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https://www.readbyqxmd.com/read/28334528/why-prodrugs-and-propesticides-succeed
#1
John E Casida
What are the advantages of bioactivation in optimizing drugs and pesticides? Why are there so many prodrugs and propesticides? These questions are examined here by considering compounds selected on the basis of economic value or market success. The 100 major drugs and 90 major pesticides are divided into ones acting directly and those definitely or possibly requiring bioactivation. Established or candidate prodrugs accounted for 19% of the total drug sales with corresponding values of 20, 37 and 17% for proinsecticides, proherbicides and profungicides...
March 23, 2017: Chemical Research in Toxicology
https://www.readbyqxmd.com/read/28333970/-epicatechin-3-o-%C3%AE-d-allopyranoside-from-davallia-formosana-prevents-diabetes-and-dyslipidemia-in-streptozotocin-induced-diabetic-mice
#2
Cheng-Hsiu Lin, Jin-Bin Wu, Jia-Ying Jian, Chun-Ching Shih
The objective of this study was to evaluate the effects and molecular mechanism of (-)-epicatechin-3-O-β-D-allopyranoside from Davallia formosana (BB) (also known as Gu-Sui-Bu) on type 1 diabetes mellitus and dyslipidemia in streptozotocin (STZ)-induced diabetic mice. This plant was demonstrated to display antioxidant activities and possess polyphenol contents. Diabetic mice were randomly divided into six groups and were given daily oral gavage doses of either BB (at three dosage levels), metformin (Metf) (at 0...
2017: PloS One
https://www.readbyqxmd.com/read/28290603/fenofibrate-exerts-protective-effects-against-gentamicin-induced-toxicity-in-cochlear-hair-cells-by-activating-antioxidant-enzymes
#3
Channy Park, Hye-Min Ji, Se-Jin Kim, Sung-Hee Kil, Joon No Lee, Seongae Kwak, Seong-Kyu Choe, Raekil Park
Fenofibrate, an activator of peroxisome proliferator-activated receptors (PPARs), has been shown to protect the kidneys and brain cells from oxidative stress; however, its role in preventing hearing loss has not been reported to date, at least to the best of our knowledge. In this study, we demonstrated the protective effects of fenofibrate against gentamicin (GM)-induced ototoxicity. We found that the auditory brainstem response threshold which was increased by GM was significantly reduced by pre-treatment with fenofibrate in rats...
March 10, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28287432/a-biologically-based-computational-approach-to-drug-repurposing-for-anthrax-infection
#4
Jane P F Bai, Theodore Sakellaropoulos, Leonidas G Alexopoulos
Developing drugs to treat the toxic effects of lethal toxin (LT) and edema toxin (ET) produced by B. anthracis is of global interest. We utilized a computational approach to score 474 drugs/compounds for their ability to reverse the toxic effects of anthrax toxins. For each toxin or drug/compound, we constructed an activity network by using its differentially expressed genes, molecular targets, and protein interactions. Gene expression profiles of drugs were obtained from the Connectivity Map and those of anthrax toxins in human alveolar macrophages were obtained from the Gene Expression Omnibus...
March 10, 2017: Toxins
https://www.readbyqxmd.com/read/28287050/the-effect-of-fenofibric-acid-on-the-pharmacokinetics-and-pharmacodynamics-of-warfarin-in-rats
#5
Chaorui Guo, Siqi Xue, Xiufen Zheng, Lu Yang, Di Zhao, Xijing Chen, Ning Li
1. Case reports have shown that coadministration of fenofibric acid (FA) could increase bleeding risks of warfarin, but the mechanisms remained unknown. We therefore investigated the pharmacokinetic and pharmacodynamic interaction between warfarin and FA in rats. 2. Rats received warfarin alone (2 mg/kg) or coadministered with FA (100 mg/kg). FA significantly increased the exposure to warfarin, and decreased that to 7-hydroxywarfarin in rats nearly by two-fold, meanwhile increased Cmax and prolonged t1/2 of warfarin...
