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Planta Med 2012; 78(1): 24-30
DOI: 10.1055/s-0031-1280217
Biological and Pharmacological Activity
Original Papers
© Georg Thieme Verlag KG Stuttgart · New York

Beneficial Effects of Capsiate on Ethanol-Induced Mucosal Injury in Rats Are Related to Stimulation of Calcitonin Gene-Related Peptide Release

Nian-Sheng Li1 [*] , Xiu-Ju Luo1 [*] , Zhong Dai2 , Bin Liu1 , Yi-Shuai Zhang1 , Zhi-Chun Yang1 , Jun Peng1
  • 1Department of Pharmacology, School of Pharmaceutical Sciences, Central South University, Changsha, China
  • 2Department of Pharmacology, Guangdong Medical College, Dongguan, Guangdong, China
Weitere Informationen

Publikationsverlauf

received May 17, 2011 revised July 13, 2011

accepted August 16, 2011

Publikationsdatum:
16. September 2011 (online)

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Abstract

Capsiate is a non-pungent analogue of capsaicin from CH-19 Sweet peppers. Capsaicin is reported to trigger calcitonin gene-related peptide (CGRP) release through activation of transient receptor potential vanilloid subfamily member 1 (TRPV1) and produces beneficial effects on gastric mucosa. This study aimed to investigate whether capsiate is able to produce beneficial effects on gastric mucosa and whether the protective effects of capsipate occur through a mechanism involving the activation of TRPV1 and CGRP release. A rat model of gastric mucosal injury was established by the oral administration of acidified ethanol. Gastric tissues were collected for analysis of the gastric ulcer index, cellular apoptosis, activities of caspase-3, catalase and superoxide dismutase (SOD), and levels of CGRP, TNF-α, and malondialdehyde (MDA). Our results show that the acute administration of ethanol significantly increased the gastric ulcer index concomitantly with an increase in cellular apoptosis, caspase-3 activity, and TNF-α and MDA levels, as well as a decrease in the activities of catalase and SOD. Pretreatment with 1 mg/kg capsiate attenuated ethanol-induced gastric mucosal injury and cellular apoptosis accompanied by an increase in CGRP level, catalase, and SOD activities, and a decrease in caspase-3 activity, and TNF-α and MDA levels. The effects of capsiate were inhibited by capsazepine, an antagonist of TRPV1. These results suggest that capsiate is able to produce beneficial effects on ethanol-induced gastric mucosal injury. These effects are related to the stimulation of CGRP release through the activation of TRPV1.

Key words

capsiate - calcitonin gene-relatedpeptide (CGRP) - gastric mucosa - transient receptor potential vanilloid subfamily member 1 (TRPV1)

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1 Nian-Sheng Li and Xiu-Ju Luo contributed equally to this work.

Prof. Dr. Jun Peng

Department of Pharmacology
School of Pharmaceutical Sciences
Central South University

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Changsha 410078

China

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eMail: Junpeng@csu.edu.cn