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Synthesis and Biological Activity of a Bis-steroid-Methanocyclobutanaphthalene- dione Derivative against Ischemia/Reperfusion Injury via Calcium Channel Activation

Author(s):

Figueroa-Valverde Lauro*, Diaz-Cedillo Francisco, Rosas-Nexticapa Marcela, Mateu-Armand Virginia, Garcimarero-Espino E. Alejandra, Lopez-Ramos Maria, Hau-Heredia Lenin, Borges-Ballote Yaritza and Cabrera-Tuz Jhair   Pages 1 - 20 ( 20 )

Abstract:


Background: There is some experimental data on the effect exerted by some steroid derivatives against ischemia/reperfusion injury; however, the molecular mechanism is very confusing, perhaps this phenomenon could be due to the protocols used and/or to differences in the chemical structure of each one of the steroid derivatives.

Objective: The aim of this study was synthesizing a new bis-steroid-methanocyclobuta-naphthalene-dione derivative using some tools chemical.

Methodology: The biological activity exerted by the bis-steroid-methanocyclobuta-naphthalene-dione derivative against ischemia/reperfusion injury was evaluated in an isolated heart model using noradrenaline, milrinone, dobutamine, levosimedan, and Bay-K-8644 as controls. In addition, other alternative experiments were carried out to evaluate the biological activity induced by the bis-steroid-methanocyclobuta-naphthalene-dione derivative against left ventricular pressure in the absence or presence of nifedipine.

Results: The results showed that 1) the bis-steroid-methanocyclobuta-naphthalene-dione derivative significantly decrease the ischemia-reperfusion injury translated as decrease the infarct area in a similar manner that levosimedan drug; 2) both bis-steroid-methanocyclobuta-naphthalene-dione and Bay-K-8644 increase the left ventricular pressure and 3) the biological activity exerted by bis-steroid-methanocyclobuta-naphthalene-dione derivative against left ventricular pressure was inhibited by nifedipine.

Conclusion: The bis-steroid-methanocyclobuta-naphthalene-dione derivative decreases the area of infarction and increase left ventricle pressure via calcium channels activation; this phenomenon could constitute a new therapy for ischemia/reperfusion injury.

Keywords:

steroid, ischemia, reperfusion, infarct, pressure, bis-steroid-methanocyclobuta-naphthalene-dione

Affiliation:

Laboratory of Pharmaco-Chemistry at the Faculty of Chemical Biological Sciences of the University Autonomous of Campeche, Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., Escuela Nacional de Ciencias Biológicas del Instituto Politécnico Nacional. Prol. Carpio y Plan de Ayala s/n Col. Santo Tomas, Facultad de Nutrición, Universidad Veracruzana. Médicos y Odontólogos s/n, 91010, Xalapa, Veracruz, Facultad de Nutrición, Universidad Veracruzana. Médicos y Odontólogos s/n, 91010, Xalapa, Veracruz, Facultad de Medicina, Universidad Veracruzana. Médicos y Odontólogos s/n, 91010, Xalapa, Veracruz, Laboratory of Pharmaco-Chemistry at the Faculty of Chemical Biological Sciences of the University Autonomous of Campeche, Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., Laboratory of Pharmaco-Chemistry at the Faculty of Chemical Biological Sciences of the University Autonomous of Campeche, Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., Laboratory of Pharmaco-Chemistry at the Faculty of Chemical Biological Sciences of the University Autonomous of Campeche, Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., Laboratory of Pharmaco-Chemistry at the Faculty of Chemical Biological Sciences of the University Autonomous of Campeche, Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam.



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