Barbaras Damien, Kaiser Marcel, Brun Reto, Gademann Karl
Laboratorium für Organische Chemie, Swiss Federal Institute of Technology (ETH), 8093 Zürich, Switzerland.
Bioorg Med Chem Lett. 2008 Aug 1;18(15):4413-5. doi: 10.1016/j.bmcl.2008.06.049. Epub 2008 Jun 19.
The quaternary beta-carbolinium alkaloid nostocarboline from the cyanobacterium Nostoc 78-12A and 10 bis-cationic dimeric derivatives were evaluated against four protozoan parasites and low micromolar values against Trypanosoma brucei, submicromolar values against Leishmania donovani and low nanomolar values against Plasmodium falciparum K1 were determined. Selectivity against rat myoblasts (L6 cells) was found to be up to >2500-fold.
对来自蓝藻念珠藻78 - 12A的季铵型β-咔啉生物碱诺斯托卡啉及其10种双阳离子二聚衍生物进行了针对四种原生动物寄生虫的评估,测定出其对布氏锥虫的活性值为低微摩尔浓度,对杜氏利什曼原虫的活性值为亚微摩尔浓度,对恶性疟原虫K1的活性值为低纳摩尔浓度。结果发现,其对大鼠成肌细胞(L6细胞)的选择性高达2500倍以上。