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Aldose reductase inhibitor

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https://www.readbyqxmd.com/read/29142407/molecular-docking-analysis-of-phytic-acid-and-4-hydroxyisoleucine-as-cyclooxygenase-2-microsomal-prostaglandin-e-synthase-2-tyrosinase-human-neutrophil-elastase-matrix-metalloproteinase-2-and-9-xanthine-oxidase-squalene-synthase-nitric-oxide-synthase-human
#1
Radhakrishnan Narayanaswamy, Lam Kok Wai, Norhaizan Mohd Esa
Background: The phytoconstituents phytic acid and 4-hydroxyisoleucine have been reported to posses various biological properties. Objective: This prompted us to carry out the docking study on these two ligands (phytic acid & 4-hydroxyisoleucine) against eleven targeted enzymes. Materials and Methods: Phytic acid & 4-hydroxyisoleucine were evaluated on the docking behaviour of cyclooxygenase-2 (COX-2), microsomal prostaglandin E synthase-2 (mPGES-2), tyrosinase, human neutrophil elastase (HNE), matrix metalloproteinase (MMP 2 and 9), xanthine oxidase (XO), squalene synthase (SQS), nitric oxide synthase (NOS), human aldose reductase (HAR) and lipoxygenase (LOX) using Discovery Studio Version 3...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29098865/novel-quinazolinone-based-2-4-thiazolidinedione-3-acetic-acid-derivatives-as-potent-aldose-reductase-inhibitors
#2
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
#3
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/29074349/structure-optimization-of-tetrahydropyridoindole-based-aldose-reductase-inhibitors-improved-their-efficacy-and-selectivity
#4
Magdalena Majekova, Jana Ballekova, Marta Prnova, Milan Stefek
In our previous study, tetrahydropyridoindoles carboxymethylated in position 8 were identified as aldose reductase (ALR2) inhibitors with mild efficacy and selectivity yet with significant antioxidant activity. In the present study we proceeded with optimization of the tetrahydropyridoindole scaffold by shifting the carboxymethyl pharmacophore from position 8 to position 5, with the aim to improve the biological activity. Commercial databases were screened for the presence of tetrahydropyridoindoles carboxymethylated in position 5 and an experimental set of eight compounds was created...
October 16, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29056677/effect-of-oral-alpha-lipoic-acid-in-preventing-the-genesis-of-canine-diabetic-cataract-a-preliminary-study
#5
David L Williams
Blinding cataract is a significant effect of canine diabetes with 75% of animals affected two years after diagnosis. Lens opacification occurs primarily through the generation of sorbitol, a sugar alcohol, through the action of aldose reductase (AR). The osmotic effect of sorbitol draws water into the lens, causing opacification. Inhibition of AR should thus prevent the generation of cataracts. A topical AR inhibitor has been shown to have this effect, as has the commercially available neutraceutical OcuGLO, containing the AR inhibitor alpha lipoic acid (ALA) together with other plant-based antioxidants...
March 16, 2017: Veterinary Sciences
https://www.readbyqxmd.com/read/29038789/diosgenin-a-novel-aldose-reductase-inhibitor-attenuates-the-galactosemic-cataract-in-rats
#6
Lixia Ji, Lixia Cheng, Zhihong Yang
OBJECTIVE: To seek efficient aldose reductase inhibitors (ARIs) with excellent in vitro and in vivo biological activities against rat galactosemic cataract. METHODS: The method was firstly optimized to screen strong ARIs from nonoriented synthetic compounds and natural extracts. Then, diosgenin was assessed on osmotic expansion of primarily cultured lens epithelial cells (LECs) induced by galactose (50 mM). Diosgenin was administered to galactosemic rats by oral (100 and 200 mg/kg) or direct drinking (0...
2017: Journal of Diabetes Research
https://www.readbyqxmd.com/read/28986187/aldose-reductase-inhibitor-fidarestat-regulates-mitochondrial-biogenesis-via-nrf2-ho-1-ampk-pathway-in-colon-cancer-cells
#7
Kirtikar Shukla, Himangshu Sonowal, Ashish Saxena, Kota V Ramana, Satish K Srivastava
Although we have shown earlier that aldose reductase (AR) inhibitors prevent colorectal cancer cell (CRC) growth in culture as well as in nude mice xenografts, the mechanism(s) is not well understood. In this study, we have investigated how AR inhibition prevents CRC growth by regulating the mitochondrial biogenesis via Nrf2/HO-1 pathway. Incubation of CRC cells such as SW-480, HT29, and HCT116 with AR inhibitor, fidarestat that non-covalently binds to the enzyme, increases the expression of Nrf2. Further, fidarestat augmented the EGF-induced expression of Nrf2 in CRC cells...
December 28, 2017: Cancer Letters
https://www.readbyqxmd.com/read/28976752/synthesis-of-potent-and-selective-inhibitors-of-aldo-keto-reductase-1b10-and-their-efficacy-against-proliferation-metastasis-and-cisplatin-resistance-of-lung-cancer-cells
#8
Satoshi Endo, Shuang Xia, Miho Suyama, Yoshifumi Morikawa, Hiroaki Oguri, Dawei Hu, Yoshinori Ao, Satoyuki Takahara, Yoshikazu Horino, Yoshihiro Hayakawa, Yurie Watanabe, Hiroaki Gouda, Akira Hara, Kazuo Kuwata, Naoki Toyooka, Toshiyuki Matsunaga, Akira Ikari
Aldo-keto reductase 1B10 (AKR1B10) is overexpressed in several extraintestinal cancers, particularly in non-small-cell lung cancer, where AKR1B10 is a potential diagnostic marker and therapeutic target. Selective AKR1B10 inhibitors are required because compounds should not inhibit the highly related aldose reductase that is involved in monosaccharide and prostaglandin metabolism. Currently, 7-hydroxy-2-(4-methoxyphenylimino)-2H-chromene-3-carboxylic acid benzylamide (HMPC) is known to be the most potent competitive inhibitor of AKR1B10, but it is nonselective...
October 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28938395/aldose-reductase-mediates-nlrp3-inflammasome-initiated-innate-immune-response-in-hyperglycemia-induced-thp1-monocytes-and-male-mice
#9
Pabitra B Pal, Himangshu Sonowal, Kirtikar Shukla, Satish K Srivastava, Kota V Ramana
Despite recent studies that show oxidative stress-generated reactive oxygen species (ROS) regulate NOD-like receptor family pyrin domain containing 3 (NLRP3) inflammasome-mediated innate immune response in various diabetic complications, the mechanism by which ROS activate innate immune response is not well understood. We have shown previously that aldose reductase (AR), besides reducing glucose, reduces lipid aldehydes and their glutathione conjugates and participates in various oxidative stress-induced inflammatory pathways...
October 1, 2017: Endocrinology
https://www.readbyqxmd.com/read/28935265/quinazolinone-based-rhodanine-3-acetic-acids-as-potent-aldose-reductase-inhibitors-synthesis-functional-evaluation-and-molecular-modeling-study
#10
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/28917123/identification-of-new-potent-inhibitor-of-aldose-reductase-from-ocimum-basilicum
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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