The role of Piper chaba Hunt. and its pure compound, piperine, on TRPV1 activation and adjuvant effect
The role of Piper chaba Hunt. and its pure compound, piperine, on TRPV1 activation and adjuvant effect
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DOI：
10.1186/s12906-020-02917-4
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发表时间：
2020-05-05
影响因子：
3.9
通讯作者：
Itharat, Arunporn
中科院分区：
文献类型：
--
作者：
Panthong, Sumalee;Imai, Yasuyuki;Itharat, Arunporn
背景：Piper chaba Hunt。是泰国传统关节炎制剂中的一种成分。其分离的化合物是胡椒碱，具有抗炎活性。胡椒碱会产生灼烧感，因为它激活了TRPV1受体。TRPV1的激活与镇痛和辅助作用有关。P.查巴·亨特。尚未报道TRPV1的激活和辅助作用。本研究旨在探讨木瓜提取物和胡椒碱对作为镇痛靶点的TRPV1受体的影响及其辅助作用，为中药镇痛药物的开发提供依据。方法：采用钙显像法检测木瓜提取物和胡椒碱对HEK细胞表达TRPV1通道的影响。采用异硫氰酸荧光素（FITC）致小鼠接触性超敏反应（CHS）模型，研究了木瓜提取物和胡椒碱的佐剂作用。结果：茶巴提取物诱导钙内流，EC50值为0.67 μ g/ml。胡椒碱诱导钙内流的EC50值分别为0.31 μ g/ml和1.08 μ m。在小鼠CHS模型中，我们发现1%胡椒碱、5%胡椒碱、1%恰巴树提取物和5%恰巴树提取物通过耳肿胀反应显著增强了对FITC的致敏性。结论：茶巴提取物和胡椒碱可激活TRPV1通道，增强对FITC的接触敏化。
Background: Piper chaba Hunt. is used as an ingredient in Thai traditional preparation for arthritis. Its isolated compound is piperine which shows anti-inflammatory activity. Piperine produces a burning sensation because it activates TRPV1 receptor. The TRPV1 activation involved with the analgesic and adjuvant effect. P. chaba Hunt. has not been reported about TRPV1 activation and adjuvant effect. The aim of this study was to investigate the effect of P. chaba extract and piperine on TRPV1 receptor, which is considered as a target for analgesic and their adjuvant effects to support the development of an analgesic drug from herbal medicine.Methods: The effect of P. chaba extract and piperine on HEK cells expressing TRPV1 channel was examined by calcium imaging assay. Adjuvant effects of P. chaba extract and piperine were investigated by a fluorescein isothiocyanate (FITC)-induced contact hypersensitivity (CHS) model in mice.Results: P. chaba extract induced calcium influx with EC50 value of 0.67 mu g/ml. Piperine induced calcium influx with EC50 value of 0.31 mu g/ml or 1.08 mu M. For mouse CHS model, we found that 1% piperine, 5% piperine, 1% P. chaba extract and 5% P. chaba extract significantly enhanced sensitization to FITC as revealed by ear swelling responses.Conclusion: P. chaba extract and piperine activated TRPV1 channel and enhanced contact sensitization to FITC.