杀稻瘟菌素及其类似物对三种利什曼原虫增殖的差异效应。
Differential effect of sinefungin and its analogs on the multiplication of three Leishmania species.
作者信息
Paolantonacci P, Lawrence F, Robert-Géro M
出版信息
Antimicrob Agents Chemother. 1985 Oct;28(4):528-31. doi: 10.1128/AAC.28.4.528.
Abstract
Sinefungin and seven analogs were evaluated in vitro for activity against promastigote multiplication of Leishmania donovani, L. tropica, and L. enrietti. Of these compounds, sinefungin, the cyclic derivative, and A9145C were leishmanicidal at concentrations ranging from 0.13 to 2.6 microM. Sinefungin was the most active of these three compounds against L. donovani, and A9145C was most active against L. enrietti. None of the remaining derivatives exhibited significant activity against any one of the three species at the highest dose tested. All agents were assayed for activity against protein methylases I and III. The results of these tests showed that there is no relationship between the inhibition of growth and inhibition of protein methylases I and III.
摘要
对西奈芬净及其七种类似物进行了体外评估，以检测它们对杜氏利什曼原虫、热带利什曼原虫和恩氏利什曼原虫前鞭毛体增殖的活性。在这些化合物中，西奈芬净、环状衍生物和A9145C在浓度范围为0.13至2.6微摩尔时具有杀利什曼原虫活性。西奈芬净是这三种化合物中对杜氏利什曼原虫活性最高的，而A9145C对恩氏利什曼原虫活性最高。在测试的最高剂量下，其余衍生物均未对这三种利什曼原虫中的任何一种表现出显著活性。所有试剂均检测了对蛋白质甲基化酶I和III的活性。这些测试结果表明，生长抑制与蛋白质甲基化酶I和III的抑制之间没有关系。
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