Read by QxMD icon Read


Yahia N Mabkhot, Mohammed M Alharbi, Salim S Al-Showiman, Hazem A Ghabbour, Nabila A Kheder, Saied M Soliman, Wolfgang Frey
BACKGROUND: The synthesis of new thiazole derivatives is very important because of their diverse biological activities. Also , many drugs containing thiazole ring in their skeletons are available in the market such as Abafungin, Acotiamide, Alagebrium, Amiphenazole, Brecanavir, Carumonam, Cefepime, and Cefmatilen. RESULTS: Ethyl cyanoacetate reacted with phenylisothiocyanate, chloroacetone, in two different basic mediums to afford the thiazole derivative 6, which reacted with dimethylformamide- dimethyl acetal in the presence of DMF to afford the unexpected thiazole derivative 11...
May 11, 2018: Chemistry Central Journal
Cigdem Toprak, Basar Sirmagul, Semra Yigitaslan
Objective: In our study, the effects of glycosylated protein cross-link breaker, alagebrium was investigated on isolated rat carotid artery using myography. Alagebrium showed vasodilator effect on carotid artery rings; particularly, this effect was significantly increased in endothelium-intact rings. Materials and Methods: To clarify the vasodilator mechanism of alagebrium, different antagonists such as N(G)-Nitro-L-arginine methyl ester (L-NAME), glibenclamide, indomethacin, metoprolol, propranolol, tetraethylammonium, and calcium channel activator BAYK-8644 were used to reverse this effect...
October 2017: Eurasian Journal of Medicine
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
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
Shengke Li, Yuan-Fu Ding, Hang Yin, Chunming Wang, David Bardelang, Lian-Hui Wang, Ruibing Wang
As determined by both1 H NMR and UV/Vis spectroscopic titration, ESI-MS, isothermal titration calorimetry, and DFT molecular modeling, advanced glycation end products (AGE) breaker alagebrium (ALA) formed 1:1 guest-host inclusion complexes with cucurbit[7]uril (CB[7]), with a binding affinity, Ka , in the order of magnitude of 105  m-1 , thermodynamically driven by both enthalpy (ΔH=-6.79 kcal mol-1 ) and entropy (TΔS=1.21 kcal mol-1 ). For the first time, a dramatic inhibition of keto-enol tautomerism of the carbonyl α-hydrogen of ALA has been observed, as evidenced by over an order of magnitude decrease of both the first step rate constant, k1 , and the second step rate constant, k2 , during hydrogen/deuterium exchange in D2 O...
November 7, 2016: Chemistry, An Asian Journal
Arti Dhar, Mary Priyanka Udumula, Brahmam Medapi, Audesh Bhat, Indu Dhar, Prasanthi Malapati, Mangali Suresh Babu, Jaspreet Kalra, Dharamrajan Sriram, Kaushik M Desai
BACKGROUND: Methylglyoxal (MG) is a byproduct of glucose metabolism and an inducer of advanced glycation end products (AGEs). AGEs are implicated in the pathogenesis of diabetes as well as hypertension. Most of the currently available MG scavengers are non-specific and have other effects as well. Alagebrium (ALA), developed by Alteon Corporation is a MG scavenger. Thus the aim of the present study was to investigate the potential of novel ALA analogs as possible MG scavengers and whether they could prevent any deleterious effects of MG...
November 15, 2016: International Journal of Cardiology
Graeme Carrick-Ranson, Naoki Fujimoto, Keri M Shafer, Jeffrey L Hastings, Shigeki Shibata, M Dean Palmer, Kara Boyd, Benjamin D Levine
Sedentary aging leads to left ventricular (LV) and vascular stiffening due in part to advanced glycation end-products (AGEs) cross-linking of extracellular matrix proteins. Vigorous lifelong exercise ameliorates age-related cardiovascular (CV) stiffening and enhances exercise LV function, although this effect is limited when exercise is initiated later in life. We hypothesized that exercise training might be more effective at improving the impact of age-related CV stiffening during exercise when combined with an AGE cross-link breaker (Alagebrium)...
August 1, 2016: Journal of Applied Physiology
Danielle J Borg, Josephine M Forbes
Advanced glycation end products (AGEs) are the final products of the Maillard reaction, a complex process that has been studied by food chemists for a century. Over the past 30 years, the biological significance of advanced glycation has also been discovered. There is mounting evidence that advanced glycation plays a homeostatic role within the body and that food-related Maillard products, intermediates such as reactive α-dicarbonyl compounds and AGEs, may influence this process. It remains to be understood, at what point AGEs and their intermediates become pathogenic and contribute to the pathogenesis of chronic diseases that inflict current society...
