Beijing Hospital of Integrated Traditional Chinese and Western Medicine, China.
Chin J Integr Med. 2010 Oct;16(5):430-4. doi: 10.1007/s11655-010-9997-y. Epub 2010 Jun 10.
To observe the effect of matrine on human ether à go-go related gene (HERG) potassium channels expressed in Chinese hamster ovary (CHO) cells and investigate whether HERG channel is a new target of the pharmacological effect of matrine on arrhythmia and tumor
HERG channel potassium current in CHO cell was recorded using whole-cell patch-clamp technique, and the influence of matrine on the current was explored.
Matrine inhibited HERG potassium current in a dose-dependent manner, and the 50% inhibitory concentration (IC IC(50)) was 411±23 μmol/L. Matrine had no significant effect on the activation kinetics, and mainly blocked HERG channels in their closed state.
The blocking effect of matrine on HERG channels might be one of the mechanisms against arrythmias and tumors. Unlike most other blockers exerting blocking effect at the intracellular sites by entering the cell with the opening of HERG channel, matrine blocked HERG channels at the extracellular sites.
观察苦参碱对中国仓鼠卵巢（CHO）细胞表达的人 ether-à-go-go 相关基因（HERG）钾通道的影响，探讨 HERG 通道是否为苦参碱抗心律失常和抗肿瘤作用的新靶点。
采用全细胞膜片钳技术记录 CHO 细胞 HERG 通道电流，观察苦参碱对电流的影响。
苦参碱呈浓度依赖性抑制 HERG 钾电流，半数抑制浓度（IC₅₀）为 411±23 μmol/L。苦参碱对 HERG 钾通道激活动力学无明显影响，主要作用于 HERG 通道的关闭状态。
苦参碱对 HERG 通道的阻断作用可能是其抗心律失常和抗肿瘤的机制之一。苦参碱不同于大多数其他以细胞内位点为作用靶点的阻断剂，后者通过 HERG 通道的开放进入细胞内发挥作用，而苦参碱则在细胞外位点阻断 HERG 通道。
