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Epalrestat

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https://www.readbyqxmd.com/read/27891351/evaluation-of-effect-of-nishamalaki-on-stz-and-hfhf-diet-induced-diabetic-neuropathy-in-wistar-rats
#1
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
#2
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...
November 11, 2016: Journal of Ocular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27666634/pterin-7-carboxamides-as-a-new-class-of-aldose-reductase-inhibitors
#3
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
#4
Hong Sun, Yunhai Bo, Mingjie Zhang, Xiao Wu, Mingyang Zhou, Longshan Zhao, Zhili Xiong
In the present work, a simple, rapid and reliable ultra high performance liquid chromatography -tandem mass spectrometric (UHPLC-MS/MS) method was developed and validated to simultaneously determine epalrestat (EPA) and puerarin (PUE) in rat plasma for evaluation the pharmacokinetic interaction of this two drugs. Both the analytes and glipizide (IS) were extracted using protein precipitation method. The separation was performed on C18 reversed phase column using acetonitrile and 5 mmol/L ammonium acetate in water as mobile phase with a gradient elution program...
September 21, 2016: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/27439473/epalrestat-upregulates-heme-oxygenase-1-superoxide-dismutase-and-catalase-in-cells-of-the-nervous-system
#5
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
https://www.readbyqxmd.com/read/27190083/ranirestat-has-a-stronger-inhibitory-activity-on-aldose-reductase-and-suppresses-inflammatory-reactions-in-high-glucose-exposed-endothelial-cells
#6
Yuji Ishibashi, Takanori Matsui, Takafumi Matsumoto, Hiroshi Kato, Sho-Ichi Yamagishi
OBJECTIVE: Under diabetic conditions, glucose is converted to sorbitol via aldose reductase, whose process could contribute to diabetic vascular complications. However, effects of aldose reductase inhibitors are modest in diabetic patients. This may be attributed to weak inhibitory activity of aldose reductase inhibitors. We compared effects of ranirestat on endothelial cell damage with those of epalrestat. MATERIALS AND METHODS: Intracellular formations of sorbitol and superoxide were measured by liquid chromatography-mass spectrometry-mass spectrometry and dihydroethidium staining, respectively...
July 2016: Diabetes & Vascular Disease Research
https://www.readbyqxmd.com/read/27073391/epalrestat-protects-against-diabetic-peripheral-neuropathy-by-alleviating-oxidative-stress-and-inhibiting-polyol-pathway
#7
Qing-Rong Li, Zhuo Wang, Wei Zhou, Shou-Rui Fan, Run Ma, Li Xue, Lu Yang, Ya-Shan Li, Hong-Li Tan, Qing-Hua Shao, Hong-Ying Yang
Epalrestat is a noncompetitive and reversible aldose reductase inhibitor used for the treatment of diabetic neuropathy. This study assumed that epalrestat had a protective effect on diabetic peripheral nerve injury by suppressing the expression of aldose reductase in peripheral nerves of diabetes mellitus rats. The high-fat and high-carbohydrate model rats were established by intraperitoneal injection of streptozotocin. Peripheral neuropathy occurred in these rats after sustaining high blood glucose for 8 weeks...
February 2016: Neural Regeneration Research
https://www.readbyqxmd.com/read/26969882/aldo-keto-reductase-1b10-protects-human-colon-cells-from-dna-damage-induced-by-electrophilic-carbonyl-compounds
#8
Xuyu Zu, Ruilan Yan, Jishen Pan, Linlin Zhong, Yu Cao, Jun Ma, Chuan Cai, Dan Huang, Jianghua Liu, Fung-Lung Chung, Duan-Fang Liao, Deliang Cao
Electrophilic carbonyl compounds are highly cytotoxic and genotoxic. Aldo-keto reductase 1B10 (AKR1B10) is an enzyme catalyzing reduction of carbonyl compounds to less toxic alcoholic forms. This study presents novel evidence that AKR1B10 protects colon cells from DNA damage induced by electrophilic carbonyl compounds. AKR1B10 is specifically expressed in epithelial cells of the human colon, but this study found that AKR1B10 expression was lost or markedly diminished in colorectal cancer, precancerous tissues, and a notable portion of normal adjacent tissues (NAT)...
March 10, 2016: Molecular Carcinogenesis
https://www.readbyqxmd.com/read/26889760/color-polymorphs-of-aldose-reductase-inhibitor-epalrestat-configurational-conformational-and-synthon-differences
#9
Battini Swapna, Kuthuru Suresh, Ashwini Nangia
We report five crystalline polymorphs and an amorphous phase of epalrestat together with configurational isomerism and color behavior: form I (deep red), form II (deep orange), form III (bright yellow), form IV (yellow), and form V (orange) are in the E,Z configuration of the drug, and a Z,Z isomer (bright yellow). Two pathways are identified for polymorph conversion: direct transformation of the E,Z isomer and another pathway via the Z,Z isomer to the E,Z polymorphs. From a pharmaceutical perspective, the stability of polymorphs was established under grinding, solvent slurry and thermal conditions: form I (thermodynamic) > form II > form V > form III > form IV (least stable)...
