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lipids lowering drugs

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https://www.readbyqxmd.com/read/29773828/single-nucleotide-polymorphisms-in-the-g-protein-coupled-receptor-kinase-5-grk5-gene-are-associated-with-plasma-ldl-cholesterol-levels-in-humans
#1
Stefan Z Lutz, Mathias Falcenberg, Fausto Machicao, Andreas Peter, Martin Kächele, Elko Randrianarisoa, Angela Lehn-Stefan, Robert Wagner, Jürgen Machann, Fritz Schick, Martin Heni, Axel Ullrich, Andreas Fritsche, Norbert Stefan, Hans-Ulrich Häring, Harald Staiger, Konstantinos Kantartzis
Genetically modified mice models suggest an important role for G-protein-coupled receptor kinase 5 (GRK5) in the pathophysiology of obesity and related disorders. We investigated whether single nucleotide polymorphisms (SNPs) in the gene encoding GRK5 affect cardiometabolic traits in humans. We genotyped 3 common SNPs in intron 1 (rs1980030, rs10466210, rs9325562) and one SNP in intron 3 (rs10886471) of GRK5 in 2332 subjects at risk for type 2 diabetes. Total- and visceral fat mass were measured by magnetic resonance (MR) tomography and liver fat content by 1 H-MR spectroscopy...
May 17, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29772998/partially-purified-aqueous-fraction-of-desmodium-gyrans-dc-improves-reverse-cholesterol-transport-and-lipoprotein-metabolism-in-wistar-rats-fed-with-high-fat-diet
#2
M S Indu, Jose Padikkala, Achuthan C Raghavamenon
Apart from the conventional hypolipidemic therapy, plaque regression through enhanced reverse cholesterol transport (RCT) has emerged as novel approach in atherosclerotic drug development. High-density lipoprotein (HDL) mimetics as well as agents that augment the functional HDL and RCT pathways are under intense exploration. Desmodium gyrans (Fabacea) has been shown to have hypolipidemic efficacy, with an HDL-enhancing property. In this study, a chromatographically purified active fraction of D. gyrans (DGMAF) significantly decreased the serum and lipid profiles as well as lipotoxicity in liver in Wistar rats fed with high-fat diet (HFD)...
2018: Journal of Environmental Pathology, Toxicology and Oncology
https://www.readbyqxmd.com/read/29772938/the-suppressive-effect-of-the-three-herb-extract-mixture-on-vascular-and-liver-inflammation-in-atherogenic-diet-with-high-fructose-fed-mice
#3
Hae Seong Song, Hyun Jung Koo, Bong Kyun Park, Jeong Eun Kwon, Seon-A Jang, Hyun Jin Baek, Se Young Kim, Sung Ryul Lee, Se Chan Kang
CONTEXT: Cynanchum wilfordii (Maximowicz) Hemsley (Apocynaceae), Arctium lappa L. var. rubescens Frivald (Asteraceae) and Dioscorea opposite Thunb (Dioscoreaceae) root extracts have been widely used as an alternative for intervening obesity. OBJECTIVES: The synergistic effect of three-herb mixture of C. wilfordii, A. lappa and D. opposita was determined on aortic and liver inflammatory responses. MATERIALS AND METHODS: CWE, ALE and DOE were prepared from the root of C...
December 2018: Pharmaceutical Biology
https://www.readbyqxmd.com/read/29771515/the-link-between-membrane-composition-and-permeability-to-drugs
#4
Chi Hang Tse, Jeffrey Comer, Yi Wang, Christophe Chipot
Prediction of membrane permeability to small molecules represents an important aspect of drug discovery. First-principle calculations of this quantity require an accurate description of both the thermodynamics and kinetics that underlie translocation of the permeant across the lipid bilayer. In this contribution, the membrane permeability to three drugs, or drug-like molecules, namely, 9-anthroic acid (ANA), 2',3'-dideoxyadenosine (DDA) and hydrocortisone (HYL) are estimated in a pure 1-palmitoyl-2-oleoyl-phosphatidylcholine (POPC) and in a POPC:cholesterol (2:1) mixture...
