异去甲乌药碱大鼠口服给药后的代谢产物
Metabolites of isocorynoxeine in rats after its oral administration.
作者信息
Chen Ya-Ping, Lu Min-Nan, Hao Jing-Chao, Li Mei-Hong, Hattori Masao, Wang Wei
机构信息
a School of Pharmaceutical Sciences and Yunnan Provincial Key Laboratory of Pharmacology for Natural Products, Kunming Medical University , Kunming 650500 , China.
出版信息
J Asian Nat Prod Res. 2015;17(4):384-90. doi: 10.1080/10286020.2014.1003182. Epub 2015 Jan 30.
This work presents the metabolites of isocorynoxeine (ICOR), which is one of four bioactive tetracyclic oxindole alkaloids isolated from Uncaria hooks used commonly in the traditional Chinese medicines and Kampo medicines. After oral administration of 40 mg kg(-1) ICOR to rats, bile was drained and analyzed by LC-MS. Two phase I metabolites, namely 11-hydroxyisocorynoxeine (M1) and 10-hydroxyisocorynoxeine (M2), and two phase II metabolites, namely 11-hydroxyisocorynoxeine 11-O-β-D-glucuronide (M3) and 10-hydroxyisocorynoxeine 10-O-β-D-glucuronide (M4), were isolated from rat excreta and bile, respectively, whose structures were elucidated on the basis of CD, NMR, and MS.
本研究展示了异柯诺辛碱（ICOR）的代谢产物，异柯诺辛碱是从传统中药和汉方药物中常用的钩藤中分离出的四种具有生物活性的四环氧化吲哚生物碱之一。给大鼠口服40 mg kg(-1)的ICOR后，收集胆汁并通过液相色谱 - 质谱联用仪进行分析。分别从大鼠排泄物和胆汁中分离出两种I相代谢产物，即11 - 羟基异柯诺辛碱（M1）和10 - 羟基异柯诺辛碱（M2），以及两种II相代谢产物，即11 - 羟基异柯诺辛碱11 - O - β - D - 葡萄糖醛酸苷（M3）和10 - 羟基异柯诺辛碱10 - O - β - D - 葡萄糖醛酸苷（M4），并根据圆二色光谱（CD）、核磁共振（NMR）和质谱（MS）对其结构进行了阐明。
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