Basselin M, Lawrence F, Robert-Gero M
Institut de Chimie des Substances Naturelles, C.N.R.S., Gif-sur-Yvette, France.
Biochem J. 1996 Apr 15;315 ( Pt 2)(Pt 2):631-4. doi: 10.1042/bj3150631.
A transport system for pentamidine in Leishmania donovani and Leishmania amazonensis promastigotes and axenic amastigotes has been identified and characterized. Pentamidine is not metabolized by these parasites. Its uptake process is saturable, carrier-mediated and energy-dependent. This drug does not inhibit purine or pyrimidine uptake, whereas it inhibits uptake of several amino acids non-competitively and that of putrescine and spermidine competitively. The results suggest that pentamidine shares polyamine-carrier systems in these parasites.
已在杜氏利什曼原虫和亚马逊利什曼原虫的前鞭毛体及无菌无鞭毛体中鉴定并表征了喷他脒的转运系统。这些寄生虫不会代谢喷他脒。其摄取过程是可饱和的、载体介导的且依赖能量。该药物不抑制嘌呤或嘧啶的摄取,而它非竞争性抑制几种氨基酸的摄取,并竞争性抑制腐胺和亚精胺的摄取。结果表明喷他脒在这些寄生虫中共享多胺载体系统。