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Aldose reductase inhibitor

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https://www.readbyqxmd.com/read/28623716/aldose-reductase-inhibitors-attenuate-%C3%AE-amyloid-induced-tnf-%C3%AE-production-in-microlgia-via-ros-pkc-mediated-nf-%C3%AE%C2%BAb-and-mapk-pathways
#1
Xiao-Min Song, Qian Yu, Xin Dong, Hyun Ok Yang, Ke-Wu Zeng, Jun Li, Peng-Fei Tu
Microglia-mediated neuroinflammation is a key risk factor to the development of Alzheimer' disease (AD). Aldose reductase (AR) has been found to be widely involved in inflammation-related diseases; however, whether aldose reductase inhibitors (ARIs) could be used to treat neuroinflammation is rarely reported. This study aims to evaluate the anti-neuroinflammatory effects of two major ARIs of Sorbinil (Sor) and Zopolrestat (Zol) in β-amyloid protein (Aβ)-induced microglia (BV-2). We find that Sor and Zol significantly inhibit TNF-α, IL-1β, IL-6 production from microglia in response to Aβ stimulation...
June 14, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28600556/aldose-reductase-inhibitor-increases-doxorubicin-sensitivity-of-colon-cancer-cells-and-decreases-cardiotoxicity
#2
Himangshu Sonowal, Pabitra B Pal, Jian-Jun Wen, Sanjay Awasthi, Kota V Ramana, Satish K Srivastava
Anthracycline drugs such as doxorubicin (DOX) and daunorubicin remain some of the most active wide-spectrum and cost-effective drugs in cancer therapy. However, colorectal cancer (CRC) cells are inherently resistant to anthracyclines which at higher doses cause cardiotoxicity. Our recent studies indicate that aldose reductase (AR) inhibitors such as fidarestat inhibit CRC growth in vitro and in vivo. Here, we show that treatment of CRC cells with fidarestat increases the efficacy of DOX-induced death in HT-29 and SW480 cells and in nude mice xenografts...
June 9, 2017: Scientific Reports
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
#3
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...
June 5, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/28567125/synthesis-and-functional-evaluation-of-novel-aldose-reductase-inhibitors-bearing-a-spirobenzopyran-scaffold
#4
Maria Digiacomo, Stefania Sartini, Giulia Nesi, Simona Sestito, Vito Coviello, Concettina La Motta, Simona Rapposelli
BACKGROUND: Aldose reductase, the first enzyme of the polyol pathway, is the key determinant for the pathogenesis of long term diabetic complications. Accordingly, its inhibition represents the major therapeutic strategy to treat this kind of pathologies. OBJECTIVES: In this work we describe the synthesis and the functional evaluation of a number of spiro-oxazolidinone and spiro-morpholinone acetic acid derivatives, and their benzyloxy analogs, developed as aldose reductase inhibitors...
