Apelin Peptides

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Introduction

Apelin is an adipokines secreted by fat cells, widely distributed in tissues in human body, especially in cardiovascular tissues. The precursor of aplin consists of 77 amino acids, which can be cleaved into multiple mature apelin active peptide fragments, such as Apelin-36, apelin-17, and apelin-13. Aplin and its receptor constitute the Apelin/APJ system, highly expressed in endothelial cells (ECs), vascular smooth muscle cells (VSMCs) and cardiomyocytes. Apelin/APJ system is involved in the maintenance and regulation of vascular function. Studies have shown that apelin has vasoactive effects and is able to relax or contract arteriovenous vessels. In addition, the expression of apelin and APJ in endothelial cells can also promote embryonic angiogenesis, indicating that apelin plays an essential role in vascular regulation.

Mechanism of action

Apelin is a dilator of arteries and veins. The mechanism is that apelin, produced and released by vascular endothelial cells, binds to and activates adjacent APJ receptors, and stimulates the production and release of NO by activating endothelial nitric oxide synthase (eNOS) of vascular endothelial cells, leading to vasodilation. Subsequent studies demonstrated that apelin-induced vasodilation increases intracellular cyclic guanosine monophosphate (cGMP) levels by directly activating the L-arginine/NOS/NO pathway in vascular endothelial cells, and induces relaxation of vascular smooth muscle cells and reduces vascular tone.

Application of Apelin Peptides

As the functions of aplin peptides mentioned above, apelin peptides are closely associated with cardiovascular diseases, such as hypertension, heart failure, acute coronary syndrome and arrhythmia. Apelin and its receptor APJ are widely distributed in the body, and accumulating evidence shows that they are involved in the cardiovascular system. Although the exact physiological functions and pathophysiological effects of the Apelin/APJ system have not been fully understood, its potential role in cardiovascular diseases may make itself a new target for the diagnosis and treatment of related diseases in the future.

References

1. Cheng B, Chen J, Bai B, et al. Neuroprotection of apelin and its signaling pathway.[J]. Peptides, 2012, 37(1):171-173.
2. Wang G, Anini Y, Wei W, et al. Apelin, a new enteric peptide: localization in the gastrointestinal tract, ontogeny, and stimulation of gastric cell proliferation and of cholecystokinin secretion[J]. Endocrinology, 2004, 145(3):1342-1348.