439 results match your criteria apelin-13


Ontology of the apelinergic system in mouse pancreas during pregnancy and relationship with β-cell mass.

Sci Rep 2021 Jul 29;11(1):15475. Epub 2021 Jul 29.

Lawson Health Research Institute, St Joseph Health Care, 268 Grosvenor St, London, ON, N6A 4V2, Canada.

The apelin receptor (Aplnr) and its ligands, Apelin and Apela, contribute to metabolic control. The insulin resistance associated with pregnancy is accommodated by an expansion of pancreatic β-cell mass (BCM) and increased insulin secretion, involving the proliferation of insulin-expressing, glucose transporter 2-low (InsGlut2) progenitor cells. We examined changes in the apelinergic system during normal mouse pregnancy and in pregnancies complicated by glucose intolerance with reduced BCM. Read More

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ACE2 and Apelin-13: Biomarkers with a Prognostic Value in Congestive Heart Failure.

Dis Markers 2021 22;2021:5569410. Epub 2021 Jun 22.

Department of Internal Medicine, "Iuliu Hatieganu" University of Medicine and Pharmacy, Cluj-Napoca, Romania.

The progression of heart failure is the result of the interaction of several pathogenetic processes that involve the activation of biomarkers belonging to the renin angiotensin aldosterone system (RAAS), to its counterregulatory mechanisms, to the sympathetic nervous system and inflammation, and to oxidative stress. This study is aimed at determining the prognostic role of biomarkers in the evolution of patients with heart failure. These biomarkers are representative of different pathogenetic pathways involved in the progression of heart failure and the possible interrelationships between them and heart remodelling. Read More

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Endothelial cell-derived Apelin inhibits tumor growth by altering immune cell localization.

Sci Rep 2021 Jul 7;11(1):14047. Epub 2021 Jul 7.

Department of Signal Transduction, Research Institute for Microbial Diseases, Osaka University, 3-1 Yamada-oka, Suita, Osaka, 565-0871, Japan.

The Apelin/APJ signalling pathway, involved in multiple physiological and pathological processes, has been attracting increasing interest recently. In our previous study, Apelin overexpression in colon26 tumor cells suppressed tumor growth by inducing vascular maturation. Here, we found that MC38 and LLC tumor growth were greater in the absence of Apelin than in wild-type (WT) mice, suggesting that Apelin acts as a tumor suppressor. Read More

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Prolyl Carboxypeptidase Mediates the C-Terminal Cleavage of (Pyr)-Apelin-13 in Human Umbilical Vein and Aortic Endothelial Cells.

Int J Mol Sci 2021 Jun 22;22(13). Epub 2021 Jun 22.

Laboratory of Medical Biochemistry, Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, University of Antwerp, 2610 Wilrijk, Belgium.

The aim of this study was to investigate the C-terminal cleavage of (pyr)-apelin-13 in human endothelial cells with respect to the role and subcellular location of prolyl carboxypeptidase (PRCP). Human umbilical vein and aortic endothelial cells, pre-treated with prolyl carboxypeptidase-inhibitor compound 8o and/or angiotensin converting enzyme 2 (ACE2)-inhibitor DX600, were incubated with (pyr)-apelin-13 for different time periods. Cleavage products of (pyr)-apelin-13 in the supernatant were identified by mass spectrometry. Read More

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Impact of the apelin/APJ axis in the pathogenesis of Parkinson's disease with therapeutic potential.

J Neurosci Res 2021 Jun 11. Epub 2021 Jun 11.

Department of Biological Chemistry, Medical School, National and Kapodistrian University of Athens, Athens, Greece.

The pathogenesis of Parkinson's disease (PD) remains elusive. There is still no available disease-modifying strategy against PD, whose management is mainly symptomatic. A growing amount of preclinical evidence shows that a complex interplay between autophagy dysregulation, mitochondrial impairment, endoplasmic reticulum stress, oxidative stress, and excessive neuroinflammation underlies PD pathogenesis. Read More

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Protective effect of Apelin/APJ system on lipopolysaccharide-related cardiac dysfunction.

Gen Physiol Biophys 2021 May;40(3):161-171

Emergency Department, The Second Hospital of Hebei Medical University, Shijiazhuang, Hebei, China.

