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 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 TRPV1 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.
引文
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