Wataya Y, Hiraoka O, Sonobe Y, Yoshioka A, Matsuda A, Miyasaka T, Saneyoshi M, Ueda T
Nucleic Acids Symp Ser. 1984(15):69-71.
Many nucleoside analogs were screened for anti-protozoa activity on Leishmania tropica in an in vitro culture system. 3'-Deoxyinosine and several tubercidin derivatives were found to be potent inhibitors for growth of the promastigote form of L. tropica. EC50 value of 3'-deoxyinosine was 4.43 X 10(-7)M. This compound was remarkably less toxic towards mouse mammary tumor FM3A cells (EC50, 1.25 X 10(-4) M). 3'-Deoxyinosine is metabolized by Leishmania promastigote to give 3'-deoxyinosine-5'-monophosphate, 3'-deoxy-adenosine(cordycepin)-5'-mono, di-, and triphosphates. This means that Leishmania can aminate the 6-position of 3'-deoxyinosine-5'-monophosphate, thereby converting it into a highly toxic compound.
在体外培养系统中筛选了许多核苷类似物对热带利什曼原虫的抗寄生虫活性。发现3'-脱氧肌苷和几种杀结核菌素衍生物是热带利什曼原虫前鞭毛体生长的有效抑制剂。3'-脱氧肌苷的EC50值为4.43×10(-7)M。该化合物对小鼠乳腺肿瘤FM3A细胞的毒性明显较低（EC50，1.25×10(-4)M）。3'-脱氧肌苷被利什曼原虫前鞭毛体代谢生成3'-脱氧肌苷-5'-单磷酸、3'-脱氧腺苷（虫草素）-5'-单磷酸、二磷酸和三磷酸。这意味着利什曼原虫可以将3'-脱氧肌苷-5'-单磷酸的6位胺化，从而将其转化为一种剧毒化合物。