2017: Open Medicinal Chemistry Journal
https://www.readbyqxmd.com/read/28512639/inhibitory-effect-of-chemical-constituents-isolated-from-artemisia-iwayomogi-on-polyol-pathway-and-simultaneous-quantification-of-major-bioactive-compounds
#5
Yoon Kyoung Lee, Eun Young Hong, Wan Kyunn Whang
Blocking the polyol pathway plays an important role preventing diabetic complications. Therefore, aldose reductase (AR) and advanced glycation endproducts (AGEs) formation has significant effect on diabetic complications. Artemisia iwayomogi has long been used as treatment of various diseases in Korea. However, no literatures have reported on AR and AGEs formation inhibitory activities of A. iwayomogi. For these reasons, we aimed to assess that A. iwayomogi had potential as anti-diabetic complications agents...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28484711/rapid-identification-and-isolation-of-inhibitors-of-rat-lens-aldose-reductase-and-antioxidant-in-maackia-amurensis
#6
Set Byeol Kim, Seung Hwan Hwang, Zhiqiang Wang, Jae Myung Yu, Soon Sung Lim
Oxidative stress and aldose reductase activity have been implicated in the development of diabetic complications. In this study, the antioxidant and aldose reductase (AR) inhibitory effects of Maackia amurensis (MA) were investigated. The ethyl acetate fraction of the MA extract showed the highest inhibitory activity in antioxidant and rat lens AR (RLAR). To identify and isolate the active components in the ethyl acetate fraction of the MA extract, high-speed countercurrent chromatography and Sephadex LH-20 column chromatography were performed and guided by an offline HPLC-ABTS assay and HPLC microfractionation AR assay...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28450000/investigation-of-the-antioxidant-and-aldose-reductase-inhibitory-activities-of-extracts-from-peruvian-tea-plant-infusions
#7
Zhiqiang Wang, Seung Hwan Hwang, Yanymee N Guillen Quispe, Paul H Gonzales Arce, Soon Sung Lim
In the present study, the antioxidant and aldose reductase inhibitory activities of 24 Peruvian infusion tea plants were investigated by 2,2'-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and aldose reductase assays. Phoradendron sp. showed the highest inhibition of aldose reductase (IC50, 1.09±0.06μg/mL) and considerable antioxidant (IC50 of DPPH, 58.36±1.65μg/mL; IC50 of ABTS, 9.91±0.43μg/mL) effects. In order to identify the antioxidants and aldose reductase inhibitors of Phoradendron sp...
September 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28447762/inhibition-of-aldose-reductase-ameliorates-ethanol%C3%A2-induced-steatosis-in-hepg2-cells
#8
Longxin Qiu, Chengchao Cai, Xiangqian Zhao, Yan Fang, Weibiao Tang, Chang Guo
Aldose reductase (AR) expression is increased in liver tissue of patients with ethanol‑induced liver disease. However, the exact role of AR in the development of ethanol‑induced liver disease has yet to be elucidated. The present study aimed to determine the effect of an AR inhibitor on ethanol‑induced steatosis in HepG2 cells and to identify possible underlying molecular mechanisms. Steatosis was induced in HepG2 cells by stimulating cells with 100 mM absolute ethanol for 48 h. Oil Red O staining was used to detect the lipid droplet accumulation in cells...
May 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28438542/identification-of-low-micromolar-dual-inhibitors-for-aldose-reductase-alr2-and-poly-adp-ribose-polymerase-parp-1-using-structure-based-design-approach
#9
Navriti Chadha, Om Silakari
Clinical studies have revealed that diabetic retinopathy is a multifactorial disorder. Moreover, studies also suggest that ALR2 and PARP-1 co-occur in retinal cells, making them appropriate targets for the treatment of diabetic retinopathy. To find the dual inhibitors of ALR2 and PARP-1, the structure based design was carried out in parallel for both the target proteins. A series of novel thiazolidine-2,4-dione (TZD) derivatives were therefore rationally designed, synthesized and their in vitro inhibitory activities against ALR2 and PARP-1 were evaluated...
April 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28406694/does-inhibition-of-aldose-reductase-contribute-to-the-anti-inflammatory-action-of-setipiprant
#10
J Ballekova, M Soltesova-Prnova, M Majekova, M Stefek
The aim of this study was to investigate aldose reductase inhibitory action of setipiprant as a potential additional mechanism contributing to its anti-inflammatory action. Aldose reductase activity was determined by spectrophotometric measuring of NADPH consumption. Setipiprant was found to inhibit aldose reductase/NADPH-mediated reduction of 4-hydroxynonenal, 4-hydroxynonenal glutathione and prostaglandin H2 substrates, all relevant to the process of inflammation. Molecular modeling simulations into the aldose reductase inhibitor binding site revealed an interaction pattern of setipiprant...
