Camacho M R, Mata R, Castaneda P, Kirby G C, Warhurst D C, Croft S L, Phillipson J D
Centre for Pharmacognosy and Phytotherapy, School of Pharmacy, University of London, UK.
Planta Med. 2000 Jun;66(5):463-8. doi: 10.1055/s-2000-8598.
Bioactivity-directed fractionation of the CHCl3-MeOH extract of the leaves of Celaenodendron mexicanum by means of the brine shrimp lethality test and chromatographic techniques led to the isolation of three carboxylic acid triterpenes, the new tirucalla-type triterpene, 3 alpha-hydroxytirucalla-7,24Z-dien-26-oic acid, 3-oxotirucalla-7,24Z-dien-26-oic acid, and epi-oleanolic acid, and three biflavonoids amentoflavone, podocarpusflavone A, and podocarpusflavone B. Four non-active compounds friedelin, maytensifolin B, 3 beta-hydroxyfriedelan-16-one, and celaenodendrolide were also obtained. epi-Oleanolic acid was the most active against brine shrimps with LC50 value of 23.3 microM. In addition, all isolates were tested for in vitro antiprotozoal and cytotoxic activities. 3-Oxotirucalla-7,24Z-dien-26-oic acid and epi-oleanolic acid showed the highest activity against Leishmania donovani promastigotes with IC50 values of 13.7 and 18.8 microM, respectively. Only 3-oxotirucalla-7,24Z-dien-26-oic acid showed activity against Trypanosoma brucei brucei bloodstream forms with IC50 value of 16.8 microM.
通过卤虫致死试验和色谱技术对墨西哥赛林藤叶的氯仿 - 甲醇提取物进行生物活性导向分离，得到了三种三萜羧酸、新的 tirucalla 型三萜 3α - 羟基 tirucalla - 7,24Z - 二烯 - 26 - 酸、3 - 氧代 tirucalla - 7,24Z - 二烯 - 26 - 酸和表齐墩果酸，以及三种双黄酮amentoflavone、罗汉松黄酮 A 和罗汉松黄酮 B。还得到了四种无活性化合物软木三萜酮、maytensifolin B、3β - 羟基软木三萜 - 16 - 酮和赛林藤内酯。表齐墩果酸对卤虫活性最强，LC50 值为 23.3 μM。此外，对所有分离物进行了体外抗原生动物和细胞毒性活性测试。3 - 氧代 tirucalla - 7,24Z - 二烯 - 26 - 酸和表齐墩果酸对杜氏利什曼原虫前鞭毛体活性最高，IC50 值分别为 13.7 和 18.8 μM。只有 3 - 氧代 tirucalla - 7,24Z - 二烯 - 26 - 酸对布氏锥虫血液型有活性，IC50 值为 16.8 μM。
