Reliability of phototoxic tests of fluoroquinolones in vitro  

体外检测氟喹诺酮类药物光毒性的可靠性(英文)

作　　者：张婷[1] 李俊岭[1] 马小超[1] 欣坚[1] 屠曾宏[1] 

机构地区：[1]中国科学院上海生命科学研究院上海药物研究所新药研究国家重点实验室

出　　处：《Acta Pharmacologica Sinica》2003年第5期453-459,480,共8页中国药理学报（英文版）

摘　　要：AIM: To make sure the reliability of phototoxic tests in vitro by comparing the phototoxic potential of 4 fluoroquinolones(FQ). METHODS: Lomefloxacin (LFLX), sparfloxacin (SPFX), ciprofloxacin (CPFX), and norfloxacin (NFLX) were tested by Wistar rat phototoxic test and Balb/c mouse phototoxic test in vivo, and Chinese hamster V79 cell micronucleus test and NIH 3T3 MTT test in vitro under the different condition of UVA irradiation. RESULTS: In all experiments, LFLX and SPFX showed higher phototoxic potential compared with the control (P<0.01 vs 1% CMC), CPFX was mild (P<0.05 vs physiological saline), NFLX did not show phototoxicity in vivo, however at a higher concentration (10μmol/L) in vitro, it also induced phototoxicity as other FQ. CONCLUSION: There are good correlations between phototoxic tests in vivo and in vitro. These results ensure the validation of phototoxic tests in vitro.目的:比较四个氟喹诺酮类抗生素的光毒性来确定体外实验的可靠性。方法:用体内Wistar大鼠光毒性实验,Balb/c小鼠光毒性实验和体外中国仓鼠V79细胞微核实验,NIH3T3 MTT实验在不同的UVA照射条件下测定四个氟喹诺酮类抗生素的光毒性。结果:在所有实验中,司帕沙星、洛美沙星显示出较强的光毒性,与对照组相比,均有非常显著性差异(P<0.01);环丙沙星光毒性较温和,有显著性差异(P<0.05);诺氟沙星在体内实验中没有显示出光毒性,但在体外实验中较高剂量(10μmol/L)能产生光毒性。结论:体内外测定药物光毒性有良好的相关性,因此体外检测氟喹诺酮类药物光毒性是可靠的。

关 键 词：PHOTOTOXICITY FLUOROQUINOLONES LOMEFLOXACIN SPARFLOXACIN 

分 类 号：R96[医药卫生—药理学]