518 results match your criteria mlx

Pharmacokinetics of meloxicam, carprofen, and tolfenamic acid after intramuscular and oral administration in Japanese quails (Coturnix coturnix japonica).

J Vet Pharmacol Ther 2021 Apr 12. Epub 2021 Apr 12.

Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Selcuk, Konya, Turkey.

The aim of this study was to determine the pharmacokinetics of meloxicam (MLX), carprofen (CRP), and tolfenamic acid (TA) in Japanese quails (Coturnix coturnix japonica) following intramuscular (IM) and oral administration at doses of 1, 10, and 2 mg/kg, respectively. A total of 72 quails were randomly divided into 3 equal groups as MLX, CRP, and TA. Each group was separated into two sub-groups that received IM and oral administration of each drug. Read More

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The ménage à trois of autophagy, lipid droplets and liver disease.

Autophagy 2021 Apr 2:1-24. Epub 2021 Apr 2.

Department of Cell Biology, University of Groningen, University Medical Center Groningen, AV Groningen, The Netherlands.

Autophagic pathways cross with lipid homeostasis and thus provide energy and essential building blocks that are indispensable for liver functions. Energy deficiencies are compensated by breaking down lipid droplets (LDs), intracellular organelles that store neutral lipids, in part by a selective type of autophagy, referred to as lipophagy. The process of lipophagy does not appear to be properly regulated in fatty liver diseases (FLDs), an important risk factor for the development of hepatocellular carcinomas (HCC). Read More

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Clinical safety of total glucosides of paeony adjuvant therapy for rheumatoid arthritis treatment: a systematic review and meta-analysis.

BMC Complement Med Ther 2021 Mar 26;21(1):102. Epub 2021 Mar 26.

Institute of Basic Research in Clinical Medicine, China Academy of Chinese Medical Sciences, Beijing, China.

Background: Total glucosides of paeony (TGP), an active compound extracted from the roots of Paeonia lactiflora Pallas, has been increasingly used as the adjunctive therapy for rheumatoid arthritis (RA) patients. Though TGP could mitigate the unanticipated adverse effects during the conventional treatment of RA, high-quality evidence-based meta-analysis data on this subject are still insufficient. The objective of this study is to evaluate the clinical safety of TGP adjuvant therapy in the RA treatment. Read More

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Synthesis of PEG-4000-co-poly (AMPS) nanogels by cross-linking polymerization as highly responsive networks for enhancement in meloxicam solubility.

Drug Dev Ind Pharm 2021 Mar 2;47(3):465-476. Epub 2021 Mar 2.

School of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan, ROC.

Poor solubility is an ongoing issue and the graph of poorly soluble drugs has increased markedly which critically affect their dissolution, bioavailability, and clinical effects. This common issue needs to be addressed, for this purpose a series of polyethylene glycol (PEG-4000) based nanogels were developed by free radical polymerization technique to enhance the solubility, dissolution, and bioavailability of poorly soluble drug meloxicam (MLX), as improved solubility is the significant application of nanosystems. Developed nanogels formulations were characterized by FTIR, XRD, SEM, zeta sizer, percent equilibrium swelling, drug loaded content (DLC), drug entrapment efficiency (DEE), solubility studies, and dissolution studies. Read More

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W2476 represses TXNIP transcription via dephosphorylation of FOXO1 at Ser319.

Chem Biol Drug Des 2021 May 16;97(5):1089-1099. Epub 2021 Feb 16.

The National Center for Drug Screening, CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences (CAS), Shanghai, China.

Thioredoxin-interacting protein (TXNIP) overexpression is implicated in the pathogenesis of type 2 diabetes. Previous studies have shown that a small molecule compound (W2476) was able to improve β-cell dysfunction and exert therapeutic effects in diabetic mice via repression of TXNIP signaling pathway. The impact of W2476 on TXNIP transcription was thus investigated using the chromatin immunoprecipitation method. Read More

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Single-cell analysis reveals the intra-tumor heterogeneity and identifies MLXIPL as a biomarker in the cellular trajectory of hepatocellular carcinoma.

Cell Death Discov 2021 Jan 18;7(1):14. Epub 2021 Jan 18.

Department of Oncology, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 200080, China.

Hepatocellular carcinoma (HCC) is a globally prevailing cancer with a low 5-year survival rate. Little is known about its intricate gene expression profile. Single-cell RNA sequencing is an indispensable tool to explore the genetic characteristics of HCC at a more detailed level. Read More

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January 2021

Transcription factor ChREBP – the coordinator of carbohydrate and lipid metabolism

Postepy Biochem 2020 03 9;66(1):30-37. Epub 2020 Jan 9.

Department of Metabolic Regulation, Institute of Biochemistry, Faculty of Biology, University of Warsaw.

