Iten M, Matovu E, Brun R, Kaminsky R
Swiss Tropical Institute, Basel, Switzerland.
Trop Med Parasitol. 1995 Sep;46(3):190-4.
Trypanosoma brucei rhodesiense isolates from South East Uganda were characterized for susceptibility to the drugs suramin, nifurtimox, melarsoprol and DL-alpha-difluoromethylornithine (DFMO). Two different assays were used to determine the drug susceptibility of the field isolates: the [3H]hypoxanthine incorporation assay (24 hours) and the long term viability assay (10 days). All trypanosome stocks were susceptible to suramin and nifurtimox. Differences in the susceptibility to melarsoprol were observed in the [3H]hypoxanthine incorporation assay, but could not be confirmed in the long term viability assay. All T. b. rhodesiense stocks were found in vitro to have innate tolerance to DFMO, under conditions where T. b. gambiense stocks from West Africa were susceptible to the drug. Ugandan T. b. rhodesiense stocks did respond to 25-100 micrograms/ml after 10 days of drug exposure, but the DFMO level reached in cerebrospinal fluid during treatment is only 16.3 +/- 7.8 micrograms/ml. Therefore, DFMO is not an appropriate alternative or backup drug for treatment of Rhodesian sleeping sickness in Uganda.
对从乌干达东南部分离出的布氏罗得西亚锥虫菌株进行了对苏拉明、硝呋替莫、美拉胂醇和DL-α-二氟甲基鸟氨酸(DFMO)的药敏特性研究。采用两种不同的检测方法来测定现场分离株的药敏性:[3H]次黄嘌呤掺入检测法(24小时)和长期生存力检测法(10天)。所有锥虫株对苏拉明和硝呋替莫敏感。在[3H]次黄嘌呤掺入检测法中观察到对美拉胂醇的药敏性存在差异,但在长期生存力检测法中未能得到证实。在体外发现,所有布氏罗得西亚锥虫株对DFMO具有固有耐受性,而来自西非的布氏冈比亚锥虫株对该药物敏感。乌干达的布氏罗得西亚锥虫株在药物暴露10天后对25 - 100微克/毫升的DFMO有反应,但治疗期间脑脊液中达到的DFMO水平仅为16.3±7.8微克/毫升。因此,DFMO不是治疗乌干达罗德西亚昏睡病的合适替代药物或备用药物。