March 13, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28279662/in%C3%A2-vivo-interactions-between-%C3%AE-7-nicotinic-acetylcholine-receptor-and-nuclear-peroxisome-proliferator-activated-receptor-%C3%AE-implication-for-nicotine-dependence
#6
Asti Jackson, Deniz Bagdas, Pretal P Muldoon, Aron H Lichtman, F Ivy Carroll, Mark Greenwald, Michael F Miles, M Imad Damaj
Chronic tobacco use dramatically increases health burdens and financial costs. Limitations of current smoking cessation therapies indicate the need for improved molecular targets. The main addictive component of tobacco, nicotine, exerts its dependency effects via nicotinic acetylcholine receptors (nAChRs). Activation of the homomeric α7 nAChR reduces nicotine's rewarding properties in conditioned place preference (CPP) test and i.v. self-administration models, but the mechanism underlying these effects is unknown...
March 7, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28270521/pathogenic-role-of-microrna-21-in-diabetic-retinopathy-through-down-regulation-of-ppar%C3%AE
#7
Qian Chen, Fangfang Qiu, Kelu Zhou, H Greg Matlock, Yusuke Takahashi, Raju V S Rajala, Yanhui Yang, Elizabeth Moran, Jian-Xing Ma
Fenofibrate, a specific agonist of peroxisome proliferator-activated receptor alpha (PPARα), displays robust therapeutic effects on diabetic retinopathy (DR) in type 2 diabetic patients. Our recent studies have shown that PPARα is down-regulated in the diabetic retina, which contributes to the pathogenesis of DR. However, the mechanism for diabetes-induced down-regulation of PPARα remains unknown. We investigated the role of microRNA-21 (miR-21) in regulating PPARα in DR. MiR-21 was over-expressed, while PPARα levels were decreased in the retina of db/db mice, a type 2 diabetic model...
March 7, 2017: Diabetes
https://www.readbyqxmd.com/read/28263809/supercritical-processed-starch-nanosponge-as-a-carrier-for-enhancement-of-dissolution-and-pharmacological-efficacy-of-fenofibrate
#8
Nitin V Jadhav, Pradeep R Vavia
In current study, supercritical processed starch nanosponge (SSNS) used as a carrier for poorly water soluble drug (fenofibrate) to enhance its in-vitro and in-vivo performance. SSNS was prepared by using sol- gel method and effective supercritical drying technique. Fenofibrate was loaded into the SSNS by using solvent immersion method with selected and optimized organic solvent. BET surface area of SSNS was evaluated by nitrogen adsorption/desorption analysis. SSNS and drug loaded SSNS were characterized by DSC, XRPD, FTIR, SEM, Contact angle study and evaluated for in-vitro, in-vivo studies...
March 2, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28251701/molecular-effect-of-fenofibrate-on-pbmc-gene-transcription-related-to-lipid-metabolism-in-metabolic-syndrome-patients
#9
I Moreno-Indias, F J Tinahones, M Clemente-Postigo, D Castellano-Castillo, J C Fernández-García, M Macias-Gonzalez, M I Queipo-Ortuño, F Cardona
BACKGROUND: Both fasting and postprandial hypertriglyceridaemia are considered independent risk factors for atherosclerosis. Treatment of hypertriglyceridaemia is based on fibrates, which activate the peroxisome proliferator-activated receptor alpha (PPARα). However, the metabolic pathways that activate or inhibit fibrates, and how the postprandial triglyceride levels are modified, have not yet been fully described. Accordingly, the aim of this study was to determine the feasibility of peripheral blood mononuclear cells (PBMC) to study the effects of fenofibrate in patients with the metabolic syndrome...
March 2, 2017: Clinical Endocrinology
https://www.readbyqxmd.com/read/28247336/the-role-of-dyslipidemia-control-in-the-progression-of-diabetic-retinopathy-in-patients-with-type-2-diabetes-mellitus
#10
Irini P Chatziralli
Diabetic retinopathy (DR) is a common microvascular complication of diabetes mellitus (DM) and is considered as the leading cause of visual impairment in working-aged adults worldwide. Dyslipidemia has been associated with DR, but not with progression to the proliferative form of DR, although the exact role in the pathogenesis of DR and diabetic macular edema (DME) remains controversial. As a result, a reasonable question arising is whether control of dyslipidemia may alter the course of DR. Statins do not appear to have an impact on DR progression...
