Borowy N K, Nelson R T, Hirumi H, Brun R, Waithaka H K, Schwartz D, Polak A
International Laboratory for Research on Animal Diseases, Nairobi, Kenya.
Ann Trop Med Parasitol. 1988 Feb;82(1):13-9. doi: 10.1080/00034983.1988.11812203.
In vitro systems for the continuous cultivation of Trypanosoma brucei brucei, T. b. gambiense, T. b. rhodesiense, T. congolense and T. vivax were used to determine the antitrypanosomal activity of the 2-substituted nitroimidazole Ro 15-0216. For all trypanosome species, the concentration which inhibited parasite growth by 50% (IC50 value) was established: 0.0957 microgram ml-1 (T. b. brucei TC221), 0.1327 microgram ml-1 (T. b. gambiense STIB 754-A), 0.0450 microgram ml-1 (T. b. rhodesiense STIB 704-BABA), 0.0896 microgram ml-1 (T. congolense ILNat 3.1) and 0.0109 microgram ml-1 (T. vivax ILRAD 1392). The IC50 value of its major metabolite Ro 19-9638 was 0.0341 microgram ml-1 (T. b. rhodesiense STIB 704-BABA). Furthermore, minimum exposure times required to render T. b. brucei non-infective for mice as well as preventing their growth in vitro have been established to be three, four, six and ten hours at drug concentrations of 30, 10, 3 and 1 microgram ml-1, respectively.
利用用于布氏布氏锥虫、冈比亚锥虫、罗德西亚锥虫、刚果锥虫和活跃锥虫连续培养的体外系统，来测定2-取代硝基咪唑Ro 15-0216的抗锥虫活性。对于所有锥虫物种，确定了抑制寄生虫生长50%的浓度（IC50值）：0.0957微克/毫升（布氏布氏锥虫TC221）、0.1327微克/毫升（冈比亚锥虫STIB 754-A）、0.0450微克/毫升（罗德西亚锥虫STIB 704-BABA）、0.0896微克/毫升（刚果锥虫ILNat 3.1）和0.0109微克/毫升（活跃锥虫ILRAD 1392）。其主要代谢产物Ro 19-9638的IC50值为0.0341微克/毫升（罗德西亚锥虫STIB 704-BABA）。此外，已确定使布氏布氏锥虫对小鼠无感染性以及阻止其在体外生长所需的最短暴露时间，在药物浓度分别为30、10、3和1微克/毫升时，分别为3、4、6和10小时。