August 2016: Glycoconjugate Journal
Özlem Atlı, Sinem Ilgın, Bülent Ergun, Dilek Burukoğlu, Ahmet Musmul, Başar Sırmagül
OBJECTIVE: In our study, sildenafil alone and everolimus or alagebrium in combination with sildenafil were investigated in terms of their additional therapeutic and anti-remodeling activity in monocrotaline-induced pulmonary hypertension (PH) model in rats. In particular, the inter-relationships between PH and matrix metalloproteinases (MMPs) were investigated. METHODS: The pulmonary artery responses of male Sprague Dawley rats were recorded using myography, and the quantities and activities of MMPs were analyzed in homogenates of the pulmonary arteries and lungs by enzyme-linked immunosorbent assays, activity assays, and gelatin zymography techniques...
January 2017: Anatolian Journal of Cardiology
Arti Dhar, Indu Dhar, Audesh Bhat, Kaushik M Desai
AIM: Diabetes mellitus associated cardiovascular complications are a leading cause of morbidity and mortality worldwide. Methylglyoxal (MG) is a reactive ketoaldehyde and a byproduct of glucose metabolism and an inducer of advanced glycation endproducts (AGEs). Alagebrium (ALA) is an AGEs crosslink breaker, however, the effects of ALA on MG levels and its consequences in cultured rat cardiomyocytes are not known. The aim of the present study was to examine the effect of high glucose and MG on cultured rat cardiomyocytes and to investigate whether ALA could prevent any deleterious effects of high glucose and MG in these cells...
February 1, 2016: Life Sciences
Chen-Yuan Chiu, Rong-Sen Yang, Meei-Ling Sheu, Ding-Cheng Chan, Ting-Hua Yang, Keh-Sung Tsai, Chih-Kang Chiang, Shing-Hwa Liu
Diabetic myopathy, a less studied complication of diabetes, exhibits the clinical observations characterized by a less muscle mass, muscle weakness and a reduced physical functional capacity. Accumulation of advanced glycation end-products (AGEs), known to play a role in diabetic complications, has been identified in ageing human skeletal muscles. However, the role of AGEs in diabetic myopathy remains unclear. Here, we investigated the effects of AGEs on myogenic differentiation and muscle atrophy in vivo and in vitro...
February 2016: Journal of Pathology
Marion J Siegman, Masumi Eto, Thomas M Butler
This study seeks to define and explain remodeling of the distal colon in the streptozotocin (STZ)-treated rat model of diabetes through analysis of resting and active length dependence of force production, chemical composition, and ultrastructure. Compared with untreated controls, the passive stiffness on extension of the diabetic muscle is high, and active force produced at short muscle lengths is amplified but is limited by an internal resistance to shortening. The latter are accounted for by a significant increase in collagen type 1, with no changes in types 3 and 4...
January 15, 2016: American Journal of Physiology. Cell Physiology
Mohamed Naguib Zakaria, Hany M El-Bassossy, Waleed Barakat
Diabetes is a chronic endocrine disorder associated with several complications as hypertension, advanced brain aging, and cognitive decline. Accumulation of advanced glycation end products (AGEs) is an important mechanism that mediates diabetic complications. Upon binding to their receptor (RAGE), AGEs mediate oxidative stress and/or cause cross-linking with proteins in blood vessels and brain tissues. The current investigation was designed to investigate the effect of agents that decrease AGEs signaling, perindopril which increases soluble RAGE (sRAGE) and alagebrium which cleaves AGEs cross-links, compared to the standard antidiabetic drug, gliclazide, on the vascular and central nervous system (CNS) complications in STZ-induced (50 mg/kg, IP) diabetes in rats...
2015: Advances in Pharmacological Sciences
Antonio Nenna, Francesco Nappi, Sanjeet Singh Avtaar Singh, Fraser W Sutherland, Fabio Di Domenico, Massimo Chello, Cristiano Spadaccio
CONTEXT: Advanced Glycation End-Products (AGEs) are signaling proteins associated to several vascular and neurological complications in diabetic and non-diabetic patients. AGEs proved to be a marker of negative outcome in both diabetes management and surgical procedures in these patients. The reported role of AGEs prompted the development of pharmacological inhibitors of their effects, giving rise to a number of both preclinical and clinical studies. Clinical trials with anti-AGEs drugs have been gradually developed and this review aimed to summarize most relevant reports...
