基于核苷结构的抗利什曼原虫药物的发明。
Invention of anti-Leishmania drugs on the basis of the nucleoside structures.
作者信息
Wataya Y, Tanifuji H, Kubochi F, Yoshioka-Hiramoto A, Morishige K, Ishii A, Morizawa Y, Nakayama T, Yasuda A, Matsuda A
机构信息
Faculty of Pharmaceutical Sciences, Okayama University, Japan.
出版信息
Nucleic Acids Symp Ser. 1990(22):23-4.
3'-Deoxy-3'-fluoroinosine is a potent inhibitor for the growth of the promastigote form of Leishmania tropica and Leishmania donovani. In culture, the EC50 values of 3'-deoxy-3'-fluoroinosine are 2.3 x 10(-7) and 1.0 x 10(-6) M for the promastigotes of L. tropica and L. donovani, respectively. It is less toxic towards mouse mammary tumor FM3A cells: the EC50 value is 2.0 x 10(-4) M. 3'-Deoxy-3'-fluoroinosine is metabolized by Leishmania promastigotes to give 3'-deoxy-3'-fluoroadenosine-5'-triphosphate. This metabolic conversion provides a mechanism for the parasite-selective toxicity of 3'-deoxy-3'-fluoroinosine.
3'-脱氧-3'-氟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，3'-脱氧-3'-氟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2.3×10⁻⁷和1.0×10⁻⁶M。它对小鼠乳腺肿瘤FM3A细胞的毒性较小：EC50值为2.0×10⁻⁴M。3'-脱氧-3'-氟肌苷被利什曼原虫前鞭毛体代谢生成3'-脱氧-3'-氟腺苷-5'-三磷酸。这种代谢转化为3'-脱氧-3'-氟肌苷的寄生虫选择性毒性提供了一种机制。
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