Antitrypanosomal activities of acetylated bruceines A and C ; a structure-activity relationship study
Antitrypanosomal activities of acetylated bruceines A and C ; a structure-activity relationship study
复制标题
乙酰化马钱子碱 A 和 C 的抗锥虫活性；
DOI：
10.1007/s11418-011-0571-5
复制
发表时间：
2012
影响因子：
3.3
通讯作者：
et al
中科院分区：
文献类型：
--
作者：
Elkhateeb A;et al
鸦胆子粗提物对伊氏锥虫具有较强的体外抑制活性。在分离的苦木素类化合物中，发现马钱子碱A、C和马钱子醇是最有效的抗T化合物。evansi为了深入了解活性与游离羟基的关系，我们合成了几种马钱子碱A和C的O-乙酰化衍生物，并对其体外抗锥虫活性进行了研究。evansi进行了检测，并与原始化合物进行了比较。结果表明：（1）C-3、C-11和C-12位的自由羟基是抗锥虫活性所必需的，（2）C-11和C-12位的羟基比C-3位的烯醇羟基更重要;（3）马钱子碱C的C-4′位游离羟基对活性无明显影响。
The crude extract ofBrucea javanicashowed strong in vitro inhibitory activity againstTrypanosoma evansi. Among the isolated quassinoids, bruceines A, C, and bruceantinol were found to be the most potent compounds againstT. evansi. To gain a deeper understanding of the relationship between the free hydroxyl groups and the activity, severalO-acetylated derivatives of bruceines A and C were synthesized and their in vitro antitrypanosomal activities against trypomastigotes ofT. evansiwere examined and compared with those of the original compounds. The following structure–activity relationships were observed: (1) the free hydroxyl groups at positions C-3, C-11, and C-12 are essential for antitrypanosomal activity; (2) the C-11 and C-12 hydroxyl groups are more important for the activity than the enolic hydroxyl group at C-3, and; (3) the free hydroxyl group at C-4′ of bruceine C does not have any significant effect on the activity.