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HMG-CoA reductase

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https://www.readbyqxmd.com/read/28627804/the-effect-of-genetic-polymorphisms-in-slco2b1-on-the-lipid-lowering-efficacy-of-rosuvastatin-in-healthy-adults-with-elevated-low-density-lipoprotein
#1
Tae-Eun Kim, Dong-Seong Shin, Namyi Gu, Byung Hwa Jung, Jayoun Kim, Young Min Cho, Kyung-Sang Yu, Joo-Youn Cho
Rosuvastatin is an HMG-CoA reductase inhibitor widely used for treating hypercholesterolaemia. We investigated whether genetic polymorphisms in solute carrier organic anion transporter 2B1 (SLCO2B1) affect the lipid-lowering effect of rosuvastatin in healthy adults with elevated low-density lipoprotein (LDL). This study included 18 volunteers with LDL levels above 130 mg/dL. Rosuvastatin (20 mg) was administered once a day for 8 weeks. Blood samples were drawn before and after the 8-week treatment to measure changes in lipid levels...
June 19, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28624574/evidence-for-a-pharmacokinetic-interaction-between-eslicarbazepine-and-rosuvastatin-potential-effects-on-xenobiotic-transporters
#2
Barry E Gidal, Scott Mintzer, Matthias Schwab, Ralph Schutz, Jahnavi Kharidia, David Blum, Todd Grinnell, Soujanya Sunkaraneni
INTRODUCTION: Patients with partial-onset seizures and comorbid cardiovascular disease may concomitantly receive eslicarbazepine acetate (ESL), an antiepileptic drug, and rosuvastatin, an HMG-CoA reductase inhibitor. This study evaluated the effect of multiple-dose ESL on the pharmacokinetic (PK) parameters of a single dose of rosuvastatin in healthy subjects. METHODS: This was a Phase I, single-center, fixed-sequence, open-label study. Healthy subjects received two treatments, in sequence...
May 18, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28623919/effects-of-karela-bitter-melon-momordica-charantia-on-genes-of-lipids-and-carbohydrates-metabolism-in-experimental-hypercholesterolemia-biochemical-molecular-and-histopathological-study
#3
Dalia Yossri Saad, Mohamed Mohamed Soliman, Ahmed A Baiomy, Magdy Hassan Yassin, Hanan Basiouni El-Sawy
BACKGROUND: Hypercholesterolemia is a serious diseases associated with type-2 diabetes, atherosclerosis, cardiovascular disorders and liver diseases. Humans seek for safe herbal medication such as karela (Momordica charantia/bitter melon) to treat such disorders to avoid side effect of pharmacotherapies widely used. METHODS: Forty male Wistar rats were divided into four equal groups; control group with free access to food and water, cholesterol administered group (40 mg/kg BW orally); karela administered group (5 g /kg BW orally) and mixture of cholesterol and karela...
June 17, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28608538/effects-of-dietary-red-yeast-sporidiobolus-pararoseus-on-production-performance-and-egg-quality-of-laying-hens
#4
W Tapingkae, K Panyachai, M Yachai, H V Doan
The purpose of this study was to evaluate the effect of dietary red yeast (Sporidiobolus pararoseus) on production performance and egg quality of laying hens. A total of 200 Esa Brown laying hens (23 weeks of age) were allocated equally to negative control group (no yeast supplement); positive control group (2 g/kg of Saccharomyces cerevisiae); 0.5, 1, 2 g/kg red yeast respectively. The experiment was lasted for 12 weeks. Feed intake, hen-day egg production and egg weight were not different between control and supplemented groups...
June 13, 2017: Journal of Animal Physiology and Animal Nutrition
https://www.readbyqxmd.com/read/28607088/skin-specific-regulation-of-srebp-processing-and-lipid-biosynthesis-by-glycerol-kinase-5
#5
Duanwu Zhang, Wataru Tomisato, Lijing Su, Lei Sun, Jin Huk Choi, Zhao Zhang, Kuan-Wen Wang, Xiaoming Zhan, Mihwa Choi, Xiaohong Li, Miao Tang, Jose M Castro-Perez, Sara Hildebrand, Anne R Murray, Eva Marie Y Moresco, Bruce Beutler
The recessive N-ethyl-N-nitrosourea-induced phenotype toku is characterized by delayed hair growth, progressive hair loss, and excessive accumulation of dermal cholesterol, triglycerides, and ceramides. The toku phenotype was attributed to a null allele of Gk5, encoding glycerol kinase 5 (GK5), a skin-specific kinase expressed predominantly in sebaceous glands. GK5 formed a complex with the sterol regulatory element-binding proteins (SREBPs) through their C-terminal regulatory domains, inhibiting SREBP processing and activation...
