Kayser O, Kiderlen A F
Freie Universität Berlin, Institute of Pharmacy II, Germany.
Tokai J Exp Clin Med. 1998 Dec;23(6):423-6.
This is the first report on aurones as a new class of natural products with leishmanicidal activity. A series of aurones with drug-potential for Leishmania infections was identified in vitro using both a direct cytotoxicity test against extracellular promastigotes of Leishmania donovani, L. infantum, L. enriettii, and L. major, and a test against intracellular amastigote L. donovani residing within murine macrophages. The compounds proved to be active at concentrations in the microgram range between 0.4 and 5.0 microg/ml. When tested against murine bone marrow-derived macrophages as a mammalian host cell control, all compounds showed only moderate cytotoxicity (EC50 2.32-25.0 microg/ml).
这是关于奥洛酮作为一类具有抗利什曼原虫活性的新型天然产物的首次报道。通过对杜氏利什曼原虫、婴儿利什曼原虫、恩氏利什曼原虫和硕大利什曼原虫的细胞外前鞭毛体进行直接细胞毒性试验,以及对存在于小鼠巨噬细胞内的杜氏利什曼原虫细胞内无鞭毛体进行试验,在体外鉴定出了一系列对利什曼原虫感染具有药物潜力的奥洛酮。这些化合物在0.4至5.0微克/毫升的微克范围内具有活性。当作为哺乳动物宿主细胞对照对小鼠骨髓来源的巨噬细胞进行测试时,所有化合物仅表现出中等细胞毒性(半数有效浓度为2.32 - 25.0微克/毫升)。