Laboratory of Toxicology, Bioanalytical Chemistry, and Applied Physical Chemistry, Institute of Pharmacy, Free University of Brussels, Brussels, Belgium.
Drug Chem Toxicol. 2009;32(4):417-23. doi: 10.1080/01480540903130666.
The cytotoxicity of oxaziridines photogenerated after irradiation of chlordiazepoxide (CDZ) and its metabolites was investigated in vitro by a MTT assay on P388 leukemia and B16 melanoma cell lines and compared with that of the anticancer drug, melphalan. For the longer time-exposure experiment, oxaziridines had the same cytotoxicity as melphalan and this toxicity was higher when oxaziridines were photogenerated in the presence of cells. In conclusion, oxaziridines generated after CDZ, demoxepam, and desmethylchlordiazepoxide ultraviolet irradiation exhibited cytotoxicity activity against cancer cell lines. A possibility of CDZ use within the context of photodynamic therapy as a treatment for small, superficial tumors should not be excluded, because oxaziridines can be generated locally by skin-tumor local irradiation after CDZ topical administration.
用 MTT 法检测了氯氮䓬（CDZ）及其代谢物经光照产生的恶唑烷的细胞毒性，在 P388 白血病和 B16 黑素瘤细胞系中进行了体外研究，并与抗癌药物苯丙氨酸进行了比较。对于较长时间暴露实验，恶唑烷的细胞毒性与苯丙氨酸相同，当恶唑烷在细胞存在的情况下光解时，其毒性更高。总之，CDZ、地西泮和去甲氯氮䓬经紫外线照射后产生的恶唑烷对癌细胞系表现出细胞毒性活性。不应排除在光动力疗法的背景下将 CDZ 作为治疗小的、表浅肿瘤的方法，因为 CDZ 局部给药后，经皮肤-肿瘤局部照射可以在局部产生恶唑烷。
