中药提取物对瞬时受体电位(TRP)通道的调节作用
2011/06/17
摘要
许多瞬时受体电位(TRP)通道能被诸多植物成分所活化或阻断。TRPV1（瞬时受体电位香草酸亚型1）和瞬时受体电位锚蛋白亚型-1 (TRPA1)都属于TRP离子通道家族，被认为是咳嗽受体。一些中药植物(TCM)提取物可用于咳嗽的治疗。本研究对4种中药提取物对咳嗽受体的影响进行了评价。研究的中药中，枇杷叶提取物，特别是50%乙醇提取物，对辣椒素诱导的TRPV1活化抑制作用最大。枇杷叶提取物能通过TRPV1和未知通道诱导钙内流。因此，枇杷叶提取物抑制TRPV1细胞辣椒素诱导的钙内流，主要与受体的脱敏有关。枇杷叶提取物对TRPA1的作用与对TRPV1的作用类似，但抑制强度要弱。另外三个纯化的成分是熊果酸(UA)、贝母素甲(PM)和贝母素乙(PN)，同时也研究了三者对咳嗽受体的影响。仅UA在100 μm时对TRPV1具有较强的拮抗活性。PM和PN单独实验时，对两种受体无作用，但两者联合给药时，能增加UA的作用。与此类似，对TRPA1也有抑制作用，但强度要弱。
（陈欣 审校）
Phytother Res. 2011 Mar 23. doi: 10.1002/ptr.3427. [Epub ahead of print]
Modulation of Transient Receptor Potential (TRP) Channels by Chinese Herbal Extracts.
Zhang Y, Sreekrishna K, Lin Y, Huang L, Eickhoff D, Degenhardt C, Xu T.
Global Health Care Connect and Develop, Procter & Gamble Technology (Beijing) Co., Ltd, Beijing, 100084, P.R. China; China Academy of Chinese Medical Sciences, Beijing, 100700, P.R. China.
Abstract
Many transient receptor potential (TRP) channels are activated or blocked by various compounds found in plants. TRPV1 (transient receptor potential vanilloid 1) and transient receptor potential ankyrin 1 (TRPA1) are members of the TRP ion channel family which are implicated as cough receptors. Several plant extracts are used in traditional Chinese medicine (TCM) for the treatment of cough. This report evaluated the effect of four such herbals for their effect on cough receptors. Of the herbals tested, Pipaye (Folium Eriobotryae) extracts, especially the 50% ethanol extract, showed the highest activity for the suppression of TRPV1 activation by its agonist capsaicin. Pipaye is able to elicit Ca-flux through TRPV1 as well as through unknown channels. Thus the inhibition of capsaicin elicited Ca-flux in TRPV1 cells by Pipaye is largely due to desensitization of the receptor. Pipaye extract has a similar, but less pronounced effect, on TRPA1. Also tested were three pure components, ursolic acid (UA), peimine (PM) and peiminine (PN) derived from TCM for their effect on cough receptors. Only UA tested at 100 μm showed potent antagonistic activity towards TRPV1. Both PM and PN had no activity when tested alone, however, both were able to enhance the UA effect. A similar, but less marked, inhibition was also noted for TRPA1.
Phytother Res. 2011 Mar 23. doi: 10.1002/ptr.3427. [Epub ahead of print]
许多瞬时受体电位(TRP)通道能被诸多植物成分所活化或阻断。TRPV1（瞬时受体电位香草酸亚型1）和瞬时受体电位锚蛋白亚型-1 (TRPA1)都属于TRP离子通道家族，被认为是咳嗽受体。一些中药植物(TCM)提取物可用于咳嗽的治疗。本研究对4种中药提取物对咳嗽受体的影响进行了评价。研究的中药中，枇杷叶提取物，特别是50%乙醇提取物，对辣椒素诱导的TRPV1活化抑制作用最大。枇杷叶提取物能通过TRPV1和未知通道诱导钙内流。因此，枇杷叶提取物抑制TRPV1细胞辣椒素诱导的钙内流，主要与受体的脱敏有关。枇杷叶提取物对TRPA1的作用与对TRPV1的作用类似，但抑制强度要弱。另外三个纯化的成分是熊果酸(UA)、贝母素甲(PM)和贝母素乙(PN)，同时也研究了三者对咳嗽受体的影响。仅UA在100 μm时对TRPV1具有较强的拮抗活性。PM和PN单独实验时，对两种受体无作用，但两者联合给药时，能增加UA的作用。与此类似，对TRPA1也有抑制作用，但强度要弱。
（陈欣 审校）
Phytother Res. 2011 Mar 23. doi: 10.1002/ptr.3427. [Epub ahead of print]
Modulation of Transient Receptor Potential (TRP) Channels by Chinese Herbal Extracts.
Zhang Y, Sreekrishna K, Lin Y, Huang L, Eickhoff D, Degenhardt C, Xu T.
Global Health Care Connect and Develop, Procter & Gamble Technology (Beijing) Co., Ltd, Beijing, 100084, P.R. China; China Academy of Chinese Medical Sciences, Beijing, 100700, P.R. China.
Abstract
Many transient receptor potential (TRP) channels are activated or blocked by various compounds found in plants. TRPV1 (transient receptor potential vanilloid 1) and transient receptor potential ankyrin 1 (TRPA1) are members of the TRP ion channel family which are implicated as cough receptors. Several plant extracts are used in traditional Chinese medicine (TCM) for the treatment of cough. This report evaluated the effect of four such herbals for their effect on cough receptors. Of the herbals tested, Pipaye (Folium Eriobotryae) extracts, especially the 50% ethanol extract, showed the highest activity for the suppression of TRPV1 activation by its agonist capsaicin. Pipaye is able to elicit Ca-flux through TRPV1 as well as through unknown channels. Thus the inhibition of capsaicin elicited Ca-flux in TRPV1 cells by Pipaye is largely due to desensitization of the receptor. Pipaye extract has a similar, but less pronounced effect, on TRPA1. Also tested were three pure components, ursolic acid (UA), peimine (PM) and peiminine (PN) derived from TCM for their effect on cough receptors. Only UA tested at 100 μm showed potent antagonistic activity towards TRPV1. Both PM and PN had no activity when tested alone, however, both were able to enhance the UA effect. A similar, but less marked, inhibition was also noted for TRPA1.
Phytother Res. 2011 Mar 23. doi: 10.1002/ptr.3427. [Epub ahead of print]
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GERD相关性咳嗽：病理生理学和诊断方法
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