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aminoguanidine

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https://www.readbyqxmd.com/read/28274869/effective-inhibition-of-protein-glycation-by-combinatorial-usage-of-limonene-and-aminoguanidine-through-differential-and-synergistic-mechanisms
#1
Madhav M Joglekar, Laxman N Bavkar, Srinivas Sistla, Akalpita U Arvindekar
Protein glycation is a major mechanism for establishing secondary complication in diabetes mellitus. Effective inhibition of this process can prevent progression of the disorder into secondary complications. Aminoguanidine (AMG) and limonene (LM) are known protein glycation inhibitors. The aim of the present study was to demonstrate their differential mechanisms of action and to study whether combinatorial therapy can act synergistically and lower dosage, and thereby lower toxicity in treatment of secondary complications in diabetes...
March 6, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28255209/do-advanced-glycation-end-products-and-its-receptor-play-a-role-in-pathophysiology-of-hypertension
#2
REVIEW
Kailash Prasad, Manish Mishra
There is a close relationship between arterial stiffness and blood pressure. The studies suggest that the advanced glycation end products (AGEs) and its cell receptor (RAGE) are involved in the arterial stiffness in two ways: changes in arterial structure and vascular function. Plasma levels of AGEs and expression of RAGE are elevated, while the levels of soluble RAGE (sRAGE) and endogenous secretory RAGE (esRAGE) are lowered in patients with hypertension (HTN). There is a positive correlation between plasma levels of AGEs and arterial stiffness, and an inverse association between arterial stiffness/HTN, and serum levels of sRAGE and esRAGE...
March 2017: International Journal of Angiology: Official Publication of the International College of Angiology, Inc
https://www.readbyqxmd.com/read/28249208/diphenylurea-derivatives-for-combating-methicillin-and-vancomycin-resistant-staphylococcus-aureus
#3
Ibrahim H Eissa, Haroon Mohammad, Omar A Qassem, Waleed Younis, Tamer M Abdelghany, Ahmed Elshafeey, Mahmoud M Abd Rabo Moustafa, Mohamed N Seleem, Abdelrahman S Mayhoub
A new class of diphenylurea was identified as a novel antibacterial scaffold with an antibacterial spectrum that includes highly resistant staphylococcal isolates, namely methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA & VRSA). Starting with a lead compound 3 that carries an aminoguanidine functionality from one side and a n-butyl moiety on the other ring, several analogues were prepared. Considering the pharmacokinetic parameters as a key factor in structural optimization, the structure-activity-relationships (SARs) at the lipophilic side chain were rigorously examined leading to the discovery of the cycloheptyloxyl analogue 21n as a potential drug-candidate...
April 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28248504/phenylthiazole-antibacterial-agents-targeting-cell-wall-synthesis-exhibit-potent-activity-in-vitro-and-in-vivo-against-vancomycin-resistant-enterococci
#4
Haroon Mohammad, Waleed Younis, Lu Chen, Christine E Peters, Joe Pogliano, Kit Pogliano, Bruce R Cooper, Jianan Zhang, Abdelrahman S Mayhoub, Eric Oldfield, Mark S Cushman, Mohamed N Seleem
The emergence of antibiotic-resistant bacterial species, such as vancomycin-resistant enterococci (VRE), necessitates the development of new antimicrobials. Here, we investigate the spectrum of antibacterial activity of three phenylthiazole-substituted aminoguanidines. These compounds possess potent activity against VRE, inhibiting growth of clinical isolates at concentrations as low as 0.5 µg/mL. The compounds exerted a rapid bactericidal effect, targeting cell wall synthesis. Transposon mutagenesis suggested three possible targets: YubA, YubB (undecaprenyl diphosphate phosphatase (UPPP)) and YubD...
March 1, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28242543/multiple-pharmacological-targets-cytotoxicity-and-phytochemical-profile-of-aphloia-theiformis-vahl-benn
#5
Marie Carene Nancy Picot, Onur Bender, Arzu Atalay, Gokhan Zengin, Loïc Loffredo, Francis Hadji-Minaglou, Mohamad Fawzi Mahomoodally
Aphloia theiformis (Vahl.) Benn. (AT) is traditionally used in Sub-Saharan African countries including Mauritius as a biomedicine for the management of several diseases. However, there is a dearth of experimental studies to validate these claims. We endeavoured to evaluate the inhibitory effects of crude aqueous extract as traditionally used together with the crude methanol extracts of AT leaves on urease, angiotensin (I) converting enzyme (ACE), acetylcholinesterase (AChE), cholesterol esterase (CEase), glycogen phosphorylase a (GPa), and glycation in vitro...
