[Metabolism, transformation and distribution of Coptis chinensis total alkaloids in rat].
[Metabolism, transformation and distribution of Coptis chinensis total alkaloids in rat].
复制标题
DOI：
10.4268/cjcmm20101523
复制
发表时间：
2010-08
期刊：
影响因子：
--
通讯作者：
Liang Wang;Xiaoli Ye;Xuegang Li;Zhu Chen;Xiaodan Chen;Ying Gao;Zhongqi Zhao;Wenwen Huang;Xin Chen;Jun Yi
中科院分区：
文献类型：
--
作者：
Liang Wang;Xiaoli Ye;Xuegang Li;Zhu Chen;Xiaodan Chen;Ying Gao;Zhongqi Zhao;Wenwen Huang;Xin Chen;Jun Yi
目的研究黄连总生物碱、药根碱、黄连碱、小檗碱和巴马汀在大鼠体内的药动学、分布及相互转化。方法大鼠灌胃总生物碱和小檗碱后，采用反相高效液相色谱法测定血浆、组织和胃肠道中总生物碱和小檗碱的含量。结果小檗碱血药浓度达峰时间分别为2.0h（Cmax 3.7mg × L（-1））和5.0h（Cmax 2.8mg × L（-1））。小檗碱在大鼠血液中可转化为药根碱。大鼠灌胃给予总生物碱后，胃内小檗碱含量单调下降，黄连碱、巴马汀和药根碱含量逐渐升高，推测小檗碱可能在胃内转化为药根碱。动物实验表明，小檗碱和巴马汀在动物体内主要分布在肺部，其次是肝脏，药根碱和黄连碱主要分布在肝脏，其次是肺部。结论小檗碱可转化为药根碱。小檗碱在血液中出现两个最大血药浓度的机制部分可以用胃肠道的推进作用来解释。
OBJECTIVE To determine the pharmacokinetics, distribution and mutual transformation of the total alkaloids, jatrorrhizine, coptisine, berberine and palmatine from Coptis chinensis in rats. METHOD After the total alkaloids and berberine were fed into rats, their contents in plasma, tissues and gastrointestinal tract were determined by reversed-phase HPLC. RESULT The peak times of berberine in blood were 2.0 h (Cmax 3.7 mg x L(-1)) and 5.0 h Cmax 2.8 mg x L(-1)), respectively. Berberine in rat blood can be transformed into jatrorrhizine. After the rats were fed with the total alkaloids by gavage, the content of berberine was decreased monotonously, while coptisine, palmatine and jatrorrhizine contents were increased gradually in the stomach, it speculated that berberine may be transformed into jatrorrhizine in the stomach. Animal experiments showed that berberine and palmatine were mainly distributed in the lungs of animals, followed by the distribution in the liver, while jatrorrhizine and coptisine was mainly in the liver, then in the lungs. CONCLUSION Berberine could transform into jatrorrhizine. The mechanism on the appearance of two maximum blood concentration of berberine in blood could be explained with the propulsion of the gastrointestinal tract partly.