羌活提取物对热敏通道TRPV1的影响

Effects of Notopterygium Incisum Extracts on the Transient Receptor Potential Vanilloid 1 of Thermosensitire Channel

目的:探讨羌活水提物和醇提物对热敏通道TRPV1的影响。方法:在瞬转人源TRPV1的HEK293细胞上,运用膜片钳技术测量羌活提取物对细胞跨膜电流的影响。结果:羌活提取物可激活TRPV1通道产生明显的跨膜电流,该跨膜电流与TRPV1激动剂辣椒素诱发的电流在电流密度和电流-电压关系各方面均类似;羌活水提物在生药1 g/ml时稀释10倍左右,对跨膜电流的影响达到最大,并可以被TRPV1竞争性抑制剂辣椒素完全阻断。结论:羌活提取物中含TRPV1激动剂,该通道活化后产生的系列效应可能是羌活解表、止痛的重要分子机制。

Objective： To investigate the effect of ethanol extracts and water extracts of Notopterygium incisum on thermosensitive channel, Transient Receptor Potential Vanilloid 1 （TRPVl）. Methods： Whole cell voltage clamp technique was used to record transmembrane currents induced by the Notopterygium extracts in HEK 293 cells that expressed human TRPV1. Results ： Both ethanol and water extracts of Notopterygium incisum evoked robust currents comparable to that by the known TRPV1 agonist, capsaicin, in current density and current-voltage relationship. The maximum effect of Notopterygium water extracts was reached at 100 mg/ml. The Notopterygium-induced TRPV! current was completely abolished by the specific TRPV1 antagonist, capsazepine （10 μM）. Conclusions： One or more components of Notopterygium extracts are TRPV1 agonists, which may underlie the analgesic and relieving exterior syndrome effects of Notopterygium.