Pierre Gueneau de Mussy, Patricia N Sidharta, Gregoire Wuerzner, Marc P Maillard, Nicolas Guérard, Marc Iglarz, Bruno Flamion, Jasper Dingemanse, Michel Burnier
Aprocitentan is a novel, oral, dual endothelin receptor antagonist (ERA) in development in difficult-to-control hypertension. As fluid retention and edema are concerns with ERAs, we investigated whether aprocitentan causes weight gain in healthy subjects on a high sodium diet and explored potential mechanisms if occurring. This double-blind, randomized, placebo-controlled, crossover study enrolled 28 subjects. Three doses of aprocitentan (10, 25 or 50 mg/day for 9 days) were compared to placebo. Increases in body weight were observed with aprocitentan (placebo-corrected mean weight gains [90% CI]) of 0...
September 8, 2020: Clinical Pharmacology and Therapeutics
María J Guil, Celeste Soria, Mayra Seijas, Liliana G Bianciotti, Marcelo S Vatta
Endothelins regulate catecholaminergic activity in the olfactory bulb (OB) in normotensive and hypertensive animals. Administration of an endothelin ETA receptor antagonist decreases blood pressure in deoxycorticosterone acetate-salt (DOCA-salt) rats along with a reduction in tyrosine hydroxylase (TH) activity and expression. In the present work, we sought to establish the role of brain endothelin ETB receptor on blood pressure regulation and its relationship with the catecholaminergic system within the OB of DOCA-Salt rats...
September 4, 2020: European Journal of Pharmacology
Chenjia He, Jie Chen, Xiongyan Luo, Bing Yan
OBJECTIVES: We aimed to reveal evidence of endothelial dysfunction in the development of anti-melanoma differentiation-associated gene 5 (MDA5) dermatomyositis (DM). METHODS: Thirty anti-MDA5 DM patients were enrolled and compared with patients with polymyositis (PM) (n=10) and healthy controls (n=20). The concentrations of soluble intercellular adhesion molecule-1 (sICAM-1), soluble vascular cell adhesion molecule-1 (sVCAM-1), endothelin-1 (ET-1) and von Willebrand factor (vWF) as well as interferon-alpha (IFN-α) and Galcetin-9 in the peripheral blood were tested by enzyme-linked immunosorbent assay (ELISA)...
September 3, 2020: Clinical and Experimental Rheumatology
Radwa Nasser Muhammad, Nada Sallam, Hanan Salah El-Abhar
5-Fluorouracil (5-FU) is used in the treatment of different solid tumors; however, its use is associated with rare, but serious cardiotoxicity. Nevertheless, the involvement of ROCK/NF-κB, Akt/eNOS and ET-1/ERK1/2 trajectories in the cardiotoxic effect and in the potential cardioprotective upshot of simvastatin has been elusive. Male Wistar rats were allocated into 5-FU (50 mg/kg/week; i.p, 6 weeks), simvastatin (15 mg/kg/day; p.o, 8 weeks) treated groups and simvastatin + 5-FU, besides the normal control group...
September 7, 2020: Scientific Reports
Xinfeng Zhao, Yahui Jin, Xinyi Yuan, Zhaoling Hou, Ziyue Chen, Xiaoying Fu, Qian Li, Jing Wang, Yajun Zhang
Protein immobilization is particularly significant in proteomics, interactomics, and in vitro drug screening. It is an essential primary step for numerous biological techniques that relies on immobilized proteins with controlled orientation, high conformational stability, and high activity (CHH). These have challenged the current immobilization strategy and demanded increasing efforts for an efficient method to meet the CHH immobilization in a single step. Herein, we proposed a covalent inhibitor-based, one-step method for GPCR immobilization inspired by the covalent reaction between a EGFR-tag and its inhibitor ibrutinib...
September 7, 2020: Analytical Chemistry
Ruijun Li, Yalin Zhou, Wei Liu, Yong Li, Yong Qin, Lanlan Yu, Yuhan Chen, Yajun Xu
Rare earth elements, which are extensively used in environmental protection, medicine, food, aerospace and other fields, have attracted widespread attention in recent years. However, the effect on atherosclerosis and its biological mechanism remains unclear. To elucidate these problems, here we performed a study that Apolipoprotein E-deficient mice were fed with high-fat diet to promote the development of atherosclerosis, meanwhile, mice were received 0.1, 0.2, 1.0, 2.0 mg/kg lanthanum nitrate (La(NO3 )3 ) for 12 weeks...
September 3, 2020: Ecotoxicology and Environmental Safety
Bozhong Wang, Rongfang Zhou, Yan Wang, Xinwen Liu, Xiaoling Shou, Yi Yang, Cuicui Yang, Qian Tong, Genxiang Mao, Qing Wu
BACKGROUND: Exercise training is beneficial for cardiac rehabilitation. Nevertheless, few study focused on the role of high-intensity interval training (HIIT) in cardiac repair. The current study aimed to elucidate the effect of HIIT on cardiac rehabilitation and the involved mechanisms after acute myocardial infarction (MI). METHODS: A total of 65 male rats underwent coronary ligation or sham operation and were randomly assigned to 4 groups: sham (n = 10), sedentary (MI-Sed, n = 12), moderate-intensity continuous training (MI-MCT, n = 12) and HIIT (MI-HIIT, n = 12)...
