The role of Piper chaba Hunt. and its pure compound, piperine, on TRPV1 activation and adjuvant effect

Sumalee Panthong,Yasuyuki Imai,Kota Sekiguchi,Tatsuo Watanabe,Yukina Endo,Wakana Suzuki,Yuko Terada,Kohta Kurohane,Arunporn Itharat,Erina Ogawa,Takeshi Matsuoka

doi:10.1186/s12906-020-02917-4

Sumalee Panthong, Yasuyuki Imai + Show 9 more

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https://doi.org/10.1186/s12906-020-02917-4

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Abstract

BackgroundPiper 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.MethodsThe 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.ResultsP. chaba extract induced calcium influx with EC50 value of 0.67 μg/ml. Piperine induced calcium influx with EC50 value of 0.31 μg/ml or 1.08 μM. 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.ConclusionP. chaba extract and piperine activated TRPV1 channel and enhanced contact sensitization to FITC.

Highlights

Piper chaba Hunt. is used as an ingredient in Thai traditional preparation for arthritis
Piperine and Piper chaba (PC) extract on human TRPV1 activation TRPV1-expressing HEK293 cells were treated with capsaicin, piperine or PC extract at various concentrations
The results show that capsaicin (TRPV1 agonist, positive control), piperine and PC extract increased calcium influx into TRPV1 HEK293 cells with EC50 value of 1.14 ng/ml (3.73 nM), 0.31 μg/ml (1.08 μM) and 0.67 μg/ml, respectively (Table 1)

Summary

Introduction

Piper chaba Hunt. is used as an ingredient in Thai traditional preparation for arthritis. Piperine produces a burning sensation because it activates TRPV1 receptor. The TRPV1 activation involved with the analgesic 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. Piperine has shown anti-inflammatory, TRPV1 or capsaicin receptor is a cation channel which consists of six transmembrane domains. It is activated by capsaicin, noxious heat, low pH and voltage [11]. It has been suggested that TRPV1 activation and desensitization are related to be analgesic and counterirritant effects [17]

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