摘要
Objective： To investigate the influence of Acorus gramineus （Soland）, a crude extract, SCP01, and a purified component, SCP02, and of Rosmarinus officinalis L., X0728 on human mast cells （HMC-1 Cell Line）. Methods： Current-voltage of P2X7 receptors on human mast cell membrane activated by ATP was recorded by the whole-cell patch clamp technique. Results： The current at -100 mV mediated by P2X7 was inhibited by （27.6 ± 2.0） % in the presence of 40 μg/mL SCP01 and by （29.5 ± 2.2） % in the presence of 40 μg/mL SCP02, which was identified as α-asarone. 42 μg/mL of the commercially available α-asarone inhibited the P2X7-mediated current by （52.2 ± 2.0） %. In contrast to SCP01 and SCP02, 40 μg/mL X0728 provoked stimulation of the current by （28.6 ± 2.8） %. All effects were voltage- independent. Conclusion： The inhibition of P2X7 by α-asarone will inhibit intracellular calcium increase and this may account for the inhibition of reported excitotoxic cell death. The pharmacological function of P2X7 stimulation by X0728 needs further investigation.
目的:探讨中草药石菖蒲粗提物 SCP01及其纯化物 SCP02(α-细辛脑)和迷迭香抽提物 X0728对人肥大细胞的作用。方法:用膜片钳技术全细胞记录人肥大细胞膜 ATP 激活的 P2X_7受体的电流。结果:40μg/mL SCP01抑制 P2X_7电流(27.6±2.0)%,而同样浓度的 SCP02抑制(29.5±2.2)%(-100 mV 电位下),笔者还比较了商业用α-细辛脑的效应,42 μg/mL 可抑制 P2X_7电流(52.2±2.0)%。相反,40μg/mL X0728激活 P2X_7电流(28.6±2.8)%,所有这些作用都是电压依赖性的。结论:α-细辛脑对 P2X_7的抑制将阻滞胞内钙的增加,从而可以解释抑制神经元死亡的原因。而 X0728刺激 P2X_7的药理学效应尚需进一步研究。
基金
the Science Foundation of Shanghai Municipal Commission of Science and Technology(05DZ19745,06DZ19732,064319053,07DZ19722,07DZ19733)
the National Basic Research Program of China (973 Program,2005CB523306)
Shanghai Leading Academic Discipline Project(B112 and T0302)
