抗生素药物——喹诺酮类引起的DNA损伤。

DNA-damage caused by antibiotic drugs - quinolones.

作者信息

Merschsundermann V, Hauff K, Braun P, Lu W, Hof H

出版信息

Int J Oncol. 1994 Oct;5(4):855-9. doi: 10.3892/ijo.5.4.855.

DOI:10.3892/ijo.5.4.855

Abstract

In the present investigation, the genotoxic potencies (SOSIP) of 10 antibiotic quinolones (topoisomerase LT inhibitors) were tested in the sfiA::lacZ fusion containing strain Escherichia coli PQ37 using a modified procedure of the SOS chromotest. A number of quinolones exhibited extremely high DNA damaging effects in the absence of an exogenous metabolizing system. The highest SOS inducing potencies (SOSIP) exhibited sparfloxacin with 2,400 Delta IF/nmole, ciprofloxacin (SOSIP = 184 Delta IF/nmole) and norfloxacin (SOSIP=120 Delta IF/nmole), whereas pipemic acid (SOSIP=4.6 Delta IF/nmole), cinoxacin (SOSIP=0.5 Delta IF/nmole) and nalidixic acid (SOSIP=0.5 Delta IF/nmole) showed only weak genotoxicity. The possibility of mutagenic effects caused by quinolones in eukaryotic cells is discussed.

摘要

在本研究中，使用改良的SOS显色试验程序，在含有sfiA::lacZ融合基因的大肠杆菌PQ37菌株中测试了10种抗生素喹诺酮类药物（拓扑异构酶LT抑制剂）的遗传毒性潜力（SOSIP）。在没有外源代谢系统的情况下，许多喹诺酮类药物表现出极高的DNA损伤作用。诱导SOS的能力（SOSIP）最高的是司帕沙星，为2400ΔIF/纳摩尔，环丙沙星（SOSIP = 184ΔIF/纳摩尔）和诺氟沙星（SOSIP = 120ΔIF/纳摩尔），而吡哌酸（SOSIP = 4.6ΔIF/纳摩尔）、西诺沙星（SOSIP = 0.5ΔIF/纳摩尔）和萘啶酸（SOSIP = 0.5ΔIF/纳摩尔）仅表现出较弱的遗传毒性。文中还讨论了喹诺酮类药物在真核细胞中引起诱变效应的可能性。