March 14, 2016: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/26487510/molecular-interactions-and-implications-of-aldose-reductase-inhibition-by-pga1-and-clinically-used-prostaglandins
#10
Beatriz Díez-Dacal, Francisco J Sánchez-Gómez, Pedro A Sánchez-Murcia, Ivana Milackova, Tahl Zimmerman, Jana Ballekova, Elena García-Martín, José A G Agúndez, Severine Gharbi, Federico Gago, Milan Stefek, Dolores Pérez-Sala
Aldose reductase (AKR1B1) is a critical drug target because of its involvement in diabetic complications, inflammation, and tumorigenesis. However, to date, development of clinically useful inhibitors has been largely unsuccessful. Cyclopentenone prostaglandins (cyPGs) are reactive lipid mediators that bind covalently to proteins and exert anti-inflammatory and antiproliferative effects in numerous settings. By pursuing targets for modification by cyPGs we have found that the cyPG PGA1 binds to and inactivates AKR1B1...
January 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/26384019/identification-of-novel-aldose-reductase-inhibitors-from-spices-a-molecular-docking-and-simulation-study
#11
Priya Antony, Ranjit Vijayan
Hyperglycemia in diabetic patients results in a diverse range of complications such as diabetic retinopathy, neuropathy, nephropathy and cardiovascular diseases. The role of aldose reductase (AR), the key enzyme in the polyol pathway, in these complications is well established. Due to notable side-effects of several drugs, phytochemicals as an alternative has gained considerable importance for the treatment of several ailments. In order to evaluate the inhibitory effects of dietary spices on AR, a collection of phytochemicals were identified from Zingiber officinale (ginger), Curcuma longa (turmeric) Allium sativum (garlic) and Trigonella foenum graecum (fenugreek)...
2015: PloS One
https://www.readbyqxmd.com/read/26349493/updates-on-aldose-reductase-inhibitors-for-management-of-diabetic-complications-and-non-diabetic-diseases
#12
REVIEW
Ajmer Singh Grewal, Shashikant Bhardwaj, Deepti Pandita, Viney Lather, Bhupinder Singh Sekhon
Diabetes mellitus occurrence has been associated to the modification of the physiological levels of glucose and is often accompanied by several long-term complications, namely neuropathy, nephropathy, retinopathy, cataract, and cardiovascular. Aldose reductase (AR) is an enzyme of aldoketo reductase super-family that catalyzes the conversion of glucose to sorbitol in the polyol pathway of glucose metabolism. In this context, aldose reductase inhibitors (ARIs) have received much attention worldwide. Decreased sorbitol flux through polyol pathway by ARIs could be an emerging target for the management of major complications of diabetes...
2016: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/26330752/amelioration-of-bleomycin-induced-pulmonary-fibrosis-of-rats-by-an-aldose-reductase-inhibitor-epalrestat
#13
Xianwei Li, Yuanyuan Shen, Yining Lu, Jieren Yang
Aldose reductase (AR) is known to play a crucial role in the mediation of diabetic and cardiovascular complications. Recently, several studies have demonstrated that allergen-induced airway remodeling and ovalbumin-induced asthma is mediated by AR. Epalrestat is an aldose reductase inhibitor that is currently available for the treatment of diabetic neuropathy. Whether AR is involved in pathogenesis of pulmonary fibrosis and whether epalrestat attenuates pulmonary fibrosis remains unknown. Pulmonary fibrosis was induced by intratracheal instillation of bleomycin (5 mg/kg) in rats...
September 2015: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/26272532/effects-of-aldose-reductase-inhibitor-on-microneurographically-assessed-peripheral-sympathetic-nerve-activity-in-rats
#14
Daisuke Sato, Masataka Kusunoki, Go Shinzawa, Zhonggang Feng, Atsuyoshi Nishina, Takao Nakamura
Autonomic neuropathy, one of the serious complications of diabetes, decreases quality of life. Aldose reductase inhibitor (ARI) blocks sorbitol production, and results in prevention of damage of nerve fibers. Beneficial effects of ARI have usually been confirmed through nerve conduction velocity tests in motor and sensory nerves. On the other hand, few reports have dealt with the effects of ARI on the small fiber activity such as sympathetic nerve one. In the present study, we administered eparlestat, ARI orally for 3weeks, to streptozotocin-induced diabetic (STZ+ARI) rats, and then recorded peripheral sympathetic nervous signal detected with microneurographic technique...
December 2015: Autonomic Neuroscience: Basic & Clinical
https://www.readbyqxmd.com/read/25997250/propofol-attenuation-of-hydrogen-peroxide-induced-injury-in-human-umbilical-vein-endothelial-cells-involves-aldose-reductase
#15
Cheng-Lan Xie, Liu-Qing Hu, Yin-Bing Pan, Yan-Ning Qian
Propofol is a widely used intravenous anesthetic agent with antioxidant/antiapoptotic properties. Aldose reductase (AR) has been implicated in oxidative stress and apoptosis in endothelial cells. AR inhibition may protect cells from cardiovascular injury. Although the cytoprotective effect of propofol against hydrogen peroxide (H2O2)-induced injury has been widely studied, there is no information about the effects of propofol on AR. We therefore investigated the effect of propofol on H2O2-mediated injury and on aldose reductase expression...
