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https://www.readbyqxmd.com/read/28651259/new-biguanides-as-anti-diabetic-agents-part-i-synthesis-and-evaluation-of-1-substituted-biguanide-derivatives-as-anti-diabetic-agents-of-type-ii-diabetes-insulin-resistant
#1
Samir Y Abbas, Wahid M Basyouni, Khairy A M El-Bayouk, Wael M Tohamy, Hanan F Aly, Azza Arafa, Mahmoud S Soliman
New 1-substituted-biguanide hydrochloride salts were synthesized via reacting benzo[1,3-d]dioxol-5-amine, phenylhydrazine, N,N-dimethylhydrazinecarboxamide, benzohydrazide and 2-phenyl acetohydrazide with dicyandiamide in acidic medium. Structures of the obtained biguanide salts were characterized by spectroscopic tools. The synthesized compounds were screened for their anti-diabetic activity with standard metformin drug. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives significantly decreased the elevated blood glucose level...
June 26, 2017: Drug Research
https://www.readbyqxmd.com/read/28649285/introduction-of-the-diagene-study-clinical-characteristics-pathophysiology-and-determinants-of-vascular-complications-of-type-2-diabetes
#2
Thijs T W van Herpt, Roosmarijn F H Lemmers, Mandy van Hoek, Janneke G Langendonk, Ronald J Erdtsieck, Bert Bravenboer, Annelies Lucas, Monique T Mulder, Harm R Haak, Aloysius G Lieverse, Eric J G Sijbrands
BACKGROUND: Type 2 diabetes is a major healthcare problem. Glucose-, lipid-, and blood pressure-lowering strategies decrease the risk of micro- and macrovascular complications. However, a substantial residual risk remains. To unravel the etiology of type 2 diabetes and its complications, large-scale, well-phenotyped studies with prospective follow-up are needed. This is the goal of the DiaGene study. In this manuscript, we describe the design and baseline characteristics of the study...
2017: Diabetology & Metabolic Syndrome
https://www.readbyqxmd.com/read/28647361/apolipoprotein-o-expression-in-mouse-liver-enhances-hepatic-lipid-accumulation-by-impairing-mitochondrial-function
#3
Feng Tian, Chen-Lu Wu, Bi-Lian Yu, Ling Liu, Jia-Rui Hu
Apolipoprotein O (ApoO) was recently observed in the cellular mitochondrial inner membrane, which plays a role in mitochondrial function and is associated with myocardiopathy. Empirical information on the physiological functions of apoO is therefore limited. In this study, we aimed to elucidate the effect of apoO on hepatic fatty acid metabolism. An adenoviral vector expressing hApoO was constructed and introduced into chow diet and high-fat diet induced mice and the L02 human hepatoma cell line. High levels of hApoO mRNA and protein were detected in the liver, and the expression of lipid metabolism genes was significantly altered compared with negative controls...
June 21, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28644091/prevention-of-cardiovascular-disease-in-patients-with-familial-hypercholesterolaemia-the-role-of-pcsk9-inhibitors
#4
Ivan Pećin, Merel L Hartgers, G Kees Hovingh, Ricardo Dent, Željko Reiner
Familial hypercholesterolaemia is an autosomal dominant inherited disorder characterised by elevated low-density lipoprotein cholesterol levels and consequently an increased risk of atherosclerotic cardiovascular disease (ASCVD). Familial hypercholesterolaemia is relatively common, but is often underdiagnosed and undertreated. Cardiologists are likely to encounter many individuals with familial hypercholesterolaemia; however, patients presenting with premature ASCVD are rarely screened for familial hypercholesterolaemia and fasting lipid levels are infrequently documented...
January 1, 2017: European Journal of Preventive Cardiology
https://www.readbyqxmd.com/read/28642135/light-is-increased-in-patients-with-coronary-disease-and-regulates-inflammatory-response-and-lipid-metabolism-in-oxldl-induced-thp-1-macrophages
#5
Xiaomei Yuan, Yonglin Gu, Xiaoyu Lai, Qing Gu
Inflammation is critical for the progression of hyperlipidemia. Although the exact mechanism through which inflammation affects hyperlipidemia is not very clear, evidence suggests that the tumor necrosis factor superfamily member 14 (TNFSF14/LIGHT)LIGHT might regulate lipid metabolism. In this study we investigated the expression of LIGHT in patients with different stages of coronary disease. The expression of lipid metabolism-related enzymes and inflammation-related proteins were further explored in oxidized low-density lipoproteins (oxLDL)-induced THP-1 macrophages...