June 12, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28578514/the-beneficial-effects-of-hmg-coa-reductase-inhibitors-in-the-processes-of-neurodegeneration
#6
REVIEW
Seyed Soheil Saeedi Saravi, Seyed Sobhan Saeedi Saravi, Alireza Arefidoust, Ahmad Reza Dehpour
Statins, cholesterol lowering drugs, have been demonstrated to exert beneficial effects in other conditions such as primary and progressing neurodegenerative diseases beyond their original role. Observation that statins ameliorate the neurodegenerative diseases such as Parkinson's disease (PD), Alzheimer's disease (AD), multiple sclerosis (MS) and cerebral ischemic stroke, the neuroprotective effects of these drugs are thought to be linked to their anti-inflammatory, anti-oxidative, and anti-excitotoxic properties...
June 3, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28559607/seasonal-variation-in-phytochemicals-and-nutraceutical-potential-of-begonia-nelumbiifolia-consumed-in-puebla-m%C3%A3-xico
#7
Nemesio Villa-Ruano, Yesenia Pacheco-Hernández, Ramiro Cruz-Durán, Edmundo Lozoya-Gloria, Martha G Betancourt-Jiménez
Begonia nelumbiifolia is a traditional edible plant consumed and commercialized in the northern highlands of Puebla, México. The present study reports the seasonal variation in proximate analysis as well as organic acids, carotenoids and flavonoids content in both leaves and stalks of this plant. The stalks contained low concentrations of protein (~3%), fiber (~1.5%) and nitrogen free extract (~0.26%) during the time of study. Both organs showed contents of oxalic acid (91-103 mg 100 g(-1) FW), ascorbic acid (50-65 mg 100 g(-1) FW), lutein (1-2...
May 2017: Journal of Food Science and Technology
https://www.readbyqxmd.com/read/28559264/synergistic-activity-between-statins-and-bisphosphonates-against-acute-experimental-toxoplasmosis
#8
Zhu-Hong Li, Catherine Li, Sergio H Szajnman, Juan B Rodriguez, Silvia N J Moreno
Bisphosphonates are widely used for the treatment of bone disorders. These drugs also inhibit growth of a variety of protozoan parasites like Toxoplasma gondii, the etiologic agent of toxoplasmosis. The target of the most potent bisphosphonates is the isoprenoid biosynthesis pathway enzyme farnesyl diphosphate synthase (FPPS). Based on our previous work on the inhibitory effect of sulfur-containing linear bisphosphonates against T. gondii, we investigated the potential synergistic interaction between one of these derivatives (1-[(n-heptylthio)ethyl]-1,1-bisphosphonate, C7S, or compound 6) with statins, which are potent inhibitors of the host 3-hydroxy-3-methyl glutaryl-coenzyme A reductase (3-HMG-CoA reductase)...
May 30, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28556206/the-differences-in-the-incidence-of-diabetes-mellitus-and-prediabetes-according-to-the-type-of-hmg-coa-reductase-inhibitors-prescribed-in-korean-patients
#9
Tong Min Kim, Hyunah Kim, Yoo Jin Jeong, Sun Jung Baik, So Jung Yang, Seung-Hwan Lee, Jae-Hyoung Cho, Hyunyong Lee, Hyeon Woo Yim, In Young Choi, Kun-Ho Yoon, Hun-Sung Kim
BACKGROUND: Very few studies conducted in Korea have investigated the relationship between statins and the incidence of diabetes. Therefore, we analyzed the progression from normal blood glucose to prediabetes and then to diabetes mellitus (DM) according to the type, intensity, and dose of statin prescribed. METHODS: Data of patients who were first prescribed statins between 2009 and 2011 were extracted from electronic medical records. Patients with normal blood glucose or prediabetes were observed for 4 years after initiation of statin therapy...
May 29, 2017: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/28546657/statins-reduce-lipopolysaccharide-induced-cytokine-and-inflammatory-mediator-release-in-an-in-vitro-model-of-microglial-like-cells
#10
A J McFarland, A K Davey, S Anoopkumar-Dukie
The anti-inflammatory effects of statins (HMG-CoA reductase inhibitors) within the cardiovascular system are well-established; however, their neuroinflammatory potential is unclear. It is currently unknown whether statins' neurological effects are lipid-dependent or due to pleiotropic mechanisms. Therefore, the assumption that all statin compounds will have the same effect within the central nervous system is potentially inappropriate, with no studies to date having compared all statins in a single model. Thus, the aim of this study was to compare the effects of the six statins (atorvastatin, fluvastatin, pitavastatin, pravastatin, rosuvastatin, and simvastatin) within a single in vitro model of neuroinflammation...
