核苷类似物的抗寄生虫活性：环碳肌苷在热带利什曼原虫和杜氏利什曼原虫前鞭毛体中的代谢及其对杜氏利什曼原虫无鞭毛体的体外活性。
Anti-parasite activity of nucleoside analogues: the metabolism of carbocyclic inosine in promastigotes of Leishmania tropica and Leishmania donovani and its activity against amastigotes of Leishmania donovani in vitro.
作者信息
Wataya Y, Satake H, Hiraoka O, Aji T, Morishige K, Kimura J Y, Ishii A, Matsuda A, Ueda T, Fukukawa K
出版信息
Nucleic Acids Symp Ser. 1986(17):149-51.
Carbocyclic inosine is a potent inhibitor for the growth of the promastigote form of Leishmania tropica and Leishmania donovani. In culture, the EC50 values of carbocyclic inosine are 8.3 X 10(-8) and 1.3 X 10(-7) M for the promastigotes of L. tropica and L. donovani, respectively. On the other hand, it is less toxic towards mouse mammary tumor FM3A cells: the EC50 value is 2.7 X 10(-4)M. Carbocyclic inosine is metabolized by Leishmania promastigotes to give carbocyclic adenosine-5'-triphosphate(aristeromycin-5'-triphosphate) and carbocyclic guanosine-5'-triphosphate. This metabolic conversion provides a mechanism for the parasite-selective toxicity of carbocyclic inosine. Carbocyclic inosine was found to be active against L. donovani amastigotes in an in vivo-like cultivation in vitro.
碳环肌苷是热带利什曼原虫和杜氏利什曼原虫前鞭毛体生长的有效抑制剂。在培养中，碳环肌苷对热带利什曼原虫和杜氏利什曼原虫前鞭毛体的EC50值分别为8.3×10⁻⁸和1.3×10⁻⁷M。另一方面，它对小鼠乳腺肿瘤FM3A细胞的毒性较小：EC50值为2.7×10⁻⁴M。碳环肌苷被利什曼原虫前鞭毛体代谢产生碳环腺苷-5'-三磷酸（阿瑞斯托霉素-5'-三磷酸）和碳环鸟苷-5'-三磷酸。这种代谢转化为碳环肌苷的寄生虫选择性毒性提供了一种机制。在体外类似体内培养的条件下，发现碳环肌苷对杜氏利什曼原虫无鞭毛体具有活性。
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