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https://www.readbyqxmd.com/read/28282493/molecular-and-vibrational-dynamics-in-a-cholesterol-lowering-agent-lovastatin-solid-state-nmr-inelastic-neutron-scattering-and-periodic-dft-study
#1
Pawel Bilski, Kacper Drużbicki, Jacek Jenczyk, Jadwiga Mielcarek, Jan Wasicki
Molecular and vibrational dynamics of a widely used cholesterol-lowering agent, lovastatin, have been studied by combining nuclear magnetic resonance relaxation experiments (1H NMR) with inelastic neutron scattering (INS) and periodic density functional theory modeling (Plane-Wave DFT). According to the complementary experimental study, lovastatin shows no phase transitions down to the cryogenic conditions, while a progressive, stepwise activation of several molecular motions is observed below the room temperature...
March 10, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28277227/-red-yeast-rice-induced-muscular-injuries-analysis-of-french-pharmacovigilance-database-and-literature-review
#2
Christelle Philibert, Virginie Bres, Marie-Josèphe Jean-Pastor, Claire Guy, Bénédicte Lebrun-Vignes, Perrine Robin, Véronique Pinzani, Dominique Hillaire-Buys
Red yeast rice (RYR) is a dietary supplement containing monacolins obtained by fermentation of Monascus purpureus strains. Because of its structural homology with lovastatin, monacolin K inhibits HMG-CoA reductase and shows hypocholesterolemic properties comparable to synthetic statins. We studied all cases of myopathy involving RYR reported in the French national pharmacovigilance database (6 cases) and in scientific literature (9 cases). Among these cases, 9 showed elevated creatine kinase, 3 rhabdomyolysis and 2 myalgia...
October 27, 2016: Thérapie
https://www.readbyqxmd.com/read/28276528/variability-in-statin-induced-changes-in-gene-expression-profiles-of-pancreatic-cancer
#3
Helena Gbelcová, Silvie Rimpelová, Tomáš Ruml, Marie Fenclová, Vítek Kosek, Jana Hajšlová, Hynek Strnad, Michal Kolář, Libor Vítek
Statins, besides being powerful cholesterol-lowering drugs, also exert potent anti-proliferative activities. However, their anti-cancer efficacy differs among the individual statins. Thus, the aim of this study was to identify the biological pathways affected by individual statins in an in vitro model of human pancreatic cancer. The study was performed on a human pancreatic cancer cell line MiaPaCa-2, exposed to all commercially available statins (12 μM, 24 h exposure). DNA microarray analysis was used to determine changes in the gene expression of treated cells...
March 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28257063/red-yeast-rice
#4
Thu Nguyen, Mitchell Karl, Antonello Santini
Red yeast rice (RYR), produced by the fermentation of the Monascus purpureus mold, has been used for a long time in Asian cuisine and traditional medicine. It consists of multiple bioactive substances, including monacolins, which potentially can be used as a nutraceutical. Monacolin K, which is chemically identical to lovastatin, has been recognized as responsible for the cholesterolreducing effect of this compound. While the European Food Safety Authority maintains that the use of monacolin K from RYR preparations of at least 10 mg can produce a normal blood cholesterol level, the United States Food and Drug Administration considers monacolin K, due to its similarity with lovastatin, an unapproved drug, and therefore marketing of products that label the monacolin content is prohibited...
March 1, 2017: Foods (Basel, Switzerland)
https://www.readbyqxmd.com/read/28247468/discovery-and-quantitative-structure-activity-relationship-study-of-lepidopteran-hmg-coa-reductase-inhibitors-as-selective-insecticides
#5
Yang-Yang Zang, Yuan-Mei Li, Yue Yin, Shan-Shan Chen, Zhen-Peng Kai
BACKGROUND: In the previous study, we have demonstrated that insect 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) can be a potential selective insecticide target. Three series of inhibitors were designed based on the difference of HMGR structures from Homo sapiens and Manduca sexta with the aim for discovering potent selective insecticide candidate. RESULTS: Bioassay in vitro showed that gem-difluoromethylenated statin analogs have potent effects on JH biosynthesis of M...
