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Ezetimibe

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https://www.readbyqxmd.com/read/28092733/enzymatic-synthesis-of-an-ezetimibe-intermediate-using-carbonyl-reductase-coupled-with-glucose-dehydrogenase-in-an-aqueous-organic-solvent-system
#1
Zhi-Qiang Liu, Si-Chuan Dong, Huan-Huan Yin, Ya-Ping Xue, Xiao-Ling Tang, Xiao-Jian Zhang, Jun-Yao He, Yu-Guo Zheng
(4S)-3-[(5S)-5-(4-Fluorophenyl)-5-hydroxypentanoyl]-4-phenyl-1,3-oxazolidin-2-one ((S)-ET-5) is an important chiral intermediate in the synthesis of chiral side chain of ezetimibe. Recombinant Escherichia coli expressing carbonyl reductase (CBR) was successfully constructed in this study. The total E. coli biomass and the specific activity of recombinant CBR in 5L fermenter culture were 10.9gDCWL(-1) and 14900.3Ug(-1)DCW, respectively. The dual-enzyme coupled biocatalytic process in an aqueous-organic biphasic solvent system was first constructed using p-xylene as the optimal organic phase under optimized reaction conditions, and 150gL(-1) (4S)-3-[5-(4-fluorophenyl)-1,5-dioxophentyl]-4-phenyl-1,3-oxazolidin-2-one (ET-4) was successfully converted to (S)-ET-5 with a conversion of 99...
January 6, 2017: Bioresource Technology
https://www.readbyqxmd.com/read/28090731/addition-of-ezetimibe-to-statins-for-patients-at-high-cardiovascular-risk-systematic-review-of-patient-important-outcomes
#2
REVIEW
Yutong Fei, Gordon Henry Guyatt, Paul Elias Alexander, Regina El Dib, Reed A C Siemieniuk, Per Olav Vandvik, Mark E Nunnally, Huda Gomaa, Rebecca L Morgan, Arnav Agarwal, Ying Zhang, Neera Bhatnagar, Frederick A Spencer
Ezetimibe is widely used in combination with statins to reduce low-density lipoprotein. We sought to examine the impact of ezetimibe when added to statins on patient-important outcomes. Medline, EMBASE, CINAHL, and CENTRAL were searched through July, 2016. Randomized controlled trials (RCTs) of ezetimibe combined with statins versus statins alone that followed patients for at least 6 months and reported on at least one of all-cause mortality, cardiovascular deaths, non-fatal myocardial infarctions (MI), and non-fatal strokes were included...
January 16, 2017: Journal of Evaluation in Clinical Practice
https://www.readbyqxmd.com/read/28087743/updates-on-prevention-obesity-ezetimibe-pcsk9-and-hiv-infection
#3
EDITORIAL
Thomas F Lüscher
No abstract text is available yet for this article.
December 21, 2016: European Heart Journal
https://www.readbyqxmd.com/read/28078998/lipoprotein-a-management-pharmacological-and-apheretic-treatment
#4
Ruth Hanssen, Ioanna Gouni-Berthold
Lipoprotein (a) [Lp(a)] is an low-density lipoprotein (LDL)-like particle with an additional apolipoprotein, apolipoprotein (a), [apo(a)] attached to apolipoprotein B. Recent epidemiologic and Mendelian randomization studies have provided evidence that Lp(a) is causally related to the pathogenesis of atherosclerosis and cardiovascular disease (CVD). The risk association between Lp(a) concentrations and CVD is still controversial but seems to be continuous and without an obvious threshold Lp(a) level. Circulating concentrations of Lp(a) are genetically determined; desirable levels are amplt; 50 mg/dl...
January 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28065787/intestinal-farnesoid-x-receptor-controls-transintestinal-cholesterol-excretion-in-mice
#5
Jan Freark de Boer, Marleen Schonewille, Marije Boesjes, Henk Wolters, Vincent W Bloks, Trijnie Bos, Theo H van Dijk, Angelika Jurdzinski, Renze Boverhof, Justina C Wolters, Jan A Kuivenhoven, Jan M van Deursen, Ronald P J Oude Elferink, Antonio Moschetta, Claus Kremoser, Henkjan J Verkade, Folkert Kuipers, Albert K Groen
BACKGROUND & AIMS: The role of the intestine in the maintenance of cholesterol homeostasis is increasingly recognized. Fecal excretion of cholesterol is the last step in the atheroprotective reverse cholesterol transport pathway, to which biliary and transintestinal cholesterol excretion (TICE) contribute. The mechanisms controlling the flux of cholesterol through the TICE pathway are, however, poorly understood. We aimed to identify mechanisms that regulate and stimulate TICE. METHODS: We performed studies with C57Bl/6J mice, as well as mice with intestine-specific knockout of the farnesoid X receptor (FXR), mice that express an FXR transgene specifically in the intestine, and ABCG8-knockout mice...