2017: Mediators of Inflammation
https://www.readbyqxmd.com/read/28542128/hmg-coa-reductase-promotes-protein-prenylation-and-therefore-is-indispensible-for-t-cell-survival
#11
Sonja M Lacher, Julia Bruttger, Bettina Kalt, Jean Berthelet, Krishnaraj Rajalingam, Simone Wörtge, Ari Waisman
Statins are a well-established family of drugs that lower cholesterol levels via the competitive inhibition of the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGCR). In addition, the pleiotropic anti-inflammatory effects of statins on T cells make them attractive as therapeutic drugs in T-cell-driven autoimmune disorders. Since statins do not exclusively target HMGCR and thus might have varying effects on different cell types, we generated a new mouse strain allowing for the tissue-specific deletion of HMGCR...
May 25, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28539592/atorvastatin-promotes-phagocytosis-and-attenuates-pro-inflammatory-response-in-human-retinal-pigment-epithelial-cells
#12
Bo Tian, Ahmad Al-Moujahed, Peggy Bouzika, Yijun Hu, Shoji Notomi, Pavlina Tsoka, Joan W Miller, Haijiang Lin, Demetrios G Vavvas
Phagocytosis of daily shed photoreceptor outer segments is an important function of the retinal pigment epithelium (RPE) and it is essential for retinal homeostasis. RPE dysfunction, especially impairment of its phagocytic ability, plays an essential role in the pathogenesis of age-related macular degeneration (AMD). Statins, or HMG CoA (3-hydroxy-3-methylglutaryl-coenzyme A) reductase inhibitors, are drugs with multiple properties that have been extensively used to treat hyperlipidemia. However, their effect on RPE cells has not been fully elucidated...
May 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28536098/rosuvastatin-and-atorvastatin-are-ligands-of-the-human-car-rxr%C3%AE-complex
#13
Tadeja Rezen, Mateja Hafner, Sandhya Kortagere, Sean Ekins, Vesna Hodnik, Damjana Rozman
Statins are well known lipid lowering agents that inhibit the enzyme HMG-CoA reductase. They also activate drug metabolism but their exact receptor-mediated action has not been proven so far. The aim of this study was to test if atorvastatin and rosuvastatin are direct ligands of human CAR. We measured binding activities of atorvastatin and rosuvastatin to the human CAR/RXRα-LBD heterodimer with surface plasmon resonance (SPR). Additionally, three-dimensional models of CAR/RXRα-LBD were constructed by ligand-based and structure-based in silico modelling...
May 23, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28533986/atorvastatin-alters-the-expression-of-genes-related-to-bile-acid-metabolism-and-circadian-clock-in-livers-of-mice
#14
Wen-Kai Li, Huan Li, Yuan-Fu Lu, Ying-Ying Li, Zidong Donna Fu, Jie Liu
AIM: Atorvastatin is a HMG-CoA reductase inhibitor used for hyperlipidemia. Atorvastatin is generally safe but may induce cholestasis. The present study aimed to examine the effects of atorvastatin on hepatic gene expression related to bile acid metabolism and homeostasis, as well as the expression of circadian clock genes in livers of mice. METHODS: Adult male mice were given atorvastatin (10, 30, and 100 mg/kg, po) daily for 30 days, and blood biochemistry, histopathology, and gene expression were examined...
2017: PeerJ
https://www.readbyqxmd.com/read/28529486/the-role-of-statins-in-prevention-of-preeclampsia-a-promise-for-the-future
#15
REVIEW
Vasiliki Katsi, Georgios Georgountzos, Manolis S Kallistratos, Ioannis Zerdes, Thomas Makris, Athanasios J Manolis, Petros Nihoyannopoulos, Dimitris Tousoulis
Preeclampsia has been linked to high morbidity and mortality during pregnancy. However, no efficient pharmacological options for the prevention of this condition are currently available. Preeclampsia is thought to share several pathophysiologic mechanisms with cardiovascular disease, which has led to investigations for the potential role of statins (HMG CoA reductase inhibitors) in its prevention and early management. Pravastatin seems to have a safer pharmacokinetic profile compared to other statins, however, the existing preclinical evidence for its effectiveness in preeclampsia treatment has been mostly restricted to animal models...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28527898/triterpenes-and-meroterpenes-from-ganoderma-lucidum-with-inhibitory-activity-against-hmgs-reductase-aldose-reductase-and-%C3%AE-glucosidase
#16
Baosong Chen, Jin Tian, Jinjin Zhang, Kai Wang, Li Liu, Bo Yang, Li Bao, Hongwei Liu
Seven new compounds including four lanostane triterpenoids, lucidenic acids Q-S (1-3) and methyl ganoderate P (4), and three triterpene-farnesyl hydroquinone conjugates, ganolucinins A-C (5-7), one new natural product ganomycin J (8), and 73 known compounds (9-81) were isolated from fruiting bodies of Ganoderma lucidum. The structures of the compounds 1-8 were determined by spectroscopic methods. Bioactivities of compounds isolated were assayed against HMG-CoA reductase, aldose reductase, α-glucosidase, and PTP1B...