May 17, 2018: Journal of Chemical Theory and Computation
https://www.readbyqxmd.com/read/29770409/acemetacin-phosphatidylcholine-interactions-are-determined-by-the-drug-ionization-state
#5
Catarina Pereira-Leite, Cláudia Nunes, Débora Grahl, José C Bozelli, Shirley Schreier, Christina S Kamma-Lorger, Iolanda M Cuccovia, Salette Reis
Gastrointestinal (GI) toxicity is a major drawback of the chronic use of nonsteroidal anti-inflammatory drugs (NSAIDs). The NSAIDs topical actions on the protective phospholipid layers of the GI mucosa seem to be a central toxicity mechanism of these pharmaceuticals. This work describes the interactions of acemetacin, a commercialized NSAID, with 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) bilayers at pH 3.0, 5.0, and 7.4. This pH range was chosen to mimic the pH gradient found in the gastric mucosa, and to ultimately gain insights into the mechanisms underlying the acemetacin-induced gastric toxicity...
May 17, 2018: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29765578/lipid-lowering-drugs-statins-and-peripheral-neuropathy
#6
Mohammadreza Emad, Hosein Arjmand, Hamid Reza Farpour, Bahareh Kardeh
Background and aim: Peripheral neuropathy is a disorder with often unknown causes. Some drugs, including statins, are proposed to be among the causes of peripheral neuropathy. This study aimed at evaluating this condition by electrodiagnostic study among patients who had received statins. Methods: This case-control study was conducted in Shiraz, Iran in 2015, and included 39 patients aged 35-55 who had received statins for at least 6 months, and 39 healthy matched controls...
March 2018: Electronic Physician
https://www.readbyqxmd.com/read/29765215/in-vivo-investigation-on-the-chronic-hepatotoxicity-induced-by-intraperitoneal-administration-of-10-nm-silicon-dioxide-nanoparticles
#7
Mansour Almansour, Saud Alarifi, Bashir Jarrar
Background: Silicon dioxide (silica) nanoparticles (SDNPs) are widely used in nanotechnology and medicine, but these nanomaterials may carry a high risk for human health while little is known about their toxicity. Methods: We investigated the alterations in morphometry, biochemistry, hematology, histology of liver tissue and gene expression of drug-metabolizing enzymes induced by 10-nm SDNPs. Healthy male Wistar albino rats were exposed to 20, 35 and 50 repeated injections of SDNPs (2 mg/kg body weight)...
2018: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29764933/discovery-of-peroxisome-proliferator-activated-receptor-%C3%AE-ppar%C3%AE-activators-with-a-ligand-screening-system-using-a-human-ppar%C3%AE-expressing-cell-line
#8
Keisuke Tachibana, Tomohiro Yuzuriha, Ryotaro Tabata, Syohei Fukuda, Takashi Maegawa, Rika Takahashi, Keiichi Tanimoto, Hirofumi Tsujino, Kazuto Nunomura, Bangzhong Lin, Yoshiharu Matsuura, Toshiya Tanaka, Takao Hamakubo, Juro Js Sakai, Tatsuhiko Kodama, Tadayuki Kobayashi, Kenji Ishimoto, Hiroyuki Miyachi, Takefumi Doi
Peroxisome proliferator-activated receptor alpha (PPARα) is a ligand-activated transcription factor that belongs to the superfamily of nuclear hormone receptors. PPARα is mainly expressed in the liver, where it activates fatty acid oxidation and lipoprotein metabolism and improves plasma lipid profiles. Therefore, PPARα activators are often used to treat patients with dyslipidemia. To discover additional PPARα activators as potential compounds for use in hypolipidemic drugs, here we established human hepatoblastoma cell lines with luciferase reporter expression from the promoters containing peroxisome proliferator responsive elements (PPRE) and tetracycline-regulated expression of full-length human PPARα to quantify the effects of chemical ligands on PPARα activity...
