强细胞生长和微管蛋白抑制剂康普瑞他汀A-4的分离与结构
Isolation and structure of the strong cell growth and tubulin inhibitor combretastatin A-4.
作者信息
Pettit G R, Singh S B, Hamel E, Lin C M, Alberts D S, Garcia-Kendall D
机构信息
Cancer Research Institute, Arizona State University, Tempe 85287.
出版信息
Experientia. 1989 Feb 15;45(2):209-11. doi: 10.1007/BF01954881.
The African tree Combretum caffrum (Combretacae) has been found to contain a powerful inhibitor of tubulin polymerization (IC50 2-3 microM), the growth of murine lymphocytic leukemia (L 1210 and P 388 with ED50 approximately 0.003 microM and human colon cancer cell lines [(e.g. LoVo (ED50 = 0.005 microgram/ml), HT 29 (ED50 0.02 microgram/ml, Colo 205 (ED50 = 0.07 microgram/ml), DLD-1 (ED50 = 0.005 microgram/ml) and HCT-15 (ED50 = 0.0009 microgram/ml] designated combretastatin A-4 (1c). The structure assigned by spectral techniques was confirmed by synthesis.
已发现非洲树木南非风车子（使君子科）含有一种强大的微管蛋白聚合抑制剂（IC50为2 - 3微摩尔），对鼠淋巴细胞白血病（L1210和P388，ED50约为0.003微摩尔）以及人结肠癌细胞系[如洛伏（LoVo，ED50 = 0.005微克/毫升）、HT29（ED50 = 0.02微克/毫升）、科洛205（Colo 205，ED50 = 0.07微克/毫升）、DLD - 1（ED50 = 0.005微克/毫升）和HCT - 15（ED50 = 0.0009微克/毫升）]有抑制作用，该抑制剂被命名为combretastatin A - 4（1c）。通过光谱技术确定的结构经合成得到证实。
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