May 17, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28511341/in-vivo-and-molecular-docking-studies-using-whole-extract-and-phytocompounds-of-aegle-marmelos-fruit-protective-effects-against-isoproterenol-induced-myocardial-infarction-in-rats
#17
Gadamsetty Saayi Krushna, Vutharadhi Leela Shivaranjani, Jolapuram Umamaheswari, Cheemanapalli Srinivasulu, Shaik Althaf Hussain, Mohammed Abdul Kareem, Vaddi Damodara Reddy, Daoud Ali, Kiran Bharat Lokhande, K Venkateswara Swamy, Lakshmi Devi Kodidhela
Myocardial infarction (MI) is a leading major health problem with increased morbidity and mortality worldwide. The present study investigates isoproterenol (ISO) induced MI and the beneficial role of Aegle marmelos fruit extract (AMFE) in rats. Our results indicated the significant augmentation of plasma nitric oxide (NOx) levels, C-reactive protein (CRP), homocysteine, apolipoprotein B (apo-B), cardiac tissue lipid peroxidation and liver 3-hydroxy-3 methyl glutaryl CoA (HMG-CoA) reductase activity in ISO treated rats (85mg/kg b...
July 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28500274/combined-hmg-coa-reductase-and-prenylation-inhibition-in-treatment-of-ccm
#18
Sayoko Nishimura, Ketu Mishra-Gorur, JinSeok Park, Yulia V Surovtseva, Said M Sebti, Andre Levchenko, Angeliki Louvi, Murat Gunel
Cerebral cavernous malformations (CCMs) are common vascular anomalies that develop in the central nervous system and, more rarely, the retina. The lesions can cause headache, seizures, focal neurological deficits, and hemorrhagic stroke. Symptomatic lesions are treated according to their presentation; however, targeted pharmacological therapies that improve the outcome of CCM disease are currently lacking. We performed a high-throughput screen to identify Food and Drug Administration-approved drugs or other bioactive compounds that could effectively suppress hyperproliferation of mouse brain primary astrocytes deficient for CCM3...
May 23, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28489008/-do-opioids-sedatives-and-proton-pump-inhibitors-increase-the-risk-of-fractures
#19
Gudlaug Thorsdottir, Elisabet Benedikz, Sigridur A Thorgeirsdottir, Magnus Johannsson
INTRODUCTION: A pharmacoepidemiological study was conducted to analyse the relationship between bone fracture and the use of certain drugs. MATERIAL/METHODS: The study includes patients 40 years and older, diagnosed with bone fractures in the Emergency Department of Landspitali University Hospital in Reykjavik, Iceland, during a 10-year period (2002-2011). Also were included those who picked up from a pharmacy 90 DDD or more per year of the drugs included in the study in the capital region of Iceland during same period...
May 2017: Læknablađiđ
https://www.readbyqxmd.com/read/28484475/de-novo-sequencing-and-transcriptome-analysis-reveal-key-genes-regulating-steroid-metabolism-in-leaves-roots-adventitious-roots-and-calli-of-periploca-sepium-bunge
#20
Jian Zhang, Xinglin Li, Fuping Lu, Shanying Wang, Yunhe An, Xiaoxing Su, Xiankuan Li, Lin Ma, Guangjian Han
Periploca sepium Bunge is a traditional medicinal plant, whose root bark is important for Chinese herbal medicine. Its major bioactive compounds are C21 steroids and periplocin, a kind of cardiac glycoside, which are derived from the steroid synthesis pathway. However, research on P. sepium genome or transcriptomes and their related genes has been lacking for a long time. In this study we estimated this species nuclear genome size at 170 Mb (using flow cytometry). Then, RNA sequencing of four different tissue samples of P...
2017: Frontiers in Plant Science
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