Piperine of Piper retrofractum Antagonizes H1 Receptor: In vitro and In silico Study on Isolated-Guinea Pig Illeum Smooth Muscle

[ABSTRACT]Piperine is a major Alkaloid that found in Piper retrofractum. Empirically, This herbs used as an antispasmodic. In the previous study. Piperin was reported may inhibit the release of histamine from mast cells by inhibiting the signal pathway mediated by IgE. Based on the fact, piperin was expected to has the antagonizm effect on the histamine receptor. The aim of this study was to investigate its activity on H1 receptor. This research was conducted by investigated the effect of piperin on the guinea pig ileum smooth muscle (in vitro model). Piperin was administered at the doses of 1 mM and 5 mM. The result showed that piperin could inhibit the contraction of isolated guinea pig ileum smooth muscle that induced by histamine. The pD2 values of H1 receptor shifted significantly at the dose of 5 mM (p < 0.05). According to the contraction response data, piperin showed non-competitive antagonists activity. Its can observed from the shape of the contraction response curve that was not reach 100% Emax. Reversibility assay showed that by replaced buffer tyrode every 5 minutes for 30 minutes , the bond of alkaloid to the receptor was able to dissociate. In the in silico study (Autodock), piperine was observed can be bind to H1 receptors (docking score :-5.70). Piperine bound at Lys179 which is one of the important proteins in the histaminergic activity. The conclusion of this research is piperin has the activity as a non-competitive antagonist at the H1 receptor.

https://opac.ll.chiba-u.jp/da/curator/107843/

https://opac.ll.chiba-u.jp/da/curator/107843/ceresIntlSympo-24-P230.pdf

Chiba University. Center for Environmental Remote Sensing

千葉大学環境リモートセンシング研究センター

会議発表用資料

Proceedings of the CEReS international symposium = CEReS国際シンポジウム資料集

24

230

240

2016-11-21

publisher

環境リモートセンシング研究センター「CEReSシンポジウム資料集」