May 15, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29763460/lipophilic-statins-limit-cancer-cell-growth-and-survival-via-involvement-of-akt-signaling
#9
Colin H Beckwitt, Keisuke Shiraha, Alan Wells
The HMG-CoA reductase inhibitors, statins, have been used as lipid lowering drugs for decades and several epidemiological studies suggest statin usage correlates with a decreased incidence of cancer specific mortality in patients. However, the mechanism of this mortality benefit remains unclear. Here, we demonstrate that statin drug lipophilicity and affinity for its target enzyme, HMGCR, determine their growth suppressive potency against various tumor cell lines. The lipophilic atorvastatin decreases cancer cell proliferation and survival in vitro...
2018: PloS One
https://www.readbyqxmd.com/read/29760294/breath-profiles-of-children-on-ketogenic-therapy
#10
Vera Ruzsanyi, Miklós Péter Kalapos, Christine Schmidl, Daniela Karall, Sabine Scholl-Buergi, Matthias Baumann
Ketogenic diets (KD) were initially introduced to clinical practice as alimentary approaches with the aim to control drug-resistant epilepsies. Therapy control, particularly at initiation, happens through regular blood analysis and control of urine ketone levels. However, there is a lack of fast, reliable and preferably non-invasive methods of analysis. The exhaled breath contains hundreds of volatile organic compounds (VOCs), which can be modified by diet. The instrumental development of VOC detection converges in the direction of low cost sensors, which can facilitate the self-monitoring of the patients in the future if reliable breath markers are available...
May 15, 2018: Journal of Breath Research
https://www.readbyqxmd.com/read/29760188/depression-in-type-1-diabetes-was-associated-with-high-levels-of-circulating-galectin-3
#11
Eva O Melin, Jonatan Dereke, Maria Thunander, Magnus Hillman
OBJECTIVE: Neuroinflammatory responses are implicated in depression. The aim was to explore whether depression in patients with type 1 diabetes (T1D) was associated with high circulating galectin-3, controlling for metabolic variables, s-creatinine, life style factors, medication, and cardiovascular complications. DESIGN: Cross-sectional. METHODS: Participants were T1D patients (n=283, 56% men, age 18-59 years, diabetes duration ≥1 year)...
May 14, 2018: Endocrine Connections
https://www.readbyqxmd.com/read/29759006/interplay-between-hypercholesterolaemia-and-inflammation-in-atherosclerosis-translating-experimental-targets-into-clinical-practice
#12
José Tuñón, Magnus Bäck, Lina Badimón, Marie-Luce Bochaton-Piallat, Bertrand Cariou, Mat J Daemen, Jesus Egido, Paul C Evans, Sheila E Francis, Daniel Fj Ketelhuth, Esther Lutgens, Christian M Matter, Claudia Monaco, Sabine Steffens, Erik Stroes, Cécile Vindis, Christian Weber, Imo E Hoefer
Dyslipidaemia and inflammation are closely interconnected in their contribution to atherosclerosis. In fact, low-density lipoprotein (LDL)-lowering drugs have anti-inflammatory effects. The Canakinumab Antiinflammatory Thrombosis Outcome Study (CANTOS) has shown that interleukin (IL)-1β blockade reduces the incidence of cardiovascular events in patients with previous myocardial infarction and C-reactive protein levels >2 mg/L. These data confirm the connection between lipids and inflammation, as lipids activate the Nod-like receptor protein 3 inflammasome that leads to IL-1β activation...
