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

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
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2012, 17(10), 11965-11977; https://doi.org/10.3390/molecules171011965
Received: 10 July 2012 / Revised: 19 September 2012 / Accepted: 5 October 2012 / Published: 11 October 2012
(This article belongs to the Section Natural Products Chemistry)
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 (IBa) 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. View Full-Text
Keywords: trans-caryophyllene; rat tracheal smooth muscle; anti-spasmodic; voltage-dependent Ca2+ channels trans-caryophyllene; rat tracheal smooth muscle; anti-spasmodic; voltage-dependent Ca2+ channels
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Pinho-da-Silva, L.; Mendes-Maia, P.V.; Teófilo, T.M.D.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.

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