629Ac的乏氧细胞毒性

目的研究丝裂霉素C（MMC）衍生物629Ac（5-吖丙啶-3-羟甲基乙酸酯基-1-甲基吲哚-4，7-二酮）的乏氧细胞毒性，为629Ac作为新型辐射增敏剂的应用提供实验和理论依据。方法在有氧和乏氧条件下用MTT法研究MMC和629Ac的IC50（半数抑制浓度）及C1.6（增敏比达1．6的化合物浓度）。结果乏氧条件下629Ac对HepG2细胞的IC50比有氧条件下低；乏氧和有氧条件下，629Ac的IC50比MMC的IC50都小；对于HepG2细胞，MMC具有乏氧选择性辐射增敏作用，其C1.6比629Ac大，且629Ac在有氧条件下也有辐射增敏效应。结论初步研究结果表明，对于HepG2细胞629Ac具有乏氧细胞毒性和辐射增敏效应，并且这些效应都强于MMC。

The hypoxia cytotoxicity of 629Ac

Purpose To study the hypoxia cytotoxicity of 629Ac(5-aziridinyl-3-hydroxy methyl acetate-1-methylindole-4,7-dione), the mitomycin C(MMC) analog,and to provide experimental and theoretical bases for application of 629Ac as a new radiosensitizer. Methods The IC_(50)(the inhibitory concentration 50%) and C_(1.6)(the concentration when the Sensitization Enhancement Ratio up to 1.6) were evaluated by MTT method under anaerobic and aerobic respectively. Results The IC_(50) of 629Ac to HepG2 cells under anaerobic was lower than that of under aerobic.Both under anaerobic and aerobic,IC_(50) of 629Ac were lower than that of MMC respectively.For HepG2 cells,hypoxia selective radiosensitization of MMC was observed,it's C_(1.6) was higher than that of 629Ac,while under aerobic 629Ac also showed radiosensitization. Conclusions In our primarily experiments,629Ac not only showed hypoxia cytotoxicity but also radiosensitization,and the biological effects of 629Ac were all stronger than that of MMC.