Myocardium is a tissue with strong energy dependence, because it is sensitive to oxygen deficiency and responds to its lack of restructuring of biochemical processes.

Thiotriazolin represents a group of metabolic drugs. It shows antioxidant, antiischemic, membrane stabilizing, antiarrhythmic, immunomodulatory, anti-inflammatory, cardioprotective, hepatoprotective, and neuroprotective and nephroprotive activity. Given the wide range of pharmacological activity thiotriazoline aim of our study was to assess the features of its effects on energy metabolism in the myocardium under conditions of acute immunocomplex process.

Studies were conducted on 40 guinea pigs, mature males weighing 380-400 g. Model of acute serum sickness (ASS) was caused by single intravenous injection of bovine serum albumin (BSA) at a dose of 500 mg/kg animal. Thiotriazolin administered at a single dose of 50 mg/kg (0,2 ml of 2,5% solution for animals weighing 100 g) for 10 days. The first thiotriazolin injection was administered simultaneously with BSA. Taking of the material (blood) was performed on the 11th day after administration of BSA. The intensity of energy processes was assessed by concentration of lactic acid (lactate), pyruvic acid (pyruvate) and lactate dehydrogenase isoenzyme.

In the experimental group, compared with the intact group of animals, the concentration of lactate increased by 14% (p<0,05), pyruvate by 70% (p<0,001), and the activity LDH1 increased by 56% (p<0,001). These changes are explained by the fact that lactate dehydrogenase is an enzyme that functions in bifurcation paths aerobic and anaerobic glycolysis. It is a marker of damage of the plasma membrane of cardiomyocytes integrity. If oxygen deficiency occurs, LDH1 properties do not change, it continues to shift the reaction toward the production of pyruvate, while high concentrations of pyruvate inhibit isoenzyme LDH1. Therefore, the concentration of pyruvate increased by 1,7 times, and lactate only 1,1 times. In cardiomyocyte hypoxia, which is characteristic of this pathological process, metabolism of pyruvate disturbs. Cell membranes are impermeable to pyruvate and its concentration in the cell increases. Pyruvic acid to cells is a toxic substance. Neutralization is achieved by conversion of pyruvate to lactate, acetyl-CoA, oxaloacetate. Lactate, which is synthesized in excess, not only accumulates in the cell and enhances intracellular acidosis, but released from it, is a sign of myocardial ischemia.

In the group of animals which were injected with thiotriasolin compared to the experimental group, the amount of lactate, pyruvate and lactate dehydrogenase decreased. However, the concentration of pyruvate in animals treated with thiotriasolin is significantly higher compared to control animals. These changes are associated with the properties of thiotriazoline. The basis of efficacy is its ability to enhance the compensatory response of anaerobic glycolysis, increase of intracellular ATP was fund to stabilize the metabolism of cells. Thiotriazolin regulates the disposal of glucose and glycogen in the cell, increasing the level of pyruvate. At the same time it reduces lactate hyperproduction manifestations uncompensated acidosis and its prooxidant action.

Conclusions: In the myocardium in experimental immunocomplex process is disrupted energy metabolism. In developing cardiac ischemia markers are: an increase in the concentration of lactate dehydrogenase and pyruvate, myocardial lactate production and anaerobic glycolysis. Influence of thiotriazoline enhanced compensatory activation of anaerobic glycolysis, decreased inhibition of oxidation in the Krebs cycle and remains intracellular ATP reserve.

Ключові слова: immune complexes, myocardium, energy metabolism, thiotriazoline

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