February 2015: Die Pharmazie
https://www.readbyqxmd.com/read/25987541/characterization-of-diabetic-osteoarthritic-cartilage-and-role-of-high-glucose-environment-on-chondrocyte-activation-toward-pathophysiological-delineation-of-diabetes-mellitus-related-osteoarthritis
#16
M-C Laiguillon, A Courties, X Houard, M Auclair, A Sautet, J Capeau, B Fève, F Berenbaum, J Sellam
OBJECTIVE: To examine the relationship between osteoarthritis (OA) and type 2 diabetes mellitus (DM). METHODS: OA cartilage from DM and non-DM patients undergoing knee replacement were stimulated by IL-1β for 24 h and release of interleukin-6 (IL-6) and prostaglandin E2 (PGE2) was measured. Primary cultured murine chondrocytes were stimulated for 24 and 72 h with or without IL-1β (5 ng/mL) under normal-glucose (5.5 mM) or high-glucose (25 mM) conditions. The expression and release of pro-inflammatory mediators (IL-6, cyclooxygenase 2 [COX2]/PGE2) were analyzed by quantitative RT-PCR and ELISA/EIA...
September 2015: Osteoarthritis and Cartilage
https://www.readbyqxmd.com/read/25529839/epalrestat-increases-glutathione-thioredoxin-and-heme-oxygenase-1-by-stimulating-nrf2-pathway-in-endothelial-cells
#17
Kaori Yama, Keisuke Sato, Natsuki Abe, Yu Murao, Ryosuke Tatsunami, Yoshiko Tampo
Epalrestat (EPS) is the only aldose reductase inhibitor that is currently available for the treatment of diabetic neuropathy. Recently, we found that EPS at near-plasma concentration increases the intracellular levels of glutathione (GSH) in rat Schwann cells. GSH plays a crucial role in protecting endothelial cells from oxidative stress, thereby preventing vascular diseases. Here we show that EPS increases GSH levels in not only Schwann cells but also endothelial cells. Treatment of bovine aortic endothelial cells (BAECs), an in vitro model of the vascular endothelium, with EPS caused a dramatic increase in intracellular GSH levels...
2015: Redox Biology
https://www.readbyqxmd.com/read/25215304/effect-of-ranirestat-a-new-aldose-reductase-inhibitor-on-diabetic-retinopathy-in-sdt-rats
#18
Fumihiko Toyoda, Yoshiaki Tanaka, Ayumi Ota, Machiko Shimmura, Nozomi Kinoshita, Hiroko Takano, Takafumi Matsumoto, Junichi Tsuji, Akihiro Kakehashi
PURPOSE: To evaluate the effect of ranirestat, a new aldose reductase inhibitor (ARI), on diabetic retinopathy (DR) in Spontaneously Diabetic Torii (SDT) rats. METHODS: The animals were divided into six groups, normal Sprague-Dawley rats (n = 8), untreated SDT rats (n = 9), ranirestat-treated SDT rats (0.1, 1.0, and 10 mg/kg/day, n = 7, 8, and 6, resp.), and epalrestat-treated SDT rats (100 mg/kg/day, n = 7). Treated rats received oral ranirestat or epalrestat once daily for 40 weeks after the onset of diabetes...
2014: Journal of Diabetes Research
https://www.readbyqxmd.com/read/24843458/recent-advances-in-the-management-of-diabetic-distal-symmetrical-polyneuropathy
#19
REVIEW
Solomon Tesfaye
There is now little doubt that poor blood glucose control is an important risk factor for the development of diabetic peripheral neuropathy (DPN). Furthermore, traditional cardiovascular risk factors for macrovascular disease appear to be associated with an increased risk of DPN. The recently established International Expert Group on Diabetic Neuropathy has recommended new criteria for the diagnosis of DPN in the context of clinical and research settings. Studies in experimental diabetes examining the pathogenesis of DPN have identified a number of metabolic abnormalities including polyol pathway hyperactivity, increased advanced glycation end-point formation, alterations in the protein kinase C beta pathway through diacylglycerol and oxidative stress...
January 24, 2011: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/24827744/undecaprenyl-diphosphate-synthase-inhibitors-antibacterial-drug-leads
#20
William Sinko, Yang Wang, Wei Zhu, Yonghui Zhang, Ferran Feixas, Courtney L Cox, Douglas A Mitchell, Eric Oldfield, J Andrew McCammon
There is a significant need for new antibiotics due to the rise in drug resistance. Drugs such as methicillin and vancomycin target bacterial cell wall biosynthesis, but methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE) have now arisen and are of major concern. Inhibitors acting on new targets in cell wall biosynthesis are thus of particular interest since they might also restore sensitivity to existing drugs, and the cis-prenyl transferase undecaprenyl diphosphate synthase (UPPS), essential for lipid I, lipid II, and thus, peptidoglycan biosynthesis, is one such target...
July 10, 2014: Journal of Medicinal Chemistry
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