Moideen S V, Houghton P J, Rock P, Croft S L, Aboagye-Nyame F
National Pharmaceutical Control Bureau, Jalan University, Petaling Jaya, Malaysia.
Planta Med. 1999 Aug;65(6):536-40. doi: 10.1055/s-1999-14011.
Dichloromethane extracts of the root bark and stem bark of Kigelia pinnata collected from Zimbabwe exhibited antitrypanosomal activity against Trypanosoma brucei brucei in vitro. Activity-guided fractionation led to the isolation of four naphthoquinones from both the root and stem bark of the plant. The compounds were identified as 2-(1-hydroxyethyl)-naphtho[2,3-b]furan-4,9-quinone (1), isopinnatal (2), kigelinol (3), and isokigelinol (4). Subsequently, the compounds were assessed for antitrypanosomal activity against T. brucei brucei and T. brucei rhodesiense bloodstream form trypomastigotes in vitro. Compound 1 with a furanonaphthoquinone structure was found to possess pronounced activity against both parasites with IC50 values of 0.12 and 0.045 microM, respectively, although it was less active than the standard drug pentamidine. Compounds 2, 3, and 4 also exhibited activity against the parasites, although to a lesser extent. The activities of the compounds were further assessed by comparison with the cytotoxic activities obtained against KB cell lines.
从津巴布韦采集的吊灯树的根皮和茎皮的二氯甲烷提取物在体外对布氏布氏锥虫表现出抗锥虫活性。活性导向分离法从该植物的根皮和茎皮中分离出四种萘醌。这些化合物被鉴定为2-(1-羟乙基)-萘并[2,3-b]呋喃-4,9-醌(1)、异平那他尔(2)、基盖林醇(3)和异基盖林醇(4)。随后，评估了这些化合物在体外对布氏布氏锥虫和罗德西亚布氏锥虫血流形式锥鞭毛虫的抗锥虫活性。发现具有呋喃萘醌结构的化合物1对两种寄生虫都具有显著活性，IC50值分别为0.12和0.045微摩尔，尽管其活性低于标准药物喷他脒。化合物2、3和4也表现出对寄生虫的活性，尽管程度较小。通过与针对KB细胞系获得的细胞毒性活性进行比较，进一步评估了这些化合物的活性。