January 5, 2017: Gastroenterology
https://www.readbyqxmd.com/read/28064554/evaluating-bempedoic-acid-for-the-treatment-of-hyperlipidaemia
#6
Peter Penson, Mary McGowan, Maciej Banach
Despite the effectiveness of statins in the treatment of lipid disorders, residual risk still exists, and hitherto studies where additional drugs were added to statin therapy have been mainly negative or the outcomes were very modest. Therefore there is still a need for new and effective oral agents in the combination therapy of lipid disorders. Areas Covered: The review covers the current state of knowledge on the mechanism of action of bempedoic acid (ETC-1002) and results from recent clinical studies. Expert Opinion: ETC-1002 is a novel oral lipid-lowering therapy...
January 9, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28059952/atp-citrate-lyase-genetics-molecular-biology-and-therapeutic-target-for-dyslipidemia
#7
Amy C Burke, Murray W Huff
PURPOSE OF REVIEW: ATP-citrate lyase (ACLY) has re-emerged as a drug target for LDL cholesterol (LDL-C) lowering. We review ACLY as a therapeutic strategy, its genetics, its molecular and cellular biology, and also its inhibition. RECENT FINDINGS: ACLY is a critical enzyme linking glucose catabolism to lipogenesis by providing acetyl-CoA from mitochondrial citrate for fatty acid and cholesterol biosynthesis. Human genetic variants have been associated with enhanced growth and survival of several cancers, and with attenuated plasma triglyceride responses to dietary fish oil...
January 5, 2017: Current Opinion in Lipidology
https://www.readbyqxmd.com/read/28058034/retrospective-analysis-of-the-effects-of-a-highly-standardized-mixture-of-berberis-aristata-silybum-marianum-and-monacolins-k-and-ka-in-patients-with-dyslipidemia
#8
Francesco Di Pierro, Pietro Putignano, Tarcisio Ferrara, Carmela Raiola, Giuliana Rapacioli, Nicola Villanova
BACKGROUND: Berberis aristata, because of its berberine content, and Monascus purpureus fermented rice, because of the presence of monacolins (naturally derived statins), are widely investigated food-grade ingredients used to formulate cholesterol-lowering supplements. Although they are extensively used, berberine is poorly absorbed and monacolins are poorly chemically characterized, not standardized, and possibly contaminated with toxic compounds. Silymarin is reported to enhance berberine absorption, while Monakopure™-K20 (MK-20) is a highly standardized red yeast rice containing monacolins K and KA in the ratio of 1:1 but not secondary monacolins, dehydromonacolins, or citrinin...
2017: Clinical Pharmacology: Advances and Applications
https://www.readbyqxmd.com/read/28057006/bisphenol-a-promotes-cholesterol-absorption-in-caco-2-cells-by-up-regulation-of-npc1l1-expression
#9
Dan Feng, Jun Zou, Shanshan Zhang, Xuechun Li, Peiyang Li, Minqi Lu
BACKGROUND: Bisphenol A (BPA), an commonly exposed environmental chemicals in humans, has been shown to have a hypercholesterolemic effect with molecular mechanism not clear. Since intestinal cholesterol absorption plays a major role in maintaining total body cholesterol homeostasis, the present study is to investigate whether BPA affects cholesterol absorption in the intestinal Caco-2 cells. METHODS: The Caco-2 cells were pretreated with BPA at different concentrations for 24 h and then incubated with radioactive micellar cholesterol for 2 h...
January 6, 2017: Lipids in Health and Disease
https://www.readbyqxmd.com/read/28034582/an-evidence-based-guide-to-cholesterol-lowering-guidelines
#10
REVIEW
David D Waters, S Matthijs Boekholdt
Since 2014, guidelines for the management of lipid disorders to reduce cardiovascular (CV) events have been updated in the United States, the United Kingdom, Europe, and Canada. Some of these guidelines are almost entirely evidence-based whereas others are a mix of evidence and expert opinion. Guidelines differ on such simple questions as to whether blood samples should be fasting or nonfasting, and whether low-density lipoprotein cholesterol (LDL-C) or another lipid parameter should be the primary focus of treatment...
