Camargo E E, Larson S M, Tepper B S, Wagner H N
Int J Lepr Other Mycobact Dis. 1975 Jul-Sep;43(3):234-8.
A simple radiometric method has been developed for evaluating the effect of drugs on the metabolism of M. lepraemurium. The method is based on the measurement of the 14CO2 produced through bacterial metabolism of acetate-U-14C. Seventeen drugs were tested: bacitracin, cephaloridine, chloramphenicol, cycloserine, dactinomycin, DDS, ethionamide, INH, kanamycin, methenamine mandelate, nitrofurantoin, oxacillin, polymyxin B, rifampicin, streptomycin, sulfadimethoxine and vancomycin. The drugs which caused most marked inhibition were chloramphenicol, INH, ethionamide and nitrofurantoin in order of increasing effectiveness. The radiometric study which is completed in 15 days permits direct study of the drug effect on the metabolism of M. lepraemurium and a more rapid screening of antileprosy drugs than has previously been possible. Currently, these observations are being extended to studies of the structure-activity relationships of antileprosy drugs and the metabolism and drug susceptibility of M. leprae in vitro.
已开发出一种简单的放射性测量方法来评估药物对鼠麻风杆菌代谢的影响。该方法基于对通过醋酸 -U-14C 的细菌代谢产生的 14CO2 的测量。测试了 17 种药物:杆菌肽、头孢噻啶、氯霉素、环丝氨酸、放线菌素 D、氨苯砜、乙硫异烟胺、异烟肼、卡那霉素、孟德立胺、呋喃妥因、苯唑西林、多粘菌素 B、利福平、链霉素、磺胺二甲氧嘧啶和万古霉素。按有效性递增顺序,引起最显著抑制作用的药物是氯霉素、异烟肼、乙硫异烟胺和呋喃妥因。这项在 15 天内完成的放射性测量研究能够直接研究药物对鼠麻风杆菌代谢的影响,并且比以往更快速地筛选抗麻风病药物。目前,这些观察结果正在扩展到抗麻风病药物的构效关系以及体外麻风分枝杆菌的代谢和药物敏感性研究。