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非洲锥虫中嘌呤碱基和核苷的摄取

Uptake of purine bases and nucleosides in African trypanosomes.

作者信息

James D M, Born G V

出版信息

Parasitology. 1980 Oct;81(2):383-93. doi: 10.1017/s0031182000056110.

Abstract

Uptake of radioactivity labelled purine bases and nucleosides by suspensions of Trypanosoma brucei and Trypanosoma congolense in bicine buffer was determined at 37 degrees C. With T. brucei, the rate of uptake of adenosine was much greater than that of the other compounds tested, the uptake of which decreased in the order adenine, inosine, guanosine and hypoxanthine. With T. brucei, adenosine uptake increased with concentration in a manner suggesting two mechanisms, one with high and the other with low affinity for adenosine. The uptake of adenine increased with concentration only up to about 1.5 microM while the uptake of guanosine increased little with concentration and that of inosine and hypoxanthine not at all. In both species adenosine strongly inhibited the uptake of both of the other nucleosides and of both purine bases. In T. brucei, guanosine and inosine caused small increases in adenosine uptake which was, however, inhibited by them in T. congolense. In T. brucei, each of the purine bases adenine and hypoxanthine inhibited its own uptake maximally but that of each other less effectively. Hypoxanthine was more effective than adenine in inhibiting the uptake of the nucleosides guanosine and inosine, but neither base effected marked inhibition of adenosine uptake. The uptake of adenosine by T. brucei was inhibited by dipyridamole and its analogue, compound RA--233, strongly at 100 microM and slightly at 10 microM. The other dipyridamole analogues, VK--744 and VK--774, were ineffective.

摘要

在37摄氏度下,测定了布氏锥虫和刚果锥虫悬浮液对放射性标记嘌呤碱基和核苷的摄取情况。对于布氏锥虫,腺苷的摄取速率远高于其他受试化合物,其他化合物的摄取速率按腺嘌呤、肌苷、鸟苷和次黄嘌呤的顺序递减。对于布布布氏锥虫,腺苷摄取量随浓度增加,表明存在两种机制,一种对腺苷具有高亲和力,另一种具有低亲和力。腺嘌呤的摄取量仅在浓度约为1.5微摩尔时随浓度增加,而鸟苷的摄取量随浓度增加很少,肌苷和次黄嘌呤的摄取量则完全不随浓度增加。在这两种锥虫中,腺苷强烈抑制其他两种核苷和两种嘌呤碱基的摄取。在布氏锥虫中,鸟苷和肌苷使腺苷摄取量略有增加,但在刚果锥虫中却抑制了腺苷摄取。在布氏锥虫中,嘌呤碱基腺嘌呤和次黄嘌呤各自最大程度地抑制自身摄取,但对彼此的摄取抑制作用较小。次黄嘌呤在抑制鸟苷和肌苷的摄取方面比腺嘌呤更有效,但两种碱基对腺苷摄取均无明显抑制作用。布氏锥虫对腺苷的摄取在100微摩尔时被双嘧达莫及其类似物化合物RA - 233强烈抑制,在10微摩尔时略有抑制。其他双嘧达莫类似物VK - 744和VK - 774无效。

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