September 2, 2020: Biomedicine & Pharmacotherapy
Yingying Ke, Mengmeng Wang, Yage Li, Zengfu Shan, Wangyang Mi, Peipei Yuan, Weisheng Feng, Xiaoke Zheng
PURPOSE: To investigate the protective effect of Oligosaccharides composition of Descurainiae sophia on doxorubicin-induced heart failure in rats, and to study its mechanism. METHOD: A rat model of heart failure was established in 180-220 g male Sprague-Dawley rats by low-dose intraperitoneal injection of doxorubicin for 6 weeks. Four weeks after continuous administration, echocardiography was used to detect left ventricular end diastolic diameter (LVEDD) and end systolic diameter (LVESD) in each group, and left ventricular short axis shortening rate (LVFS) and ejection fraction (LVEF) were calculated...
September 2020: Biomedicine & Pharmacotherapy
Yen-Lin Chen, Robert H Rosa, Lih Kuo, Travis W Hein
Purpose: Endothelin-1 (ET-1) is a potent vasoactive factor implicated in development of diabetic retinopathy, which is commonly associated with retinal edema and hyperglycemia. Although the vasomotor activity of venules contributes to the regulation of tissue fluid homeostasis, responses of human retinal venules to ET-1 under euglycemia and hyperglycemia remain unknown and the ET-1 receptor subtype corresponding to vasomotor function has not been determined. Herein, we addressed these issues by examining the reactivity of isolated human retinal venules to ET-1, and results from porcine retinal venules were compared...
August 2020: Translational Vision Science & Technology
Haitao Feng, Le Thanh Nam, Takuma Yoshikawa, Akihiro Kishimura, Takeshi Mori, Yoshiki Katayama
Enhancing blood flow to tumors is a prominent strategy for improving the tumor accumulation of macromolecular drugs through the enhanced permeability and retention (EPR) effect. IRL-1620 is an agonist of the endothelin B receptor, and is a promising molecule to enhance tumor blood flow by activating endothelial nitric oxide synthase. However, contradictory effects on tumor blood flow modulation have been reported because the effects of IRL-1620 may differ in different animal models. Here, we examined for the first time the effect of IRL-1620 on the EPR effect for PEGylated liposomes in a CT-26 murine colon cancer model...
2020: Biological & Pharmaceutical Bulletin
Markus Johansson, Benjamin Ulfenborg, Christian X Andersson, Sepideh Heydarkhan-Hagvall, Anders Jeppsson, Peter Sartipy, Jane Synnergren
Cardiac hypertrophy is an important and independent risk factor for the development of heart failure. To better understand the mechanisms and regulatory pathways involved in cardiac hypertrophy, there is a need for improved in vitro models. In this study, we investigated how hypertrophic stimulation affected human induced pluripotent stem cell (iPSC)-derived cardiomyocytes (CMs). The cells were stimulated with endothelin-1 (ET-1) for 8, 24, 48, 72, or 96h. Parameters including cell size, ANP-, proBNP-, and lactate concentration were analyzed...
September 2, 2020: Biology Open
Dong-Hyuk Lee, Seung-Yeon Cho, Seung-Bo Yang, Hyoung-Min Lee, Hee Sup Shin, Seung Hwan Lee, Jun Seok Koh, Seungwon Kwon, Woo-Sang Jung, Sang-Kwan Moon, Jung-Mi Park, Chang-Nam Ko, Ho Kim, Seong-Uk Park
Objectives: To investigate the efficacy of acupuncture in preventing cerebral vasospasm following aneurysmal subarachnoid hemorrhage (SAH) and explore its underlying mechanism. Design: A randomized, double-blinded, and placebo-controlled trial. Setting/Location: Subjects were recruited from Kyung Hee University Hospital at Gangdong, Seoul, Korea Subjects: A total of 50 patients admitted with acute SAH. Interventions: The study group received acupuncture treatments ( n  = 25), while the control group underwent mock transcutaneous electrical nerve stimulation and sham acupuncture ( n  = 25) six times/week for 2 weeks...
September 1, 2020: Journal of Alternative and Complementary Medicine: Research on Paradigm, Practice, and Policy
L C M Coelho, J V Cruz, I K Maba, Aleksander Roberto Zampronio
Sex differences in the immune response can also affect the febrile response, particularly the fever induced by lipopolysaccharide (LPS). However, other pathogen-associated molecular patterns, such as zymosan A (Zym) and polyinosinic-polycytidylic acid (Poly I:C), also induce fever in male rats with a different time course of cytokine release and different mediators such as endothelin-1 (ET-1). This study investigated whether female sex hormones affect Zym- and Poly I:C-induced fever and the involvement of ET-1 in this response...
September 1, 2020: Inflammation
Amanda Almeida de Oliveira, Kenia Pedrosa Nunes
A diagnostic of hypertension increases the risk of erectile dysfunction (ED); likewise, ED can be an early sign of hypertension. In both cases, there is evidence that endothelial dysfunction is a common link between the two conditions. During hypertension, the sustained and widespread release of pro-contractile factors (e.g., angiotensin II, endothelin 1, aldosterone) impairs the balance between vasoconstrictors and vasodilators and, in turn, detrimentally impacts vascular and erectile structures. This pro-hypertensive state associates with an enhancement in the generation of reactive oxygen species, which is not compensated by internal antioxidant mechanisms...
September 1, 2020: American Journal of Hypertension
Xiao-Yao Li, Shuang Zhao, Xiao-Han Fan, Ke-Ping Chen, Wei Hua, Zhi-Min Liu, Xiao-Di Xue, Bin Zhou, Shu Zhang
Objective: To investigate whether plasma big endothelin-1 (ET-1) predicts ventricular arrythmias (VAs) and end-stage events in primary prevention implantable cardioverter-defibrillator (ICD) indication patigents. Methods: In total, 207 patients fulfilling the inclusion criteria from Fuwai Hospital between January 2013 and December 2015 were retrospectively analyzed. The cohort was divided into three groups according to baseline plasma big ET-1 tertiles: tertile 1 (< 0...
July 28, 2020: Journal of Geriatric Cardiology: JGC
Stacy A Mandras, Hirsch S Mehta, Anjali Vaidya
Pulmonary hypertension (PH) is classified into 5 clinical subgroups: pulmonary arterial hypertension (PAH), PH due to left-sided heart disease, PH due to chronic lung disease, chronic thromboembolic PH (CTEPH), and PH with an unclear and/or multifactorial mechanisms. A range of underlying conditions can lead to these disorders. Overall, PH affects approximately 1% of the global population, and over half of patients with heart failure may be affected. Cardiologists are therefore likely to encounter PH in their practice...
September 2020: Mayo Clinic Proceedings
Anna Sellmer, Vibeke E Hjortdal, Jesper V Bjerre, Michael R Schmidt, Bodil H Bech, Tine B Henriksen
BACKGROUND: The evaluation of the patent ductus arteriosus (PDA) in the very premature neonate is a challenge. Echocardiography provides an interpretation of the hemodynamic condition. It is however, only a snapshot. Biomarkers may represent a physiological response to the hemodynamic alterations brought on by the PDA and may add to the identification of the clinical significant PDA. AIM: To investigate the association between mid regional proadrenomodulin (MR-proADM), N-terminal pro b-type natriuretic peptide (NT-proBNP), mid regional pro-atrial natriuretic peptide (MR-proANP), C-terminal pro endothelin-1 (CT-proET1) and copeptin and echocardiographic measures of PDA...
August 1, 2020: Early Human Development
Piera Tocci, Roberta Cianfrocca, Rosanna Sestito, Laura Rosanò, Valeriana Di Castro, Giovanni Blandino, Anna Bagnato
The majority of ovarian cancer (OC) patients recur with a platinum-resistant disease. OC cells activate adaptive resistance mechanisms that are only partially described. Here we show that OC cells can adapt to chemotherapy through a positive-feedback loop that favors chemoresistance. In platinum-resistant OC cells we document that the endothelin-1 (ET-1)/endothelin A receptor axis intercepts the YAP pathway. This cross-talk occurs through the LATS/RhoA/actin-dependent pathway and contributes to prevent the chemotherapy-induced apoptosis...
August 26, 2020: Cancer Letters
Yu-Hsuan Chen, Hsiao-Ling Chen, Hueng-Chuen Fan, Yu-Tang Tung, Chia-Wen Kuo, Min-Yu Tu, Chuan-Mu Chen
The increased prevalence of renal dysfunction and chronic kidney disease (CKD) and the high costs and poor outcomes of treatment are a significant health issue. The consequence of chronic high blood pressure is the increased prevalence of target organ end-stage renal disease, which has been proven to be a strong independent risk factor for adverse cardiovascular disease. A previous study showed that kefir products have anti-inflammatory and anti-hypertensive activities and immunological modulation functions...
August 26, 2020: Antioxidants (Basel, Switzerland)
Manting Au, Zhongyu Liu, Limin Rong, Yongping Zheng, Chunyi Wen
OBJECTIVES: This study aimed to investigate the role of endothelin-1 (ET-1), originally known as the potent vasoconstrictor, and its receptors in chondrocyte senescence and osteoarthritis (OA) development. METHOD: Temporal changes of ET-1 and its receptors with OA development were characterized in a posttraumatic OA (PTOA) mouse model at time zero, 1-month and 4-month after surgical induction via destabilization of medial meniscus (DMM). A transgenic ET-1 overexpression (TET-1) mouse model was deployed to assess the impact of upregulated ET-1 on chondrocyte senescence and cartilage degradation...
August 25, 2020: Osteoarthritis and Cartilage
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