[新制癌菌素斯他莫辛（YM881）的作用机制]
[Action mechanisms of zinostatin stimalamer (YM881)].
作者信息
Tanaka S, Numasaki Y, Maeda H
机构信息
Department of Research II, Yamanouchi Pharmaceutical Co., Ltd., Tokyo, Japan.
出版信息
Gan To Kagaku Ryoho. 1991 Oct;18(13):2295-300.
The mechanism of action of zinostatin stimalamer (YM881) was studied. YM881 suppressed colony formation of HeLa cells dose-dependently, and showed cytocidal activity. The compound inhibited DNA synthesis, but neither RNA nor protein synthesis in L1210 cells, and caused cellular DNA strand breaks in HeLa cells and DNA cleavage of PM2 phage supercoiled DNA. YM881 was also shown to cause typical G2/M arrest on L1210 cell cycle, and inhibited DNA polymerase alpha of HeLa cells, but only at high concentrations. Present study showed that antitumor and cytotoxic mechanisms of YM881 were identical to neocarzinostatin (NCS) and due to the cellular DNA strand breaks caused by direct DNA-cleaving activity and the subsequent inhibition of DNA synthesis.
对锌抑素斯替马兰（YM881）的作用机制进行了研究。YM881剂量依赖性地抑制HeLa细胞的集落形成，并表现出杀细胞活性。该化合物抑制L1210细胞中的DNA合成，但不抑制RNA或蛋白质合成，并导致HeLa细胞中的细胞DNA链断裂以及PM2噬菌体超螺旋DNA的DNA切割。YM881还显示出在L1210细胞周期上引起典型的G2/M期阻滞，并抑制HeLa细胞的DNA聚合酶α，但仅在高浓度时才起作用。目前的研究表明，YM881的抗肿瘤和细胞毒性机制与新制癌菌素（NCS）相同，是由于直接DNA切割活性导致的细胞DNA链断裂以及随后对DNA合成的抑制。
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