The Open Pharmacology Journal

2018, 8 : 10-20
Published online 2018 October 17. DOI: 10.2174/1874143601808010010
Publisher ID: TOPHARMJ-8-10

RESEARCH ARTICLE
New Amino-steroid-anthracenone with Biological Activity Against Ischemia-reperfusion Injury in a Wistar Rat Model

Figueroa-Valverde Lauro1, * , Rosas-Nexticapa Marcela2, * , Mateu-Armand Virginia2 , Herrera-Meza Socorro3 , Díaz-Cedillo Francisco4 , Montano-Tapia Elizabeth2 , García-Cervera Elodia1 , Pool-Gómez Eduardo1 , Hau-Heredia Lenin1 , García-Martínez Rolando1 , Lopez-Ramos Maria1 , Cauich-Carrillo Regina1 and Parra-Galindo Perla2
1 Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, University Autonomous of Campeche, Av. Agustín Melgar s/n, Col Buenavista, C.P. 24039, Campeche, México
2 Facultad de Nutrición, Universidad Veracruzana, Médicos y Odontologos s/n C.P. 91010, Unidad del Bosque, Xalapa, Veracruz, México
3 Instituto de Investigaciones Psicológicas, Universidad Veracruzana, Av. Dr. Luis Castelazo Ayala s/n Col Industrial Animas, C.P. 91190, Xalapa, Veracruz, México
4 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

* Address correspondence to these authors at the Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, University Autonomous of Campeche, Av. Agustín Melgar s/n, Col Buenavista, C.P. 24039, Campeche, México; Facultad de Nutrición, Universidad Veracruzana, Médicos y Odontologos s/n C.P. 91010, Unidad del Bosque, Xalapa, Veracruz, México; Tel: 9818119800; E-mails: , lauro_1999@yahoo.com

ABSTRACT

Objective:

The main objective of this study was to evaluate the biological activity of an ASA (Amino-Steroid-Anthracenone derivative) against heart failure caused by the ischemia- reperfusion injury (translated as infarct area).

Methods:

Biological activity exerted by ASA (0.001-100 nM) on infarct area was determined using an ischemia-reperfusion injury model. In addition, to characterize the molecular mechanism involved in the effect exerted by ASA on left ventricular pressure, some drugs such as estrone (0.001-100 nM), tamoxifen (1 nM), butoxamine (1 nM) and ZM-241385 (1 nM) were used.

Results:

The experimental data showed that ASA decreased the infarction area significantly (p = 0.05) compared to estrone. Other results indicated that ASA decreased left ventricular pressure and this effect was inhibited by ZM-241385. In addition, ASA increased cAMP levels in a time-dependent manner compared to control conditions.

Conclusion:

The results showed that ASA decreases ischemia-reperfusion injury (translated as infarct area) via A2 adenosine receptor activation and these phenomena involve changes in cAMP levels.

Keywords:

Amino-steroid-anthracenone, Ischemia, Reperfusion, cAMP, Adenosine, ZM-241385.