February 28, 2017: Diabetes Therapy: Research, Treatment and Education of Diabetes and related Disorders
https://www.readbyqxmd.com/read/28244156/the-a-priori-design-and-selection-of-ionic-liquids-as-solvents-for-active-pharmaceutical-ingredients
#11
Andreas Jonas Kunov-Kruse, Cameron Weber, Robin Rogers, Allan Myerson
In this paper we derive a straightforward computational approach to predict the optimal ionic liquid (IL) solvent for a given compound, based on COSMO-RS calculations. These calculations were performed on 18 different active pharmaceutical ingredients (APIs) using a matrix of 240 hypothetical ILs. These results indicated that the 18 APIs could be classified into 3 distinct categories based on their relative hydrogen bond donating or accepting ability, with similar optimal IL solvent predictions within each class...
February 28, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28243111/fenofibrate-simvastatin-fixed-dose-combination-in-the-treatment-of-mixed-dyslipidemia-safety-efficacy-and-place-in-therapy
#12
REVIEW
Nicola Tarantino, Francesco Santoro, Luisa De Gennaro, Michele Correale, Francesca Guastafierro, Antonio Gaglione, Matteo Di Biase, Natale Daniele Brunetti
Lipids disorder is the principal cause of atherosclerosis and may present with several forms, according to blood lipoprotein prevalence. One of the most common forms is combined dyslipidemia, characterized by high levels of triglycerides and low level of high-density lipoprotein. Single lipid-lowering drugs may have very selective effect on lipoproteins; hence, the need to use multiple therapy against dyslipidemia. However, the risk of toxicity is a concerning issue. In this review, the effect and safety of an approved combination therapy with simvastatin plus fenofibrate are described, with an analysis of pros and cons resulting from randomized multicenter trials, meta-analyses, animal models, and case reports as well...
2017: Vascular Health and Risk Management
https://www.readbyqxmd.com/read/28223873/development-and-validation-of-bioanalytical-uhplc-uv-method-for-simultaneous-analysis-of-unchanged-fenofibrate-and-its-metabolite-fenofibric-acid-in-rat-plasma-application-to-pharmacokinetics
#13
Rayan G Alamri, Kazi Mohsin, Ajaz Ahmad, Mohammad Raish, Fars K Alanazi
A simple, precise, selective and fast ultra-high performance liquid chromatography (UHPLC-UV) method has been developed and validated for the simultaneous determination of a lipid regulating agent fenofibrate and its metabolite fenofibric acid in rat plasma. The chromatographic separation was carried out on a reversed-phase Acquity® BEH C18 column using methanol-water (65:35, v/v) as the mobile phase. The isocratic flow was 0.3 ml/min with rapid run time of 2.5 min and UV detection was at 284 nm. The method was validated over a concentration range of 100-10000 ng/ml (r(2) ⩾ 0...
January 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28195199/pemafibrate-a-novel-selective-peroxisome-proliferator-activated-receptor-alpha-modulator-improves-the-pathogenesis-in-a-rodent-model-of-nonalcoholic-steatohepatitis
#14
Yasushi Honda, Takaomi Kessoku, Yuji Ogawa, Wataru Tomeno, Kento Imajo, Koji Fujita, Masato Yoneda, Toshiaki Takizawa, Satoru Saito, Yoji Nagashima, Atsushi Nakajima
The efficacy of peroxisome proliferator-activated receptor α-agonists (e.g., fibrates) against nonalcoholic fatty liver disease (NAFLD)/nonalcoholic steatohepatitis (NASH) in humans is not known. Pemafibrate is a novel selective peroxisome proliferator-activated receptor α modulator that can maximize the beneficial effects and minimize the adverse effects of fibrates used currently. In a phase-2 study, pemafibrate was shown to improve liver dysfunction in patients with dyslipidaemia. In the present study, we first investigated the effect of pemafibrate on rodent models of NASH...