April 12, 2017: Physiological Research
https://www.readbyqxmd.com/read/28404521/diabetic-complications-in-the-cornea
#11
Alexander V Ljubimov
Diabetic corneal alterations, such as delayed epithelial wound healing, edema, recurrent erosions, neuropathy/loss of sensitivity, and tear film changes are frequent but underdiagnosed complications of both type 1 (insulin-dependent) and type 2 (non-insulin-dependent) diabetes mellitus. The disease affects corneal epithelium, corneal nerves, tear film, and to a lesser extent, endothelium, and also conjunctiva. These abnormalities may appear or become exacerbated following trauma, as well as various surgeries including retinal, cataract or refractive...
April 28, 2017: Vision Research
https://www.readbyqxmd.com/read/28399135/structure-based-comprehensive-modelling-spatial-fingerprints-mapping-and-adme-screening-of-curcumin-analogues-as-novel-alr2-inhibitors
#12
Sant Kumar Verma, Suresh Thareja
Aldose reductase (ALR2) inhibition is the most legitimate approach for the management of diabetic complications. The limited triumph in the drug development against ALR2 is mainly because of its close structural similarity with the other members of aldo-keto reductase (AKR) superfamily viz. ALR1, AKR1B10; and lipophilicity problem i.e. poor diffusion of synthetic aldose reductase inhibitors (ARIs) to target tissues. The literature evidenced that naturally occurring curcumin demonstrates relatively specific and non-competitive inhibition towards human recombinant ALR2 over ALR1 and AKR1B10; however β-diketone moiety of curcumin is a specific substrate for liver AKRs and accountable for it's rapid in vivo metabolism...
2017: PloS One
https://www.readbyqxmd.com/read/28392277/n-aroyl-n-arylmethyloxy-%C3%AE-alanines-selective-inhibitors-of-aldose-reductase
#13
Susanna Nencetti, Concettina La Motta, Armando Rossello, Stefania Sartini, Elisa Nuti, Lidia Ciccone, Elisabetta Orlandini
Aldose reductase (ALR2), a NADPH-dependent reductase, is the first and rate-limiting enzyme of the polyol pathway of glucose metabolism and is implicated in the pathogenesis of secondary diabetic complications. In the last decades, this enzyme has been targeted for inhibition but despite the numerous efforts made to identify potent and safe ALR2 inhibitors, many clinical candidates have been a failure. For this reason the research of new ALR2 inhibitors highly effective, selective and with suitable pharmacokinetic properties is still of great interest...
March 28, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28386557/renoprotective-effects-of-aldose-reductase-inhibitor-epalrestat-against-high-glucose-induced-cellular-injury
#14
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/28322781/characterization-of-akr1b16-a-novel-mouse-aldo-keto-reductase
#15
Joan Giménez-Dejoz, Susanne Weber, Oleg A Barski, Gabriele Möller, Jerzy Adamski, Xavier Parés, Sergio Porté, Jaume Farrés
Aldo-keto reductases (AKRs) are distributed in three families and multiple subfamilies in mammals. The mouse Akr1b3 gene is clearly orthologous to human AKR1B1, both coding for aldose reductase, and their gene products show similar tissue distribution, regulation by osmotic stress and kinetic properties. In contrast, no unambiguous orthologs of human AKR1B10 and AKR1B15.1 have been identified in rodents. Although two more AKRs, AKR1B7 and AKR1B8, have been identified and characterized in mouse, none of them seems to exhibit properties similar to the human AKRs...
March 17, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28302016/validation-of-tzd-scaffold-as-potential-aris-pharmacophore-modelling-atom-based-3d-qsar-and-docking-studies
#16
Lalita Dahiya, Manoj Kumar Mahapatra, Ramandeep Kaur, Vipin Kumar, Manoj Kumar
Metabolic disorders associated with diabetic patients are a serious concern. Aldose reductase (ALR2) has been identified as first rate-limiting enzyme in the polyol pathway which catalyzes the reduction of glucose to sorbitol. It represents one of the validated targets to develop potential new chemical entities for the prevention and subsequent progression of microvascular diabetic complications. In order to further understand the intricate structural prerequisites of molecules to act as ALR2 inhibitors, ligand-based pharmacophore model, atom-based 3D-QSAR and structure based drug design studies have been performed on a series of 2,4-thiazolidinedione derivatives with ALR2 inhibitory activity...
