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Aldose reductase inhibitor

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https://www.readbyqxmd.com/read/28194018/protective-role-of-fructokinase-blockade-in-the-pathogenesis-of-acute-kidney-injury-in-mice
#1
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
https://www.readbyqxmd.com/read/28192136/inhibition-of-glycation-and-aldose-reductase-activity-using-dietary-flavonoids-a-lens-organ-culture-studies
#2
Kapil K Patil, Rajesh N Gacche
On the eve of increasing incidence of diabetes mellitus and related complications, the search for novel, safe and alternatives therapeutic approaches are evolving. In the present investigation, a panel of ten dietary flavonoids such as 4'-methoxyflavanone, formononetin, hesperetin, hesperidin, naringenin, naringin, rutin, diadzin, silibinin and silymarin was evaluated as possible inhibitors of sugar induced cataractogenesis using bovine lens organ culture studies. The effect of selected flavonoids was observed on glycation induced lens opacity, AGE fluorescence, carbonyl group formation (a biomarker of glycation), protein aggregation and aldose reductase (AR) inhibition...
February 10, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28161411/structural-basis-for-the-inhibition-of-akr1b10-by-the-c3-brominated-ttnpb-derivative-uvi2008
#3
Francesc X Ruiz, Isidro Crespo, Susana Álvarez, Sergio Porté, Joan Giménez-Dejoz, Alexandra Cousido-Siah, André Mitschler, Ángel R de Lera, Xavier Parés, Alberto Podjarny, Jaume Farrés
UVI2008, a retinoic acid receptor (RAR) β/γ agonist originated from C3 bromine addition to the parent RAR pan-agonist 4-[(E)-2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)-1-propenyl]benzoic acid (TTNPB), is also a selective inhibitor of aldo-keto reductase family member 1B10 (AKR1B10). Thus, it might become a lead drug for the design of compounds targeting both activities, as an AKR1B10 inhibitor and RAR agonist, which could constitute a novel therapeutic approach against cancer and skin-related diseases...
February 1, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28159579/edible-vegetables-as-a-source-of-aldose-reductase-differential-inhibitors
#4
Francesco Balestri, Carlo Sorce, Roberta Moschini, Mario Cappiello, Livia Misuri, Antonella Del Corso, Umberto Mura
The hyperactivity of aldose reductase (AR) on glucose in diabetic conditions or on glutathionyl-hydroxynonenal in oxidative stress conditions, the source of cell damage and inflammation, appear to be balanced by the detoxifying action exerted by the enzyme. This detoxification acts on cytotoxic hydrophobic aldehydes deriving from membrane peroxidative processes. This may contribute to the failure in drug development for humans to favorably intervene in diabetic complications and inflammation, despite the specificity and high efficiency of several available aldose reductase inhibitors...
January 31, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28153595/phenolic-compounds-the-inhibition-effect-on-polyol-pathway-enzymes
#5
Hatice Esra Aslan, Şükrü Beydemir
The polyol pathway called as sorbitol way is a small part of glycose metabolism. The pathway is regarded as an important element in the pathogenesis of various diabetic complications in individuals with diabetes mellitus. The pathway plays a crucial role in hyperglycemia. The polyol pathway contains two enzymes as aldose reductase (AR) and sorbitol dehydrogenase (SDH). In the present study, AR and SDH were purified from sheep liver by using simple chromatographic methods. AR was purified with a yield of 2.11% and approximately 162 fold and SDH was purified with a yield of 0...
January 30, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28137510/influence-of-aldose-reductase-on-epithelial-to-mesenchymal-transition-signaling-in-lens-epithelial-cells
#6
Kun-Che Chang, Biehuoy Shieh, J Mark Petrash
Cataract is the most frequent cause of blindness worldwide and is treated by surgical removal of the opaque lens to restore the light path to the retina. While cataract surgery is a safe procedure, some patients develop a complication of the surgery involving opacification and wrinkling of the posterior lens capsule. This process, called posterior capsule opacification (PCO), requires a second clinical treatment that can in turn lead to additional complications. Prevention of PCO is a current unmet need in the vision care enterprise...