June 19, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28638928/-fat-deposition-in-skeletal-muscle-and-its-regulation
#6
Li-Fang Zheng, Pei-Jie Chen, Yong-Zhan Zhou, Wei-Hua Xiao
Under normal condition, there are a few lipid droplets in skeletal muscle. But in skeletal muscle acute injury, muscular dystrophy, muscle atrophy, obesity, diabetes and other pathological conditions, the fat deposition in skeletal muscle increases, which implicate that the fat deposition may play an important role in the pathogenesis of these diseases. However, the mechanisms of development and regulation of fat deposition in skeletal muscle are not clear. Clarifying the key signaling pathways and regulatory factors that affect fat deposition in skeletal muscle, and exploring new ways to improve the fat deposition in skeletal muscle will not only help to deepen our understanding of the pathogenesis of these diseases, but also provide new ideas for the treatment of these diseases...
June 25, 2017: Sheng Li Xue Bao: [Acta Physiologica Sinica]
https://www.readbyqxmd.com/read/28630182/study-of-biodistribution-and-in-vivo-anti-leishmanial-activity-of-a-distigmasterylhemisuccinoyl-glycero-phosphocholine-liposome-intercalated-amphotericin-b
#7
Maryam Iman, Zhaohua Huang, Seyedeh Hoda Alavizadeh, Francis C Szoka, Mahmoud R Jaafari
Distigmasterylhemisuccinoyl-sn-glycero-3- phosphocholine (DSHemsPC) is a new lipid in which two molecules of stigmasterol (an inexpensive plant sterol) are covalently linked via a succinic acid to glycerophosphocholine. Our previous study revealed that a liposome-intercalated Amphotericin B prepared from DSHemsPC (DSHemsPC-Lip-AmB) possess excellent colloidal properties and in vitro antifungal and anti-leishmanial activity similar to AmBisome™. The aim of this study was to determine biodistribution and evaluate the anti-leishmanial effects of DSHemsPC-Lip-AmB in Leishmania major-infected BALB/c mice...
June 19, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28629388/the-albumin-exendin-4-recombinant-protein-e2hsa-improves-glycemic-control-and-%C3%AE-cell-function-in-spontaneous-diabetic-kkay-mice
#8
Caina Li, Shaocong Hou, Shuainan Liu, Yi Huan, Sujuan Sun, Quan Liu, Zhufang Shen
BACKGROUND: E2HSA is a genetic fusion protein that consists of two tandem exendin-4 molecules that are covalently bonded to recombinant human serum albumin via a peptide linker. Previous studies have demonstrated that E2HSA significantly decreased blood glucose levels, improved β-cell function and promoted β-cell proliferation in diabetic db/dB mice. This study aimed to evaluate the benefits of E2HSA on glucose and lipid metabolism in a spontaneous diabetes animal model, KKAy mice. METHODS: E2HSA was acutely administered at doses of 1, 3 and 9 mg/kg by subcutaneous injection in diabetic KKAy mice with exendin-4 (2 μg/kg) as a positive reference, and then the non-fasting blood glucose and food intake levels were dynamically monitored...
June 19, 2017: BMC Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28627930/randomized-comparative-efficacy-and-safety-study-of-intermittent-simvastatin-versus-fenofibrate-in-hemodialysis
#9
Aya M Abdel Magid, Maggie M Abbassi, Essam Eldin M Iskander, Osama Mohamady, Samar F Farid
AIM: Compare the safety and efficacy of intermittent fenofibrate versus simvastatin in chronic hemodialysis patients. PATIENTS & METHODS: Sixty patients received either fenofibrate 100 mg or simvastatin 20 mg after their dialysis session (parallel study). The safety and efficacy of drugs on lipid profile, oxidized low-density lipoprotein (Ox-LDL), glutathione peroxidase and C-reactive protein were compared before and after 16-week treatment. RESULTS: After treatment, significant increase in glutathione peroxidase, significant decrease in total cholesterol, triglycerides, low density lipoprotein (LDL) and ox-LDL (p < 0...
June 19, 2017: Journal of Comparative Effectiveness Research
https://www.readbyqxmd.com/read/28627773/oleanolic-acid-derivative-dks26-exerts-antidiabetic-and-hepatoprotective-effects-in-diabetic-mice-and-promotes-glp-1-secretion-and-expression-in-intestinal-cells
#10
Fei-Fei Chen, Jian-Ta Wang, Li-Xia Zhang, Shu-Fang Xing, Yun-Xia Wang, Kai Wang, Shu-Li Deng, Ji-Quan Zhang, Lei Tang, Hao-Shu Wu
BACKGROUND AND PURPOSE: Glucagon-like peptide-1 (GLP-1) is an important target for diabetes therapy based on its key role in maintaining glucose and lipid homeostasis. This study was designed to investigate antidiabetic and hepatoprotective effects of novel oleanolic acid derivative DKS26 in diabetic mice and elucidate its underlying GLP-1 related antidiabetic mechanisms in vitro and in vivo. EXPERIMENTAL APPROACH: The therapeutic effects of DKS26 were inspected in streptozotocin (STZ)-induced and db/db diabetic mouse models including levels of plasma glucose, glycosylated serum protein (GSP), lipid profiles, insulin, alanine aminotransferase (ALT) and aspartate aminotransferase (AST), oral glucose tolerance (OGT), pancreatic islets and hepatic histopathological morphology, liver lipid levels and expression of pro-inflammation cytokines...