At present, the pathogenesis of sepsis-induced myocardial dysfunction (SIMD) is not completely clear and effective treatment measures are lacking. Apelin is an endogenous ligand of the angiotensin like G protein coupled receptor APJ and a cardiovascular peptide with multiple functions. Our aim is to analyze the protective effect and mechanism of Apelin/APJ system on lipopolysaccharide (LPS)-induced myocardial dysfunction. Read More

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Amidation-Modified Apelin-13 Regulates PPAR and Perilipin to Inhibit Adipogenic Differentiation and Promote Lipolysis.

Bioinorg Chem Appl 2021 7;2021:3594630. Epub 2021 May 7.

Department of Endocrinology, The First Affiliated Hospital, Changsha Medical University, Changsha, Hunan 410219, China.

With the adjustment of human diet and lifestyle changes, the prevalence of obesity is increasing year by year. Obesity is closely related to the excessive accumulation of white adipose tissue (WAT), which can synthesize and secrete a variety of adipokines. Apelin is a biologically active peptide in the adipokines family. Read More

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Apelin receptor upregulation in spontaneously hypertensive rat contributes to the enhanced vascular smooth muscle cell proliferation by activating autophagy.

Ann Transl Med 2021 Apr;9(8):627

Department of Geriatric Medicine, The First Affiliated Hospital, Nanjing Medical University, Nanjing, China.

Background: Proliferation of vascular smooth muscle cells (VSMCs) plays a vital role in the progression of vascular remodeling and hypertension. Apelin-13 promotes VSMC proliferation of normal rats. This study was designed to investigate the roles of apelin receptor (APJ) and apelin-13 in VSMC proliferation of hypertension rats and underlying mechanisms. Read More

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Apelin-13 protects human neuroblastoma SH-SY5Y cells against amyloid-beta induced neurotoxicity: Involvement of anti oxidant and anti apoptotic properties.

J Basic Clin Physiol Pharmacol 2021 May 10. Epub 2021 May 10.

Golestan Neuroscience Research Center (GNRC), Department of Anatomy, Faculty of Medicine, Golestan University of Medical Sciences, Gorgan, Iran.

Objectives: We investigated the effect of apelin-13 on the cellular model of AD, amyloid-β (Aβ) treated SH-SY5Y cells in rats.

Methods: The SH-SY5Y cells were pretreated with different doses of apelin-13 (1, 2.5, 5, and 10 μg/mL), half an hour before adding 50% Aβ treatment. Read More

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Apelin improves cardiac function mainly through peripheral vasodilation in a mouse model of dilated cardiomyopathy.

Peptides 2021 Aug 12;142:170568. Epub 2021 May 12.

Cardiovascular & Metabolism Therapeutic Area, Sanofi R&D, 1 avenue Pierre Brossolette, 91385, Chilly-Mazarin, France. Electronic address:

There is growing evidence that apelin plays a role in the regulation of the cardiovascular system by increasing myocardial contractility and acting as a vasodilator. However, it remains unclear whether apelin improves cardiac contractility in a load-dependent or independent manner in pathological conditions. For this purpose we investigated the cardiovascular effects of apelin in α-actin transgenic mice (mActin-Tg mice), a model of cardiomyopathy. Read More

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Expression and localization of apelin and its receptor in the testes of diabetic mice and its possible role in steroidogenesis.

Cytokine 2021 Aug 4;144:155554. Epub 2021 May 4.

Department of Zoology, Mizoram University, Aizawl, Mizoram 796 004, India. Electronic address:

Type 1 diabetes mellitus (T1DM) is a metabolic disorder with severe hyperglycemia, one of the complications of which is testicular dysfunctions, androgen deficiency and decreased male fertility. In the diabetic testes, the expression and signaling pathways of leptin and a number of other adipokines are significantly changed. However, there is no information on the localization and expression of adipokine, apelin and its receptor (APJ) in the diabetic testes, although there is information on the involvement of apelin in the regulation of reproductive functions. Read More

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Molecular mechanism of apelin-13 regulation of colonic motility in rats.

Eur J Pharmacol 2021 Aug 5;904:174149. Epub 2021 May 5.