January 27, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28123157/olive-and-ginkgo-extracts-as-potential-cataract-therapy-with-differential-inhibitory-activity-on-aldose-reductase
#7
Diaaeldin Mohamed Abdelkawi Elimam, Ahmed Salah Uddin Ibrahim, Gregory Ing Liou, Farid Abd-Elrehim Abd-Elaziz Badria
Aldose reductase (AR) has been the leading target in the treatment of diabetic cataract. Although numerous synthetic AR inhibitors (ARI) have been identified, their adverse side effects currently preclude their use. Olive leaf extract (OLE) as well as ginkgo leaf extract (GLE) are natural supplements that have wide therapeutic indices and a plethora of salutary effects during diabetes that so far untested on sugar cataract progression. As such, the present study sought to evaluate the AR-inhibiting properties of OLE and GLE using the isolated enzyme from rabbit lens...
January 26, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28111996/inhibition-behaviours-of-some-phenolic-acids-on-rat-kidney-aldose-reductase-enzyme-an-in-vitro-study
#8
Zuhal Alim, Namik Kilinç, Bülent Şengül, Şükrü Beydemir
Aldose reductase (AR) inhibitors have vital importance in the treatment and prevention of diabetic complications. In this study, rat kidney AR was purified 19.34-fold with a yield of 3.49% and a specific activity of 0.88 U/mg using DE-52 Cellulose anion exchange chromatography, gel filtration chromatography and 2'5' ADP Sepharose-4B affinity chromatography, respectively. After purification, the in vitro inhibition effects of some phenolic acids (tannic acid, chlorogenic acid, sinapic acid, protocatechuic acid, 4-hydroxybenzoic acid, p-coumaric acid, ferulic acid, vanillic acid, syringic acid, α-resorcylic acid, 3-hydroxybenzoic acid and gallic acid) were investigated on purified enzyme...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28109789/synthesis-and-structure-activity-relationship-studies-of-phenolic-hydroxyl-derivatives-based-on-quinoxalinone-as-aldose-reductase-inhibitors-with-antioxidant-activity
#9
Xin Hao, Zhongfei Han, Yang Li, Chenying Li, Xing Wang, Xin Zhang, Qin Yang, Bing Ma, Changjin Zhu
To enhance aldose reductase (ALR2) inhibition and add antioxidant ability, phenolic hydroxyl was introduced both to the quinoxalinone core and C3 side chain, resulting in a series of derivatives as ALR2 inhibitors. Biological activity tests suggested that most of the derivatives were potent and selective inhibitors with IC50 values ranging from 0.059 to 6.825μM, and 2-(3-(4-hydroxystyryl)-7-methoxy-2-oxoquinoxalin-1(2H)-yl)acetic acid (6b) was the most active. Particularly, it was encouraging to find that some derivatives endowed with obvious antioxidant activity, and among them the phenolic 3,4-dihydroxyl compound 6f with 7-hydroxyl in the quinoxalinone core showed the most potent activity, even comparable with the well-known antioxidant Trolox...
January 11, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28057038/aldose-reductase-mediates-endothelial-cell-dysfunction-induced-by-high-uric-acid-concentrations
#10
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
#11
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/27942436/engineering-a-wild-type-diploid-saccharomyces-cerevisiae-strain-for-second-generation-bioethanol-production
#12
Hongxing Li, Yu Shen, Meiling Wu, Jin Hou, Chunlei Jiao, Zailu Li, Xinli Liu, Xiaoming Bao
BACKGROUND: The cost-effective production of second-generation bioethanol, which is made from lignocellulosic materials, has to face the following two problems: co-fermenting xylose with glucose and enhancing the strain's tolerance to lignocellulosic inhibitors. Based on our previous study, the wild-type diploid Saccharomyces cerevisiae strain BSIF with robustness and good xylose metabolism genetic background was used as a chassis for constructing efficient xylose-fermenting industrial strains...
2016: Bioresources and Bioprocessing
https://www.readbyqxmd.com/read/27835059/epalrestat-an-aldose-reductase-inhibitor-prevents-glucose-induced-toxicity-in-human-retinal-pigment-epithelial-cells-in-vitro
#13
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/27769036/green-fluorescent-protein-chromophore-derivatives-as-a-new-class-of-aldose-reductase-inhibitors
#14
Ryota Saito, Maiko Hoshi, Akihiro Kato, Chikako Ishikawa, Toshiya Komatsu
A number of (Z)-4-arylmethylene-1H-imidazol-5(4H)-ones, which are related to the fluorescent chromophore of the Aequorea green fluorescent protein (GFP), have been synthesized and evaluated their in vitro inhibitory activity against recombinant human aldose reductase for the first time. The GFP chromophore model 1a, with a p-hydroxy group on the 4-benzylidene and a carboxymethyl group on the N1 position, exhibited strong bioactivity with an IC50 value of 0.36 μM. This efficacy is higher than that of sorbinil, a known highly potent aldose reductase inhibitor...
