A為低。另外，穗花衫雙黃酮對於胰蛋白酵素(bovine trypsin)，則不具抑制活性。由此顯示，穗花衫雙黃酮對於HIV-1蛋白酵素，具有特殊之抑制性。

Five biflavones with methoxy and hydroxy substituents at different positions were isolated from the herbal plant of Selaginella moellendorffii. These compounds were tested for the inhibition on HIV-1 protease in vitro. One biflavone, amentoflavone, was active on the inhibition of this viral enzyme whereas the other four gave no detectable activity. However, the inhibitory activity of amentoflavone was weaker than that of pepstatin A, a known aspartyl protease inhibitor. Amentoflavone was further tested on a pancreatic protease, bovine trypsin, and no inhibition was observed. These results suggest that amentollavone inhibits HIV-1 protease specifically.