In-vitro characterization of the pharmacological effects induced by (–)-α-bisabolol in rat smooth muscle preparations

Author:

de Siqueira Rodrigo J.B.1,Freire Walter B.S.1,Vasconcelos-Silva Alfredo A.1,Fonseca-Magalhães Patrícia A.2,Lima Francisco J.B.1,Brito Teresinha S.1,Mourão Lívia T.C.1,Ribeiro Ronaldo A.1,Lahlou Saad3,Magalhães Pedro J.C.124

Affiliation:

1. Departamento de Fisiologia e Farmacologia, Faculdade de Medicina, Universidade Federal do Ceará, Fortaleza, CE, Brazil.

2. Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Odontologia e Enfermagem, Universidade Federal do Ceará, Fortaleza, CE, Brazil.

3. Instituto Superior de Ciências Biomédicas, Universidade Estadual do Ceará, Fortaleza, CE, Brazil.

4. Rua Cel Nunes de Melo 1127, Rodolfo Teófilo, Fortaleza, CE, CEP 60430-270 Brasil.

Abstract

The present study deals with the pharmacological effects of the sesquiterpene alcohol (–)-α-bisabolol on various smooth-muscle preparations from rats. Under resting tonus, (–)-α-bisabolol (30–300 µmol/L) relaxed duodenal strips, whereas it showed biphasic effects in other preparations, contracting endothelium-intact aortic rings and urinary bladder strips, and relaxing these tissues at higher concentrations (600–1000 µmol/L). In preparations precontracted either electromechanically (by 60 mmol/L K+) or pharmacomechanically (by phenylephrine or carbachol), (–)-α-bisabolol showed only relaxing properties. The pharmacological potency of (–)-α-bisabolol was variable, being higher in mesenteric vessels, whereas it exerted relaxing activity with a lesser potency on tracheal or colonic tissues. In tissues possessing spontaneous activity, (–)-α-bisabolol completely decreased spontaneous contractions in duodenum, whereas it increased their amplitude in urinary bladder tissue. Administered in vivo, (–)-α-bisabolol attenuated the increased responses of carbachol in tracheal rings of ovalbumin-sensitized rats challenged with ovalbumin, but was without effect in the decreased responsiveness of urinary bladder strips in mice treated with ifosfamide. In summary, (–)-α-bisabolol is biologically active in smooth muscle. In some tissues, (–)-α-bisabolol preferentially relaxed contractions induced electromechanically, especially in tracheal smooth muscle. The findings from tracheal rings reveal that (–)-α-bisabolol may be an inhibitor of voltage-dependent Ca2+ channels.

Publisher

Canadian Science Publishing

Subject

Physiology (medical),Pharmacology,General Medicine,Physiology

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