Department of Gastroenterology, Renmin Hospital of Wuhan University, 430060, Wuhan, Hubei Province, China. Electronic address:

Apelin is a novel neuropeptide identified as the endogenous ligand for the apelin receptor. Apelin and its receptor are widely distributed in the gastrointestinal tract. Studies have reported that apelin-13 is involved in modulating gastrointestinal motility; however, the evidence is insufficient and the relevant mechanism is still not fully clear. Read More

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Fucoxanthin alters the apelin-13/APJ pathway in certain organs of γ-irradiated mice.

J Radiat Res 2021 Jul;62(4):600-617

Radiation Biology Department, National Centre for Radiation Research and Technology (NCRRT), Egyptian Atomic Energy Authority, Cairo, Egypt.

Apelin-13 and APJ are implicated in different key physiological processes. This work aims at exploring the radioprotective effect of fucoxanthin (FX) on γ-radiation (RAD)-induced changes in the apelin-13/APJ pathway, which causes damage in the liver, kidney, lung and spleen of mice. Mice were administered FX (10 mg kg-1 day-1, i. Read More

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Diuretic Action of Apelin-13 Mediated by Inhibiting cAMP/PKA/sPRR Pathway.

Front Physiol 2021 31;12:642274. Epub 2021 Mar 31.

Department of Internal Medicine, University of Utah and Veterans Affairs Medical Center, Salt Lake City, UT, United States.

Emerging evidence is showing that apelin plays an important role in regulating salt and water balance by counteracting the antidiuretic action of vasopressin (AVP). However, the underlying mechanism remains unknown. Here, we hypothesized that (pro) renin receptor (PRR)/soluble prorenin receptor (sPRR) might mediate the diuretic action of apelin in the distal nephron. Read More

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Apelin-13 Protects Corpus Cavernosum Against Fibrosis Induced by High-Fat Diet in an MMP-Dependent Mechanism.

J Sex Med 2021 05 15;18(5):875-888. Epub 2021 Apr 15.

Institute of Bioengineering, Ecole Polytechnique Fédérale de Lausanne, Lausanne, Switzerland.

Background: An increased fibrosis of the corpora cavernosa is a prevalent process that underlies most cases of erectile dysfunction. Apelin, an endogenous circulating peptide, has been documented as an important effector on cardiovascular homeostasis, controlling vascular function and reducing fibrosis in multiple pathological conditions. Recently, initial studies have shown that Apelin, acting through the APJ receptor, also modulates penile erection, however, the role of this system on penile structure and intracorporal collagen remodeling has not been investigated yet. Read More

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Ameliorative effect of apelin-13 against renal complications in L-NAME-induced preeclampsia in rats.

PeerJ 2021 31;9:e11110. Epub 2021 Mar 31.

Medical Physiology Department - Faculty of Human Medicine, Zagazig University, Zagazig, Egypt.

Pre-eclampsia (PE) accompanying acute liver and kidney injury has remained a master cause of both fetal and maternal mortality and morbidity. Vasoactive mediators, oxidative stress and inflammatory imbalanceshave an important role in PE pathogenesis. Apelin is an adipokine that improves endothelial dysfunction; has anti-inflammatory and antioxidant effects; moreover, its level reduced during PE. Read More

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Apelin-13 activates the hippocampal BDNF/TrkB signaling pathway and suppresses neuroinflammation in male rats with cisplatin-induced cognitive dysfunction.

Behav Brain Res 2021 Jun 15;408:113290. Epub 2021 Apr 15.

Recep Tayyip Erdogan University, Faculty of Medicine, Department of Biochemistry, Rize, Turkey. Electronic address:

It has been established that cisplatin causes neuronal damage and cognitive impairment. However, the mechanism is not sufficiently clear. Apelin-13 is an endogenous peptide with strong neuroprotective effects through the synthesis of neurotrophic factors and suppression of inflammation. Read More

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Apelin-13 prevents apoptosis in the cochlear tissue of noise-exposed rat via Sirt-1 regulation.

J Chem Neuroanat 2021 Jul 5;114:101956. Epub 2021 Apr 5.

Hearing Disorders Research Center, Loghman Hakim Hospital, Shahid Beheshti University of Medical Sciences, Tehran, Iran. Electronic address:

Noise-induced hearing loss (NIHL) is the second most common cause of acquired hearing loss. Acoustic trauma can cause oxidative damage in the cochlear hair cells (HCs) through apoptotic pathways. Apelin is a newly discovered neuropeptide with neuroprotective effects against the oxidative stress in neurodegenerative disorder. Read More

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Apelin-13 regulates electrical activity in the globus pallidus and induces postural changes in rats.

