蛇床子素对L-和N-型钙通道的影响

Effect of Osthole on L-and N-type Calcium Channels

目的:比较蛇床子素对不同钙通道亚型的作用差异方法:首先在tsA201细胞上瞬时转染Cav1.2,Cav1.3,Cav2.2e[37a],和Cav2.2e[37b]通道,然后采用全细胞膜片钳技术,记录tsA201细胞上的钙电流,并观察蛇床子素对各种钙通道亚型的影响结果:蛇床子素可以浓度依赖性抑制Cav1.2和Cav1.3电流,抑制的半有效浓度分别为162.1μmol·L^(-1)和56.2μmol·L^(-1)。此外,蛇床子素对Cav2.2通道也有一定的抑制作用,在300μmol·L^(-1)的浓度下,抑制38%的Cav2.2e[37a]电流和61%的Cav2.2e[37b]电流蛇床子素对钙电流的抑制是快速可逆的蛇床子素在各个测试电位水平均能抑制上述四种钙通道电流,但不改变电流的激活阈值和最大峰值电流的激活电压。

Objective： To determine the effects ofosthole on voltage-dependent calcium channel subtypes. Methods： tsA-201 cells were transfected with the calcium channel subtypes of Cavl.2, Cavl.3, Cav2.2e [37a],and Cav2.2e [37b]. The calcium currents were recorded in tsA-201 cells using whole cell patch clamp technique. The effects of osthole on calcium currents were investigated. Results： Osthole could inhibit Cavl.2 and Cavl.3 currents in a concentration - dependent manner. The half-effective concentration of the inhibition was 162.1μmol·L-1, and 56.2μmol·L-1, respectively. In addition, Osthole reduced the Cav2.2e [37a],and Cav2.2e [37b] currents by 38 %, and 61%, respectively, at the concentration of 300μmol·L-1. The inhibition was fast and reversible. Osthole decreased the current amplitudes at all tested potentials, but showed no significant influence on the activation kinetics of the above calcium channels subtypes. Conclusions： Osthole concentration - dependently inhibited calcium currents and displayed different affinity to the calcium channel subtypes.