Ho C K, Law S L, Chiang H, Hsu M L, Wang C C, Wang S Y
Department of Medical Research, Veterans General Hospital, Taipei, Republic of China.
Biochem Biophys Res Commun. 1991 Oct 15;180(1):118-23. doi: 10.1016/s0006-291x(05)81263-x.
We have found that mitoxantrone can inhibit the polymerization of brain tubulin in a dose dependent manner. MXT had relatively high affinity for tubulin but had no appreciable effect on tubulin associated guanosine-triphosphatase (GTPase) activity nor could it compete with vinblastine (VB) and colchicine (Col) for tubulin binding sites. Furthermore, MXT (0.1-10 microM) is antiproliferative to cold-treated (0 degree C) epithelial cells after only brief exposure (30 min). These results indicated that MXT is a microtubule inhibitory agent and can exert its anticellular effect through modulation of microtubule assembly.
我们发现米托蒽醌能够以剂量依赖的方式抑制脑微管蛋白的聚合。米托蒽醌对微管蛋白具有相对较高的亲和力，但对与微管蛋白相关的鸟苷三磷酸酶（GTP酶）活性没有明显影响，也不能与长春碱（VB）和秋水仙碱（Col）竞争微管蛋白结合位点。此外，仅短暂暴露（30分钟）后，米托蒽醌（0.1 - 10 microM）对经冷处理（0摄氏度）的上皮细胞具有抗增殖作用。这些结果表明，米托蒽醌是一种微管抑制药物，可通过调节微管组装发挥其抗细胞作用。
