el-Zayat A A, Degen D, Drabek S, Clark G M, Pettit G R, Von Hoff D D
Cancer Therapy and Research Center, San Antonio, TX 78229.
Anticancer Drugs. 1993 Feb;4(1):19-25. doi: 10.1097/00001813-199302000-00002.
Combretastatin A-4 is a natural product which was isolated from the South African tree Combretum caffrum. In this study, the cytotoxic activity of combretastatin A-4 was tested in radiometric and human tumor cloning assays against eight different tumor cell lines and against 15 patient tumors in the human tumor cloning assay. To test the preferential cytotoxicity of combretastatin A-4 against tumor cells versus non-tumor cells, it was also tested in the radiometric assay against both normal human diploid fibroblasts and human bone marrow cells. Of the eight cell lines used, combretastatin A-4 showed preferential cytotoxicity for six of them. In addition, combretastatin A-4 showed a concentration-dependent cytotoxicity against a variety of human tumors. Based on the data generated in this study, combretastatin A-4 should be further tested in in vivo preclinical models.
康普瑞他汀A-4是一种从南非灌木非洲风车子中分离出的天然产物。在本研究中,采用放射性测定法和人肿瘤克隆试验检测了康普瑞他汀A-4对8种不同肿瘤细胞系的细胞毒性活性,并在人肿瘤克隆试验中检测了其对15例患者肿瘤的细胞毒性活性。为了测试康普瑞他汀A-4对肿瘤细胞相对于非肿瘤细胞的优先细胞毒性,还采用放射性测定法对正常人二倍体成纤维细胞和人骨髓细胞进行了检测。在所使用的8种细胞系中,康普瑞他汀A-4对其中6种显示出优先细胞毒性。此外,康普瑞他汀A-4对多种人类肿瘤显示出浓度依赖性细胞毒性。基于本研究产生的数据,康普瑞他汀A-4应在体内临床前模型中进一步测试。