January 1, 2018: European Journal of Preventive Cardiology
https://www.readbyqxmd.com/read/29753395/quantitative-extent-of-atherosclerotic-plaque-in-the-major-epicardial-coronary-arteries-in-patients-with-fatal-coronary-heart-disease-in-coronary-endarterectomy-specimens-in-aorta-coronary-saphenous-venous-conduits-and-means-to-prevent-the-plaques-a-review
#13
William C Roberts
This review tries to answer the following 15 questions: Is atherosclerosis a systemic or a regional disease? Is atherosclerosis in any particular region focal or diffuse? What is the quantity of atherosclerotic plaques in endarterectomy specimens of the right coronary artery in patients undergoing coronary artery bypass grafting (CABG) compared to that in the right coronary artery in patients with fatal coronary artery disease? How do the units used for measuring arterial narrowing by angiography compare to the units used for measuring arterial narrowing at necropsy? What do atherosclerotic plaques consist of in coronary arteries in patients with fatal coronary disease? What is the quantity of atherosclerotic plaque in bypassed -vs- non-bypassed native coronary arteries in patients dying early (<60 days) or late (>60 days) after coronary artery bypass grafting? What is the frequency of acute coronary lesions and multi-luminal channels at necropsy in patients with unstable angina pectoris, sudden coronary death, and acute myocardial infarction? What is the mechanism of luminal widening by angioplasty in the coronary arteries? What observations suggest that atherosclerotic plaques are the result at least in part of organization of thrombi? Is atherosclerosis a multifactoral or a unifactoral disease? What characteristics distinguish carnivores and herbivores? What are reasonable guidelines for whom to treat with lipid-altering agents? What is the rule of 5 and the rule of 7 in statin therapy? What is the effect of lipid lowering drug therapy on coronary luminal narrowing? What are some requisites for a healthy life?...
March 27, 2018: American Journal of Cardiology
https://www.readbyqxmd.com/read/29749101/understanding-patient-adherence-and-concerns-with-statins-and-medication-discussions-with-physicians-action-a-survey-on-the-patient-perspective-of-dialogue-with-healthcare-providers-regarding-statin-therapy
#14
Eliot A Brinton
BACKGROUND: Statin therapy is used first-line for cholesterol lowering and prevention of atherosclerotic cardiovascular disease (CVD), but side effects and the potential for drug-drug interactions may complicate its use. Provider-patient communication is essential for shared decision-making, which, in turn, is recommended by guidelines to reduce or overcome these challenges. Unfortunately, relatively little is known about provider-patient communication surrounding statin use. METHOD: We conducted an online survey of 5,014 patients, U...
May 10, 2018: Clinical Cardiology
https://www.readbyqxmd.com/read/29745454/effects-of-short-term-clomipramine-on-anxiety-like-behavior-cellular-metabolism-and-oxidative-stress-in-primary-fibroblast-cells-of-male-and-female-rats
#15
Ana G Jimenez, Joshua D Winward, Dana M Smith, Christina M Ragan
Anxiety is the most prevalent mental disorder among adults in the United States and females tend to have significantly higher rates of anxiety compared with men. Common treatments for anxiety include usage of selective serotonin reuptake inhibitors (SSRIs) and tricyclic antidepressants, however, sex differences in the efficacy of these drugs exist. In this study, we were interested in determining if acutely manipulating serotonin mechanisms at the whole-animal level affects cellular metabolism and oxidative stress in primary fibroblast cells from clomipramine-treated Sprague-Dawley rats...
May 2018: Physiological Reports
https://www.readbyqxmd.com/read/29738245/enzyme-responsive-charge-reversal-polymer-mediated-effective-gene-therapy-for-intraperitoneal-tumors
#16
Nasha Qiu, Jianqing Gao, Qi Liu, Jinqiang Wang, Youqing Shen
Gene therapy has demonstrated effectiveness in many genetic diseases as evidenced by recent clinical applications. Viral vectors have been extensively tested in clinical gene-therapy trials, but nonviral vectors such as cationic polymers or lipids are much less used due to their lower gene-transfection efficiencies. However, the advantages of nonviral vectors, such as easily tailored structures, nonimmunogenetics, and relatively low cost, still drive great efforts to improve their transfection efficiencies...
