, Volume 6, Issue 5, pp 286-288,
Open Access This content is freely available online to anyone, anywhere at any time.
Date: 22 Oct 2008

Inhibition of P2X7 receptor by extracts of Chinese medicine

摘要

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P2X7受体的电流。

结果

40 μg/mL SCP01 抑制P2X7 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P2X7 电流 (52.2 ± 2.0) %.相反, 40 μg/mL X0728 激活P2X7 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P2X7 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P2X7 的药理学效应尚需进一步研究。

Abstract

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.

Fund Items: Supported by 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) and Shanghai Leading Academic Discipline Project (B112 and T0302)
Author: Andreas Spielmann, PhD Student, Max-Planck-Institute for Biophysics, and Goethe University, Frankfurt, Germany Cellular Mechanisms in response to treatment by TCM