February 24, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28242320/a-positive-feedback-loop-between-nitric-oxide-and-amyloid-%C3%AE-1-42-accelerates-mitochondrial-damage-in-human-lens-epithelial-cells
#6
Noriaki Nagai, Yoshimasa Ito, Teppei Shibata, Eri Kubo, Hiroshi Sasaki
We have reported that excessive nitric oxide (NO), like other reactive oxygen species (ROS), causes a decrease in cytochrome c oxidase (CCO) activity and ATP levels (mitochondrial damage) resulting in lens opacity. In addition, previous reports have shown that oxidative stress caused by ROS enhances amyloid β (Aβ) production in mammalian lenses, and that Aβ1-42 stimulates inducible nitric oxide synthase (iNOS) promoter activity. Based on these reports, we investigated the relationship between NO and Aβ1-42 production in human lens epithelial (HLE) cells...
April 15, 2017: Toxicology
https://www.readbyqxmd.com/read/28228071/a-rat-model-of-ischemic-enteritis-pathogenic-importance-of-enterobacteria-inos-no-and-cox-2-pge2
#7
Koji Takeuchi, Yoshino Komatsu, Yuka Nakamori, Tohru Kotani
BACKGROUND: We introduced a rat model of ischemic enteritis and investigated the roles of enterobacteria, nitric oxide (NO), and prostaglandins (PGs) in its pathogenesis. METHODS: Male rats were used after 18 h of fasting. Ischemic enteritis was induced by partial ligation of the superior mesenteric artery (SMA). Under ether anesthesia, SMA was isolated, and a stenosis was made by placing a needle (23 guage) on the vessel and ligating both the vessel and needle, and then a needle was removed from the ligature...
February 20, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28223158/aminoguanidine-alleviated-mma-induced-impairment-of-cognitive-ability-in-rats-by-downregulating-oxidative-stress-and-inflammatory-reaction
#8
Qiliang Li, Wenqi Song, Ze Tian, Peichang Wang
Methylmalonic acidemia (MMA) is the most common organic acidemia in childhood. Many "treated" patients continued to display various degrees of mental retardation and psychomotor delay, which could be caused by brain damage from elevated oxidative stress. Aminoguanidine (AG), a synthetic antioxidant, was tested in a MMA rat model for its potential therapeutic effects on memory impairment. The effects of AG on MMA-induced cognitive impairment in Wistar rats were evaluated with Morris Water Maze. The levels of nerve cell apoptosis and microglial activation were investigated to illustrate the mechanisms of the improvement of cognition with AG treatment in MMA rats...
February 13, 2017: Neurotoxicology
https://www.readbyqxmd.com/read/28150470/jakyakgamcho-tang-and-its-major-component-paeonia-lactiflora-exhibit-potent-anti-glycation-properties
#9
Junghyun Kim, Chan-Sik Kim, Young Sook Kim, Ik Soo Lee, Jin Sook Kim
Purpose: Advanced glycation end products (AGEs) have been implicated in the pathogenesis of diabetes and other age-related diseases. AGE inhibitors or breakers, such as aminoguanidine and alagebrium, have been proposed as therapeutic agents for AGE-related disorders. Jakyakgamcho-tang (JGT) is a well-known traditional herbal formula, which consists of the radix of Paeonia lactiflora Pallas (PR) and the radix and rhizome of Glycyrrhiza uralensis Fisch (GR). The purpose of this study was to evaluate the inhibitory and breaking activities of JGT, PR, and GR against AGEs...
December 31, 2016: Journal of Exercise Nutrition & Biochemistry
https://www.readbyqxmd.com/read/28132874/glycation-inhibitors-extend-yeast-chronological-lifespan-by-reducing-advanced-glycation-end-products-and-by-back-regulation-of-proteins-involved-in-mitochondrial-respiration
#10
Rubina S Kazi, Reema M Banarjee, Arati B Deshmukh, Gouri V Patil, Mashanipalya G Jagadeeshaprasad, Mahesh J Kulkarni
Advanced Glycation End products (AGEs) are implicated in aging process. Thus, reducing AGEs by using glycation inhibitors may help in attenuating the aging process. In this study using Saccharomyces cerevisiae yeast system, we show that Aminoguanidine (AMG), a well-known glycation inhibitor, decreases the AGE modification of proteins in non-calorie restriction (NR) (2% glucose) and extends chronological lifespan (CLS) similar to that of calorie restriction (CR) condition (0.5% glucose). Proteomic analysis revealed that AMG back regulates the expression of differentially expressed proteins especially those involved in mitochondrial respiration in NR condition, suggesting that it switches metabolism from fermentation to respiration, mimicking CR...
