title: Evaluation of activity of an estrogen-derivative as cardioprotector drug using an ischemia-reperfusion injury model.
abstract: Myocardial ischemia/reperfusion injury is a serious problem involved in cardiovascular diseases. There data which indicate that some steroids induce cardioprotective effects on myocardial ischemia-reperfusion injury; however their activity and the molecular mechanism involved on myocardial ischemia-reperfusion injury are very confusing. Therefore, in this study some estrogen derivatives (compound 3 to 7) were synthesized with the objective of evaluating its activity on myocardial ischemia/reperfusion injury using an isolated heart model. Additionally, molecular mechanism involved in the activity exerted by the compounds 3 to 7 on perfusion pressure and coronary resistance was evaluated by measuring left ventricular pressure in absence or presence of following compounds; prazosin, metoprolol, indomethacin and nifedipine. The results showed that 7 reduce infarct size compared with the estrone and other estrogen derivatives (compounds 3, 4, 5, and 6). Other results showed that 7 significantly increase the perfusion pressure and coronary resistance in isolated heart in comparison with estrone, 3, 4, 5, and 6. Finally, other data indicate that 7 increased the left ventricular pressure in a dose-dependent manner; however, this phenomenon was significantly inhibited by nifedipine. In conclusion, all these data suggest that 7 exert a cardioprotective effect through calcium channels activation and consequently induce changes in the left ventricular pressure levels. This phenomenon results in decrease of myocardial necrosis after ischemia and reperfusion.
authors.affiliation: Laboratory of Pharmaco-Chemistry at The Faculty of Chemical Biological Sciences From The 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 D.F. C.P. 11340, México.
authors.forename: Díaz-Cedillo
authors.initials: DC
authors.lastname: Francisco
authors.affiliation: Laboratory of Pharmaco-Chemistry at The Faculty of Chemical Biological Sciences From The 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: Facultad de Nutrición, Universidad Veracruzana, Médicos y Odontólogos s/n Xalapa Veracruz 91010, México.
authors.forename: Rosas-Nexticapa
authors.initials: RN
authors.lastname: Marcela
authors.affiliation: Laboratory of Pharmaco-Chemistry at The Faculty of Chemical Biological Sciences From The 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 at The Faculty of Chemical Biological Sciences From The University Autonomous of Campeche Av. Agustín Melgar s/n, Col Buenavista C.P. 24039 Campeche Cam., México.
authors.forename: Lopéz-Ramos
authors.initials: LR
authors.lastname: Maria
authors.affiliation: Laboratory of Pharmaco-Chemistry at The Faculty of Chemical Biological Sciences From The University Autonomous of Campeche Av. Agustín Melgar s/n, Col Buenavista C.P. 24039 Campeche Cam., México.
authors.forename: Rodriguez-Hurtado
authors.initials: RH
authors.lastname: Fernanda
authors.affiliation: Laboratory of Pharmaco-Chemistry at The Faculty of Chemical Biological Sciences From The University Autonomous of Campeche Av. Agustín Melgar s/n, Col Buenavista C.P. 24039 Campeche Cam., México.
authors.forename: Chan-Salvador
authors.initials: CS
authors.lastname: Marissa
keywords: Estrogen; ischemia/reperfusion injury left ventricular pressure; nifedipine