佛甲草中细胞毒活性成分的研究

采用中压柱色谱和制备高效液相色谱法对中国传统民族药佛甲草(Sedum lineare Thunb)的甲醇提取物化学成分进行分离，从中分离得到6个化合物.首次对化合物山奈酚7-O-6″-O-丙二酸单酰-D-吡喃葡萄糖苷(1)的波谱数据进行了归属，用MTT法测试6个单体成分对人肝癌细胞株HepG2和Hep3B的抑制作用.结果显示6个化合物均对HepG2和Hep3B细胞表现出抗肿瘤活性，并且IC50值在22.6～91.5 μg/mL之间，在浓度大于100 μg/mL时也没有表现出对人正常肝细胞L－02的抑制作用.相比于黄酮类化合物1、2，苯丙酸类化合物3～6(IC50＝22.6～44.3 μg/mL)对HepG2和Hep3B细胞表现出更强的抑制作用.其中，顺式苯丙酸类化合物5对HepG2和Hep3B细胞的抑制作用最明显.其IC50值范围在22.6～28.2 μg/mL，能明显抑制人肝癌细胞的增殖，诱导其凋亡.

Cytotoxic chemical constituents of Sedum lineare Thunb

Bioassay-guided purification on the methanol extract of the traditional Chinese ethnic medicine “Fojiacao” (Sedum lineare Thunb) was performed on the medium pressure column chromatograph and preparative HPLC. Six compounds has been isolated and the 1H- and 13C-NMR data of kaempferol 7-O-6″-O-malonyl-β-D-glucopyranoside (1) was firstly confirmed. The anti-HCC activities of compounds 1～6 were evaluated by the MTT assay using HepG2 and Hep3B hepatocellular carcinoma cell lines. All compounds exhibited anticancer activities against HepG2 and Hep3B tumor cell lines with IC50 value range of 22.6～91.5 μg/mL， respectively， and showed no cytotoxity against L－02 cell line up to 100 μg/mL. Phenylpropionic acids 3～6 displayed higher anti-HCC activity against HepG2 and Hep3B tumor cell lines with IC50 value range between 22.6 and 44.3 μg/mL than flavonoids 1， 2 in which the cis phenylpropanoid acid 5 exhibited the strongest anti-HCC activity against HepG2 and Hep3B tumor cell lines with IC50 values of 22.6 and 28.2 μg/mL， respectively.