Stoffel Sabine A, Rodenko Boris, Schweingruber Anne-Marie, Mäser Pascal, de Koning Harry P, Schweingruber M Ernst
Institute of Cell Biology, University of Bern, Baltzerstrasse 4, 3012 Bern, Switzerland.
Int J Parasitol. 2006 Feb;36(2):229-36. doi: 10.1016/j.ijpara.2005.10.003. Epub 2005 Nov 21.
Bloodstream forms of Trypanosoma brucei brucei were cultivated in the presence and absence of thiamine (vitamin B1) and pyridoxine (vitamin B6). The vitamins do not change growth behaviour, indicating that Trypanosoma brucei is prototrophic for the two vitamins even though in silico no bona-fide thiamine-biosynthetic genes could be identified in the T. brucei genome. Intracellularly, thiamine is mainly present in its diphosphate form. We were unable to detect significant uptake of [3H]thiamine and structural thiamine analogues such as pyrithiamine, oxithiamine and amprolium were not toxic for the bloodstream forms of T. brucei, indicating that the organism does not have an efficient uptake system for thiamine and its analogues. We have previously shown that, in the fission yeast Saccharomyces pombe, the toxicity of melarsen oxide, the pharmacologically active derivative of the frontline sleeping sickness drug melarsoprol, is abolished by thiamine and the drug is taken up by a thiamine-regulated membrane protein which is responsible for the utilization of thiamine. We show here that thiamine also has weak effects on melarsen oxide-induced growth inhibition and lysis in T. brucei. These effects were consistent with a low affinity of thiamine for the P2 adenosine transporter that is responsible for uptake of melaminophenyl arsenicals in African trypanosomes.
在有和没有硫胺素(维生素B1)及吡哆醇(维生素B6)的情况下培养布氏布氏锥虫的血流形式。这些维生素不会改变生长行为,这表明布氏锥虫对这两种维生素是原养型的,尽管在布氏锥虫基因组中通过计算机分析未鉴定出真正的硫胺素生物合成基因。在细胞内,硫胺素主要以其二磷酸形式存在。我们无法检测到[3H]硫胺素的显著摄取,并且结构硫胺素类似物如嘧硫胺、氧硫胺和氨丙啉对布氏锥虫的血流形式无毒,这表明该生物体没有有效的硫胺素及其类似物摄取系统。我们之前已经表明,在裂殖酵母粟酒裂殖酵母中,一线昏睡病药物美拉胂醇的药理活性衍生物氧化美拉胂的毒性可被硫胺素消除,并且该药物可被一种硫胺素调节的膜蛋白摄取,该膜蛋白负责硫胺素的利用。我们在此表明,硫胺素对布氏锥虫中氧化美拉胂诱导的生长抑制和裂解也有微弱影响。这些影响与硫胺素对负责非洲锥虫中美拉明苯基砷化合物摄取的P2腺苷转运蛋白的低亲和力一致。