October 24, 2016: Canadian Journal of Cardiology
https://www.readbyqxmd.com/read/28028755/effects-of-ezetimibe-simvastatin-and-their-combination-on-inflammatory-parameters-in-a-rat-model-of-adjuvant-induced-arthritis
#11
REVIEW
Carmem Patrícia Barbosa, Lívia Bracht, Franciele Queiroz Ames, Francielli Maria de Souza Silva-Comar, Rafael Prizon Tronco, Ciomar Aparecida Bersani-Amado
Statins are hypocholesterolemic drugs that are prescribed for patients with an increased risk of cardiovascular and cerebrovascular complications. Ezetimibe has an atheroprotective activity through inhibition of the expression of vascular adhesion molecule-I and vascular CD14, a marker of the infiltration of mononuclear leukocytes. Ezetimibe reduces the amount of chemoattractant protein-1 that is available for monocytes and macrophages and alters the activity of nuclear factor κB in leukocytes. The mechanisms of action of statins complement those of ezetimibe...
December 28, 2016: Inflammation
https://www.readbyqxmd.com/read/28028192/evidence-for-reverse-causality-in-the-association-between-blood-pressure-and-cardiovascular-risk-in-patients-with-chronic-kidney-disease
#12
William Herrington, Natalie Staplin, Parminder K Judge, Marion Mafham, Jonathan Emberson, Richard Haynes, David C Wheeler, Robert Walker, Charlie Tomson, Larry Agodoa, Andrzej Wiecek, Sarah Lewington, Christina A Reith, Martin J Landray, Colin Baigent
: Among those with moderate-to-advanced chronic kidney disease, the relationship between blood pressure (BP) and cardiovascular disease seems U shaped but is loglinear in apparently healthy adults. The SHARP (Study of Heart and Renal Protection) randomized 9270 patients with chronic kidney disease to ezetimibe/simvastatin versus matching placebo and measured BP at each follow-up visit. Cox regression was used to assess the association between BP and risk of cardiovascular disease among (1) those with a self-reported history of cardiovascular disease and (2) those with no such history and, based on plasma troponin-I concentration, a low probability of subclinical cardiac disease...
December 27, 2016: Hypertension
https://www.readbyqxmd.com/read/28027412/inhibitory-effect-of-ezetimibe-can-be-prevented-by-an-administration-interval-of-4%C3%A2-h-between-%C3%AE-tocopherol-and-ezetimibe
#13
Shunsuke Nashimoto, Yuki Sato, Yoh Takekuma, Mitsuru Sugawara
Tocopherol is used not only as an ethical drug but also as a supplement. In 2008, Narushima et al. reported that α-tocopherol is partly transported via an intestinal cholesterol transporter, Niemann-Pick C1-Like 1 (NPC1L1). Ezetimibe, a selective inhibitor of NPC1L1, is administered for a long time to inhibit cholesterol absorption and there is a possibility that absorption of α-tocopherol is also inhibited by ezetimibe. In this study, we investigated the influence of ezetimibe on the absorption of α-tocopherol with single administration and long-term administration...
December 27, 2016: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28019114/-lipids-and-cerebrovascular-disease-new-therapeutic-options-in-lowering-ldl-cholesterol
#14
Emese Lovadi, Péter Csécsei, Csenge Lovig, Zsófia Karádi, László Szapáry
Stroke is the third most common cause of death worldwide following myocardial infaction and malignancies, furthermore, its functional outcome is the worst of all conditions. Cholesterol, especially LDL-cholesterol plays a key role in the formation of atherosclerotic plaques. It has been verified recently that escalating incidence and mortality of cerebrovascular diseases are proportional to increased levels of LDL-cholesterol. Statin therapy undeniably reduces the risk of stroke, however other methods for decreasing lipid levels have not been proved significantly effective...
December 2016: Orvosi Hetilap
https://www.readbyqxmd.com/read/28007331/combination-therapy-of-rosuvastatin-and-ezetimibe-in-patients-with-high-cardiovascular-risk
#15
Young-June Yang, Sang-Hak Lee, Byung Soo Kim, Yun-Kyeong Cho, Hyun-Jai Cho, Kyoung Im Cho, Seok-Yeon Kim, Jae Kean Ryu, Jin-Man Cho, Joong-Il Park, Jong-Seon Park, Chang Gyu Park, Woo Jung Chun, Myung-A Kim, Dong-Kyu Jin, Namho Lee, Byung Jin Kim, Kwang Kon Koh, Jon Suh, Seung-Hwan Lee, Byoung-Kwon Lee, Seung-Jin Oh, Han-Young Jin, Youngkeun Ahn, Sang-Gon Lee, Jang-Ho Bae, Woo Jung Park, Sang-Chol Lee, Han Cheol Lee, Jaewon Lee, Cheolwon Park, Backhwan Lee, Yangsoo Jang
PURPOSE: The aim of this study was to evaluate the efficacy and tolerability of rosuvastatin/ezetimibe combination therapy in Korean patients with high cardiovascular risk. METHODS: This was a 12-week, randomized, double-blind, placebo-controlled, multicenter study. A total of 337 patients were screened. After a 4-week run-in period, 245 of these patients with high or moderately high risk as defined by the National Cholesterol Education Program Adult Treatment Panel III guidelines were randomly assigned...
