Laboratory of Pharmacokinetics, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
J Ethnopharmacol. 2010 Mar 24;128(2):357-64. doi: 10.1016/j.jep.2010.01.047. Epub 2010 Feb 1.
Rhizoma Coptidis (Huanglian) is a widely used Traditional Chinese Medicine. However, it causes human as well as animal toxicities. In this study, we aimed to ascertain the toxic constituents in Rhizoma Coptidis.
The acute toxicity of both the total extract and the alkaloid-rich extract of Rhizoma Coptidis were tested in mice. The dose related tissue concentration of the Rhizoma Coptidis alkaloids in mice was determined using high performance liquid chromatography with ultraviolet detection. The influence of phenobarbital sodium [a non-selective hepatic enzyme (P450) inducer] on the acute toxicity of Rhizoma Coptidis as well as the tissue concentration of the alkaloids was investigated. The cytotoxicity of the Rhizoma Coptidis alkaloids was tested in six cell lines using the MTT assay.
The median acute oral lethal dose of the total extract of Rhizoma Coptidis was 2.95g/kg in mice. The alkaloid-rich extract was much more toxic than the total extract of Rhizoma Coptidis. Four Rhizoma Coptidis alkaloids were detected in brain, heart, and lung tissues of mice that received the oral total extract of Rhizoma Coptidis. Tissue concentration increased nonlinearly with higher doses. Phenobarbital sodium decreased the tissue concentration of every alkaloid as well as the toxicity of Rhizoma Coptidis. All alkaloids, especially berberine, showed dose and time dependent cytotoxicity.
The toxic constituents of Rhizoma Coptidis were the alkaloids, mainly berberine.
黄连是一种广泛使用的中药，但它会引起人类和动物的毒性。本研究旨在确定黄连中的有毒成分。
在小鼠中测试了黄连总提取物和富含生物碱的提取物的急性毒性。采用高效液相色谱法结合紫外检测，测定了黄连生物碱在小鼠体内的剂量相关组织浓度。研究了苯巴比妥钠（一种非选择性肝酶（P450）诱导剂）对黄连急性毒性以及生物碱组织浓度的影响。采用 MTT 法在六种细胞系中测试了黄连生物碱的细胞毒性。
黄连总提取物的小鼠口服半数致死剂量为 2.95g/kg。富含生物碱的提取物比黄连总提取物毒性更大。在接受黄连总提取物口服的小鼠的脑、心和肺组织中检测到四种黄连生物碱。组织浓度随剂量的增加呈非线性增加。苯巴比妥钠降低了每种生物碱以及黄连毒性的组织浓度。所有生物碱，尤其是小檗碱，表现出剂量和时间依赖性细胞毒性。
黄连的有毒成分是生物碱，主要是小檗碱。
