文冠果种皮中的香豆素类化合物及抗HIV-1活性研究

Inhibitory activities against HIV-1 of coumarins from the seed coats of Xanthoceras sorbifolia Bunge

利用多种分离技术对文冠果种皮甲醇提取物的乙酸乙酯和正丁醇萃取部分进行分离纯化,根据理化性质和光谱数据鉴定结构,得到3个香豆素类化合物Ⅰ（臭矢菜素B）、Ⅱ（秦皮素）、Ⅲ（秦皮苷）,其中化合物Ⅰ为首次从无患子科中分离得到,Ⅱ、Ⅲ为首次从文冠果种皮中分离得到。通过对HIV-1ⅢB诱导感染C8166细胞致细胞病变的抑制试验及对HIV-1ⅢB感染MT4细胞的保护试验进行抗HIV-1活性研究,结果表明,化合物Ⅰ具有较强的体外抗HIV-1活性,CC50〉200μg/mL,EC50为8.61～12.76μg/mL,选择指数（SI）〉15.67～23.23;对HIV-1ⅢB感染的MT4细胞具有一定的保护作用。

The ethyl acetate and n-butanol fractions from methanolic extract of the seed coats of shinyleaf yellowhorn（Xanthoceras sorbifolia Bunge） were partitioned and purified by means of several separation methods.The structures of these isolates were elucidated by physico-chemical characters and spectroscopic evidences.Three coumarins,ie cleomiscosin B（Ⅰ）,fraxetin（Ⅱ） and fraxin（Ⅲ） were isolated and for the first time,compound Ⅰ was obtained from this plant family, and Ⅱ as well as Ⅲ were obtained from its seed coat.Their inhibitory activities against HIV-1 were studied with inhibition test to cytopathic effect of C8166 cells induced by HIV-1ⅢB and the protection test to infected MT-4 cells by HIV-1ⅢB.Cleomiscosin B（Ⅰ） was found to show the potent anti-HIV-1 activity in vitro with CC-（50） value to exceed 200 μg/mL,EC-（50） value of 8.61-12.76 μg/mL and a selective index of more than 15.67-23.23,and also has protective effects on MT4 cells infected by HIV-1ⅢB.