Franzblau S G, White K E
Laboratory Research Branch, Gillis W. Long Hansen's Disease Center, Carville, Louisiana 70721.
Antimicrob Agents Chemother. 1990 Feb;34(2):229-31. doi: 10.1128/AAC.34.2.229.
The in vitro activities of 20 fluoroquinolones against Mycobacterium leprae were evaluated by using the BACTEC 460 system. M. leprae was incubated in BACTEC 12B medium at 33 degrees C under reduced oxygen for 2 to 3 weeks in the presence of fluoroquinolones at 0.31 to 5 micrograms/ml. Activity was determined by a reduction in 14CO2 evolution compared with that of drug-free controls. Of the commercially available agents, ofloxacin was most active, while enoxacin and norfloxacin were inactive. However, a number of newer fluoroquinolones (AT-4140, OPC-17100, OPC-17066, PD-117596, PD-124816, PD-127391, and WIN-57273), all containing a cyclopropyl group at R-1 and, with the exception of WIN-57273, either a halogen or methyl group at R-8, were more active than ofloxacin in vitro. Further in vivo evaluations of these agents should help determine their potential for use against leprosy.
采用BACTEC 460系统评估了20种氟喹诺酮类药物对麻风分枝杆菌的体外活性。将麻风分枝杆菌在含0.31至5微克/毫升氟喹诺酮类药物的情况下，于33℃、低氧条件下在BACTEC 12B培养基中培养2至3周。通过与无药对照相比14CO2释放量的减少来确定活性。在市售药物中，氧氟沙星活性最高，而依诺沙星和诺氟沙星无活性。然而，一些较新的氟喹诺酮类药物（AT-4140、OPC-17100、OPC-17066、PD-117596、PD-124816、PD-127391和WIN-57273），在R-1位均含有一个环丙基，除WIN-57273外，在R-8位含有一个卤素或甲基，其体外活性比氧氟沙星更强。对这些药物进一步进行体内评估应有助于确定它们用于治疗麻风病的潜力。
