Apelin is a recently discovered biologically active peptide present in several isoforms that are agonists for orphan receptor APJ. Apelin and APJ receptor were found in the central nervous system and in different peripheral tissues. In the cardiovascular system the peptide is present both in the heart and in the endothelium and smooth muscles cells of the vascular wall. Acting on cardiomyocytes apelin exerts positive inotropic effect, in the endothelium it releases nitric oxide, which mediates its vasodilatory action, while acting directly on smooth muscles cells it causes vasoconstriction. Apelin interacts with other compounds regulating blood pressure; for instance with angiotensin II, vasopressin, and with the sympathetic nervous system. Special attention is focused on the possibility of positive role of apelin in hypertension, initial stages of heart failure and ischaemic heart disease. Synthesis of apelin in adipocytes permits to include this peptide among adipokines. In the adipose tissue its production is increased in obesity and by insulin. It appears that apelin may play essential role in pathogenesis of insulin-resistant obesity. In patients with type 2 diabetes apelin improves glucose tolerance in initial stages of the illness. However, further experimental and clinical studies are required for full evaluation of significance of positive and negative aspects of the role of apelin in the cardiovascular and metabolic diseases.
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Pharmacol Res
January 2025
Department of Pharmacology-Physiology, Faculty of Medicine and Health Sciences, Université de Sherbrooke, Sherbrooke, QC, Canada; Institut de Pharmacologie de Sherbrooke, Université de Sherbrooke, Sherbrooke, QC, Canada; RECITAL International Partnership Lab, Université de Caen-Normandie, Caen, France & Université de Sherbrooke, Sherbrooke, QC, Canada. Electronic address:
β-arrestins play pivotal roles in seven transmembrane receptor (7TMR) signalling and trafficking. To study their functional role in regulating specific receptor systems, current research relies mainly on genetic tools, as few pharmacological options are available. To address this issue, we designed and synthesised a novel lipidated phosphomimetic peptide inhibitor targeting β-arrestins, called ARIP, which was developed based on the C-terminal tail (A343-S371) of the vasopressin V2 receptor.
View Article and Find Full Text PDFAnimals (Basel)
December 2024
State Key Laboratory of Animal Biotech Breeding, Institute of Animal Science, Chinese Academy of Agricultural Sciences, Beijing 100193, China.
The photoperiod has been considered to be a key environmental factor in sheep reproduction, and some studies have shown that the thyroid gland plays an important role in mammalian reproduction, but the molecular mechanism is still unclear. In this study, we used the artificial-light-controlled, ovariectomized, and estradiol-treated model (OVX + E2 model); healthy and consistent 2-3-year-old Sunite multiparous ewes were collected; and thyroids were collected for testing, combined with RNA-seq technology and bioinformatics analysis, to analyze the effects of different photoperiods (long photoperiod treatment for 42 days, LP42; short photoperiod treatment for 42 days, SP42; SP42 transferred to LP42, SPLP42) on the variations in the miRNA profiles of the thyroid gland. A total of 105 miRNAs were differentially expressed in the thyroid gland, most of which were new miRNAs.
View Article and Find Full Text PDFJ Nanobiotechnology
January 2025
School of Pharmaceutical Science, University of South China, Hengyang, 421001, China.
Spinal cord injury (SCI) is a chronic condition whereby persistent aberrant macrophage activation hinders the repair process. During acute trauma, dominant M1 macrophages produce high levels of reactive oxygen species (ROS), leading to increased apoptosis in neurons, glial cells, and oligodendrocytes. This study investigated the specific effects of a ROS-responsive hydrogel loaded with Apelin-13 (Apelin-13@ROS-hydrogel) on macrophage polarization and neuroinflammation, thereby exploring its role in boosting SCI repair.
View Article and Find Full Text PDFJ Nutr Health Aging
January 2025
Division of Endocrinology and Metabolism, Department of Internal Medicine, Asan Medical Center, University of Ulsan College of Medicine, Seoul 05505, South Korea. Electronic address:
Background: Based on the compelling experimental evidence supporting apelin's beneficial effects on muscle metabolism, our study aimed to evaluate the role of circulating apelin levels as a biomarker for muscle health in humans.
Methods: This investigation employed a cross-sectional design, encompassing 237 community-dwelling older adults aged ≥65 years who underwent comprehensive geriatric evaluations in South Korea. Sarcopenia diagnosis was based on Asian-specific criteria, and serum apelin concentrations were determined using enzyme immunoassay techniques.
J Physiol Investig
January 2025
Department of Emergency, Shijiazhuang Traditional Chinese Medicine Hospital, Shijiazhuang, China.
Sepsis is a life-threatening condition that often results in severe brain injury, primarily due to excessive inflammation and mitochondrial dysfunction. This study aims to investigate the neuroprotective effects of Apelin-13, a bioactive peptide, in a rat model of sepsis-induced brain injury (SBI). Specifically, we examined the role of Apelin-13 in regulating mitophagy through the phosphatase and tensin homolog-induced putative kinase 1 (PINK1)/Parkin pathway and its impact on nucleotide-binding oligomerization domain-like receptor pyrin domain-containing 3 (NLRP3) inflammasome-mediated pyroptosis and oxidative stress.
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