Gonzalez N S, Cazzulo J J
Instituto de Investigaciones Bioquimicas, Fundacion Campomar, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Argentina.
Biochem Pharmacol. 1989 Sep 1;38(17):2873-7. doi: 10.1016/0006-2952(89)90444-9.
Nifurtimox (NF) and benznidazole (BZ), drugs used in the treatment of Chagas' disease, did not inhibit protein biosynthesis in in vitro homologous cell-free systems isolated from Trypanosoma cruzi and Crithidia fasciculata; nevertheless, their addition to growing cultures caused polyribosomal depolymerization. On the other hand, Berenil, Antrycide and suramin, used against African trypanosomiasis, inhibited protein biosynthesis in vitro but did not affect ribosomal distribution, probably due to low permeability to the drugs. The results suggest that the inhibition by NF and BZ of protein synthesis, measured as [14C]leucine incorporation by other authors, is indirect, probably through inhibition of nucleic acid synthesis and energy metabolism.
用于治疗恰加斯病的硝呋替莫(NF)和苯硝唑(BZ),在从克氏锥虫和fasiculata锥虫分离出的体外同源无细胞系统中,并不抑制蛋白质生物合成;然而,将它们添加到生长的培养物中会导致多核糖体解聚。另一方面,用于治疗非洲锥虫病的贝尼尔、安锥赛和苏拉明在体外抑制蛋白质生物合成,但不影响核糖体分布,这可能是由于药物的低渗透性。结果表明,其他作者以[14C]亮氨酸掺入量衡量的NF和BZ对蛋白质合成的抑制是间接的,可能是通过抑制核酸合成和能量代谢实现的。