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PHARMACOLOGICAL PROTECTION OF THE ISCHEMIC MYOCARDIUM BY DERIVATIVES OF 3-(2,2,2-TRIMETHYLHYDRAZINIUM) PROPIONATE AND EVALUATION OF THEIR ANTIOXIDANT ACTIVITY

The paper presents results of a study of antioxidant (in vitro) and anti-ischemic effect of a number derivatives of 3-(2,2,2-trimethylhydrazinium) propionate. It was revealed that among other compounds 5-hydroxynicotinate of 3-(2,2,2-trimethylhydrazinium) propionate had the most pronounced antioxidant activity. The effect of 3-(2,2,2-trimethylhydrazinium) propionate and its derivatives on the necrotized area of the myocardium of the left ventricle in the course of simulation of myocardial infarction with coronary occlusion in rabbits showed that pharmacological preconditioning by 3-(2,2,2-trimethylhydrazinium) propionate and its derivatives could be considered as prevention of a syndrome of ischemia/reperfusion injury in case of myocardial infarction. Thus it was demonstrated that both 3-(2,2,2-trimethylhydrazinium) propionate (40 mg/kg) and its derivatives, namely nicotinate (84.1 mg/kg), 5-bromonicotinate (105.5 mg/kg), 5-hydroxynicotinate (88.5 mg/kg) and glycine (71.0 mg/kg) had anti-ischemic activity expressed in effective decrease of the area of necrotized infarction and reduction of the level of Tn I in the blood plasma as compared to the reference substance, i.e. Mildronate®.

Иллюстрации

Figure 1. Calibration plot of dependence between the output signal and the ascorbic acid concentration.

Figure 2. The signals recorded during four successive administrations of the solution of 5-hydroxynicotinate of 3-(2,2,2-trimethylhydrazinium) propionate (199 mg / kg) with the aid of a device “Color Jauza-01-AA”.

Table 1. The effect of Mildronate® (40 mg/kg) and its derivatives administered intravenously on the necrosis zone size and the level of Troponin I in case of acute coronary occlusion (60 min) with further reperfusion (90 min) in anesthetized rabbits (M±m; in % of the mass of the left ventricle; n=6)

DOI: 10.18413/2500-235X-2015-1-4-25-31
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