Transcription factor ChREBP, in complex with MLX, binds to carbohydrate-response element (ChoRE) located in the promoters of genes related to glycolysis, gluconeogenesis, pentosephosphate pathway and lipogenesis, activating their transcription following stimulation with glucose, insulin-independently. In this article the mechanisms of ChREBP regulation and ChREBP functions under both physiological and pathophysiological conditions are described in detail. The possible use of ChREBP activity modulation as a therapeutic tool, e. Read More

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Meloxicam encapsulated nanostructured colloidal self-assembly for evaluating antitumor and anti-inflammatory efficacy in 3D printed scaffolds.

J Biomed Mater Res A 2020 Dec 1. Epub 2020 Dec 1.

Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur, India.

Nanostructured colloidal self-assembly (NCS) is one of the most promising drug delivery carriers in cancer treatment. The present research work aimed towards synthesizing meloxicam (MLX) loaded NCS for its improved circulation half-life and increased cellular internalization. NCS was formulated using glyceryl monoolein, Pluronic® F127, and MLX. Read More

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December 2020

Effect of doxycycline and meloxicam on cytokines, brain-derived neurotrophic factor, matrix metalloproteinase-3, tissue inhibitor of metalloproteinase-3 and cyclooxygenase-2 in brain.

Iran J Basic Med Sci 2020 Oct;23(10):1328-1334

Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, Selcuk University, Konya, Turkey.

Objectives: Prevention of inflammation in early stages will be useful in maintaining vitality of the organism. The objective of this study was to evaluate the effects of doxycycline (DOX) or meloxicam (MLX) monotherapy and combination therapy on the levels of inflammatory mediators in the brain tissues of rats with lipopolysaccharide (LPS)-induced brain inflammation.

Materials And Methods: Seventy-eight rats were divided into the following groups: control (n=6), LPS (0. Read More

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October 2020

99-Case Study of Sporadic Aortic Dissection by Whole Exome Sequencing Indicated Novel Disease-Associated Genes and Variants in Chinese Population.

Biomed Res Int 2020 2;2020:7857043. Epub 2020 Oct 2.

Department of Cardiac Surgery, Fuwai Hospital Chinese Academy of Medical Sciences, Shenzhen, Guangdong, China.

Background: In this study, the whole exome sequencing in human aortic dissection, a highly lethal cardiovascular disease, was investigated to explore the aortic dissection-associated genes and variants in Chinese population.

Methods: Whole exome sequencing was performed in 99 cases of aortic dissection. All single nucleotide polymorphisms (SNPs), insertions/deletions (InDels), and copy number variations (CNVs) were filtered to exclude the benign variants. Read More

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October 2020

On the effect of pre-strain and pre-fatigue on the monotonic behaviour of ultra-high strength steels.

Heliyon 2020 Jul 14;6(7):e04440. Epub 2020 Jul 14.

Materials Research Centre, College of Engineering, Swansea University, SA1 8EN, UK.

The mechanical behaviour of three ultra-high strength steels has been assessed; AerMet100, 300M and the recently developed corrosion resistant high strength steel, MLX-17. Material heat treatment profiles have been utilised to provide performance optimised for the aerospace industry and specimens have been tested to explore tensile and fatigue properties, in particular when combined with pre-strain to simulate the effects of overload. Testing of this kind has not been reported within the literature, particularly amongst ultra-high strength and corrosion-resistant steels. Read More

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MondoA:MLX complex regulates glucose-dependent gene expression and links to circadian rhythm in liver and brain of the freeze-tolerant wood frog, Rana sylvatica.

Mol Cell Biochem 2020 Oct 7;473(1-2):203-216. Epub 2020 Jul 7.

Department of Biology, Carleton University, 1125 Colonel By Drive, Ottawa, ON, K1S 5B6, Canada.

The wood frog, Rana sylvatica, is one of only a few vertebrate species that display natural freeze tolerance. Frogs survive the freezing of about two-thirds of their body water as extracellular ice over the winter months. Multiple adaptations support freeze tolerance including metabolic rate depression and the production of huge amounts of glucose (often 200 mM or more) as a cryoprotectant that protects cells from freeze damage. Read More

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October 2020

A novel combination of Soluplus/Poloxamer for Meloxicam solid dispersions via hot melt extrusion for rapid onset of action. Part 2: comparative bioavailability and IVIVC.

Drug Dev Ind Pharm 2020 Aug 10;46(8):1362-1372. Epub 2020 Jul 10.

Medicinal  and Pharmaceutical Chemistry Department, Division of Pharmaceutical and Drug Industries Research, Industrial Pharmacy Laboratory, National Research Centre, Giza, Egypt.

Objective: Bioavailability of Meloxicam (MLX) from solid dispersions (SDs), against innovator product Mobic in humans was conducted. Furthermore, to establish a good - correlation (IVIVC); dissolution studies were carried-out in different media.

Methods: MLX/SDs was prepared using Soluplus/Poloxamer via hot-melt-extrusion (EXT-SD) and fusion melt (FUS-SD) techniques. Read More

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The role of pH and dose/solubility ratio on cocrystal dissolution, drug supersaturation and precipitation.

Eur J Pharm Sci 2020 Sep 10;152:105422. Epub 2020 Jun 10.

