title: Evaluation of activity inotropic of a new steroid derivative using an isolated rat heart model.
abstract: There are studies which indicate that some steroid derivatives have inotropic activity; nevertheless, the cellular site and mechanism of action at cardiovascular level is very confusing. In order, to clarify these phenomena in this study, a new estradiol derivative was synthesized with the objective of to evaluate its biological activity on left ventricular pressure and characterize their molecular mechanism. The Langendorff technique was used to measure changes on perfusion pressure and coronary resistance in an isolated rat heart model in absence or presence of the estradiol derivative. Additionally, to characterize the molecular mechanism involved in the inotropic activity induced by the OTBDS-estradiol-hexanoic acid derivative was evaluated by measuring left ventricular pressure in absence or presence of following compounds; tamoxifen, prazosin, metoprolol, indomethacin and nifedipine. The results showed that the OTBDS-estradiol-hexanoic acid derivative significantly increased the perfusion pressure and coronary resistance in comparison with the control conditions. Additionally, other data indicate that OTBDS-estradiol-hexanoic acid derivative increase left ventricular pressure in a dose-dependent manner (0.001 to 100 nM); nevertheless, this phenomenon was significantly inhibited only by nifedipine at a dose of 1 nM. These data suggest that positive inotropic activity induced by the OTBDS-estradiol-hexanoic acid derivative is via activation of L-type calcium channel. This phenomenon is a particularly interesting because the positive inotropic activity induced by this steroid derivative involves a molecular mechanism different in comparison with other positive inotropic drugs.
authors.affiliation: Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, University Autonomous of Campeche Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., México.
authors.forename: Figueroa-Valverde
authors.initials: FV
authors.lastname: Lauro
authors.affiliation: Escuela Nacional de Ciencias Biológicas del Instituto Politécnico Nacional. Prol. Carpio y Plan de Ayala s/n Col. Santo Tomas México, D.F. C.P. 11340.
authors.forename: Díaz-Cedillo
authors.initials: DC
authors.lastname: Francisco
authors.affiliation: Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, University Autonomous of Campeche Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., México.
authors.forename: García-Cervera
authors.initials: GC
authors.lastname: Elodia
authors.affiliation: Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, University Autonomous of Campeche Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., México.
authors.forename: Pool-Gómez
authors.initials: PG
authors.lastname: Eduardo
authors.affiliation: Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, University Autonomous of Campeche Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., México.
authors.forename: López-Ramos
authors.initials: LR
authors.lastname: Maria
authors.affiliation: Facultad de Nutrición, Universidad Veracruzana Médicos y Odontologos s/n C.P. 91010, Unidad del Bosque Xalapa Veracruz, México.
authors.forename: Rosas-Nexticapa
authors.initials: RN
authors.lastname: Marcela
authors.affiliation: Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, University Autonomous of Campeche Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., México.
authors.forename: Hau-Heredia
authors.initials: HH
authors.lastname: Lenin
authors.affiliation: Faculty of Medicine, University Autonomous of Campeche Av. Patricio Trueba de Regil s/n, Col Lindavista C.P.24090 Campeche Cam., México.
authors.forename: Sarabia-Alcocer
authors.initials: SA
authors.lastname: Bety
authors.affiliation: Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, University Autonomous of Campeche Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., México.
authors.forename: Campos-Ramos
authors.initials: CR
authors.lastname: Landy
keywords: Steroid derivative; indomethacin; inotropic activity; nifedipine