March 15, 2017: Combinatorial Chemistry & High Throughput Screening
https://www.readbyqxmd.com/read/28287485/chemical-constituents-of-smilax-china-l-stems-and-their-inhibitory-activities-against-glycation-aldose-reductase-%C3%AE-glucosidase-and-lipase
#17
Hee Eun Lee, Jin Ah Kim, Wan Kyunn Whang
The search for natural inhibitors with anti-diabetes properties has gained increasing attention. Among four selected Smilacaceae family plants, Smilax china L. stems (SCS) showed significant in vitro anti-glycation and rat lens aldose reductase inhibitory activities. Bioactivity-guided isolation was performed with SCS and four solvent fractions were obtained, which in turn yielded 10 compounds, including one phenolic acid, three chlorogenic acids, four flavonoids, one stilbene, and one phenylpropanoid glycoside; their structures were elucidated using nuclear magnetic resonance and mass spectrometry...
March 11, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28259841/enhancing-activity-and-selectivity-in-a-series-of-pyrrol-1-yl-1-hydroxypyrazole-based-aldose-reductase-inhibitors-the-case-of-trifluoroacetylation
#18
Nikolaos Papastavrou, Maria Chatzopoulou, Jana Ballekova, Mario Cappiello, Roberta Moschini, Francesco Balestri, Alexandros Patsilinakos, Rino Ragno, Milan Stefek, Ioannis Nicolaou
Aldose reductase (ALR2) has been the target of therapeutic intervention for over 40 years; first, for its role in long-term diabetic complications and more recently as a key mediator in inflammation and cancer. However, efforts to prepare small-molecule aldose reductase inhibitors (ARIs) have mostly yielded carboxylic acids with rather poor pharmacokinetics. To address this limitation, the 1-hydroxypyrazole moiety has been previously established as a bioisostere of acetic acid in a group of aroyl-substituted pyrrolyl derivatives...
April 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28217947/mechanism-of-capsaicin-inhibition-of-aldose-reductase-activity
#19
Zuhal Alim, Namık Kilinc, Bulent Sengul, Sukru Beydemir
Aldose reductase (AR) inhibitors play a vital importance as a potential therapeutic and preventive medicine when it comes to hyperglycemia associated diabetic complications. Additionally, capsaicin is used as a food additive and a drug in a number of diverse clinical trials. The aim of this study is to determine the in vitro inhibition behavior of capsaicin on AR enzyme activity, which was obtained from different rat tissues (heart, kidney, liver, and brain). We showed that AR was inhibited by capsaicin in the micromolar range and noncompetitive manner in all of the tissues...
February 20, 2017: Journal of Biochemical and Molecular Toxicology
https://www.readbyqxmd.com/read/28194018/protective-role-of-fructokinase-blockade-in-the-pathogenesis-of-acute-kidney-injury-in-mice
#20
Ana Andres-Hernando, Nanxing Li, Christina Cicerchi, Shinichiro Inaba, Wei Chen, Carlos Roncal-Jimenez, Myphuong T Le, Michael F Wempe, Tamara Milagres, Takuji Ishimoto, Mehdi Fini, Takahiko Nakagawa, Richard J Johnson, Miguel A Lanaspa
Acute kidney injury is associated with high mortality, especially in intensive care unit patients. The polyol pathway is a metabolic route able to convert glucose into fructose. Here we show the detrimental role of endogenous fructose production by the polyol pathway and its metabolism through fructokinase in the pathogenesis of ischaemic acute kidney injury (iAKI). Consistent with elevated urinary fructose in AKI patients, mice undergoing iAKI show significant polyol pathway activation in the kidney cortex characterized by high levels of aldose reductase, sorbitol and endogenous fructose...
February 13, 2017: Nature Communications
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