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https://www.readbyqxmd.com/read/28430117/fluvastatin-therapy-could-not-decrease-progression-of-paroxysmal-atrial-fibrillation-in-non-valvular-disease-patients
#1
Qiang Tan, Shuangyue Zhang, Xiaoyi Zou, Jun Zhao, Jia Hao, Qian Sun
OBJECTIVE: This study aimed to evaluate whether fluvastatin therapy could decrease the probability of atrial fibrillation (AF) progression from paroxysmal AF to permanent AF and decrease the recurrence frequency of AF. METHODS: Analyses were performed using two-tailed Student's t test or Mann-Whitney U tests. Categorical variables were compared with the χ2 statistics or Fisher's exact test. Patients with paroxysmal AF were randomized case-control, prospective into either the fluvastatin group (n=61) or control group (n=57)...
April 10, 2017: Anatolian Journal of Cardiology
https://www.readbyqxmd.com/read/28423574/synergistic-anti-tumor-efficacy-of-sorafenib-and-fluvastatin-in-hepatocellular-carcinoma
#2
Yang Cheng, RongCheng Luo, Hang Zheng, Biao Wang, YaHui Liu, DingLi Liu, JinZhang Chen, WanFu Xu, AiMin Li, Yun Zhu
Drug resistance to sorafenib is common in patients with hepatocellular carcinoma(HCC). We examined the effects of a combination of sorafenib and fluvastatin on HCC using in vitro and in vivo models. The dual treatment induced apoptosis and reduced cellular viability in HCC more effectively than either drug alone. The combination treatment also inhibited activation of hepatic stellate cells, whereas single drug treatments did not. On a molecular level, combined treatment inhibited activation of the MAPK and NF-κB pathways via Toll-like receptor 4 in HCC cells...
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28384560/very-low-dose-fluvastatin-valsartan-combination-decreases-parameters-of-inflammation-and-oxidative-stress-in-patients-with-type-1-diabetes-mellitus
#3
Mojca Lunder, Miodrag Janić, Vedran Savić, Andrej Janež, Karin Kanc, Mišo Šabovič
AIMS: Previously we revealed the effectiveness of a new therapeutic approach with a short-term, very-low dose fluvastatin-valsartan combination on the improvement of arterial function in type 1 diabetes mellitus patients (T1DM). In this study we explored whether this approach influences inflammation and oxidative stress and explored any association of these effects with arterial function improvement. METHODS: This was a supplementary analysis of the two previous double blind randomized studies (included 44 T1DM patients)...
March 22, 2017: Diabetes Research and Clinical Practice
https://www.readbyqxmd.com/read/28303595/single-intra-articular-injection-of-fluvastatin-plga-microspheres-reduces-cartilage-degradation-in-rabbits-with-experimental-osteoarthritis
#4
Norio Goto, Ken Okazaki, Yukio Akasaki, Kohei Ishihara, Koji Murakami, Kiyoshi Koyano, Yasunori Ayukawa, Noriyuki Yasunami, Tomohiro Masuzaki, Yasuharu Nakashima
Statins are cholesterol-lowering drugs that inhibit 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, a rate-limiting enzyme of the mevalonate pathway. The anti-inflammatory effect of statins has been reported in recent years. The present study investigated therapeutic effects of the local administration of statin in osteoarthritis (OA). We assessed clinically used statins and selected fluvastatin for further experimentation, as it showed potent anabolic and anti-catabolic effects on human OA chondrocytes...
March 17, 2017: Journal of Orthopaedic Research: Official Publication of the Orthopaedic Research Society
https://www.readbyqxmd.com/read/28302946/influence-of-lyophilization-factors-and-gelatin-concentration-on-pore-structures-of-atelocollagen-gelatin-sponge-biomaterial
#5
Longqiang Yang, Koji Tanabe, Tadashi Miura, Masao Yoshinari, Shinji Takemoto, Seikou Shintani, Masataka Kasahara
This study aimed to investigate influences of lyophilization factors and gelatin concentration on pore structures of ACG sponge. ACG sponges of different freezing temperatures (-30, -80 and -196(o)C), freezing times (1, 2 and 24 h), gelatin concentrations (0.6%AC+0.15%G, 0.6%AC+0.6%G and 0.6%AC+2.4%G), and with 500 μM fluvastatin were fabricated. Pore structures including porosity and pore size were analyzed by scanning electron microscopy and ImageJ. The cytotoxic effects of ACG sponges were evaluated in vitro...