Neural Regen Res 2021 Nov;16(11):2264-2268

Department of Physiology, School of Basic Medicine, Qingdao University, Qingdao, Shandong Province, China.

The globus pallidus is the relay nucleus of the basal ganglia, and changes in its electrical activity can cause motor impairment. Apelin-13 is widely distributed in the central and peripheral nervous systems. It has been demonstrated that apelin-13 plays important roles in the regulation of blood pressure and other non-motor functions. Read More

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November 2021

The Effects of Apelin and Elabela Ligands on Apelin Receptor Distinct Signaling Profiles.

Front Pharmacol 2021 4;12:630548. Epub 2021 Mar 4.

Neurobiology Key Laboratory of Jining Medical University in Colleges of Shandong, Jining Medical University, Jining, China.

Apelin and Elabela are endogenous peptide ligands for Apelin receptor (APJ), a widely expressed G protein-coupled receptor. They constitute a spatiotemporal dual ligand system to control APJ signal transduction and function. We investigated the effects of Apelin-13, pGlu-apelin-13, Apelin-17, Apelin-36, Elabela-21 and Elabela-32 peptides on APJ signal transduction. Read More

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The G Protein Biased Small Molecule Apelin Agonist CMF-019 is Disease Modifying in Endothelial Cell Apoptosis and Induces Vasodilatation Without Desensitisation .

Front Pharmacol 2020 21;11:588669. Epub 2021 Jan 21.

Department of Medicine, Experimental Medicine and Immunotherapeutics, Addenbrooke's Hospital, University of Cambridge, Cambridge, United Kingdom.

Signaling through the apelin receptor is beneficial for a number of diseases including pulmonary arterial hypertension. The endogenous small peptides, apelin and elabela/toddler, are downregulated in pulmonary arterial hypertension but are not suitable for exogenous administration owing to a lack of bioavailability, proteolytic instability and susceptibility to renal clearance. CMF-019, a small molecule apelin agonist that displays strong bias towards G protein signaling over β-arrestin (∼400 fold), may be more suitable. Read More

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January 2021

Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.

J Med Chem 2021 03 9;64(6):3086-3099. Epub 2021 Mar 9.

Bristol Myers Squibb Company, Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.

Apelin-13 is an endogenous peptidic agonist of the apelin receptor (APJ) receptor with the potential for improving cardiac function in heart failure patients. However, the low plasma stability of apelin-13 necessitates continuous intravenous infusion for therapeutic use. There are several approaches to increase the stability of apelin-13 including attachment of pharmacokinetic enhancing groups, stabilized peptides, and Fc-fusion approaches. Read More

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In Vitro and In Vivo Evaluation of a Small-Molecule APJ (Apelin Receptor) Agonist, BMS-986224, as a Potential Treatment for Heart Failure.

Circ Heart Fail 2021 03 5;14(3):e007351. Epub 2021 Mar 5.

Bristol Myers Squibb, Drug Discovery, Princeton, NJ (P.G., P.W., J.O., H.F., T.W., M.Y., E.C., C.X., X.-Q.C., C.G., M.L., R.W., D.G.).

Background: New heart failure therapies that safely augment cardiac contractility and output are needed. Previous apelin peptide studies have highlighted the potential for APJ (apelin receptor) agonism to enhance cardiac function in heart failure. However, apelin's short half-life limits its therapeutic utility. Read More

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Evodiamine alleviates lipopolysaccharide-induced pulmonary inflammation and fibrosis by activating apelin pathway.

Phytother Res 2021 Jun 3;35(6):3406-3417. Epub 2021 Mar 3.

State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, China.

Inflammation can cause a series of inflammatory lung disease, which seriously endangers human health. Pulmonary fibrosis is a kind of inflammatory disease with end-stage lung pathological changes. It has complicated and unknown pathogenesis and is still lack of effective therapeutic drugs. Read More

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Apelin-13 attenuates spatial memory impairment by anti-oxidative, anti-apoptosis, and anti-inflammatory mechanism against ethanol neurotoxicity in the neonatal rat hippocampus.

Neuropeptides 2021 Jun 18;87:102130. Epub 2021 Feb 18.