December 19, 2016: Clinical Therapeutics
https://www.readbyqxmd.com/read/27998977/a-novel-mechanism-causing-familial-hypercholesterolemia-the-proprotein-convertase-subtilisin-kexin-type-9-resistant-arg410ser-ldl-receptor-mutation
#16
Delia Susan-Resiga, Emmanuelle Girard, Robert Scott Kiss, Rachid Essalmani, Josée Hamelin, Marie-Claude Asselin, Zuhier Awan, Chutikarn Butkinaree, Alexandre Fleury, Armand Soldera, Yves L Dory, Alexis Baass, Nabil G Seidah
Familial hypercholesterolemia (FH) is characterized by severely elevated low-density lipoprotein (LDL) cholesterol. Herein, we identified an FH patient presenting novel compound heterozygote mutations R410S and G592E of the LDL receptor (LDLR). The patient responded modestly to maximum rosuvastatin plus ezetimibe therapy, even in combination with a PCSK9-monoclonal-antibody injection. Using cell biology and molecular-dynamics simulations, we aimed to define the underlying mechanism(s) by which these LDLR mutations affect LDL metabolism and lead to hypercholesterolemia...
December 20, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/27998714/a-nutraceutical-approach-armolipid-plus-to-reduce-total-and-ldl-cholesterol-in-individuals-with-mild-to-moderate-dyslipidemia-review-of-the-clinical-evidence
#17
Vivencio Barrios, Carlos Escobar, Arrigo Francesco Giuseppe Cicero, David Burke, Peter Fasching, Maciej Banach, Eric Bruckert
Compelling evidence supports the effectiveness of the reduction of total and LDL cholesterol (TC and LDL-C) in primarily preventing cardiovascular events, within the framework of life-long prevention programs mainly consisting in lifestyle changes. Pharmacological treatment should be introduced when lifestyle changes, including use of nutraceuticals, have failed. ESC/EAS guidelines list a number of nutraceutical compounds and functional foods which have been individually studied in randomized, controlled clinical trials (RCTs)...
February 2017: Atherosclerosis. Supplements
https://www.readbyqxmd.com/read/27988827/atherogenic-dyslipidemia-remission-1%C3%A2-year-after-bariatric-surgery
#18
Elisenda Climent, David Benaiges, Juan Pedro-Botet, Juana A Flores-Le Roux, Jose M Ramón, Montserrat Villatoro, Laia Fontané, Juan J Chillarón, Albert Goday
PURPOSE: Given the lack of evidence of the effect of bariatric surgery (BS) on atherogenic dyslipidemia (AD), which is a characteristic of obese subjects, this study aimed to describe the remission rate of AD 1 year after BS in severely obese patients. MATERIALS AND METHODS: A non-randomised, prospective cohort study was conducted in patients undergoing laparoscopic Roux-en-Y gastric bypass or laparoscopic sleeve gastrectomy with a 1-year follow-up. AD was defined as triglycerides ≥1...
December 17, 2016: Obesity Surgery
https://www.readbyqxmd.com/read/27967828/homozygous-familial-hypercholesterolaemia-update-on-management
#19
Michael France
Homozygous familial hypercholesterolaemia (HoFH) is an inherited disease causing an approximately fourfold increase in blood low-density lipoprotein cholesterol (LDLC) from birth compared with the age-matched normal population owing to reduced low-density lipoprotein receptor (LDLR) activity. Such elevated cholesterol is associated with accelerated atheromatous disease, particularly of the aortic root and coronary arteries. However, HoFH is clinically heterogeneous, reflecting residual low-density lipoprotein receptor (LDLR) activity...
November 2016: Paediatrics and International Child Health
https://www.readbyqxmd.com/read/27960021/-dyslipidemia-in-kidney-transplant-recipients
#20
Giovanni Mosconi, Camilla Gambaretto, Loretta Zambianchi, Maria Francesca Lifrieri, Marco De Fabritiis, Stefania Cristino, Claudio Americo, Maria Laura Angelini
The kidney transplant recipients' population shows pronounced alterations of the lipidic profile, with hypercholesterolemia (total cholesterol, LDL, VLDL), normal HDL and hypertriglyceridemia. Multiple factors contribute to the development of dyslipidemia, towards these, immunosuppressive therapy plays an important role. The impact on cardiovascular outcomes is less well defined than in general population. This work is a revaluation of the clinical approach to dyslipidemia in kidney transplant based on the more recent Guide Lines and literature...
2016: Giornale Italiano di Nefrologia: Organo Ufficiale Della Società Italiana di Nefrologia
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