March 1, 2017: Pest Management Science
https://www.readbyqxmd.com/read/28246253/association-between-statin-use-and-ischemic-stroke-or-major-hemorrhage-in-patients-taking-dabigatran-for-atrial-fibrillation
#6
Tony Antoniou, Erin M Macdonald, Zhan Yao, Simon Hollands, Tara Gomes, Mina Tadrous, Muhammad M Mamdani, David N Juurlink
BACKGROUND: Dabigatran etexilate is a prodrug whose absorption is opposed by intestinal P-glycoprotein and which is converted by carboxylesterase to its active form, dabigatran. Unlike other statins, simvastatin and lovastatin are potent inhibitors of P-glycoprotein and carboxylesterase, and might either increase the risk of hemorrhage with dabigatran etexilate or decrease its effectiveness. METHODS: We conducted 2 population-based, nested case-control studies involving Ontario residents 66 years of age and older who started dabigatran etexilate between May 1, 2012, and Mar...
January 9, 2017: CMAJ: Canadian Medical Association Journal, Journal de L'Association Medicale Canadienne
https://www.readbyqxmd.com/read/28217821/physicians-experiences-as-patients-with-statin-side-effects-a-case-series
#7
Hayley J Koslik, Athena Hathaway Meskimen, Beatrice Alexandra Golomb
Physicians are among those prescribed statins and therefore, subject to potential statin adverse effects (AEs). There is little information on the impact of statin AEs on physicians affected by them. We sought to assess the character and impact of statin AEs occurring in physicians and retired physicians, and to ascertain whether/how personal experience of AEs moderated physicians' attitude toward statin use. Seven active or retired physicians from the United States communicated with the Statin Effects Study group regarding their personal experience of statin AEs...
December 2017: Drug Safety—Case Reports
https://www.readbyqxmd.com/read/28212283/the-effects-of-tocotrienol-and-lovastatin-co-supplementation-on-bone-dynamic-histomorphometry-and-bone-morphogenetic-protein-2-expression-in-rats-with-estrogen-deficiency
#8
Kok-Yong Chin, Saif Abdul-Majeed, Norazlina Mohamed, Soelaiman Ima-Nirwana
Both tocotrienol and statins are suppressors of the mevalonate pathway. Supplementation of tocotrienol among statin users could potentially protect them against osteoporosis. This study aimed to compare the effects of tocotrienol and lovastatin co-supplementation with individual treatments on bone dynamic histomorphometric indices and bone morphogenetic protein-2 (BMP-2) gene expression in ovariectomized rats. Forty-eight female Sprague-Dawley rats were randomized equally into six groups. The baseline was sacrificed upon receipt...
February 15, 2017: Nutrients
https://www.readbyqxmd.com/read/28197521/impact-of-kelussia-odoratissima-mozaffarian-lipid-profile-and-fasting-blood-sugar-in-hyperlipidemia-patients
#9
Marzieh Kafeshani, Mahmoud Mirhosseini, Ali Momeni, Rahmatollah Rabiei, Mahmoud Rafieian-Kopaei
Introduction: Hyperlipidemia is associated with increased risk of cardiovascular disease. Each type of medication works differently and has different types of side effects. Flavonoids are a group of polyphenolic compounds with antioxidant properties that help reducing the cardiovascular risk factors. Kelussia odoratissima is a flavonoid containing plant. Objectives: The aim of this study was investigating the effect of this herb on lipid and glucose profile in hyperlipidemia patients. PATIENTS AND METHODS: This study performed on 61 hyperlipidemia patients...
2017: J Nephropharmacol
https://www.readbyqxmd.com/read/28153650/development-of-enteric-coated-fixed-dose-combinations-of-amorphous-solid-dispersions-of-ezetimibe-and-lovastatin-investigation-of-formulation-and-process-parameters
#10
Manoela K Riekes, Aswin Dereymaker, Philippe Berben, Patrick Augustijns, Hellen K Stulzer, Guy Van den Mooter
Enteric-coated fixed-dose combinations of ezetimibe and lovastatin were prepared by fluid bed coating aiming to avoid the acidic conversion of lovastatin to its hydroxyacid derivative. In a two-step process, sucrose beads were layered with a glass solution of ezetimibe, lovastatin and Soluplus(®), top-coated with an enteric layer. The impact of different bead size, enteric polymers (Eudragit L100(®) and Eudragit L100-55(®)) and coating time was investigated. Samples were evaluated by X-ray diffraction, scanning electron microscopy, laser diffraction and in vitro studies in 0...
