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https://www.readbyqxmd.com/read/29419686/the-clinical-efficacy-of-epalrestat-combined-with-%C3%AE-lipoic-acid-in-diabetic-peripheral-neuropathy-protocol-for-a-systematic-review-and-meta-analysis
#1
Xiaotong Wang, Haixiong Lin, Shuai Xu, Yuanlin Jin, Ren Zhang
BACKGROUND: Diabetic peripheral neuropathy (DPN) is a common long-term complication of diabetes mellitus, affecting patients in the world. Epalrestat combined with α-lipoic acid (ALA) is the most frequent combine therapy used in the DPN researches. We aim to assess the effectiveness and safety of epalrestat combined with ALA in patients with DPN, compare with epalrestat alone. METHODS: We will search Cochrane Library, PubMed, Wanfang Data, China National Knowledge Infrastructure, VIP Chinese Science and Technology Journals Database, and Chinese Biomedical Database from inception until October 31th, 2017...
February 2018: Medicine (Baltimore)
https://www.readbyqxmd.com/read/29371030/regulation-on-sirt1-pgc-1%C3%AE-nrf2-pathway-together-with-selective-inhibition-of-aldose-reductase-makes-compound-hr5f-a-potential-agent-for-the-treatment-of-diabetic-complications
#2
Zhihua Wang, Sheng Yuan, Yanbing Li, Zhe Zhang, Wei Xiao, Dan Tang, Kaihe Ye, Zhijun Liu, Congcong Wang, Yixiong Zheng, Hong Nie, Heru Chen
(R,E)-N-(3-(2-acetamido-3-(benzyloxy) propanamido)propyl)-2-cyano-3-(4-hydroxy phenyl)acrylamide (hr5F) was design-synthesized based on bioactivity focus strategy as a potential agent to treat diabetic complicates. With in vitro enzyme assay, it is confirmed that hr5F is an effective ALR2 inhibitor with IC50 value of 2.60±0.15 nM, and selectivity index of 86.0 over ALR1, which is a little bit better than the reference Epalrestat (Epa). hr5F inhibits the increase of ALR2 enzyme activity and expression in human lens epithelial cells (HLECs) induced by high glucose...
January 22, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29181125/protective-effects-and-possible-mechanisms-of-ergothioneine-and-hispidin-against-methylglyoxal-induced-injuries-in-rat-pheochromocytoma-cells
#3
Tuzz-Ying Song, Nae-Cherng Yang, Chien-Lin Chen, Thuy Lan Vo Thi
Diabetic encephalopathy (DE) is often a complication in patients with Alzheimer's disease due to high blood sugar induced by diabetic mellitus. Ergothioneine (EGT) and hispidin (HIP) are antioxidants present in Phellinus linteus. Methylglyoxal (MGO), a toxic precursor of advanced glycated end products (AGEs), is responsible for protein glycation. We investigated whether a combination EGT and HIP (EGT + HIP) protects against MGO-induced neuronal cell damage. Rat pheochromocytoma (PC12) cells were preincubated with EGT (2 μM), HIP (2 μM), or EGT + HIP, then challenged with MGO under high-glucose condition (30 μM MGO + 30 mM glucose; GLU + MGO) for 24-96 h...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/29125108/lipoic-acid-combined-with-epalrestat-versus-lipoic-acid-in-treating-diabetic-peripheral-neuropathy-a-meta-analysis
#4
Xiao-Tong Wang, Hai-Xiong Lin, Shu-Ai Xu, Ying-Kun Lu
Objective To compare the clinical effectiveness of lipoic acid combined with epalrestat versus lipoic acid in treating diabetic peripheral neuropathy(DPN). Methods Randomized controlled trials(RCTs) and clinical controlled trials on lipoic acid versus epalrestat for DPN before February 2016 were searched through five databases:CNKI,CBM,VIP,Wanfang,and PubMed. The quality of the included trials were assessed using Cochrane software and Jadad scores. Data were analyzed with Review Manager 5.3 software. Results Nine studies were included in the analysis...
October 30, 2017: Zhongguo Yi Xue Ke Xue Yuan Xue Bao. Acta Academiae Medicinae Sinicae
https://www.readbyqxmd.com/read/29098865/novel-quinazolinone-based-2-4-thiazolidinedione-3-acetic-acid-derivatives-as-potent-aldose-reductase-inhibitors
#5
Kamel Metwally, Harris Pratsinis, Dimitris Kletsas, Luca Quattrini, Vito Coviello, Concettina La Motta, Ahmed A El-Rashedy, Mahmoud Es Soliman
AIM: Targeting aldose reductase enzyme with 2,4-thiazolidinedione-3-acetic acid derivatives having a bulky hydrophobic 3-arylquinazolinone residue. MATERIALS & METHODS: All the target compounds were structurally characterized by different spectroscopic methods and microanalysis, their aldose reductase inhibitory activities were evaluated, and binding modes were studied by molecular modeling. RESULTS: All the synthesized compounds proved to inhibit the target enzyme potently, exhibiting IC50 values in the nanomolar/low nanomolar range...
