REVIEW: Apelin C-Terminal Fragments: Biological Properties and Therapeutic Potential

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Oleg I. Pisarenko^1,a* and Irina M. Studneva¹

¹Chazov National Medical Research Center of Cardiology, 121552 Moscow, Russia

^* To whom correspondence should be addressed.

Received May 30, 2023; Revised September 10, 2023; Accepted September 11, 2023

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Creation of bioactive molecules for treatment of cardiovascular diseases based on natural peptides is the focus of intensive experimental research. In the recent years, it has been established that C-terminal fragments of apelin, an endogenous ligand of the APJ receptor, reduce metabolic and functional disorders in experimental heart damage. The review presents literature data and generalized results of our own experiments on the effect of apelin-13, [Pyr]apelin-13, apelin-12, and their chemically modified analogues on the heart under normal and pathophysiological conditions in vitro and in vivo. It has been shown that the spectrum of action of apelin peptides on the damaged myocardium includes decrease in the death of cardiomyocytes from necrosis, reduction of damage to cardiomyocyte membranes, improvement in myocardial metabolic state, and decrease in formation of reactive oxygen species and lipid peroxidation products. The mechanisms of protective action of these peptides associated with activation of the APJ receptor and manifestation of antioxidant properties are discussed. The data presented in the review show promise of the molecular design of APJ receptor peptide agonists, which can serve as the basis for the development of cardioprotectors that affect the processes of free radical oxidation and metabolic adaptation.

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KEY WORDS: apelin, structural analogs, heart, experimental pathology, metabolism, cardiomyocyte membranes, lipid peroxidation, reactive oxygen species, antioxidant enzymes

DOI: 10.1134/S0006297923110160

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