Sumalee Panthong1,2, Yasuyuki Imai3, Takeshi Matsuoka3, Wakana Suzuki3, Tatsuo Watanabe4, Yuko Terada4, Kohta Kurohane3, Kota Sekiguchi3, Erina Ogawa3, Yukina Endo3, Arunporn Itharat5,6. 1. Department of Applied Thai Traditional Medicine, Faculty of Medicine, Thammasat University, Klongluang, Pathumthani, 12120, Thailand. 2. Centre of Excellence in Applied Thai Traditional Medicine Research (CEATMR), Thammasat University, Klongluang, Pathumthani, 12120, Thailand. 3. Laboratory of Microbiology and Immunology, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka-shi, Shizuoka, 422-8526, Japan. 4. Laboratory of Food Chemistry, School of Food and Nutritional Sciences|, University of Shizuoka, Shizuoka-shi, Shizuoka, 422-8526, Japan. 5. Department of Applied Thai Traditional Medicine, Faculty of Medicine, Thammasat University, Klongluang, Pathumthani, 12120, Thailand. iarunporn@yahoo.com. 6. Centre of Excellence in Applied Thai Traditional Medicine Research (CEATMR), Thammasat University, Klongluang, Pathumthani, 12120, Thailand. iarunporn@yahoo.com.
Abstract
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 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. CONCLUSION: P. chaba extract and piperine activated TRPV1 channel and enhanced contact sensitization to FITC.
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 μg/ml. Piperine induced calcium influx with EC50 value of 0.31 μg/ml or 1.08 μM. For mouseCHS 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.
Authors: Nikolai F Bunkin; Polina N Bolotskova; Elena V Bondarchuk; Valery G Gryaznov; Valeriy A Kozlov; Maria A Okuneva; Oleg V Ovchinnikov; Oleg P Smoliy; Igor F Turkanov; Catherine A Galkina; Alexandr S Dmitriev; Alexandr F Seliverstov Journal: Polymers (Basel) Date: 2022-02-11 Impact factor: 4.329