Presence or absence of microbiome modulates the response of mice organism to administered drug nabumetone
Physiol Res. 2020 Dec 31;69(Suppl 4):S583-S594.ABSTRACTThe gut microbiota provides a wide range of beneficial functions for the host, and has an immense effect on the host's health status. The presence of microbiome in the gut may often influence the effect of an orally administered drug. Molecular mechanisms of this process are however mostly unclear. We investigated how the effect of a nonsteroidal drug nabumetone on expression of drug metabolizing enzymes (DMEs) in mice intestine and liver is changed by the presence of microbiota, here, using the germ free (GF) and specific pathogen free (SPF) BALB/c mice. First, we hav...
Source: Physiological Research - March 1, 2021 Category: Physiology Authors: L Jourov á B Li šková K Ln ěničková N Zemanov á P Anzenbacher P Hermanov á T Hudcovic H Koz áková E Anzenbacherov á Source Type: research
Role of human flavin-containing monooxygenase (FMO) 5 in the metabolism of nabumetone: Baeyer-Villiger oxidation in the activation of the intermediate metabolite, 3-hydroxy-nabumetone, to the active metabolite, 6-methoxy-2-naphthylacetic acid in vitro.
Abstract
Nabumetone (NAB) is a non-steroidal anti-inflammatory drug used clinically, and its biotransformation includes the major active metabolite 6-methoxy-2-naphthylacetic acid (6-MNA). One of the key intermediates between NAB and 6-MNA may be 3-hydroxy nabumetone (3-OH-NAB). The aim of the present study was to investigate the role of flavin-containing monooxygenase (FMO) isoform 5 in the formation of 6-MNA from 3-OH-NAB. To elucidate the biotransformation of 3-OH-NAB to 6-MNA, an authentic standard of 3-OH-NAB was synthesized and used as a substrate in an incubation with human liver samples or recombin...
Source: Xenobiotica - November 4, 2020 Category: Research Authors: Matsumoto K, Hasegawa T, Ohara K, Kamei T, Koyanagi J, Akimoto M Tags: Xenobiotica Source Type: research
Photochemistry of nabumetone in aqueous solution of sodium dodecyl sulfate (SDS) micelles
Publication date: Available online 21 August 2020Source: Journal of Molecular LiquidsAuthor(s): Margarita Valero, Peter P. Levin, Natalya B. Sultimova, Judith E. Houston (Source: Journal of Molecular Liquids)
Source: Journal of Molecular Liquids - August 21, 2020 Category: Molecular Biology Source Type: research
[ASAP] Selectivity Engineering in One-Pot Selective Synthesis of Drug Nabumetone over Novel Ni-Promoted La-Mg Oxide/Mesoporous Cellular Foam as Catalyst and Kinetic Modeling
Industrial& Engineering Chemistry ResearchDOI: 10.1021/acs.iecr.9b06210 (Source: Industrial and Engineering Chemical Research)
Source: Industrial and Engineering Chemical Research - February 10, 2020 Category: Chemistry Authors: Devendra S. Pisal and Ganapati D. Yadav* Source Type: research
A metabolic pathway for the prodrug nabumetone to the pharmacologically active metabolite, 6-methoxy-2-naphthylacetic acid (6-MNA) by non-cytochrome P450 enzymes.
Abstract
1. The pathway for the transformation of the prodrug nabumetone, 4-(6-methoxynaphthalen-2-yl)butan-2-on, to the active metabolite 6-methoxy-2-naphthylacetic acid (6-MNA), a potent cyclooxygenase-2 inhibitor, has not yet been clarified in humans.2. To confirm the activation pathway, authentic standards of the nabumetone intermediates, 2-(6-methoxynaphthalen-2-yl)ethyl acetate (6-MNEA), 2-(6-methoxynaphthalen-2-yl)ethan-1-ol (6-MNE-ol) and 2-(6-methoxynaphthalen-2-yl)acetaldehyde (6-MN-CHO) were synthesized. High performance liquid-chromatography and gas chromatography-mass spectrometry on nabumeton...
