Zinsstag J, Brun R, Craciunescu D G, Parrondo Iglesias E
Swiss Tropical Institute, Basel.
Trop Med Parasitol. 1991 Mar;42(1):41-4.
A series of organometallic drugs were tested in a photometric in vitro assay for trypanocidal activity against the three subspecies of the Trypanosoma brucei group. Trypanosoma b. rhodesiense, T. b. gambiense and T. b. brucei displayed a similar sensitivity pattern. The following IC50 values (drug concentration inhibiting decrease of extinction by 50%) could be determined: IrCl6 (IV)-Pentamidine (1.5 ng/ml), IrCl6(IV)-Ro15-0216 (10 micrograms/ml), PtBr6-Metamidium (30 micrograms/ml), PtBr6(IV)-Benznidazole (20 micrograms/ml), PtBr6(IV)-Ro15-0216 (50 micrograms/ml), cis-Pt(II)-Pentamidine (0.1 micrograms/ml), Rh(I)-COD-Pentamidine (5-10 ng/ml), Rh(I)-COD-Benznidazole (10 micrograms/ml), Rh(III)-Ethylxanthate (30 micrograms/ml) and Pt(II)-Pentamidine-cis-Pt(II)(Pentamidine)(Cl)2 (2 ng/ml). The four Pentamidine complexes were the most active compounds and showed activities comparable to that of Pentamidine (IC50: 0.5 to 1 ng/ml). Since the toxicity of the Ir- and Pt-Pentamidine complexes is ten to twenty fold lower (400 to 1000 mg/kg) than that of Pentamidine (50 mg/kg), the complexes might be candidates for investigation as safer trypanocidal drugs.
一系列有机金属药物在体外光度分析中进行了测试，以检测其对布氏锥虫组三个亚种的杀锥虫活性。罗德西亚布氏锥虫、冈比亚布氏锥虫和布氏布氏锥虫表现出相似的敏感性模式。可以确定以下IC50值（抑制吸光度下降50%的药物浓度）：六氯铱（IV）-喷他脒（1.5纳克/毫升）、六氯铱（IV）-Ro15-0216（10微克/毫升）、六溴铂-美他密啶（30微克/毫升）、六溴铂（IV）-苄硝唑（20微克/毫升）、六溴铂（IV）-Ro15-0216（50微克/毫升）、顺铂（II）-喷他脒（0.1微克/毫升）、铑（I）-环辛二烯-喷他脒（5-10纳克/毫升）、铑（I）-环辛二烯-苄硝唑（10微克/毫升）、铑（III）-乙基黄原酸盐（30微克/毫升）和顺铂（II）-喷他脒-顺铂（II）（喷他脒）（氯）2（2纳克/毫升）。四种喷他脒络合物是活性最高的化合物，其活性与喷他脒相当（IC50：0.5至1纳克/毫升）。由于铱和铂-喷他脒络合物的毒性比喷他脒（50毫克/千克）低10至20倍（400至1000毫克/千克），这些络合物可能是作为更安全的杀锥虫药物进行研究的候选物。