November 3, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29079419/epalrestat-loaded-silicone-hydrogels-as-contact-lenses-to-address-diabetic-eye-complications
#6
Fernando Alvarez-Rivera, Angel Concheiro, Carmen Alvarez-Lorenzo
Most treatments for diabetic eye conditions rely on systemic (oral) or intravitreal administration, and there is still a demand of efficient and comfortable ocular dosage forms. Our purpose was to design contact lenses (CLs) suitable for local prophylaxis/treatment of diabetes-related ocular pathologies, by means of the incorporation of bioinspired functional groups that can reversibly interact with epalrestat, an aldose reductase inhibitor. Several sets of silicone hydrogels were synthesized varying the contents in 2-hydroxyethyl methacrylate (HEMA), monomethacryloxypropyl-sym-polydimethylsiloxane hydroxypropyl terminated (MCS-MC12), and aminopropyl methacrylamide (APMA)...
October 24, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28935265/quinazolinone-based-rhodanine-3-acetic-acids-as-potent-aldose-reductase-inhibitors-synthesis-functional-evaluation-and-molecular-modeling-study
#7
Sherihan El-Sayed, Kamel Metwally, Abdalla A El-Shanawani, Lobna M Abdel-Aziz, Ahmed A El-Rashedy, Mahmoud E S Soliman, Luca Quattrini, Vito Coviello, Concettina la Motta
A series of quinazolinone-based rhodanine-3-acetic acids was synthesized and tested for in vitro aldose reductase inhibitory activity. All the target compounds displayed nanomolar activity against the target enzyme. Compounds 3a, 3b, and 3e exhibited almost 3-fold higher activity as compared to the only marketed reference drug epalrestat. Structure-activity relationship studies indicated that bulky substituents at the 3-phenyl ring of the quinazolinone moiety are generally not tolerated in the active site of the enzyme...
October 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28585087/corticosteroids-and-aldose-reductase-inhibitor-epalrestat-modulates-cardiac-action-potential-via-kv%C3%AE-1-1-akr6a8-subunit-of-voltage-gated-potassium-channel
#8
Jared Tur, Sachin L Badole, Feng Cheng, Aparoop Das, Rakesh C Kukreja, Srinivas M Tipparaju
We previously demonstrated the role of Kvβ1.1 subunit of voltage-activated potassium channel in heart for its sensory roles in detecting changes in NADH/NAD and modulation of ion channel. However, the pharmacological role for the association of Kvβ1 via its binding to ligands such as cortisone and its analogs remains unknown. Therefore, we investigated the significance of Kvβ1.1 binding to cortisone analogs and AR inhibitor epalrestat. In addition, the aldose reductase (AR) inhibitor epalrestat was identified as a pharmacological target and modulator of cardiac activity via binding to the Kvβ1 subunit...
December 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28546106/enhanced-dissolution-and-skin-permeation-profiles-of-epalrestat-with-%C3%AE-cyclodextrin-derivatives-using-a-cogrinding-method
#9
Takayuki Furuishi, Shoma Takahashi, Noriko Ogawa, Mihoko Gunji, Hiromasa Nagase, Toyofumi Suzuki, Tomohiro Endo, Haruhisa Ueda, Etsuo Yonemochi, Kazuo Tomono
Epalrestat (EPL) is a water-insoluble drug (14μM) that inhibits aldose reductase. This study investigated the interactions between β-cyclodextrin (CD) derivatives and EPL to determine the solubilizing effect on EPL from phase solubility diagrams. We improved the solubility of EPL in water by adding β-CD derivatives. Moreover, the solubility of EPL mixed with β-CD derivatives by cogrinding in a ball mill method was about 2-3 times higher than those of EPL with the same CD concentration (5mM) calculated from phase solubility diagrams...
