González-Coloma Azucena, Guadaño Ana, de Inés Concepción, Martínez-Díaz Rafael, Cortes Diego
Centro de Ciencias Medioambientales, CSIC, Serrano 115-dpdo., 28006 Madrid, Spain.
Z Naturforsch C J Biosci. 2002 Nov-Dec;57(11-12):1028-34. doi: 10.1515/znc-2002-11-1213.
Five annonaceous acetogenins, rolliniastatin-1 [structure: see text], rolliniastatin-2 [structure: see text], laherradurin [structure: see text], squamocin [structure: see text], annonacin [structure: see text], and rotenone as a reference, differing in their NADH oxidase inhibition activity, have been evaluated for antifeedant, insecticidal, trypanocidal and cytotoxic effects on insect, mammalian and tumor cells. All the test compounds were toxic to Leptinotarsa decemlineata, demonstrated selective cytotoxicity to insect Sf9 cells and a panel of tumor cell lines with the multidrug-resistant SW480 (P-glycoprotein+, Pgp+) being the most sensitive one. Compounds [structure: see text] and rotenone had post-ingestive effects against Spodoptera littoralis larvae while [structure: see text] and rotenone were active against Trypanosoma cruzi. Based on their biochemical properties (inhibition of the mitochondrial NADH oxidase activity), the in vivo effects of these compounds on S. littoralis and their cytotoxic effects on Sf9 and tumor cells were more predictable than their effect on T. cruzi and mammalian cells.
已对五种番荔枝内酯类化合物（罗利那司他汀 -1 [结构：见原文]、罗利那司他汀 -2 [结构：见原文]、拉赫拉杜林 [结构：见原文]、鳞尾木素 [结构：见原文]、番荔枝宁 [结构：见原文]）以及作为参照的鱼藤酮进行了评估，这些化合物在烟酰胺腺嘌呤二核苷酸（NADH）氧化酶抑制活性方面存在差异，评估内容包括它们对昆虫、哺乳动物和肿瘤细胞的拒食、杀虫、杀锥虫及细胞毒性作用。所有受试化合物对马铃薯甲虫均有毒性，对昆虫Sf9细胞以及一组肿瘤细胞系表现出选择性细胞毒性，其中具有多药耐药性的SW480（P - 糖蛋白阳性，Pgp +）细胞系最为敏感。化合物[结构：见原文]和鱼藤酮对海滨夜蛾幼虫有取食后效应，而[结构：见原文]和鱼藤酮对克氏锥虫有活性。基于它们的生化特性（抑制线粒体NADH氧化酶活性），这些化合物对海滨夜蛾的体内效应以及对Sf9和肿瘤细胞的细胞毒性效应比它们对克氏锥虫和哺乳动物细胞的效应更具可预测性。
