trans-Caryophyllene, a Natural Sesquiterpene, Causes Tracheal Smooth Muscle Relaxation through Blockade of Voltage-Dependent Ca2+ Channels

doi:10.3390/molecules171011965

This article is

freely available
re-usable

Molecules 2012, 17(10), 11965-11977; doi:10.3390/molecules171011965

Article

trans-Caryophyllene, a Natural Sesquiterpene, Causes Tracheal Smooth Muscle Relaxation through Blockade of Voltage-Dependent Ca²⁺ Channels

Leidiane Pinho-da-Silva^1,2,†, Paula Virgínia Mendes-Maia^1,2,†, Taylena Maria do Nascimento Garcia Teófilo¹, Roseli Barbosa¹, Vania Marilande Ceccatto¹, Andrelina Noronha Coelho-de-Souza¹, Jader Santos Cruz^3,* and José Henrique Leal-Cardoso^1,*

¹ Laboratório de Eletrofisiologia, Instituto Superior de Ciências Biomédicas, Universidade Estadual do Ceará, Av. Paranjana #1700, Fortaleza 60740-000, Ceará, Brazil ² Programa de Pos-Graduação em Fisiologia e Farmacologia, Universidade Federal de Minas Gerais, Avenida Antonio Carlos #6627, ICB-UFMG, Belo Horizonte 31270-010, Minas Gerais, Brazil ³ Departamento de Bioquímica e Imunologia, Universidade Federal de Minas Gerais, Avenida Antonio Carlos #6627, ICB-UFMG, Belo Horizonte 31270-010, Minas Gerais, Brazil ^† These authors contributed equally to this work.

* Authors to whom correspondence should be addressed.

Received: 10 July 2012; in revised form: 19 September 2012 / Accepted: 5 October 2012 / Published: 11 October 2012

(This article belongs to the Section Natural Products)

Download PDF Full-Text [690 KB, uploaded 11 October 2012 10:01 CEST]

Abstract: trans-Caryophyllene is a major component in the essential oils of various species of medicinal plants used in popular medicine in Brazil. It belongs to the chemical class of the sesquiterpenes and has been the subject of a number of studies. Here, we evaluated the effects of this compound in airway smooth muscle. The biological activities of trans-caryophyllene were examined in isolated bath organs to investigate the effect in basal tonus. Electromechanical and pharmacomechanical couplings were evaluated through the responses to K⁺ depolarization and exposure to acetylcholine (ACh), respectively. Isolated cells of rat tracheal smooth muscle were used to investigate trans-caryophyllene effects on voltage-dependent Ca²⁺ channels by using the whole-cell voltage-clamp configuration of the patch-clamp technique. trans-Caryophyllene showed more efficiency in the blockade of electromechanical excitation-contraction coupling while it has only minor inhibitory effect on pharmacomechanical coupling. Epithelium removal does not modify tracheal smooth muscle response elicited by trans-caryophyllene in the pharmacomechanical coupling. Under Ca²⁺-free conditions, pre-exposure to trans-caryophyllene did not reduce the contraction induced by ACh in isolated rat tracheal smooth muscle, regardless of the presence of intact epithelium. In the whole-cell configuration, trans-caryophyllene (3 mM), inhibited the inward Ba²⁺ current (I_Ba) to approximately 50% of control levels. Altogether, our results demonstrate that trans-caryophyllene has anti-spasmodic activity on rat tracheal smooth muscle which could be explained, at least in part, by the voltage-dependent Ca²⁺ channels blockade.

Keywords: trans-caryophyllene; rat tracheal smooth muscle; anti-spasmodic; voltage-dependent Ca²⁺ channels

Article Statistics

Click here to load and display the download statistics.

Cite This Article

MDPI and ACS Style

Pinho-da-Silva, L.; Mendes-Maia, P.V.; Teófilo, T.M.N.G.; Barbosa, R.; Ceccatto, V.M.; Coelho-de-Souza, A.N.; Santos Cruz, J.; Leal-Cardoso, J.H. trans-Caryophyllene, a Natural Sesquiterpene, Causes Tracheal Smooth Muscle Relaxation through Blockade of Voltage-Dependent Ca²⁺ Channels. Molecules 2012, 17, 11965-11977.

AMA Style

Pinho-da-Silva L, Mendes-Maia PV, Teófilo TMNG, Barbosa R, Ceccatto VM, Coelho-de-Souza AN, Santos Cruz J, Leal-Cardoso JH. trans-Caryophyllene, a Natural Sesquiterpene, Causes Tracheal Smooth Muscle Relaxation through Blockade of Voltage-Dependent Ca²⁺ Channels. Molecules. 2012; 17(10):11965-11977.

Chicago/Turabian Style

Pinho-da-Silva, Leidiane; Mendes-Maia, Paula Virgínia; Teófilo, Taylena Maria N.G.; Barbosa, Roseli; Ceccatto, Vania Marilande; Coelho-de-Souza, Andrelina Noronha; Santos Cruz, Jader; Leal-Cardoso, José Henrique. 2012. "trans-Caryophyllene, a Natural Sesquiterpene, Causes Tracheal Smooth Muscle Relaxation through Blockade of Voltage-Dependent Ca²⁺ Channels." Molecules 17, no. 10: 11965-11977.

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert