Comprehensive review on neprilysin (NEP) inhibitors: design, structure-activity relationships, and clinical applications DOI Creative Commons
Xinyue Zhang, Chao Hu, Erkang Tian

et al.

Frontiers in Pharmacology, Journal Year: 2024, Volume and Issue: 15

Published: Dec. 23, 2024

Neprilysin (NEP), a zinc-dependent membrane-bound metallopeptidase, regulates various bioactive peptides, particularly in kidneys, vascular endothelium, and the central nervous system. NEP’s involvement metabolizing natriuretic insulin, enkephalins makes it promising target for treating cardiovascular Alzheimer’s diseases. Several NEP inhibitors, such as sacubitril omapatrilat, have been approved clinical use, which inhibit activity to prolong bioactivity of beneficial thereby exerting therapeutic effects. However, despite broad application prospects they still specific adverse reactions side effects, hypotension, renal impairment, potentially increased risk disease. This manuscript comprehensively reviews progress on single-target dual-target inhibitors. Dual-target inhibitors often combine with other targets, angiotensin receptors, enhance effects reduce reactions. The article also emphasizes these inhibitors' design strategies, structure-activity relationships (SAR), safety, performance.

Language: Английский

A composite patch loaded with 2-Deoxy Glucose facilitates cardiac recovery after myocardial infarction via attenuating local inflammatory response DOI Creative Commons
Weizhang Xiao, Zhen Zhu, Zhiming Yu

et al.

Scientific Reports, Journal Year: 2024, Volume and Issue: 14(1)

Published: Sept. 2, 2024

Local inflammatory microenvironment in the early stage of myocardial infarction (MI) severely impaired cardiac recovery post-MI. Macrophages play a pivotal role this process. A classical glycolytic inhibitor, 2-Deoxy-Glucose (2-DG), has been found to regulate excessive pro-inflammatory macrophage polarization infarcted myocardium. This study investigated effect 2-DG-loaded chitosan/gelatin composite patch on infarct post-MI and its impact repair. The results showed that 2-DG significantly inhibited expression cytokines, alleviated reactive oxygen species (ROS) accumulation, repressed proinflammatory macrophages, attenuated local ischemic hearts, as well improved function, reduced scar size, promoted angiogenesis In terms mechanism, exerts anti-inflammatory effects through inhibiting NF-κB signaling pathway reducing assembly activation NLRP3 inflammasome. These findings suggest may represent promising therapeutic strategy for repair after MI.

Language: Английский

Citations

4

Angiotensin 1–7 Attenuates the Development of Ischemia–Reperfusion‐Induced Arrhythmia in Rats: Electrophysiology, Molecular, and Immunohistochemical Study DOI Open Access
Amy F. Boushra, Ghada Farouk Soliman, Walaa Ibrahim

et al.

Microscopy Research and Technique, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 27, 2025

ABSTRACT Arrhythmia is a common and serious global health problem, contributing to cardiovascular morbidity mortality. The cardiac muscle susceptible ischemia–reperfusion (I/R) injury, which can lead fatal arrhythmias during open‐heart surgery. We investigated the potential prophylactic effect of angiotensin 1–7 (Ang 1–7) using an in vivo rat model I/R injury examined underlying mechanisms. Rats were treated with Ang (1 mg/kg, IP) 30 min before surgical procedures. Twenty‐four rats equally divided into four groups: sham control, sham‐treated 1–7, group, group 1–7. In was induced by clamping left coronary artery for min, followed 1 hour reperfusion. showed abnormal electrophysiological changes arrhythmic episodes electrocardiography (ECG) recording, increased oxidative stress, downregulation peroxisome proliferator‐activated receptor gamma (PPAR‐γ), upregulation C‐X‐C motif chemokine ligand 16 (CXCL16) expression tissue, NF‐kB IL‐17 levels. Moreover, caused significant histological disruption cyclooxygenase 2 (COX‐2) heat shock protein 90 (HSP90) immunoreactions, correlating extent damage. However, preoperative administration significantly improved electrophysiological, biochemical, histopathological injury. This study demonstrated that exerted protective anti‐arrhythmic, anti‐inflammatory, pro‐healing effects upregulating PPAR‐γ downregulating CXCL16, IL‐17, pathways, suggesting it promising cardioprotective agent preventing

Language: Английский

Citations

0

Alamandin and especially melatonin attenuate pulmonary arterial hypertension induced by monocrotalin DOI
Seyhan Ayik, Mehmet Günata, Onural Özhan

et al.

Fundamental and Clinical Pharmacology, Journal Year: 2024, Volume and Issue: 38(6), P. 1143 - 1154

Published: Aug. 11, 2024

Abstract Background Despite the available treatments, pulmonary arterial hypertension (PAH) prognosis is poor. Objectives We aimed to investigate effects of alamandine (ALA), melatonin (MEL), and ALA + MEL in PAH. Methods The rats were randomly divided into Control ( n = 10), monocrotaline (MCT) 12), 12) groups. PAH was induced by MCT. ALA, MEL, groups received 50 μg/kg/day 10 mg/kg/day respectively, for 35 days. Echocardiographic hemodynamic measurements tissue analyses (morphometric, histopathological, ELISA, western blot) performed. Results Monotherapies, especially reduced right ventricular (RV) systolic pressure. Only increased artery acceleration time. MCT RV/left ventricle (LV) interventricular septum (IVS) ratio. While slightly decreased RV/(LV IVS), significantly restored it. tunica intima‐media (TIM) thickness, PCNA α‐SMA arterioles, histopathological score (HS) (inflammatory infiltration etc.) lung, RV. All treatments TIM thickness (especially MEL), PCNA, α‐SMA. HS lung; however, produced greater benefits. attenuated caused a significant increase lung lysyl oxidase (LOX) activity. LOX; provided improvement. Nrf‐2 MCT‐treated rats, Conclusion attenuate protect RV via antiproliferative, anti‐remodeling, antihypertrophic, anti‐inflammatory, free radical scavenging (only MEL) capabilities. Overall, best outcomes.

Language: Английский

Citations

2

Comprehensive review on neprilysin (NEP) inhibitors: design, structure-activity relationships, and clinical applications DOI Creative Commons
Xinyue Zhang, Chao Hu, Erkang Tian

et al.

Frontiers in Pharmacology, Journal Year: 2024, Volume and Issue: 15

Published: Dec. 23, 2024

Neprilysin (NEP), a zinc-dependent membrane-bound metallopeptidase, regulates various bioactive peptides, particularly in kidneys, vascular endothelium, and the central nervous system. NEP’s involvement metabolizing natriuretic insulin, enkephalins makes it promising target for treating cardiovascular Alzheimer’s diseases. Several NEP inhibitors, such as sacubitril omapatrilat, have been approved clinical use, which inhibit activity to prolong bioactivity of beneficial thereby exerting therapeutic effects. However, despite broad application prospects they still specific adverse reactions side effects, hypotension, renal impairment, potentially increased risk disease. This manuscript comprehensively reviews progress on single-target dual-target inhibitors. Dual-target inhibitors often combine with other targets, angiotensin receptors, enhance effects reduce reactions. The article also emphasizes these inhibitors' design strategies, structure-activity relationships (SAR), safety, performance.

Language: Английский

Citations

0