June 19, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28627427/144-week-efficacy-and-safety-of-a-once-daily-single-tablet-regimen-of-tenofovir-lamivudine-and-efavirenz-among-arv-na%C3%A3-ve-and-arv-experienced-hiv-1-infected-thai-adults
#11
Anchalee Avihingsanon, Wirach Maek-A-Nantawat, Sivaporn Gatechompol, Vorapot Sapsirisavat, Wanida Thiansanguankul, Jiratchaya Sophonphan, Narujakorn Thammajaruk, Sasiwimol Ubolyam, David M Burger, Kiat Ruxrungtham
OBJECTIVES: To assess the efficacy and safety of a new single tablet regimen(STR) of tenofovir disoproxil fumarate(TDF) 300mg, lamivudine(3TC) 300mg and efavirenz(EFV) 600mg in HIV-infected Thais. METHODS: This was a 144 week, prospective study among 51 treatment naïve and 49 experienced patients on separated pill of TDF, 3TC and EFV with HIV RNA<50 copies/ml. CD4, HIV RNA, liver, renal functions and lipid profiles were assessed at baseline, weeks 12, 24, 48 and then every 24 weeks...
June 13, 2017: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/28624659/surface-engineering-of-solid-lipid-nanoparticle-assemblies-by-methyl-%C3%AE-d-mannopyranoside-for-the-active-targeting-to-macrophages-in-anti-tuberculosis-inhalation-therapy
#12
Eleonora Maretti, Luca Costantino, Cecilia Rustichelli, Eliana Leo, Maria Antonietta Croce, Francesca Buttini, Eleonora Truzzi, Valentina Iannuccelli
This study describes the development of new mannosylated Solid Lipid Nanoparticle assemblies (SLNas) delivering rifampicin for an inhaled treatment of tuberculosis. SLNas were surface engineered with mannose residues to recognize mannose receptors located on infected alveolar macrophages and facilitate cell internalization. Two sets of SLNas were produced by the melt emulsifying technique using biocompatible lipid components, i.e. cholesteryl myristate combined with palmitic acid (PA set) or tripalmitin (TP set), in the presence of the targeting moiety, methyl α-d-mannopyranoside...
June 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28623936/safety-and-potential-efficacy-of-gemfibrozil-as-a-supportive-treatment-for-children-with-late-infantile-neuronal-ceroid-lipofuscinosis-and-other-lipid-storage-disorders
#13
REVIEW
Kyeongsoon Kim, Hynda K Kleinman, Hahn-Jun Lee, Kalipada Pahan
Neuronal Ceroid Lipofuscinosis (NCL), also known as Batten disease, is a group of genetically distinct lysosomal disorders that mainly affect the central nervous system, resulting in progressive motor and cognitive decline primarily in children. Multiple distinct genes involved in the metabolism of lipids have been identified to date with various mutations in this family of diseases. There is no cure for these diseases but some new therapeutic approaches have been tested that offer more hope than the standard palliative care...
June 17, 2017: Orphanet Journal of Rare Diseases
https://www.readbyqxmd.com/read/28623000/medical-ozone-promotes-nrf2-phosphorylation-reducing-oxidative-stress-and-pro-inflammatory-cytokines-in-multiple-sclerosis-patients
#14
Livan Delgado-Roche, Mario Riera-Romo, Fernando Mesta, Yanet Hernández-Matos, Juan M Barrios, Gregorio Martínez-Sánchez, Said M Al-Dalaien
Oxidative stress and inflammation play key roles in the pathogenesis of Multiple sclerosis (MS). Different drugs have been used in the clinical practice, however, there is not a completely effective treatment. Due to its potential therapeutic action, medical ozone represents a promising approach for neurodegenerative disorders. The aim of the present study was to address the role of ozone therapy on the cellular redox state in MS patients. Ozone (20μg/ml) was administered three times per week during a month by rectal insufflation...
June 13, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28618905/effective-low-density-lipoprotein-lowering-therapy-implementation-in-clinical-practice
#15
David Sinning, Ulf Landmesser
Although age-adjusted mortality of coronary heart disease has been successfully reduced over recent years, coronary heart disease still represents a leading cause of death and morbidity, in particular in patients at very high cardiovascular risk. Dyslipidaemia plays a major and causal role in the development and clinical progression of coronary heart disease. At present, low-density lipoprotein cholesterol represents the primary target of lipid-directed therapies for the prevention of cardiovascular disease and events...