May 8, 2018: Biomacromolecules
https://www.readbyqxmd.com/read/29737302/drug-effect-of-atorvastatin-on-middle-cerebral-atherosclerotic-stenosis-and-high-resolution-nmr-diagnosis
#17
Xingchi Chen, Sainan Wang, Lulu Lin, Yu Li, Hui Zhang
Atherosclerosis (AS) is a chronic inflammatory reaction with the pathological changes in the lipid deposition of arterial intima. The disorder of blood lipid metabolism is the main factor of the occurrence and development of AS, and the inflammatory reaction and autoimmune reaction also run through the development of AS. In this study, we compared the efficacy and safety of atorvastatin, simvastatin, pravastatin and rosuvastatin in the treatment of AS. At the same time, we used high resolution magnetic resonance imaging (MRI) to assess the changes in plaque area in the middle cerebral artery and the patch area before and after drug treatment...
May 2018: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29737301/flurbiprofen-axetil-analgesic-effect-and-adverse-reaction
#18
Xiaodong Zhao, Leting Ji
Flurbiprofen axetil is a targeted analgesic and non steroidal analgesic with lipid microspheres as drug carrier. It can selectively accumulate in surgical incision and reduce the allodynia a caused by surgical trauma. In this paper, the experimental subjects were divided into three groups to analyze the difference in the analgesic effect of different doses of flurbiprofen axetil for postoperative analgesia. The patients in group A, B and C were treated with flurbiprofen axetil injection 100, 150, 200mg, respectively...
May 2018: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29736827/generalized-anxiety-disorder-gad-and-comorbid-major-depression-with-gad-are-characterized-by-enhanced-nitro-oxidative-stress-increased-lipid-peroxidation-and-lowered-lipid-associated-antioxidant-defenses
#19
Michael Maes, Kamila Landucci Bonifacio, Nayara Rampazzo Morelli, Heber Odebrecht Vargas, Estefânia Gastaldello Moreira, Drozdstoy St Stoyanov, Décio Sabbatini Barbosa, André F Carvalho, Sandra Odebrecht Vargas Nunes
Accumulating evidence shows that nitro-oxidative pathways play an important role in the pathophysiology of major depressive disorder (MDD) and bipolar disorder (BD) and maybe anxiety disorders. The current study aims to examine superoxide dismutase (SOD1), catalase, lipid hydroperoxides (LOOH), nitric oxide metabolites (NOx), advanced oxidation protein products (AOPP), malondialdehyde (MDA), glutathione (GSH), paraoxonase 1 (PON1), high-density lipoprotein cholesterol (HDL), and uric acid (UA) in participants with and without generalized anxiety disorder (GAD) co-occurring or not with BD, MDD, or tobacco use disorder...
May 7, 2018: Neurotoxicity Research
https://www.readbyqxmd.com/read/29736825/bleeding-events-attributable-to-concurrent-use-of-warfarin-and-other-medications-in-high-risk-elderly-meta-analysis-and-italian-population-based-investigation
#20
Rosanna Irene Comoretto, Federico Rea, Ersilia Lucenteforte, Alessandro Mugelli, Gianluca Trifirò, Silvia Cascini, Giuseppe Roberto, Alessandro Chinellato, Amelia Filippelli, Giovanni Corrao
PURPOSE: The aim of this study was to estimate the proportion of bleedings that occurred among warfarin users attributable to the concomitant use of other medications. A general approach for measuring the impact of the prescriptive inappropriateness on drug adverse outcomes at the population level is described. METHODS: A meta-analysis was conducted to obtain summary relative risks of bleeding associated with concurrent use of warfarin and other medications compared to warfarin use alone...
May 7, 2018: European Journal of Clinical Pharmacology
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