March 8, 2017: Dental Materials Journal
https://www.readbyqxmd.com/read/28302944/release-properties-of-atelocollagen-gelatin-complexes-as-carriers-for-local-administration-of-fluvastatin
#6
Koichi Kida, Koji Tanabe, Hodaka Sasaki, Yoshitaka Furuya, Tadashi Miura, Masao Yoshinari, Yasutomo Yajima
The aim of this study was to investigate properties of atelocollagen/gelatin complexes (AC/Gel) and their characteristics of sustained statin release, to assess the utility of AC/Gel. AC/Gel were prepared by changing the mixing ratio of AC (0 to 40% of AC). Analysis of spectra of fluvastatin (Flu), gelatin (Gel), and Flu with Gel complex using a Fourier transform-infrared spectrometer indicates that Flu was bound to Gel through a bond involving the carboxyl and amino groups. Evaluation of characteristics of sustained release of Flu from the AC/Gel using an ultraviolet-visible spectrophotometer showed that the release rate of Flu decreased with increasing the AC content...
March 8, 2017: Dental Materials Journal
https://www.readbyqxmd.com/read/28295913/identification-and-characterization-of-fluvastatin-metabolites-in-rats-by-uhplc-q-tof-ms-ms-and-in-silico-toxicological-screening-of-the-metabolites
#7
Balasaheb B Chavan, Pradipbhai D Kalariya, Rakesh D Nimbalkar, Prabha Garg, R Srinivas, M V N Kumar Talluri
The present study reports the in vivo and in vitro identification and characterization of metabolites of fluvastatin (FLU), the HMG CoA reductase inhibitor, using liquid chromatography-mass spectrometry (LC-MS). In vitro studies were conducted by incubating the drug with human liver microsomes (HLM) and rat liver microsomes (RLM). In vivo studies were carried out by administration of the drug in the form of suspension to the Sprague-Dawley (SD) rats followed by collection of urine, faeces and blood at different time points upto 24 h...
March 11, 2017: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/28214901/protective-effects-of-fluvastatin-on-reproductive-function-in-obese-male-rats-induced-by-high-fat-diet-through-enhanced-signaling-of-mtor
#8
Xiangrong Cui, Chunlan Long, Jing Zhu, Jie Tian
BACKGROUND: Statins can reduce reproductive damage induced by obesity or high-fat diet (HFD), but the specific regulatory mechanisms are largely unknown. Since mTOR/p70s6k sinaling promotes spermatogonia proliferation and spermatogenesis, we hypothesized that this pathway will be involved in the protective effects of statin in HFD-induced reproductive dysfunction. METHODS: Male Sprague Dawley rats (3 weeks old) were randomly divided into a control group (standard diet), HFD group, and a fluvastatin group (HFD + fluvastatin at 6mg/kg, once daily by oral gavage)...
February 3, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28190756/organic-anion-transporting-polypeptide-oatp-2b1-contributes-to-the-cellular-uptake-of-theaflavin
#9
Ayuko Kondo, Katsuya Narumi, Jiro Ogura, Ai Sasaki, Keisuke Yabe, Taku Kobayashi, Ayako Furugen, Masaki Kobayashi, Ken Iseki
Organic anion-transporting polypeptide (OATP) 2B1 has been reported in the apical membranes of the human small intestinal epithelium, where it contributes to the intestinal absorption of pharmacologically active drugs. To investigate the potential for OATP2B1-mediated drug-food interactions, the effects of several polyphenolic compounds on OATP2B1-mediated estrone-3-sulfate (E3S) transport were studied by using OATP2B1-expressing HEK293 cells. Our results showed that some compounds, especially theaflavin, were strong inhibitors of OATP2B1-mediated E3S uptake...
November 22, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28188574/reliable-rate-measurements-for-active-and-passive-hepatic-uptake-using-plated-human-hepatocytes
#10
Yi-An Bi, Renato J Scialis, Sarah Lazzaro, Sumathy Mathialagan, Emi Kimoto, Julie Keefer, Hui Zhang, Anna M Vildhede, Chester Costales, A David Rodrigues, Larry M Tremaine, Manthena V S Varma
Transporter-mediated hepatic uptake is proven to be the rate-determining step in the systemic clearance of several drugs. Therefore, accurate measurement of active and passive uptake clearances in vitro is critical to facilitate pharmacokinetics and drug-drug interaction predictions. Here, we evaluated the plated human hepatocytes (PHH) and studied the effect of incubation temperature and inhibitor concentration on uptake measurements, in order to reliably estimate hepatic uptake components. Uptake rates measured using PHH, at 37°C without and with rifamycin SV, were comparable with those obtained from suspension hepatocytes and sandwich-cultured hepatocytes for a set of 10-13 compounds...
