Balaña-Fouce R, Ordóñez D, Alunda J M
Departamento de Farmacología y Toxicología, Facultad de Veterinaria, Universidad Complutense de Madrid, Spain.
Mol Biochem Parasitol. 1989 Jun 1;35(1):43-50. doi: 10.1016/0166-6851(89)90140-0.
A transport system for putrescine in Leishmania infantum (= L. donovani infantum) promastigotes has been identified and characterized by measuring the uptake of radioactively labelled putrescine. Putrescine uptake was time- and temperature-dependent without any accumulation taking place at 0 degrees C. Uptake of putrescine was maximal at pH values near neutrality. Putrescine uptake showed an apparent Km = 1.08 +/- 0.12 microM and a Vmax = 1.74 + 0.62 pmol min-1 (10(6) cells)-1. The effect of metabolic poisons and uncoupling agents suggests that the putrescine uptake was energy-dependent. The transport system seemed to be highly specific for putrescine as neither aminoacids nor related compounds tested showed any competition with putrescine uptake. The trypanocide Berenil inhibited almost completely the putrescine uptake with non-competitive kinetics and a value of Ki = 43 microM.
通过测量放射性标记腐胺的摄取,已鉴定并表征了婴儿利什曼原虫(=杜氏利什曼原虫婴儿亚种)前鞭毛体中腐胺的转运系统。腐胺摄取具有时间和温度依赖性,在0℃时没有任何积累。腐胺摄取在接近中性的pH值下最大。腐胺摄取的表观Km = 1.08 +/- 0.12微摩尔,Vmax = 1.74 + 0.62皮摩尔·分钟-1(10^6个细胞)-1。代谢毒物和解偶联剂的作用表明腐胺摄取是能量依赖性的。该转运系统似乎对腐胺具有高度特异性,因为所测试的氨基酸和相关化合物均未显示与腐胺摄取有任何竞争。杀锥虫剂贝尼尔以非竞争性动力学几乎完全抑制腐胺摄取,Ki值为43微摩尔。