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体外检测氟喹诺酮类药物光毒性的可靠性
作者姓名:Zhang T  Li JL  Ma XC  Xin J  Tu ZH
作者单位: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,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,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,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,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 上海 200031 中国,上海 200031 中国,上海 200031 中国,上海 200031 中国,上海 200031 中国
摘    要: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,NIH 3T3 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:氟喹诺酮类抗生素  光毒性  体外实验  司帕沙星  洛美沙星

Reliability of phototoxic tests of fluoroquinolones in vitro
Zhang T,Li JL,Ma XC,Xin J,Tu ZH.Reliability of phototoxic tests of fluoroquinolones in vitro[J].Acta Pharmacologica Sinica,2003,24(5):453-459,480.
Authors:Zhang Ting  Li Jun-Ling  Ma Xiao-Chao  Xin Jian  Tu Zeng-Hong
Institution:State Key Laboratory of Drug Research, Shanghai Institue of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 200031, China.
Abstract: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 (10 micromol/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.
Keywords:phototoxicity  fluoroquinolones  lomefloxacin  sparfloxacin
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