新型吲哚醌类生物还原活性物629的细胞毒性和辐射增敏作用的研究

5-(aziridin-1-yl)-3-hydroxymethyl-1-methylindole-4,7-dione:Its cytotoxicity to HepG2 cells and the radiation sensitizing effect

研究丝裂霉素C(MitomycinC,MMC)的衍生物-新型吲哚醌类生物还原活性物629的细胞毒性和辐射增敏作用。采用四氮甲基唑蓝(Methylthiazolyltetrazolium,MMT)比色法研究MMC和629对HepG2细胞的细胞毒性以及629对肝原代细胞的细胞毒性,结果表明629对肝原代细胞无毒性作用,而其对HepG2肝癌细胞的毒性要高于其母体化合物MMC;此外,采用体外细胞克隆培养法观察MMC和629对HepG2细胞的辐射增敏作用,结果显示629的辐射增敏效果强于MMC。上述研究提示,629具有低毒的增敏效果,在临床上将具有广泛的应用远景。

The object of this work is to study the radiation sensitizing effect and cytotoxicity to HepG2 cells of a newtapy bioreduction activity-5-（aziridin-1-y1）-3-hydroxymethyl-1-methylindole-4,7-dione（629） in vitro. Cytotoxicity of 629 or MMC in vitro were evaluated in HepG2 cells or hepatocyte by MMT method under anaerobic and aerobic, in vitro radiosensitizing ability was estimated using Cells Cloning Technology. The results suggested that the cytotoxicity of 629 to HepG2 cells has significant enhanced （p〈0.05） than MMC, and no significant cytotoxicity to hepatocyte; in addition, 629 has radiosensitizing effect in vitro on HepG2 cells and the SER value ranged from 1.17 to1.92, it is showed that 629 have powerful radiosensitizing effect than MMC. The results indicated that 629 has radiosensitizing characteristic with high efficiency and low toxicity, and it is promising for clinic applications.