March 6, 2017: Journal of Proteomics
https://www.readbyqxmd.com/read/28122174/synthesis-qsar-studies-and-metabolic-stability-of-novel-2-alkylthio-4-chloro-n-5-oxo-4-5-dihydro-1-2-4-triazin-3-yl-benzenesulfonamide-derivatives-as-potential-anticancer-and-apoptosis-inducing-agents
#11
Beata Żołnowska, Jarosław Sławiński, Aneta Pogorzelska, Krzysztof Szafrański, Anna Kawiak, Grzegorz Stasiłojć, Mariusz Belka, Joanna Zielińska, Tomasz Bączek
A series of novel 2-alkylthio-4-chloro-N-(5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)benzenesulfonamide derivatives 12-46 have been synthesized by the reaction of aminoguanidines with an appropriate alpha-oxo-acids hydrates in glacial acetic acid. All the synthesized compounds were evaluated for their anticancer activity against HeLa, HCT-116, and MCF-7 human tumor cell lines. Two compounds 33 and 34 displayed outstanding cytotoxic effect selectively toward HeLa cancer cells (IC50  = 19 μm) and did not exhibit toxicity to the non-cancerous HaCaT cells...
January 25, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28105567/effects-of-oleuropein-on-pentylenetetrazol-induced-seizures-in-mice-involvement-of-opioidergic-and-nitrergic-systems
#12
Nastaran Rahimi, Bahram Delfan, Nazgol Motamed-Gorji, Ahmad R Dehpour
Oleuropein, a well-known olive polyphenol, has been shown to mediate neuroprotection in Alzheimer's disease and cerebral ischemia. We investigated the effects of oleuropein on pentylenetetrazole (PTZ)-induced seizures in male NMRI mice, with diazepam as the standard drug. We also examined the possible involvement of opioidergic/nitrergic pathways in the probable effects of oleuropein. Intraperitoneal (i.p.) administration of different doses of oleuropein (10, 20 and 30 mg/kg) significantly increased the seizure threshold 60 min prior to induction of seizure, in a dose-dependent manner...
January 19, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/28101475/anticonvulsive-effects-of-licofelone-on-status-epilepticus-induced-by-lithium-pilocarpine-in-wistar-rats-a-role-for-inducible-nitric-oxide-synthase
#13
Seyyed Majid Eslami, Mohammad Mobin Moradi, Mehdi Ghasemi, Ahmad Reza Dehpour
BACKGROUND AND PURPOSE: Status epilepticus (SE) is a neurological disorder with high prevalence and mortality rates, requiring immediate intervention. Licofelone is a cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitor, which its effectiveness to treat osteoarthritis has been approved. Increasing evidence suggests an involvement of COX and LOX enzymes in epileptic disorders. Thus, in the present study we investigate possible effects of licofelone on prevention and termination of SE...
December 2016: Journal of Epilepsy Research
https://www.readbyqxmd.com/read/28101189/inhibition-of-cytoskeletal-protein-carbonylation-may-protect-against-oxidative-damage-in-traumatic-brain-injury
#14
Qiusheng Zhang, Meng Zhang, Xianjian Huang, Xiaojia Liu, Weiping Li
Oxidative stress is the principal factor in traumatic brain injury (TBI) that initiates protracted neuronal dysfunction and remodeling. Cytoskeletal proteins are known to be carbonylated under oxidative stress; however, the complex molecular and cellular mechanisms of cytoskeletal protein carbonylation remain poorly understood. In the present study, the expression levels of glutathione (GSH) and thiobarbituric acid reactive substances (TBARS) were investigated in PC12 cells treated with H2O2. Western blot analysis was used to monitor the carbonylation levels of β-actin and β-tubulin...
December 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28099126/aminoguanidine-pretreatment-prevents-methotrexate-induced-small-intestinal-injury-in-the-rat-by-attenuating-nitrosative-stress-and-restoring-the-activities-of-vital-mitochondrial-enzymes
#15
Kasthuri Natarajan, Premila Abraham, Rekha Kota, Dhayakani Selvakumar
BACKGROUND: One of the major toxic side effects of methotrexate (MTX) is enterocolitis, for which there is no efficient standard treatment. Nitric oxide overproduction has been reported to play an important role in MTX-induced mucositis. This study was designed to investigate whether pretreatment with aminoguanidine (AG) - a selective iNOS inhibitor - prevents MTX-induced mucositis in rats. MATERIALS AND METHODS: Rats were pretreated with AG (30 and 50 mg/kg body weight) i...
