Antitrypanosomal action of cis-diamminedichloroplatinum (II) analogs.
Antitrypanosomal action of cis-diamminedichloroplatinum (II) analogs.
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顺式二氨二氯铂 (II) 类似物的抗锥虫作用。
作者：
A. Osuna;L. Ruiz‐Pérez;M. C. López;S. Castanys;F. Gamarro;D. Craciunescu;C. Alonso
本报告讨论了顺式二氨二氯铂（II）（DDP），和它的类似物：顺式铂（II）（反苯环丙胺）2Cl 2和顺式铂（II）（苯并噻唑）2Cl 2在培养的克氏锥虫的外鞭毛体形式产生的变化。在超微结构水平上进行了研究，并研究了这些复合物对大分子合成的抑制作用，通过3 H-胸苷，3 H-尿苷和3 H-亮氨酸掺入进行了评价。浓度为50和100 μ g/ml的DDP不显著抑制放射性前体的掺入，但观察到2种类似物明显降低。以10微克/毫升的浓度处理8小时，在所有3例病例中均出现自噬空泡和脂质增加以及核染色质异常凝聚。
The present report deals with the alterations produced by cis-diamminedichloroplatinum (II) (DDP), and 2 of its analogs: cis-Pt(II)(tranylcypromine)2Cl2 and cis-Pt(II)(benzothiazole)2Cl2 in cultured epimastigote forms of Trypanosoma cruzi. Studies have been performed at the ultrastructural level and the inhibitory effect of these complexes on macromolecule synthesis, evaluated by 3H-thymidine, 3H-uridine, and 3H-leucine incorporation, has been investigated. DDP at concentrations of 50 and 100 micrograms/ml does not inhibit significantly the incorporation of radioactive precursors, but a clear decrease was observed with the 2 analogs. Eight hours of treatment at a concentration of 10 micrograms/ml rendered in all 3 cases an increase in autophagic vacuoles and lipids as well as an abnormal condensation of the nucleus chromatin.