August 30, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28445852/sensitive-analysis-and-pharmacokinetic-study-of-epalrestat-in-c57bl-6j-mice
#10
Jingqiu Huang, Runbin Sun, Siqi Feng, Jun He, Fei Fei, Haoxue Gao, Yuqing Zhao, Yue Zhang, Huilin Gu, Jiye Aa, Guangji Wang
Epalrestat is clinically applied for the management of diabetic peripheral neuropathy, yet its pharmacokinetic properties are not well understood. In this study, a rapid and sensitive LC-MS/MS method was established for assaying epalrestat in bio-samples of mice. The method was validated and it showed a good linearity over the range of 2-5000ng/mL, a precision of less than 12.3%, and recovery and matrix effects of 112.5-123.6% and 87.9-89.5%, respectively. After administration of a single dose of epalrestat administered, the exposure level of AUC0-∞ was positively dose-dependent and the mean Cmax, AUC0-12h, T1/2, and MRT were 36...
June 15, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28386557/renoprotective-effects-of-aldose-reductase-inhibitor-epalrestat-against-high-glucose-induced-cellular-injury
#11
Heba El Gamal, Ali Hussein Eid, Shankar Munusamy
Diabetic nephropathy (DN) is the leading cause of end stage renal disease worldwide. Increased glucose flux into the aldose reductase (AR) pathway during diabetes was reported to exert deleterious effects on the kidney. The objective of this study was to investigate the renoprotective effects of AR inhibition in high glucose milieu in vitro. Rat renal tubular (NRK-52E) cells were exposed to high glucose (30 mM) or normal glucose (5 mM) media for 24 to 48 hours with or without the AR inhibitor epalrestat (1 μM) and assessed for changes in Akt and ERK1/2 signaling, AR expression (using western blotting), and alterations in mitochondrial membrane potential (using JC-1 staining), cell viability (using MTT assay), and cell cycle...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28270406/akr1b1-promotes-basal-like-breast-cancer-progression-by-a-positive-feedback-loop-that-activates-the-emt-program
#12
Xuebiao Wu, Xiaoli Li, Qiang Fu, Qianhua Cao, Xingyu Chen, Mengjie Wang, Jie Yu, Jingpei Long, Jun Yao, Huixin Liu, Danping Wang, Ruocen Liao, Chenfang Dong
Basal-like breast cancer (BLBC) is associated with high-grade, distant metastasis and poor prognosis. Elucidating the determinants of aggressiveness in BLBC may facilitate the development of novel interventions for this challenging disease. In this study, we show that aldo-keto reductase 1 member B1 (AKR1B1) overexpression highly correlates with BLBC and predicts poor prognosis in breast cancer patients. Mechanistically, Twist2 transcriptionally induces AKR1B1 expression, leading to nuclear factor κB (NF-κB) activation...
April 3, 2017: Journal of Experimental Medicine
https://www.readbyqxmd.com/read/28204799/epalrestat-stimulated-oxidative-stress-inflammation-and-fibrogenesis-in-mouse-liver
#13
Yuan Le, Liming Chen, Yue Zhang, Pengli Bu, Guoli Dai, Xingguo Cheng
No abstract text is available yet for this article.
February 15, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/28057038/aldose-reductase-mediates-endothelial-cell-dysfunction-induced-by-high-uric-acid-concentrations
#14
Zhiyong Huang, Quan Hong, Xueguang Zhang, Wenzhen Xiao, Liyuan Wang, Shaoyuan Cui, Zhe Feng, Yang Lv, Guangyan Cai, Xiangmei Chen, Di Wu
BACKGROUND: Uric acid (UA) is an antioxidant found in human serum. However, high UA levels may also have pro-oxidant functions. According to previous research, aldose reductase (AR) plays a vital role in the oxidative stress-related complications of diabetes. We sought to determine the mechanism by which UA becomes deleterious at high concentrations as well as the effect of AR in this process. METHOD: Endothelial cells were divided into three groups cultured without UA or with 300 μM or 600 μM UA...
January 5, 2017: Cell Communication and Signaling: CCS
https://www.readbyqxmd.com/read/27960106/aldose-reductase-deficiency-leads-to-oxidative-stress-induced-dopaminergic-neuronal-loss-and-autophagic-abnormality-in-an-animal-model-of-parkinson-s-disease
#15
Patrick K K Yeung, Angela K W Lai, Hyo Jin Son, Xu Zhang, Onyou Hwang, Stephen S M Chung, Sookja K Chung
Fungicide exposure causes degeneration of dopaminergic neurons and contributes to Parkinson's disease (PD). Benomyl inhibits enzymes responsible for detoxifying the reactive dopamine metabolite 3,4-dihydroxyphenylacetaldehyde. Aldose reductase (AR) is known as tetrahydrobiopterin (BH4) reductase that generates BH4, a cofactor for tyrosine hydroxylase (TH) involved in dopamine synthesis. AR also acts as an aldehyde reductase involved in detoxifying 3,4-dihydroxyphenylacetaldehyde. In PD patients, the level of AR is significantly lower in the cerebellum...