Source: Xenobiotica - December 18, 2019 Category: Research Authors: Matsumoto K, Hasegawa T, Ohara K, Takei C, Kamei T, Koyanagi J, Takahashi T, Akimoto M Tags: Xenobiotica Source Type: research
Identification of antiparkinsonian drugs in the 6-hydroxydopamine zebrafish model
Publication date: Available online 28 November 2019Source: Pharmacology Biochemistry and BehaviorAuthor(s): Rita L. Vaz, Sara Sousa, Diana Chapela, Herma C. van der Linde, Rob Willemsen, Ana D. Correia, Tiago F. Outeiro, Nuno D. AfonsoAbstractParkinson's disease (PD) is known as a movement disorder due to characteristic motor features. Existing therapies for PD are only symptomatic, and their efficacy decreases as disease progresses. Zebrafish, a vertebrate in which parkinsonism has been modelled, offers unique features for the identification of molecules with antiparkinsonian properties. Here, we developed a screening ass...
Source: Pharmacology Biochemistry and Behavior - November 28, 2019 Category: Biochemistry Source Type: research
Preparation, characterization and in vitro cytotoxicity of Fenofibrate and Nabumetone loaded solid lipid nanoparticles
Publication date: January 2020Source: Materials Science and Engineering: C, Volume 106Author(s): Raj Kumar, Ashutosh Singh, Kajal Sharma, Divya Dhasmana, Neha Garg, Prem Felix SirilAbstractThere is an increasing attention on solid lipid nanoparticles (SLNs) due to their high biocompatibility and ability to enhance bioavailability for poorly water-soluble drugs. Preparation of SLNs that are capable of high drug loading and sustained drug release through hot melt sonication method is reported here. SLNs of palmitic acid and stearic acid loaded with poorly water-soluble drugs, viz. fenofibrate (FF) and nabumetone (NBT) having...
Source: Materials Science and Engineering: C - October 6, 2019 Category: Materials Science Source Type: research
Does medication administration affect the rate of orthodontic tooth movement and root resorption development in humans? A systematic review
ConclusionsThe aforementioned substances may show varying effects on the rate of orthodontic tooth movement and root resorption development in human subjects. Despite the observed limitations, the orthodontist should be able to identify patients taking pharmaceuticals and consider any implications related to orthodontic treatment.RegistrationPROSPERO (CRD42017078208). (Source: The European Journal of Orthodontics)
Source: The European Journal of Orthodontics - August 18, 2019 Category: Dentistry Source Type: research
Does medication administration affect the rate of orthodontic tooth movement and root resorption development in humans? A systematic review.
CONCLUSIONS: The aforementioned substances may show varying effects on the rate of orthodontic tooth movement and root resorption development in human subjects. Despite the observed limitations, the orthodontist should be able to identify patients taking pharmaceuticals and consider any implications related to orthodontic treatment.
REGISTRATION: PROSPERO (CRD42017078208).
PMID: 31421637 [PubMed - as supplied by publisher] (Source: European Journal of Orthodontics)
Source: European Journal of Orthodontics - August 17, 2019 Category: Dentistry Authors: Kaklamanos EG, Makrygiannakis MA, Athanasiou AE Tags: Eur J Orthod Source Type: research
Gut microbiota metabolizes nabumetone in vitro: Consequences for its bioavailability in vivo in the rodents with altered gut microbiome.
Abstract
1. The underlying microbial metabolic activity toward xenobiotics is among the least explored factors contributing to the inter-individual variability in drug response. 2. Here, we analyzed the effect of microbiota on a non-steroidal anti-inflammatory drug nabumetone. 3. First, we cultivated the drug with the selected gut commensal and probiotic bacteria under both aerobic and anaerobic conditions and analyzed its metabolites by high-performance liquid chromatography (HPLC) with UV detection. To analyze the effect of microbiota on nabumetone pharmacokinetics in vivo, we administered a single oral ...