February 10, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28114645/association-of-daily-dosage-and-type-of-statin-agent-with-risk-of-open-angle-glaucoma
#11
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/28089347/virtual-screening-and-experimental-validation-identify-novel-modulators-of-nuclear-receptor-rxr%C3%AE-from-drugbank-database
#12
Dan Xu, Lijun Cai, Shangjie Guo, Lei Xie, Meimei Yin, Ziwen Chen, Hu Zhou, Ying Su, Zhiping Zeng, Xiaokun Zhang
Retinoid X receptor alpha (RXRα), an important ligand-dependent transcription factor, plays a critical role in the development of various cancers and metabolic and neurodegenerative diseases. Therefore, RXRα represents one of the most important targets in modern drug discovery. In this study, Drugbank 2.0 with 1280 old drugs were virtually screened by Glide according to the crystal structure of ligand-binding domain (LBP) of RXRα. 15 compounds selected were tested for their binding and transcriptional activity toward RXRα by Biacore and reporter gene assay, respectively...
December 26, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28073164/protective-role-of-endogenous-plasmalogens-against-hepatic-steatosis-and-steatohepatitis
#13
Jung Eun Jang, Han-Sol Park, Hyun Ju Yoo, In-Jeoung Baek, Ji Eun Yoon, Myoung Seok Ko, Ah-Ram Kim, Hyoun Sik Kim, Hye-Sun Park, Seung Eun Lee, Seung-Whan Kim, Su Jung Kim, Jaechan Leem, Yu Mi Kang, Min Kyo Jung, Chan-Gi Pack, Chong Jai Kim, Chang Ohk Sung, In-Kyu Lee, Joong-Yeol Park, José C Fernández-Checa, Eun Hee Koh, Ki-Up Lee
Free cholesterol (FC) accumulation in the liver is an important pathogenic mechanism of nonalcoholic steatohepatitis (NASH). Plasmalogens, key structural components of the cell membrane, act as endogenous antioxidants and are primarily synthesized in the liver. However, the role of hepatic plasmalogens in metabolic liver disease is unclear. In this study, we found that hepatic levels of docosahexaenoic acid (DHA)-containing plasmalogens, expression of glyceronephosphate O-acyltransferase (Gnpat, the rate-limiting enzyme in plasmalogen biosynthesis), and expression of Pparα were lower in mice with NASH caused by accumulation of free cholesterol (FC) in the liver...
January 10, 2017: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/28013371/the-effect-of-fluvastatin-on-cardiac-fibrosis-and-angiotensin-converting-enzyme-2-expression-in-glucose-controlled-diabetic-rat-hearts
#14
Young Hee Shin, Jeong Jin Min, Jong-Hwan Lee, Eun-Hee Kim, Go Eun Kim, Myung Hee Kim, Jeong Jin Lee, Hyun Joo Ahn
Independently of the lipid-lowering effects, statin has been reported to attenuate the development of diabetic cardiomyopathy. However, the effect of statin in glucose-controlled diabetic condition has not been demonstrated. We evaluated the effect of fluvastatin on cardiac function, fibrosis, and angiotensin-converting enzyme-2 (ACE2) expression in glucose-controlled diabetic rats. Male Wistar rats were randomly divided into four groups: control (Group C), diabetes (Group D), diabetes with insulin (Group I), and diabetes with insulin and fluvastatin (Group I+F)...
December 24, 2016: Heart and Vessels
https://www.readbyqxmd.com/read/28012835/impaired-endothelial-function-and-arterial-stiffness-in-patients-with-type-2-diabetes-the-effect-of-a-very-low-dose-combination-of-fluvastatin-and-valsartan
#15
Maja Boncelj Svetek, Barbara Eržen, Karin Kanc, Mišo Šabovič
AIM: Patients with type 2 diabetes are at increased cardiovascular risk. The aim was to explore whether the impaired arterial wall characteristics typical of these patients could be improved by the unique beneficial effects of a very low-dose combination of fluvastatin and valsartan (low-flu/val). METHODS: Forty middle-aged males (50.4±6.1years) with type 2 diabetes were recruited to a double-blind, randomized study. Patients (N=20) received low-flu/val (10/20mg) or placebo (N=20) over 30days in addition to their regular therapy...
