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

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 EC 50 value of 0.67 μg/ml. Piperine induced calcium influx with EC 50 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.

Stochastic Ultralow-Frequency Oscillations of the Luminescence Intensity from the Surface of a Polymer Membrane Swelling in Aqueous Salt Solutions

“…We can say that the Nafion polymer membrane is similar to synthetic biological polymer membranes; see the recent review [20]. In this regard, the alkaloid piperine (C 17 H 19 NO 3 ), which stimulates the conductivity of calcium [21] and potassium [22] ions in human cell channels, is of particular interest to study. Indeed, because the Nafion membrane contains negatively charged channels that are the conductors of protons, it is very important to study the interaction of piperine with Nafion.…”

Development and optimization of Benjakul microemulsion formulations for enhancing topical anti-inflammatory effect and delivery

“…Piperine, as a major active compound in BJK, showed moderate activity on NO-production inhibition with an IC 50 value of 38.89 ± 0.79 mg/mL ( 10 ). Moreover, piperine also has been suggested to activate transient receptor potential vanilloid 1 which is related to being analgesic and counterirritant effects ( 22 ). However, when BJK was loaded into the formula at the concentration of 0.5% w/w, only piperine was detected with the maximum absorbance at 340 nm.…”

Characterization and Isolation of Piperamides from Piper nigrum Cultivated in Costa Rica

“…Several studies have reported different biological activities for retrofractamide B. For instance, some authors proposed that besides piperine, retrofractamide B can be responsible for the transient receptor potential vanilloid 1 (TRPV1) activation [47,48]. TRPV1 has become an attractive target for many pathologies, as its activation has roles in the pathogenesis of chronic inflammatory skin diseases, thermogenesis [48], diabetes, and bladder and lung function [49].…”