January 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27685794/in-vitro-and-in-vivo-inhibition-of-aldose-reductase-and-advanced-glycation-end-products-by-phloretin-epigallocatechin-3-gallate-and-6-gingerol
#15
Chethan Sampath, Shengmin Sang, Mohamed Ahmedna
Hyperglycemic stress activates polyol pathway and aldose reductase (AR) key enzyme responsible for generating secondary complications during diabetes. In this study the therapeutic potential of phloretin, epigallocatechin 3-gallate (EGCG) and [6]-gingerol were evaluated for anti-glycating and AR inhibitory activity in vitro and in vivo systems. Human retinal pigment epithelial (HRPE) cells were induced with high glucose supplemented with the phloretin, EGCG and [6]-gingerol. Aldose reductase activity, total advanced glycation end products (AGEs) and enzyme inhibitor kinetics were assessed...
December 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27666634/pterin-7-carboxamides-as-a-new-class-of-aldose-reductase-inhibitors
#16
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/27639366/design-and-synthesis-of-chiral-2h-chromene-n-imidazolo-amino-acid-conjugates-as-aldose-reductase-inhibitors
#17
Gudipudi Gopinath, Venu Sankeshi, Shaym Perugu, Malini D Alaparthi, Srinivas Bandaru, Vijay K Pasala, Prasad Rao Chittineni, G L David Krupadanam, Someswar R Sagurthi
Aldose reductase (ALR2) inhibitors provide a viable mode to fight against diabetic complications. ALR2 exhibit plasticity in the active site vicinities and possible shifts in the nearby two supporting alpha helices. Therefore, a novel series of amino acid conjugates of chromene-3-imidazoles (13-15) were designed and synthesized based on natural isoflavonoids. The compounds were identified on the basis of spectral ((1)H NMR, (13)C NMR and MS) data and tested in vitro for ALR2 inhibitory activity with an IC50 value ranges from 0...
November 29, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27637378/construct-explicit-models-to-correlate-the-structure-and-the-inhibitory-activity-of-aldose-reductase-flavonoids-and-sulfonyl-pyridazinones-as-inhibitors
#18
Fengchao Cui, Lunyang Liu, Haifeng Tang, Kecheng Yang, Yunqi Li
The correlation between binding energies and bioactivities is the core of structure-based computer-aided drug design. However, many models to address this correlation are still strongly system-dependent at current stage. We constructed two explicit models to correlate the binding energies with the inhibitory activities of flavonoids and sulfonyl-pyridazinones as inhibitors of aldose reductase. The introduction of multiple complex states comprised of protein, coenzyme, substrate and inhibitor can remarkably improve the correlation coefficients, comparing with that using single complex state...
September 16, 2016: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/27544072/coumarin-thiazole-and-oxadiazole-derivatives-synthesis-bioactivity-and-docking-studies-for-aldose-aldehyde-reductase-inhibitors
#19
Aliya Ibrar, Yildiz Tehseen, Imtiaz Khan, Abdul Hameed, Aamer Saeed, Norbert Furtmann, Jürgen Bajorath, Jamshed Iqbal
In continuation of our previous efforts directed towards the development of potent and selective inhibitors of aldose reductase (ALR2), and to control the diabetes mellitus (DM), a chronic metabolic disease, we synthesized novel coumarin-thiazole 6(a-o) and coumarin-oxadiazole 11(a-h) hybrids and screened for their inhibitory activity against aldose reductase (ALR2), for the selectivity against aldehyde reductase (ALR1). Compounds were also screened against ALR1. Among the newly designed compounds, 6c, 11d, and 11g were selective inhibitors of ALR2...
October 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/27536992/sirt6-is-a-positive-regulator-of-aldose-reductase-expression-in-u937-and-hela-cells-under-osmotic-stress-in-vitro-and-in-silico-insights
#20
Ahmet Can Timucin, Huveyda Basaga
SIRT6 is a protein deacetylase, involved in various intracellular processes including suppression of glycolysis and DNA repair. Aldose Reductase (AR), first enzyme of polyol pathway, was proposed to be indirectly associated to these SIRT6 linked processes. Despite these associations, presence of SIRT6 based regulation of AR still remains ambiguous. Thus, regulation of AR expression by SIRT6 was investigated under hyperosmotic stress. A unique model of osmotic stress in U937 cells was used to demonstrate the presence of a potential link between SIRT6 and AR expression...
2016: PloS One
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