嘌呤类似物对杜氏利什曼原虫的体内活性。
Activity of purine analogs against Leishmania donovani in vivo.
作者信息
Berman J D, Hanson W L, Lovelace J K, Waits V B, Jackson J E, Chapman W L, Klein R S
出版信息
Antimicrob Agents Chemother. 1987 Jan;31(1):111-3. doi: 10.1128/AAC.31.1.111.
Abstract
The dose of orally administered 9-deazainosine calculated to suppress 50% of Leishmania donovani amastigotes in hamster livers was 19 mg/kg (body weight) per day; 96 to 99% of Leishmania organisms were eliminated from the liver and spleen of squirrel monkeys by 50 mg/kg per day. Because these activities were greater than that of the experimental clinical agent allopurinol and comparable to that of the classical agent parenteral pentavalent antimony, 9-deazainosine should be considered for clinical development for visceral leishmaniasis.
摘要
经计算，口服9-去氮肌苷以抑制仓鼠肝脏中50%的杜氏利什曼原虫无鞭毛体的剂量为每天19毫克/千克（体重）；每天50毫克/千克可使松鼠猴肝脏和脾脏中的利什曼原虫减少96%至99%。由于这些活性高于实验性临床药物别嘌呤醇，且与经典药物肠胃外五价锑相当，因此9-去氮肌苷应考虑用于内脏利什曼病的临床开发。
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