March 30, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28142219/the-influence-of-oxygen-concentration-on-the-extracellular-matrix-production-of-human-nucleus-pulposus-cells-during-isolation-expansion-process
#11
Shu-Hua Yang, Ming-Hsiao Hu, Wan-Yu Lo, Yuan-Hui Sun, Chang-Chin Wu, Kai-Chiang Yang
Nucleus pulposus (NP) cells locate in the center of avascular intervertebral discs, and thus have presumably adapted to a hypoxic environment. The purpose of this study was to investigate the influences of hypoxic condition, during isolation-expansion of human NP cells, on the cellular proliferation and extracellular matrix (ECM) synthesis in later three-dimensional cultures. Human NP tissues were obtained from patients who underwent lumbar disc surgeries. Immediately after retrieval, NP tissues from each patient were divided into two aliquots for in vitro cultivation either under classical normoxic (21% O2 ) or hypoxic (3...
January 31, 2017: Journal of Biomedical Materials Research. Part A
https://www.readbyqxmd.com/read/28135339/inhibition-of-nf-%C3%AE%C2%BAb-pathway-and-modulation-of-mapk-signaling-pathways-in-glioblastoma-and-implications-for-lovastatin-and-tumor-necrosis-factor-related-apoptosis-inducing-ligand-trail-combination-therapy
#12
Pi Chu Liu, Gang Lu, Yi Deng, Cheng Dong Wang, Xian Wei Su, Jing Ye Zhou, Tat Ming Chan, Xiang Hu, Wai Sang Poon
Glioblastoma is a common malignant brain tumor and it is refractory to therapy because it usually contains a mixture of cell types. The tumor necrosis factor-related apoptosis inducing ligand (TRAIL) has been shown to induce apoptosis in a range of tumor cell types. Previously, we found that two human glioblastoma cell lines are resistant to TRAIL, while lovastatin sensitizes these glioblastoma cells to TRAIL-induced cell death. In this study, we investigated the mechanisms underlying the TRAIL-induced apoptosis in human glioblastoma cell lines by lovastatin...
2017: PloS One
https://www.readbyqxmd.com/read/28128718/prehispanic-functional-foods-and-nutraceuticals-in-the-treatment-of-dyslipidemia-associated-to-cardiovascular-disease-a-mini-review
#13
Alejandro Ríos-Hoyo, Alejandra Romo-Araiza, Marcos Meneses-Mayo, Gabriela Guttiérrez-Salmeán
Dyslipidemia is an important modifi able risk factor for cardiovascular and metabolic diseases, which are responsible for a large number of mortality and disability cases around the globe. Different strategies have been used within the treatment of dyslipidemia, including lifestyle modifi cations, pharmacologic therapy, as well as functional foods and nutraceuticals. Functional foods have been used worldwide since ancient times, particularly, the prehispanic civilizations utilized several as medicinal foods...
January 27, 2017: International Journal for Vitamin and Nutrition Research. Journal International de Vitaminologie et de Nutrition
https://www.readbyqxmd.com/read/28127721/stabilization-and-amorphization-of-lovastatin-using-different-types-of-silica
#14
Mai Khanfar, Suhair Al-Nimry
Lovastatin (LOV), an antihyperlipidimic agent, is characterized by low solubility/poor dissolution and, thus, low bioavailability (<5%). A beneficial effect on its bioavailability could result from improving its dissolution. One of the most common methods used to enhance dissolution is the preparation of solid dispersions. Solid dispersions of LOV and silica with different surface areas were prepared. The effects of the type of silica, ratio of drug/silica, incubation period with silica, and the effect of surface area were all studied...
January 26, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28114645/association-of-daily-dosage-and-type-of-statin-agent-with-risk-of-open-angle-glaucoma
#15
Nidhi Talwar, David C Musch, Joshua D Stein
Importance: There is growing evidence that statins may protect against the development or worsening of open-angle glaucoma (OAG). As researchers plan clinical trials to more definitively study whether statins indeed protect against OAG, it would be helpful to know whether specific daily dosages or types of statin confer a greater protective effect than others. Objective: To assess whether the protective effect of statins on the risk of glaucoma varies depending on the daily dosage or type of statin taken...