June 2017: European Journal of Preventive Cardiology
https://www.readbyqxmd.com/read/28618903/planning-secondary-prevention-room-for-improvement
#16
Alejandro Cortés-Beringola, Donna Fitzsimons, Antonio Pelliccia, Guillermo Moreno, Roberto Martín-Asenjo, Héctor Bueno
The prognosis of patients after acute coronary syndromes is still suboptimal, mainly due to the risk of recurrent adverse coronary events, which is greatest during the first year, but persists over one's lifetime. Meaningful progress in preventing cardiovascular events has been achieved. However, there remains much room for improvement by embracing innovative therapies and investing in multidisciplinary approaches. Pharmacological interventions focused on optimising antithrombotic and lipid-lowering therapies are both pillars of secondary prevention that have seen recent ground-breaking advances...
June 2017: European Journal of Preventive Cardiology
https://www.readbyqxmd.com/read/28618760/changes-in-the-serum-liver-and-renal-cortical-lipids-and-electrolytes-in-rabbits-with-cisplatin-induced-nephrotoxicity
#17
Abdelgayoum Ahmed Abdel-Gayoum, Mohamed Hamza Sulaiman Ahmida
BACKGROUND/AIM: Cisplatin is an anticancer drug that can induce nephrotoxicity. Its toxicity is associated with dyslipidemia and disturbed electrolyte balance. In the present study we investigated the changes in serum lipid profile and electrolyte levels and their contents in kidney and liver tissues of rabbits treated with cisplatin. MATERIALS AND METHODS: Twenty-eight adult male New Zealand White rabbits were used in the experiment. Animals of groups C, P1, and P2 were injected with saline, cisplatin (4...
June 12, 2017: Turkish Journal of Medical Sciences
https://www.readbyqxmd.com/read/28617537/spirulina-maxima-improves-insulin-sensitivity-lipid-profile-and-total-antioxidant-status-in-obese-patients-with-well-treated-hypertension-a-randomized-double-blind-placebo-controlled-study
#18
M Szulinska, M Gibas-Dorna, E Miller-Kasprzak, J Suliburska, A Miczke, M Walczak-Gałezewska, M Stelmach-Mardas, J Walkowiak, P Bogdanski
OBJECTIVE: Spirulina maxima consumption is known to be associated with enhanced cardiovascular and metabolic health. Human studies on this topic have recently been described in a few papers; however, potential protective cardiovascular properties of Spirulina in obese patients receiving standard pharmacological antihypertensive treatment remain to be elucidated. Putative beneficial cardiovascular effects of Spirulina supplementation in well treated, obesity-related hypertension were studied in a double-blind placebo-controlled trial...
May 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28615707/-99m-tc-labeled-bevacizumab-for-detecting-atherosclerotic-plaque-linked-to-plaque-neovascularization-and-monitoring-antiangiogenic-effects-of-atorvastatin-treatment-in-apoe-mice
#19
Hui Tan, Jun Zhou, Xiangdong Yang, Mieradilijiang Abudupataer, Xiao Li, Yan Hu, Jie Xiao, Hongcheng Shi, Dengfeng Cheng
Atherosclerotic neovascularization plays a significant role in plaque instability as it provides additional lipids and inflammatory mediators to lesions, and resulting in intraplaque hemorrhage. Vascular endothelial growth factor-A (VEGF-A) is considered the predominant proangiogenic factor in angiogenesis. Bevacizumab, a humanized monoclonal antibody, specifically binds to all VEGF-A isoforms with high affinity. Therefore, in this study, we designed (99m)Tc-MAG3-bevacizumab as a probe, and then investigated its usefulness as a new imaging agent for the detection of plaque neovessels, while also assessing the therapeutic effect of atorvastatin treatment...
June 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28615513/thioredoxin-plays-a-key-role-in-retinal-neuropathy-prior-to-endothelial-damage-in-diabetic-mice
#20
Xiang Ren, Chen Li, Junli Liu, Chenghong Zhang, Yuzhen Fu, Nina Wang, Haiying Ma, Heyuan Lu, Hui Kong, Li Kong
Diabetes is a chronic metabolic syndrome that results in changes in carbohydrate, lipid and protein metabolism. With diabetes for a long time, it increases the risk of diabetic retinopathy (DR) and long-term morbidity and mortality. Moreover, emerging evidence suggests that neuron damage occurs earlier than microvascular complications in DR patients, but the underlying mechanism is unclear. We investigated diabetes-induced retinal neuropathy and elucidated key molecular events to identify new therapeutic targets for the clinical treatment and prevention of DR...
May 24, 2017: Oncotarget
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