Source: Xenobiotica - February 22, 2019 Category: Research Authors: Jourova L, Anzenbacher P, Matuskova Z, Vecera R, Strojil J, Kolar M, Nobilis M, Hermanova P, Hudcovic T, Kozakova H, Kverka M, Anzenbacherova E Tags: Xenobiotica Source Type: research
Determination of the Absolute Configuration of the Nabumetone Metabolite 4-(6-Methoxy-2-naphthyl)butan-2-ol Using the Chiral Derivatizing Agent, 1-Fluoroindan-1-carboxylic Acid.
Abstract
The absolute configuration of (+)-4-(6-methoxy-2-naphthyl)butan-2-ol ((+)-MNBO), a nabumetone metabolite, was determined using 1-fluoroindan-1-carboxylic acid (FICA). Both enantiomers of the FICA methyl esters were derivatized to diastereomeric esters of (+)-MNBO by an ester exchange reaction. The results of 1H- and 19F-NMR spectroscopy of the diastereomeric FICA esters of (+)-MNBO confirmed the absolute configuration of (+)-MNBO was (S).
PMID: 30606953 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - January 6, 2019 Category: Drugs & Pharmacology Authors: Kamei T, Kimura Y, Koyanagi J, Matsumoto K, Hasegawa T, Akimoto M, Takahashi T Tags: Chem Pharm Bull (Tokyo) Source Type: research
The importance of the structure similarity of drugs used for depression and inflammation, two comorbid diseases.
Abstract
Growing evidence links inflammation to depression and the combination of anti-inflammatory drugs with antidepressant to treat depressive symptoms is currently suggested. There is only few studies concerning the molecular mechanism underlying this comorbidity and many of them point out the importance of the tryptophan pathway. There is yet no data that analyzes the structural similarity of the molecules used for the treatment of these comorbid diseases. This review aimed first to classify current antidepressant drugs and non-steroidal anti-inflammatory drugs (NSAIDs) according to their structure. M...
Source: Current Topics in Medicinal Chemistry - August 21, 2018 Category: Chemistry Authors: Bayram FEO, Reis R, Tuncer B, Sipahi H Tags: Curr Top Med Chem Source Type: research
Determining the Molecular Pathways Underlying the Protective Effect of Non-Steroidal Anti-Inflammatory Drugs for Alzheimer's Disease: A Bioinformatics Approach
In this study, we use pathway enrichment and fuzzy logic to identify pathways (KEGG database) simultaneously affected in both AD and by NSAIDs (Sulindac, Piroxicam, Paracetamol, Naproxen, Nabumetone, Ketoprofen, Diclofenac and Aspirin). Gene expression signatures were derived for disease from both blood (n = 344) and post-mortem brain (n = 690), and for drugs from immortalised human cell lines exposed to drugs of interest as part of the Connectivity Map platform. Using this novel approach to combine datasets we find striking overlap between AD gene expression in blood and NSAID induced changes in KEGG p...
Source: Computational and Structural Biotechnology Journal - July 10, 2018 Category: Biotechnology Source Type: research
Thiodipeptides targeting the intestinal oligopeptide transporter as a general approach to improving oral drug delivery.
Abstract
The broad substrate capacity of the intestinal oligopeptide transporter, PepT1, has made it a key target of research into drug delivery. Whilst the substrate capacity of this transporter is broad, studies have largely been limited to small peptides and peptide-like drugs. Here, we demonstrate for the first time that a diverse range of drugs can be targeted towards transport by PepT1 using a hydrolysis resistant carrier. Eleven prodrugs were synthesized by conjugating modified dipeptides containing a thioamide bond to the approved drugs ibuprofen, gabapentin, propofol, aspirin, acyclovir, nabumeton...
Source: European Journal of Medicinal Chemistry - June 30, 2018 Category: Chemistry Authors: Foley DW, Pathak RB, Phillips TR, Wilson GL, Bailey PD, Pieri M, Senan A, Meredith D Tags: Eur J Med Chem Source Type: research
