Antigiardial activity of triterpenoids from root bark of Hippocratea excelsa
Antigiardial activity of triterpenoids from root bark of Hippocratea excelsa
复制标题
DOI：
10.1021/np060559y
复制
发表时间：
2007-05-01
影响因子：
5.1
通讯作者：
Quijano, Leovigildo
中科院分区：
文献类型：
--
作者：
Mena-Rejon, Gonzalo J.;Perez-Espadas, Aida R.;Quijano, Leovigildo
从希波克拉底（Hippocratea excelsa）的根皮中分离到两个新的三萜，21 β -羟基齐墩烯-12-烯-3-one(1)和原始碱的二阶衍生物dzununcanone(2)。它们的结构是根据光谱证据确定的，主要是H-1和C-13的1D和2D NMR，包括DEPT、COSY、ROESY、HSQC和HMBC实验，以及EIMS和HREIMS。已知的21 α -羟基-3-氧杂环己烷(3)是该物种的新化合物，已知的甲基醌类化合物pritimerine (4) tiningenone(5)和xuxuarine E β(7)也被分离出来。测定其对肠贾第虫的抗虫活性。与目前常用药物甲硝唑的IC50值（1.23 μ M）相比，原草碱和丁烯酮的IC50值分别为0.11和0.74 μ M，是抗心包活性最高的化合物。
Two new triterpenoids, 21 beta-hydroxyolean-12-en-3-one (1) and a seco-dinor derivative of pristimerine named dzununcanone (2), were isolated from the root bark of Hippocratea excelsa. Their structures were assigned on the basis of spectroscopic evidence, mainly H-1 and C-13 1D and 2D NMR including DEPT, COSY, ROESY, HSQC, and HMBC experiments, as well as EIMS and HREIMS. The known 21 alpha-hydroxy-3-oxofriedelane (3), a compound new to the species, and the known methide quinones pristimerine (4) tingenone (5), and xuxuarine E beta (7) were also isolated. The antiprotozoal activities were determined against Giardia intestinalis. Pristimerine and tingenone were the most active antigiardial compounds, with IC50 values of 0.11 and 0.74 mu M, respectively, compared with metronidazole, the current drug of choice (IC50 1.23 mu M).