Basic Medical Department, School of Pharmacy, Yantai University, No. 30, Qingquan Road, Laishan District, Yantai, Shandong, China.
Neurochem Res. 2012 Oct;37(10):2143-9. doi: 10.1007/s11064-012-0836-8. Epub 2012 Jul 20.
In order to observe antinociceptive effect of Oxymatrine (OMT) and its effect on voltage-activated K(+) channel, the acetic acid-induced abdominal contraction model of mouse was used to test the antinociceptive effect in vivo, and in vitro, the delayed rectifier K(+) currents (Ik) in PC12 cells (rat pheochromocytoma cells) was recorded using the automated patch-clamp method. The results indicated that after application of OMT, the number of acetic acid-induced animal abdominal contraction was significantly decreased, Ik in PC12 cells was significantly decreased, and showed a concentration-dependent manner. After application of OMT, both the activation and inactivation curves of Ik of PC12 cells were shifted to negative potentials. This study revealed that OMT showed antinociceptive effect in mice. The inhibition of voltage-activated K(+) channel might be one of mechanisms in which the enhanced both activation and inactivation of K(+) channel were involved and might play important roles.
为观察苦参碱(OMT)的镇痛作用及其对电压门控钾(K+)通道的影响,采用醋酸诱导的小鼠扭体模型检测体内镇痛作用,采用自动膜片钳技术记录 PC12 细胞(大鼠嗜铬细胞瘤细胞)中的延迟整流钾(K+)电流(Ik)。结果表明,苦参碱作用后,醋酸诱导的动物扭体次数明显减少,PC12 细胞 Ik 明显减少,并呈浓度依赖性。苦参碱作用后,PC12 细胞 Ik 的激活和失活曲线均向负电位移动。本研究表明,苦参碱对小鼠具有镇痛作用。抑制电压门控 K+通道可能是增强 K+通道的激活和失活的机制之一,可能发挥重要作用。