Ruiz-Pérez L M, Osuna A, Castanys S, Gamarro F, Craciunescu D, Doadrio A
Arzneimittelforschung. 1986;36(1):13-6.
In the present study the activity of 15 complexes of Rh(III) and 19 of Pt(II) against Trypanosoma cruzi epimastigote forms was investigated. The results obtained show that complexes of Rh(III) with the highest antitumoural activity also appear to be more effective against cultured epimastigotes. Thus, complexes [Rh(L)4X2]+X- where L is a derivative of thiazole present high activity against the parasite, and were even more active when Cl- (X) was present in their structure. Complexes cis-Pt(L)m(X)n that present 1,2-diamminecyclohexane (DDH) in their molecule, e.g. cis-Pt(DDH)Cl2 and cis-Pt(DDH)(metafluorobenzoic)2 of high and moderate antitumoural activity, respectively, have shown greater effectiveness than cis-Pt(NH3)2Cl2 (DDP). The effect produced by cis-Pt(pentamidine)Cl2 complex, obtained in order to enforce the action of pentamidine, was considerably high. On the other hand, no positive correlation can be established between the antitumour effects of the Pt(II) complexes and its antitrypanosomic activity.
在本研究中，对15种铑（III）配合物和19种铂（II）配合物针对克氏锥虫前鞭毛体形式的活性进行了研究。所得结果表明，具有最高抗肿瘤活性的铑（III）配合物似乎对培养的前鞭毛体也更有效。因此，[Rh(L)4X2]+X-型配合物（其中L为噻唑衍生物）对该寄生虫具有高活性，当其结构中存在Cl-（X）时活性甚至更高。分子中含有1,2 - 二氨基环己烷（DDH）的顺式 - Pt(L)m(X)n配合物，例如分别具有高和中等抗肿瘤活性的顺式 - Pt(DDH)Cl2和顺式 - Pt(DDH)(间氟苯甲酸)2，已显示出比顺式 - Pt(NH3)2Cl2（顺铂，DDP）更高的有效性。为增强喷他脒的作用而获得的顺式 - Pt(喷他脒)Cl2配合物产生的效果相当高。另一方面，铂（II）配合物的抗肿瘤作用与其抗锥虫活性之间无法建立正相关。
