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Aldose reductase inhibitor

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https://www.readbyqxmd.com/read/28917123/identification-of-new-potent-inhibitor-of-aldose-reductase-from-ocimum-basilicum
#1
Huma Aslam Bhatti, Yildiz Tehseen, Kiran Maryam, Maliha Uroos, Bina S Siddiqui, Abdul Hameed, Jamshed Iqbal
Recent efforts to develop cure for chronic diabetic complications have led to the discovery of potent inhibitors against aldose reductase (AKR1B1, EC 1.1.1.21) whose role in diabetes is well-evident. In the present work, two new natural products were isolated from the ariel part of Ocimum basilicum; 7-(3-hydroxypropyl)-3-methyl-8-β-O-d-glucoside-2H-chromen-2-one (1) and E-4-(6'-hydroxyhex-3'-en-1-yl)phenyl propionate (2) and confirmed their structures with different spectroscopic techniques including NMR spectroscopy etc...
September 5, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28888096/exploration-of-thioxothiazolidinone-sulfonate-conjugates-as-a-new-class-of-aldehyde-aldose-reductase-inhibitors-a-synthetic-and-computational-investigation
#2
Hina Andleeb, Yildiz Tehseen, Farrukh Jabeen, Imtiaz Khan, Jamshed Iqbal, Shahid Hameed
In the present study, the pharmacophore integration methodology provided an efficient access to a new library of thioxothiazolidinone-sulfonate conjugates (8a-r) from easily available synthetic precursors. The approach was excellently high yielding with flexible structural sites for chemical modifications. The designed hybrid scaffolds were assessed for aldehyde/aldose reductase inhibition activities. The results for the in vitro bioassays were promising with the identification of compound 8e as the lead and selective candidate for ALR2 inhibition with an IC50 value of 0...
August 31, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28856935/the-use-of-dimethylsulfoxide-as-a-solvent-in-enzyme-inhibition-studies-the-case-of-aldose-reductase
#3
Livia Misuri, Mario Cappiello, Francesco Balestri, Roberta Moschini, Vito Barracco, Umberto Mura, Antonella Del-Corso
Aldose reductase (AR) is an enzyme devoted to cell detoxification and at the same time is strongly involved in the aetiology of secondary diabetic complications and the amplification of inflammatory phenomena. AR is subjected to intense inhibition studies and dimethyl sulfoxide (DMSO) is often present in the assay mixture to keep the inhibitors in solution. DMSO was revealed to act as a weak but well detectable AR differential inhibitor, acting as a competitive inhibitor of the L-idose reduction, as a mixed type of non-competitive inhibitor of HNE reduction and being inactive towards 3-glutathionyl-4-hydroxynonanal transformation...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28820747/involvement-of-hyperglycemia-in-the-development-of-platelet-procoagulant-response-the-role-of-aldose-reductase-and-platelet-swelling
#4
Tomasz Rusak, Tomasz Misztal, Malgorzata Rusak, Justyna Branska-Januszewska, Marian Tomasiak
: Rise in mean platelet volume (MPV) has been demonstrated to be associated with increased platelet reactivity. In diabetes patients, augmented MPV was proposed to contribute to increased risk of thrombotic complications. Therefore, the aim of this study was to investigate whether under hyperglycemic conditions, aldose reductase (AR)-mediated sorbitol formation and associated rise in cell volume, which subsequently results in platelet hyperactivation. Platelets were obtained from 30 healthy volunteers and 13 patients with diabetes...
September 2017: Blood Coagulation & Fibrinolysis: An International Journal in Haemostasis and Thrombosis
https://www.readbyqxmd.com/read/28802633/1-acetyl-5-phenyl-1h-pyrrol-3-ylacetate-an-aldose-reductase-inhibitor-for-the-treatment-of-diabetic-nephropathy
#5
Zhi-Ming Xiu, Li-Ping Wang, Jun Fu, Jia Xu, Li Liu
Diabetic nephropathy (DN) is the most common and serious complication in diabetes mellitus, but the efficacy of available strategies for preventing this disorder remains poor. The aim of this study was to investigate the possible beneficial effects of 1-acetyl-5-phenyl-1H-pyrrol-3-ylacetate (APPA), an aldose reductase inhibitor, on DN. In the present study, a model of rat glomerular mesangial cells (HBZY-1) damaged by high glucose was used to confirm the protective effects of APPA in vitro. Then, a rat model of streptozotocin-induced diabetes was used to assess the effects of APPA in vivo...
September 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28740855/aldose-reductase-inhibitor-protects-against-hyperglycemic-stress-by-activating-nrf2-dependent-antioxidant-proteins
#6
Kirtikar Shukla, Pabitra Bikash Pal, Himangshu Sonowal, Satish K Srivastava, Kota V Ramana
We have shown earlier that pretreatment of cultured cells with aldose reductase (AR) inhibitors prevents hyperglycemia-induced mitogenic and proinflammatory responses. However, the effects of AR inhibitors on Nrf2-mediated anti-inflammatory responses have not been elucidated yet. We have investigated how AR inhibitor fidarestat protects high glucose- (HG-) induced cell viability changes by increasing the expression of Nrf2 and its dependent phase II antioxidant enzymes. Fidarestat pretreatment prevents HG (25 mM)-induced Thp1 monocyte viability...
2017: Journal of Diabetes Research
https://www.readbyqxmd.com/read/28720470/molecular-docking-prediction-and-in-vitro-studies-elucidate-anti-cancer-activity-of-phytoestrogens
#7
Shreelekha Dutta, Prashant S Kharkar, Niteshkumar U Sahu, Aparna Khanna
AIM: The study is aimed at evaluating the chemosensitization and apoptotic effect of aglycone rich extracts of dietary phytoestrogens (derived from soybean and flaxseed) on estrogen receptor positive, MCF-7 and estrogen receptor negative, MDA-MB-231 cells. The extracts show potent activity on both the cell lines, hence, in silico studies have been carried out to find the possible reason for their activity. MAIN METHODS: MTT assay was carried to assess chemosensitization effect and activated caspase-3/7 activity was studied using flow-cytometry and western blotting...
September 15, 2017: Life Sciences
https://www.readbyqxmd.com/read/28677809/inhibition-of-aldose-reductase-ameliorates-alcoholic-liver-disease-by-activating-ampk-and-modulating-oxidative-stress-and-inflammatory-cytokines
#8
Changxuan Shi, Yuanfang Wang, Jing Gao, Si Chen, Xiangqian Zhao, Chengchao Cai, Chang Guo, Longxin Qiu
Aldose reductase (AR) expression is elevated in the livers of patients with alcoholic liver diseases. However, the role of AR in the development of alcoholic liver diseases remains unclear. The aim of the present study was to determine the effect of AR inhibition on ethanol‑induced hepatosteatosis in vivo and in vitro, and to identify possible underlying molecular mechanisms. Alcoholic fatty livers were induced in C57BL/6 mice by feeding the mice with Lieber‑DeCarli liquid diets. The expression of AR protein was elevated in the liver tissue of C57BL/6 mice fed with an ethanol diet and in mouse AML12 liver cells exposed to ethanol...
September 2017: Molecular Medicine Reports
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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...
June 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28406694/does-inhibition-of-aldose-reductase-contribute-to-the-anti-inflammatory-action-of-setipiprant
#18
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
#19
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
#20
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
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