February 2017: Neurobiology of Aging
https://www.readbyqxmd.com/read/27891351/evaluation-of-effect-of-nishamalaki-on-stz-and-hfhf-diet-induced-diabetic-neuropathy-in-wistar-rats
#16
Jayshree Shriram Dawane, Vijaya Anil Pandit, Madhura Shirish Kumar Bhosale, Pallawi Shashank Khatavkar
INTRODUCTION: Diabetic neuropathy is one of the most common complications affecting 50% of diabetic patients. Neuropathic pain is the most difficult types of pain to treat. There is no specific treatment for neuropathy. Nishamalaki (NA), combination of Curcuma longa and Emblica officinalis used to treat Diabetes Mellitus (DM). So, efforts were made to test whether NA is useful in prevention of diabetic neuropathy. AIM: To evaluate the effect of NA on diabetic neuropathy in type 2 diabetic wistar rats...
October 2016: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/27835059/epalrestat-an-aldose-reductase-inhibitor-prevents-glucose-induced-toxicity-in-human-retinal-pigment-epithelial-cells-in-vitro
#17
Srinivasan Senthilkumari, Rajendran Sharmila, Gowripriya Chidambaranathan, Ayyasamy Vanniarajan
PURPOSE: Aldose reductase (ALR), the first and rate-limiting enzyme involved in polyol pathway plays a central role in diabetes and its related complications, including diabetic retinopathy (DR). Inhibition of ALR may also be an ideal target for reducing the deleterious effects of DR. Therefore, the purpose of the present study was to investigate the protective effect of epalrestat (EPL), ALR inhibitor on glucose-induced toxicity in ARPE-19 cells. METHODS: ARPE-19 cells were challenged with normal glucose (NG, 5 mM) and high glucose (HG1, 25 mM and HG2, 50 mM) in the presence or absence of EPL...
January 2017: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27666634/pterin-7-carboxamides-as-a-new-class-of-aldose-reductase-inhibitors
#18
Ryota Saito, Saori Suzuki, Kaname Sasaki
Aldose reductase is related to the onset and progression of diabetic complications, such as neuropathy, retinopathy, angiopathy, and so on: therefore molecules that are capable of inhibiting the enzyme are potential drugs for treatment of diabetic complications. Epalrestat is the sole aldose reductase inhibitor that is clinically used, but still has some drawbacks. Thus, the development of new aldose reductase inhibitors is still desired. We have synthesized a series of new pterin-7-carboxamides, and evaluated their in vitro inhibitory activities against human aldose reductase...
October 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27650591/simultaneous-determination-of-epalrestat-and-puerarin-in-rat-plasma-by-uhplc-ms-ms-application-to-their-pharmacokinetic-interaction-study
#19
Hong Sun, Yunhai Bo, Mingjie Zhang, Xiao Wu, Mingyang Zhou, Longshan Zhao, Zhili Xiong
In the present study, a simple, rapid and reliable ultrahigh-performance liquid chromatography-tandem mass spectrometric (UHPLC-MS/MS) method was developed and validated to determine simultaneously epalrestat (EPA) and puerarin (PUE) in rat plasma for evaluation of the pharmacokinetic interaction of these two drugs. Both the analytes and glipizide (internal standard, IS) were extracted using a protein precipitation method. The separation was performed on a C18 reversed phase column using acetonitrile and 5 mmol/L ammonium acetate in water as the mobile phase with a gradient elution program...
April 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/27439473/epalrestat-upregulates-heme-oxygenase-1-superoxide-dismutase-and-catalase-in-cells-of-the-nervous-system
#20
Kaori Yama, Keisuke Sato, Yu Murao, Ryosuke Tatsunami, Yoshiko Tampo
Heme oxygenase (HO)-1 has potent antioxidant and anti-inflammatory functions. Recent studies have shown that the upregulation of HO-1 is beneficial to counteract neuroinflammation, making HO-1 a new therapeutic target for neurological diseases. We have reported that epalrestat (EPS), which is currently used for the treatment of diabetic neuropathy, increases HO-1 levels through the activation of nuclear factor erythroid 2-related factor 2 (Nrf2) in bovine aortic endothelial cells. In this study, we tested the hypothesis that EPS upregulates HO-1 via Nrf2 activation in the component cells of the nervous system, by using rat Schwann cells and human SH-SY5Y cells...
September 1, 2016: Biological & Pharmaceutical Bulletin
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