Min B S, Kim Y H, Lee S M, Jung H J, Lee J S, Na M K, Lee C O, Lee J P, Bae K
College of Pharmacy, Chungnam National University, Taejon, Korea.
Arch Pharm Res. 2000 Apr;23(2):155-8. doi: 10.1007/BF02975505.
Bioassay-guided fractionation of Crataegus pinnatifida (Rosaceae) gave two cytotoxic ursane-type triterpenes which were identified as uvaol (1) and ursolic acid (2) by physicochemical and spectroscopic methods. 3-Oxo-ursolic acid (3) was synthesized from ursolic acid (2) by Jones method. The cytotoxic activities of these compounds were tested against murine L1210 and human cancer cell lines (A549, SK-OV-3, SK-MEL-2, XF498, and HCT15) in vitro. Compounds 1 and 2 showed moderate cytotoxicities against L1210, whereas they showed weak activities against human cancer cell lines. However, compound 3 exhibited potent cytotoxic activities both in murine and in human cancer cell lines.
对山楂（蔷薇科）进行生物测定指导的分级分离得到了两种具有细胞毒性的乌苏烷型三萜，通过物理化学和光谱方法将其鉴定为羽扇豆醇（1）和熊果酸（2）。3-氧代熊果酸（3）由熊果酸（2）通过琼斯方法合成。在体外测试了这些化合物对小鼠L1210和人癌细胞系（A549、SK-OV-3、SK-MEL-2、XF498和HCT15）的细胞毒性活性。化合物1和2对L1210显示出中等细胞毒性，而对人癌细胞系显示出较弱活性。然而，化合物3在小鼠和人癌细胞系中均表现出强效细胞毒性活性。