Addiction Research Center, Shahroud University of Medical Sciences, Shahroud, Iran. Electronic address:

It has been shown that alcohol consumption by pregnant women can have detrimental effects on the developing fetus and lead to fetal alcohol spectrum disorders (FASD). Exposure to alcohol in rat pups during this period causes long-term changes in the structure of the animal's hippocampus, leading to impaired hippocampal-related brain functions such as navigation tasks and spatial memory. Apelin-13, a principal neuropeptide with inhibitory effects on neuroinflammation and brain oxidative stress production, has beneficial properties on memory impairment and neuronal injury. Read More

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Gαi-biased apelin analog protects against isoproterenol-induced myocardial dysfunction in rats.

Am J Physiol Heart Circ Physiol 2021 04 26;320(4):H1646-H1656. Epub 2021 Feb 26.

Département de Médecine, Faculté de Médecine et des Sciences de la Santé, Institut de Pharmacologie de Sherbrooke, Centre de Recherche du CHUS, Université de Sherbrooke, Sherbrooke, Québec, Canada.

Apelin receptor (APJ) activation by apelin-13 (APLN-13) engages both Gαi proteins and β-arrestins, stimulating distinct intracellular pathways and triggering physiological responses like enhanced cardiac contractility. Substituting the C-terminal phenylalanine of APLN-13 with α-methyl-l-phenylalanine [(l-α-Me)Phe] or p-benzoyl-l-phenylalanine (Bpa) generates biased analogs inducing APJ functional selectivity toward Gαi proteins. Using these original analogs, we proposed to investigate how the canonical Gαi signaling of APJ regulates the cardiac function and to assess their therapeutic impact in a rat model of isoproterenol-induced myocardial dysfunction. Read More

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[Effects of Apelin-13 on barrier injury of human umbilical vein endothelial cells induced by LPS].

Zhongguo Ying Yong Sheng Li Xue Za Zhi 2020 Sep;36(5):390-393

The Second Affiliated Hospital and Yuying Children's Hospital, Wenzhou Medical University, Wenzhou 325035.

To investigate the effects of Apelin-13 on barrier function injury of human umbilical vein endothelial cells (HUVECs) induced by LPS. The HUVECs cultured were divided into 4 groups: Control group, LPS group, Apelin-13+LPS group, Apelin-13 group. HUVECs were treated by 5 μg/ml LPS for 24 h to replicate the model with endothelial barrier impaired. Read More

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September 2020

Induced dysregulation of ACE2 by SARS-CoV-2 plays a key role in COVID-19 severity.

Biomed Pharmacother 2021 May 5;137:111363. Epub 2021 Feb 5.

Department of Biochemistry, Faculty of Biological Sciences, Tarbiat Modares University, Tehran, Iran.

Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), the cause of COVID-19, is reported to increase the rate of mortality worldwide. COVID-19 is associated with acute respiratory symptoms as well as blood coagulation in the vessels (thrombosis), heart attack and stroke. Given the requirement of angiotensin converting enzyme 2 (ACE2) receptor for SARS-CoV-2 entry into host cells, here we discuss how the downregulation of ACE2 in the COVID-19 patients and virus-induced shift in ACE2 catalytic equilibrium, change the concentrations of substrates such as angiotensin II, apelin-13, dynorphin-13, and products such as angiotensin (1-7), angiotensin (1-9), apelin-12, dynorphin-12 in the human body. Read More

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Therapeutics effects of [Pyr1] apelin-13 on rat contusion model of spinal cord injury: An experimental study.

J Chem Neuroanat 2021 Apr 7;113:101924. Epub 2021 Feb 7.

Department of Biology and Anatomical sciencese, School of Medicine, Shahid Beheshti University of Medical Sciences, Tehran, Iran; Hearing Disorders Research Center, Loghman Hakim Hospital, Shahid Beheshti University of Medical Sciences, Tehran, Iran; Laser Application in Medical Sciences Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran. Electronic address:

Spinal cord injury (SCI) can cause various symptoms, including pain, complete or incomplete loss of autonomic, sensory, motor and functions inferior to the site of the damage. Despite wondrous advances in medicine, treating spinal cord injuries remains a thorny issue yet. Recently, the control of inflammatory processes after damage to the nervous system has been noticed as a promising therapeutic target. Read More

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