March 1, 2017: JAMA Ophthalmology
https://www.readbyqxmd.com/read/28109635/impact-of-high-cholesterol-in-a-parkinson-s-disease-model-prevention-of-lysosomal-leakage-versus-stimulation-of-%C3%AE-synuclein-aggregation
#16
Ida Eriksson, Sangeeta Nath, Per Bornefall, Ana Maria Villamil Giraldo, Karin Öllinger
Parkinson's disease is characterized by accumulation of intraneuronal cytoplasmic inclusions, Lewy bodies, which mainly consist of aggregated α-synuclein. Controversies exist as to whether high blood cholesterol is a risk factor for the development of the disease and whether statin treatment could have a protective effect. Using a model system of BE(2)-M17 neuroblastoma cells treated with the neurotoxin 1-methyl-4-phenylpyridinium (MPP(+)), we found that MPP(+)-induced cell death was accompanied by cholesterol accumulation in a lysosomal-like pattern in pre-apoptotic cells...
January 16, 2017: European Journal of Cell Biology
https://www.readbyqxmd.com/read/28102516/production-of-lovastatin-and-itaconic-acid-by-aspergillus-terreus-a-comparative-perspective
#17
REVIEW
Tomasz Boruta, Marcin Bizukojc
Aspergillus terreus is a textbook example of an industrially relevant filamentous fungus. It is used for the biotechnological production of two valuable metabolites, namely itaconic acid and lovastatin. Itaconic acid serves as a precursor in polymer industry, whereas lovastatin found its place in the pharmaceutical market as a cholesterol-lowering statin drug and a precursor for semisynthetic statins. Interestingly, their biosynthetic gene clusters were shown to reside in the common genetic neighborhood. Despite the genomic proximity of the underlying biosynthetic genes, the production of lovastatin and itaconic acid was shown to be favored by different factors, especially with respect to pH values of the broth...
February 2017: World Journal of Microbiology & Biotechnology
https://www.readbyqxmd.com/read/28093797/adverse-reactions-to-dietary-supplements-containing-red-yeast-rice-assessment-of-cases-from-the-italian-surveillance-system
#18
Gabriela Mazzanti, Paola Angela Moro, Emanuel Raschi, Roberto Da Cas, Francesca Menniti-Ippolito
AIMS: Red yeast rice (RYR) is contained in dietary supplements for patients with dyslipidemia. RYR supplements contain monacolin K, which is chemically identical to lovastatin, a licensed drug with a well-known risk profile. We aim to describe the safety profile of RYR by analysing spontaneous reports of suspected adverse reactions (ARs). METHODS: Within the Italian Surveillance System of Natural Health Products, suspected ARs were collected and evaluated by a multidisciplinary group of experts to assess causality using the WHO-UMC system or the CIOMS/RUCAM score, for hepatic reactions...
April 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28061433/lovastatin-upregulates-microrna-29b-to-reduce-oxidative-stress-in-rats-with-multiple-cardiovascular-risk-factors
#19
Fu Wang, Hui Ma, Wen-Jing Liang, Jing-Jing Yang, Xue-Qing Wang, Mei-Rong Shan, Yuan Chen, Min Jia, Ya-Ling Yin, Xue-Ying Sun, Jia-Ning Zhang, Qi-Sheng Peng, Yu-Guo Chen, Li-Ying Liu, Peng Li, Tao Guo, Shuang-Xi Wang
AIMS: Proteasome-linked oxidative stress is believed to cause endothelial dysfunction, an early event in cardiovascular diseases (CVD). Statin, as HMG-CoA reductase inhibitor, prevents endothelial dysfunction in CVD. However, the molecular mechanism of statin-mediated normalization of endothelial function is not completely elucidated. METHODS AND RESULTS: Lovastatin time/dose-dependently increased miR-29b expression and decreased proteasome activity in cultured human umbilical vein endothelial cells (HUVECs)...
February 7, 2017: Oncotarget
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
#20
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
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