In this study, a new naphthalene-prazosin derivative (compound 5) was synthetized with the objective of evaluating its activity on ischemia/reperfusion injury. The Langendorff technique was used to evaluate the effect of the compound 5 on ischemia/reperfusion injury. Additionally, the mechanism of action involved in the activity exerted by the compound 5 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 the compound 5 reduced infarct size compared with the control conditions. Other results showed that the compound 5 significantly increases (p = 0.05) the perfusion pressure and coronary resistance in isolated rat heart. In addition, other data indicate that the compound 5 increases left ventricular pressure in a dose-dependent manner (0.001 to 100 nM); however, this phenomenon was significantly inhibited by nifedipine at a dose of 1 nM (p = 0.05) and this effect was independent of cAMP levels. In conclusion, these data suggest that the naphthalene-prazosin derivative exerts a cardio protective effect via the calcium channels activation and consequently induces changes in the left ventricular pressure levels. This phenomenon results in a decrease of * Corresponding author. B. Sarabia-Alcocer et al. 1131 myocardial necrosis after ischemia and reperfusion.
The aim of this study was synthesizing a steroid-oxazole-oxazete derivative (4) to evaluate their biological activity in vitro. The first stage was achieved by the preparation of a steroid-oxazole-1,2′-[1,3]oxazete] derivative using a series of reactions such as; (1) addition; (2) nitration and (3) cyclization. Then, the biological activity of steroid analog against infarct area was evaluated on an ischemia/reperfusion model using quinalizarin as a control. In addition, the interaction of steroid derivative with kinase protein (CK2) was evaluated using a docking model. The results showed a decrease infarct area (0.001 nM] in a similar form that quinalizarin. In addition, the theoretical analysis suggests that steroid derivative could interact with some aminoacid residues (Gln 86 , Lys 96 , Leu 97 , Leu 98) of 3FL5 protein surface. All these data indicate that steroid derivative can decrease the infarct area via CK2 inhibition.
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