羌活提取物对热敏通道TRPV1的影响

摘要

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 (TRPV1).Methods:Whole cell voltage clamp technique was used to record transmembrane currents induced by the Notopterygium extracts in HEK 293 coils 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 TRPV1 current was completely abolished by the specific TRPV1 antagonist,capsazepine (10 pM).Conclusions:One or more components of Notopterygium extracts are TRPV1 agonists,which may underlie the analgesic and relieving exterior syndrome effects of Notopterygium.