Navas I M, García-Fernández A J, Johnson R A, Reguera R M, Balaña-Fouce R, Ordóñez D
Dept. Ciencias Sociosanitarias, Facultad de Veterinaria, Universidad de Murcia, Spain.
Biol Chem. 1996 Dec;377(12):833-6. doi: 10.1515/bchm3.1996.377.12.833.
The effect of a heterologous series of cationic diamidines has been tested on cell growth and polyamine uptake on the model of insect Trypanosomatid Crithidia fasciculata. The maximum inhibitory effect on both parameters was found for pentamidine and dibromopropamidine, which exhibit a longer distance between amino and imino substituents. A minimum inhibitory effect was found with amicarbalide. A good relationship was obtained when the distance between amino moieties was plotted versus the inhibitory effect on putrescine uptake, suggesting a role of this structural property on polyamine transport in Crithidia fasciculata. In addition, a similar correlation was obtained for another Trypanosomatid parasite, Leishmania infantum.
已在昆虫锥虫克氏锥虫模型上测试了一系列异源阳离子双脒对细胞生长和多胺摄取的影响。对于喷他脒和二溴丙脒,在这两个参数上发现了最大抑制作用,它们的氨基和亚氨基取代基之间的距离更长。氨甲酰甲胆碱的抑制作用最小。当绘制氨基部分之间的距离与对腐胺摄取的抑制作用时,得到了良好的关系,表明这种结构特性在克氏锥虫的多胺转运中起作用。此外,对于另一种锥虫寄生虫婴儿利什曼原虫也获得了类似的相关性。