羌活提取物对热敏通道TRPV1的影响
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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.
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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[6]陈虹宇,尹显梅,陈玲,等.不同商品规格等级羌活的镇痛抗炎作用对比研究[J].中药与临床,2016,7(2):15-17.
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[8]陈智煌,廖华军,刘晨,等.羌活挥发油的GC-MS分析及其抗炎镇痛的药理作用初探[J],海峡药学,2015,27(8):20-23.
[9]易增兴.羌活与独活水煎液的抗炎镇痛作用[J].宜春学院学报,2013(3):68-70.
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[11]ROMANOVSKY AA.Thermoregulation:some concepts have changed.Functional architecture of the thermoregulatory system[J].American journal of physiology Regulatory,integrative and comparative physiology,2007,292(1):R37-46.
[12]ROMANOVSKY AA,ALMEIDA MC,GARAMI A,et al.The transient receptor potential vanilloid-1 channel in thermoregulation:a thermosensor it is not[J].Pharmacological reviews,2009,61(3):228-261.
[13]MORRISON SF,NAKAMURA K,MADDEN CJ.Central control of thermogenesis in mammals[J].Experimental physiology,2008,93(7):773-797.
[14]GAWA NR.Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1[J].Trends in pharmacological sciences,2008,29(11):550-557.
[15]JULIUS D.TRP channels and pain[J].Annual review of cell and developmental biology,2013,29:355-384.
[16]孙洪兵,蒋舜媛,周毅,等.羌活临床应用的本草考证及处方分析[J].四川中医,2016,34(7):33-37.
[17]罗鑫,王雪晶,赵祎武,等.羌活化学成分研究[J].中草药,2016,47(9):1492-1495.
[2]CATERINA MJ,SCHUMACHER MA,TOMINAGA M,et al.The capsaicin receptor:a heat-activated ion channel in the pain pathway[J].Nature,1997,389(6653):816-824.
[3]CHEN X,SUN W,GIANARIS NG,et al.Furanocoumarins are a novel class of modulators for the transient receptor potential vanilloid type 1(TRPV1)channel[J].The Journal of biological chemistry,2014,289(14):9600-9610.
[4]李巧云,琼鹏,李霞,等.不同羌活提取物镇痛作用比较[J].四川生理科学杂志,1995(Z1):137.
[5]张明发,沈雅琴,朱自平,等.羌活的镇痛抗炎抗血栓形成作用研究[J].中西医结合脑血管病杂志,1996(6):51-53.
[6]陈虹宇,尹显梅,陈玲,等.不同商品规格等级羌活的镇痛抗炎作用对比研究[J].中药与临床,2016,7(2):15-17.
[7]周毅,蒋舜媛,马小军,等.川产羌活基源及镇痛作用研究[J].中药药理与临床,2003,19(6):22-23.
[8]陈智煌,廖华军,刘晨,等.羌活挥发油的GC-MS分析及其抗炎镇痛的药理作用初探[J],海峡药学,2015,27(8):20-23.
[9]易增兴.羌活与独活水煎液的抗炎镇痛作用[J].宜春学院学报,2013(3):68-70.
[10]杨桢,汪文来,刘珍洪,等.热敏通道与辛味中药的解表原理[J].中国中医基础医学杂志,2016,22(10):1386-1390.
[11]ROMANOVSKY AA.Thermoregulation:some concepts have changed.Functional architecture of the thermoregulatory system[J].American journal of physiology Regulatory,integrative and comparative physiology,2007,292(1):R37-46.
[12]ROMANOVSKY AA,ALMEIDA MC,GARAMI A,et al.The transient receptor potential vanilloid-1 channel in thermoregulation:a thermosensor it is not[J].Pharmacological reviews,2009,61(3):228-261.
[13]MORRISON SF,NAKAMURA K,MADDEN CJ.Central control of thermogenesis in mammals[J].Experimental physiology,2008,93(7):773-797.
[14]GAWA NR.Body-temperature maintenance as the predominant function of the vanilloid receptor TRPV1[J].Trends in pharmacological sciences,2008,29(11):550-557.
[15]JULIUS D.TRP channels and pain[J].Annual review of cell and developmental biology,2013,29:355-384.
[16]孙洪兵,蒋舜媛,周毅,等.羌活临床应用的本草考证及处方分析[J].四川中医,2016,34(7):33-37.
[17]罗鑫,王雪晶,赵祎武,等.羌活化学成分研究[J].中草药,2016,47(9):1492-1495.