Cytotoxicity of acridine compounds for Leishmania promastigotes in vitro.
Cytotoxicity of acridine compounds for Leishmania promastigotes in vitro.
复制标题
吖啶化合物对利什曼原虫前鞭毛体的体外细胞毒性。
DOI：
10.1128/aac.36.2.495
复制
发表时间：
1992
影响因子：
4.9
通讯作者：
Pearson,RD
中科院分区：
文献类型：
--
作者：
Werbovetz,KA;Lehnert,EK;Macdonald,TL;Pearson,RD
体外研究了哺乳动物和细菌拓扑异构酶 II 抑制剂对利什曼原虫前鞭毛体的影响。将寄生虫与药物一起孵育，并根据 48 小时后鞭毛运动的丧失和细胞裂解来评估细胞毒性。 9-氨基吖啶在结构上与已知的抗利什曼原虫化合物奎纳克林和氯丙嗪相关，在10至20微摩尔浓度范围内显示出对抗寄生虫的活性。阿霉素的活性要低得多，而依托泊苷和几种喹诺酮类药物在 100 µM 浓度下则无活性。这些结果表明，特定结构类别的化合物对利什曼原虫物种具有细胞毒性。发现的独特结构-活性关系表明利什曼原虫拓扑异构酶 II 可能是化疗的有用靶标。
The effect of mammalian and bacterial topoisomerase II inhibitors on Leishmania promastigotes was studied in vitro. Parasites were incubated with drugs, and cytotoxicity was assessed on the basis of the loss of flagellar motility and cell lysis after 48 h. 9-Aminoacridines, which are structurally related to the known antileishmanial compounds quinacrine and chlorpromazine, showed activity against the parasite at concentrations in the range of 10 to 20 microM. Adriamycin showed far less activity, while etoposide and several quinolones were inactive at 100-microM concentrations. These results demonstrate that a particular structural class of compounds is cytotoxic to Leishmania species. The unique structure-activity relationship discovered suggests that leishmanial topoisomerase II could be a useful target for chemotherapy.