February 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28179883/new-microrna-biomarkers-for-drug-induced-steatosis-and-their-potential-to-predict-the-contribution-of-drugs-to-non-alcoholic-fatty-liver-disease
#15
Mireia López-Riera, Isabel Conde, Laia Tolosa, Ángela Zaragoza, José V Castell, María J Gómez-Lechón, Ramiro Jover
Background and Aims: Drug-induced steatosis is a major reason for drug failure in clinical trials and post-marketing withdrawal; and therefore, predictive biomarkers are essential. These could be particularly relevant in non-alcoholic fatty liver disease (NAFLD), where most patients show features of the metabolic syndrome and are prescribed with combined chronic therapies, which can contribute to fatty liver. However, specific biomarkers to assess the contribution of drugs to NAFLD are lacking. We aimed to find microRNAs (miRNAs) responsive to steatotic drugs and to investigate if they could become circulating biomarkers for drug-induced steatosis...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28177239/visible-light-copper-photoredox-catalyzed-aerobic-oxidative-coupling-of-phenols-and-terminal-alkynes-regioselective-synthesis-of-functionalized-ketones-via-c%C3%A2-c-triple-bond-cleavage
#16
Arunachalam Sagadevan, Vaibhav Pramod Charpe, Ayyakkannu Ragupathi, Kuo Chu Hwang
Direct oxidative coupling of phenols and terminal alkynes was achieved at room temperature by a visible-light-mediated copper-catalyzed photoredox process. This method allows regioselective synthesis of hydroxyl-functionalized aryl and alkyl ketones from simple phenols and phenylacetylene via C≡C triple bond cleavage. 47 examples were presented. From a synthetic perspective, this protocol offers an efficient synthetic route for the preparation of pharmaceutical drugs, such as pitofenone and fenofibrate.
February 15, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28163820/apolipoprotein-ciii-overexpression-induced-hypertriglyceridemia-increases-nonalcoholic-fatty-liver-disease-in-association-with-inflammation-and-cell-death
#17
Adriene A Paiva, Helena F Raposo, Amarylis C B A Wanschel, Tarlliza R Nardelli, Helena C F Oliveira
Nonalcoholic fatty liver disease (NAFLD) is the principal manifestation of liver disease in obesity and metabolic syndrome. By comparing hypertriglyceridemic transgenic mice expressing apolipoprotein (apo) CIII with control nontransgenic (NTg) littermates, we demonstrated that overexpression of apoCIII, independent of a high-fat diet (HFD), produces NAFLD-like features, including increased liver lipid content; decreased antioxidant power; increased expression of TNFα, TNFα receptor, cleaved caspase-1, and interleukin-1β; decreased expression of adiponectin receptor-2; and increased cell death...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28159867/fenofibrate-but-not-ezetimibe-prevents-fatty-liver-disease-in-mice-lacking-phosphatidylethanolamine-n-methyltransferase
#18
Jelske N van der Veen, Susanne Lingrell, Xia Gao, Abhijit Takawale, Zamaneh Kassiri, Dennis E Vance, René L Jacobs
BACKGROUND AND AIMS: Mice lacking phosphatidylethanolamine N-methyltransferase (PEMT) are protected from high-fat diet (HFD)-induced obesity and insulin resistance. However, these mice develop severe non-alcoholic fatty liver disease (NAFLD) when fed the HFD, which is mainly due to inadequate secretion of VLDL particles. Our aim was to prevent NAFLD development in mice lacking PEMT. METHODS: We treated Pemt-/- mice with either ezetimibe or fenofibrate to see if either could ameliorate liver disease in these mice...
February 3, 2017: Journal of Lipid Research
https://www.readbyqxmd.com/read/28150806/dyslipidaemia-small-triumph-for-fenofibrate-therapy-in-dyslipidaemia
#19
Robert S Rosenson
No abstract text is available yet for this article.
February 2, 2017: Nature Reviews. Cardiology
https://www.readbyqxmd.com/read/28139735/nutritional-background-changes-the-hypolipidemic-effects-of-fenofibrate-in-nile-tilapia-oreochromis-niloticus
#20
Li-Jun Ning, An-Yuan He, Dong-Liang Lu, Jia-Min Li, Fang Qiao, Dong-Liang Li, Mei-Ling Zhang, Li-Qiao Chen, Zhen-Yu Du
Peroxisome proliferation activated receptor α (PPARα) is an important transcriptional regulator of lipid metabolism and is activated by high-fat diet (HFD) and fibrates in mammals. However, whether nutritional background affects PPARα activation and the hypolipidemic effects of PPARα ligands have not been investigated in fish. In the present two-phase study of Nile tilapia (Oreochromis niloticus), fish were first fed a HFD (13% fat) or low-fat diet (LFD; 1% fat) diet for 10 weeks, and then fish from the first phase were fed the HFD or LFD supplemented with 200 mg/kg body weight fenofibrate for 4 weeks...
January 31, 2017: Scientific Reports
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