May 2015: Research in Cardiovascular Medicine
Hongfeng Wang, Dorothee Weihrauch, Judy R Kersten, Jeffrey M Toth, Anthony G Passerini, Anita Rajamani, Sonja Schrepfer, John F LaDisa
Mechanisms of restenosis in type 2 diabetes mellitus (T2DM) are incompletely elucidated, but advanced glycation end-product (AGE)-induced vascular remodeling likely contributes. We tested the hypothesis that AGE-related collagen cross-linking (ARCC) leads to increased downstream vascular resistance and altered in-stent hemodynamics, thereby promoting neointimal hyperplasia (NH) in T2DM. We proposed that decreasing ARCC with ALT-711 (Alagebrium) would mitigate this response. Abdominal aortic stents were implanted in Zucker lean (ZL), obese (ZO), and diabetic (ZD) rats...
October 2015: American Journal of Physiology. Heart and Circulatory Physiology
Sébastien Cadau, Sabrina Leoty-Okombi, Sabine Pain, Nicolas Bechetoille, Valérie André-Frei, François Berthod
Glycation is one of the major processes responsible for skin aging through induction of the detrimental formation of advanced glycation end-products (AGEs). We developed an innovative tissue-engineered skin combining both a capillary-like and a nerve networks and designed a protocol to induce continuous AGEs formation by a treatment with glyoxal. We determined the optimal concentration of glyoxal to induce AGEs formation identified by carboxymethyl-lysin expression while keeping their toxic effects low. We showed that our tissue-engineered skin cultured for 44 days and treated with 200 μm glyoxal for 31 days displayed high carboxymethyl-lysine expression, which induced a progressively increased alteration of its capillary and nerve networks between 28 and 44 days...
May 2015: Biomaterials
Junghyun Kim, Chan-Sik Kim, Min Kyong Moon, Jin Sook Kim
The accumulation of advanced glycation end products (AGEs) is associated with many of the complications of diabetes mellitus, including diabetic retinopathy. AGE-breakers, such as N-phenacylthiazolium and alagebrium, have been proposed as therapeutic agents for reversing the increase in protein crosslinking in diabetes. (-)-Epicatechin is a major dietary flavonoid with a wide range of health-promoting biological activities. The aim of this study was to determine the potential effect of (-)-epicatechin in reducing the burden of AGEs in vitro and in vivo and to evaluate whether the reduced AGE burden could translate into improvement in retinal vascular function in exogenously AGE-injected rats...
February 5, 2015: European Journal of Pharmacology
Michiaki Miyamoto, Kazuhiko Kotani, Nobuyuki Taniguchi
Hypertension (HTN) is a major risk factor for atherosclerosis. Flow-mediated vasodilation (FMD) is an ultrasonic method used to evaluate endothelial function, which is associated with HTN and related complications. We summarized clinical trials focusing on the effects of non-antihypertensive drugs on endothelial function, as evaluated by FMD, in patients with HTN. Hypercholesterolemic patients with HTN who used the cholesterol- lowering drugs HMG-CoA reductase inhibitors (statins) had improved FMD with a reduction in cholesterol levels and no significant change in blood pressure (BP)...
2015: Current Vascular Pharmacology
Bing Zhang, Kunlun He, Wei Chen, Xianfa Cheng, Hao Cui, Wu Zhong, Song Li, Lili Wang
Combining drugs with complementary mechanisms of action may contribute to improved hypertension control in diabetic patients. Advanced glycation end-product (AGE) breakers, a new class of candidate drugs targeting aging-related cardiovascular dysfunction, may be useful as novel adjuvant agents to improve the efficacy of diabetic hypertension (DH) treatment. This study evaluated the effects of alagebrium (ALT-711), an AGE breaker, combined with nifedipine, a Ca(2+) channel blocker, in a rat model of streptozotocin-induced DH...
October 2014: Hypertension Research: Official Journal of the Japanese Society of Hypertension
Madelijn H Oudegeest-Sander, Marcel G M Olde Rikkert, Paul Smits, Dick H J Thijssen, Arie P J van Dijk, Benjamin D Levine, Maria T E Hopman
Aging leads to accumulation of irreversible advanced glycation end-products (AGEs), contributing to vascular stiffening and endothelial dysfunction. When combined with the AGE-crosslink breaker Alagebrium, exercise training reverses cardiovascular aging in experimental animals. This study is the first to examine the effect of Alagebrium, with and without exercise training, on endothelial function, arterial stiffness and cardiovascular risk in older individuals. Forty-eight non-exercising individuals (mean age 70±4years) without manifest diseases or use of medication were allocated into 4 groups for a 1-year intervention: Exercise training & Alagebrium (200mg/day); Exercise training & placebo; No exercise training & Alagebrium (200mg/day); No exercise training & placebo...
October 26, 2013: Experimental Gerontology
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"