Meldonium is a structural analogue of a precursor of carnitine – gamma-butyrobetaine (GBB), which has one carbon atom replaced by nitrogen atom.
Meldonium inhibits the activity of butyrobetainhydroxylase, causing a decrease of carnitine biosynthesis and long-chain fatty acids transport through cell membranes. It prevents the accumulation of the metabolites of long-chain fatty acids – Acyl-CoA and Acyl-carnitine – in cells, thus diminishing their adverse effects.
Under the conditions of ischemia, meldonium activates the anaerobic glycolysis and stimulates the ATP production and transport, restores the balance between oxygen delivery and consumption.
A temporary decrease in the content of fatty acids takes place in a healthy organism’s cell upon an increased load as a result of intensive energy consumption.This activates the metabolism of fatty acids, especially the synthesis of carnitine.
It is clear that the biosynthesis of carnitine is regulated by the blood plasma concentration of carnitine and stress; Meldonium inhibits the transformation of GBB to carnitine and so decreases its concentration in blood, thus activating the synthesis of carnitine precursors, i. e. GBB.
The biosynthesis of carnitine resumes, and the concentration of fatty acids become normal in the cell as the concentration of meldonium decreases. The cells are trained regularly in this way and are stimulated to survive when the concentration of fatty acids is low under conditions of increased load and when the load decreases, the content of fatty acids is quickly restored.
Meldonium “trained” cells survive conditions of real overload, whereas “untrained” cells die under the same conditions.
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