January 18, 2017: Journal of Basic and Clinical Physiology and Pharmacology
https://www.readbyqxmd.com/read/28096959/the-effect-of-aminoguanidine-on-sperm-motility-and-mitochondrial-membrane-potential-in-varicocelized-rats
#16
Rafieh Alizadeh, Shadan Navid, Niloofar Abbasi, Abazar Yari, Zohreh Mazaheri, Erfan Daneshi, Ashok Agarwal, Mehdi Abbasi
OBJECTIVES: Increased levels of nitric oxide (NO) in the testicular veins of people suffering from varicocele have already been reported. However, the role of NO-synthase (NOS) isozymes and their inhibitors have not been extensively studied. We aimed to evaluate the inhibitory effects of aminoguanidine (AG), on sperm motility, vitality, and mitochondrial membrane potential (MMP) in varicocelized rats. MATERIALS AND METHODS: Twenty fore male Wister rats were divided into control, sham, varicocele, and treatment groups...
December 2016: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28077315/inhibition-of-inos-alleviates-cognitive-deficits-and-depression-in-diabetic-mice-through-downregulating-the-no-sgc-cgmp-pkg-signal-pathway
#17
Xiao Yan Zhou, Fang Zhang, Chang Jiang Ying, Jing Chen, Ling Chen, Jing Dong, Yue Shi, Mang Tang, Xiao Tong Hu, Zhi Hua Pan, Na Na Xu, Kui Yang Zheng, Ren Xian Tang, Yuan Jian Song
Diabetes mellitus often results in a number of complications involving impaired brain function, including cognitive deficits and depression. However, the potential mechanisms for diabetes-related cognitive deficits and depression are not fully understood. Neurons in the hippocampal, cortical and amygdala functional regions are more susceptible to damage during hyperglycemia. Neuroprotection in the brain can rescue cognitive deficits and depression induced by hyperglycemia. This study investigated the potential mechanisms underlying diabetes-related congnitive deficits and depression, determined whether the inflammatory factor inducible nitric oxide synthase (iNOS) and the nitric oxide (NO)/soluble guanylyl cyclases (sGC)/cyclic guanosine monophosphate (cGMP)/protein kinase G (PKG) pathway, play key roles in cognitive deficits and depression associated...
January 8, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28065581/nitric-oxide-synthase-inhibitor-aminoguanidine-reduces-intracerebroventricular-colchicine-induced-neurodegeneration-memory-impairments-and-changes-of-systemic-immune-responses-in-rats
#18
Susmita Sil, Tusharkanti Ghosh, Rupsa Ghosh, Pritha Gupta
Intracerebroventricular (i.c.v.) injection of colchicine induces neurodegeneration, memory impairments and changes of some systemic immune responses in rats. Though the role of cox 2 in these colchicine induced changes have been evaluated, the influence of nitric oxide synthase (NOS) remains to be studied. The present study was designed to assess the role of NOS on the i.c.v. colchicine induced neurodegeneration, memory impairments and changes of some systemic immune responses by inhibiting its activity with aminoguanidine...
December 13, 2016: Journal of Neuroimmunology
https://www.readbyqxmd.com/read/28055264/inos-inhibition-improves-autonomic-dysfunction-and-oxidative-status-in-hypertensive-obese-rats
#19
Natalia Veronez da Cunha, Fernanda Novi Cortegoso Lopes, Carolina Panis, Rubens Cecchini, Phileno Pinge-Filho, Marli Cardoso Martins-Pinge
It has been suggested that nitric oxide (NO) from iNOS source is involved in inflammation and oxidative stress, and hypertension in obese subjects involves an inflammatory process. However, no study evaluated the participation of iNOS inhibition on cardiovascular, autonomic, and inflammatory parameters in obese rats. Obesity was induced by the administration of 4 mg/g body weight of monosodium glutamate (MSG) or equimolar saline (CTR) in newborn rats. On the 60th day, treatment with aminoguanidine (Amino, 50 mg/kg), an iNOS inhibitor, or 0...
2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28025796/ifn-%C3%AE-regulates-xanthine-oxidase-mediated-inos-independent-oxidative-stress-in-maneb-and-paraquat-treated-rat-polymorphonuclear-leukocytes
#20
Deepali Singh, Vinod Kumar, Chetna Singh
Maneb (MB) and paraquat (PQ) provoke oxidative stress-mediated cell damage. Role of xanthine oxidase (XO) in oxidative stress and its association with nitric oxide (NO)/NO synthase (NOS) have been widely reported. While inducible NOS (iNOS) is implicated in MB+PQ-induced toxicity in rat polymorphonuclear leukocytes (PMNs), role of XO and its alliance with iNOS have not yet been established. The study investigated the role of XO in MB+PQ-induced oxidative stress in rat PMNs and its regulation by iNOS and inflammatory cytokines...
March 2017: Molecular and Cellular Biochemistry
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