March 2017: Journal of Diabetes and its Complications
https://www.readbyqxmd.com/read/28011020/environmental-photochemical-fate-of-selected-pharmaceutical-compounds-in-natural-and-reconstituted-suwannee-river-water-role-of-reactive-species-in-indirect-photolysis
#16
Hanoz Santoke, William J Cooper
This study reports the impact of two reactive species, hydroxyl radical and singlet oxygen, on the photochemical degradation of three selected pharmaceutical compounds in natural and reconstituted solutions of Suwannee River water. Absolute bimolecular rate constants (M(-1)s(-1)) were determined for the reaction of hydroxyl radical and singlet oxygen with danofloxacin ((6.15±0.11)×10(9); (7.50±0.13)×10(4)), fluvastatin ((6.96±0.16)×10(9); (1.64±0.18)×10(8)), and paroxetine ((8.65±0.12)×10(9), (1.18±0...
February 15, 2017: Science of the Total Environment
https://www.readbyqxmd.com/read/28005438/interactions-of-crizotinib-and-gefitinib-with-organic-anion-transporting-polypeptides-oatp-1b1-oatp1b3-and-oatp2b1-gefitinib-shows-contradictory-interaction-with-oatp1b3
#17
Toshihiro Sato, Hajime Ito, Ayaka Hirata, Takaaki Abe, Nariyasu Mano, Hiroaki Yamaguchi
1. The drug-drug interaction (DDI) mediated by organic anion-transporting polypeptide (OATP)1B1, OATP1B3 and OATP2B1 has a major impact on the hepatic clearance of drugs. The effects of tyrosine kinase inhibitors (TKIs) on OATPs have not been well studied. In the present study, we evaluated the contribution of OATPs to the hepatic uptake of crizotinib and gefitinib and the interaction of those TKIs with OATPs to estimate DDIs. 2. To clarify whether crizotinib and gefitinib were substrates for OATPs, we performed uptake studies...
January 12, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27989745/interaction-of-different-statins-with-model-membranes-by-nmr-data
#18
L F Galiullina, O V Aganova, I A Latfullin, G S Musabirova, A V Aganov, V V Klochkov
Hydroxy-methyl-glutaryl-coenzyme A (HMG-CoA) reductase inhibitors or statins reduce the amount of low-density lipoprotein (LDL) cholesterol, which is known as a well-established risk factor for atherosclerosis. Despite the fact that statins have a common pharmacologic target essential to sterol biosynthesis, their efficacy, safety, and potential non-LDL actions vary significantly for different statins. There is a hypothesis that pharmacological features of statins depend on their location in cell membrane, but to the present day there is a lack of information in literature on interactions of statins with the surface of the cell membrane in liquid media...
December 16, 2016: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/27924788/effect-of-statins-type-on-incident-prostate-cancer-risk-a-meta-analysis-and-systematic-review
#19
Ping Tan, Chen Zhang, Shi-You Wei, Zhuang Tang, Liang Gao, Lu Yang, Qiang Wei
The aim of this study is to investigate the effect of statins type or even when grouping statins by hydrophilic or hydrophobic nature on prostate cancer risk. A literature search was performed without language restrictions using the databases of PubMed (1984.1-2015.3), MEDLINE (1984.1-2015.3), and EMBASE (1990.1-2015.3). Two independent reviewers appraised eligible studies and extracted data. Weighted averages were reported as relative risk (RR) with 95% confidence intervals (CI). Statistic heterogeneity scores were assessed with the standard Cochran's Q-test and I2 statistic...
December 2, 2016: Asian Journal of Andrology
https://www.readbyqxmd.com/read/27888640/chronotherapy-versus-conventional-statins-therapy-for-the-treatment-of-hyperlipidaemia
#20
REVIEW
Jose Manuel Izquierdo-Palomares, Jesus Maria Fernandez-Tabera, Maria N Plana, Almudena Añino Alba, Pablo Gómez Álvarez, Inmaculada Fernandez-Esteban, Luis Carlos Saiz, Pilar Martin-Carrillo, Óscar Pinar López
BACKGROUND: Elevated levels of total cholesterol and low-density lipoprotein play an important role in the development of atheromas and, therefore, in cardiovascular diseases. Cholesterol biosynthesis follows a circadian rhythm and is principally produced at night (between 12:00 am and 6:00 am). The adjustment of hypolipaemic therapy to biologic rhythms is known as chronotherapy. Chronotherapy is based on the idea that medication can have different effects depending on the hour at which it is taken...
November 26, 2016: Cochrane Database of Systematic Reviews
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