Department of Pharmaceutical Sciences, College of Pharmacy, University of Michigan, Ann Arbor, Michigan 48109-1065, United States. Electronic address:

Cocrystals that are more soluble than the constituent drug, generate supersaturation levels during dissolution and are predisposed to conversion to the less soluble drug. Drug release studies during cocrystal dissolution generally compare several cocrystals and their crystal structures. However, the influence of drug dose and solubility in different dissolution media has been scarcely reported. Read More

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September 2020

Synthesis and characterization of meloxicam eutectics with mandelic acid and saccharin for enhanced solubility.

Drug Dev Ind Pharm 2020 Jul 12;46(7):1092-1099. Epub 2020 Jun 12.

Department of Analytical Chemistry, Institute of Chemistry - São Paulo State University (UNESP), Araraquara, Brazil.

Meloxicam (MLX) is a non-steroidal anti-inflammatory which is practically insoluble in water, requiring high concentrations to reach therapeutic levels and causing frequently gastrointestinal effects. In this way, the aim of this study was to synthesize two eutectic mixtures of MLX with mandelic acid (MND) and saccharin (SAC) by liquid-assisted grinding resulting in a multicomponent material with enhanced solubility. Mixtures were studied in different stoichiometric and eutectic point was found for each eutectic by Binary phase diagram and Tamman's triangle, with 0. Read More

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Role for carbohydrate response element-binding protein (ChREBP) in high glucose-mediated repression of long noncoding RNA Tug1.

J Biol Chem 2020 11 28;295(47):15840-15852. Epub 2020 May 28.

Section of Nephrology, Division of Internal Medicine, The University of Texas at MD Anderson Cancer Center, Houston, Texas, USA; Department of Pharmacology & Chemical Biology, Baylor College of Medicine, Houston, Texas, USA. Electronic address:

Long noncoding RNAs (lncRNAs) have been shown to play key roles in a variety of biological activities of the cell. However, less is known about how lncRNAs respond to environmental cues and what transcriptional mechanisms regulate their expression. Studies from our laboratory have shown that the lncRNA Tug1 (taurine upregulated gene 1) is crucial for the progression of diabetic kidney disease, a major microvascular complication of diabetes. Read More

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November 2020

Meloxicam Carrier Systems Having Enhanced Release and Aqueous Wettability Prepared Using Micro-suspensions in Different Liquid Media.

AAPS PharmSciTech 2020 May 24;21(5):155. Epub 2020 May 24.

Department of Organic Technology, University of Chemistry and Technology, Technická 5, 166 28, Prague 6, Czech Republic.

One of the conventional methods of alleviating the problem of poor drug solubility is the particle size reduction. The efficiency of this approach depends on successful formulation suppressing the drug agglomeration. The aim of this study was to circumvent the dissolution problems of model hydrophobic meloxicam drug (MLX) by using liquid media of different wetting capacity to comminute and formulate a rapidly dissolving carrier system without the use of surfactants. Read More

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SMaRT lncRNA controls translation of a G-quadruplex-containing mRNA antagonizing the DHX36 helicase.

EMBO Rep 2020 06 26;21(6):e49942. Epub 2020 Apr 26.

Department of Biology and Biotechnology, Charles Darwin, Sapienza University of Rome, Rome, Italy.

Guanine-quadruplexes (G4) included in RNA molecules exert several functions in controlling gene expression at post-transcriptional level; however, the molecular mechanisms of G4-mediated regulation are still poorly understood. Here, we describe a regulatory circuitry operating in the early phases of murine muscle differentiation in which a long non-coding RNA (SMaRT) base pairs with a G4-containing mRNA (Mlx-γ) and represses its translation by counteracting the activity of the DHX36 RNA helicase. The time-restricted, specific effect of lnc-SMaRT on the translation of Mlx-γ isoform modulates the general subcellular localization of total MLX proteins, impacting on their transcriptional output and promoting proper myogenesis and mature myotube formation. Read More

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Oral Administration System Based on Meloxicam Nanocrystals: Decreased Dose Due to High Bioavailability Attenuates Risk of Gastrointestinal Side Effects.

Pharmaceutics 2020 Apr 1;12(4). Epub 2020 Apr 1.

Faculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashi-Osaka, Osaka 577-8502, Japan.

Meloxicam (MLX) is widely applied as a therapy for rheumatoid arthritis (RA); however, it takes far too long to reach its peak plasma concentration for a quick onset effect, and gastrointestinal toxicity has been observed in RA patients taking it. To solve these problems, we designed MLX solid nanoparticles (MLX-NPs) by the bead mill method and used them to prepare new oral formulations. The particle size of the MLX-NPs was approximately 20-180 nm, and they remained in the nano-size range for 1 month. Read More

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Smart phase transformation system based on lyotropic liquid crystalline@hard capsules for sustained release of hydrophilic and hydrophobic drugs.

Drug Deliv 2020 Dec;27(1):449-459

School of Pharmaceutical Science, Jinan University, Guangzhou, PR China.

Smart phase transformation systems@hard capsule (SPTS@hard capsule) based on lyotropic liquid crystalline (LLC) were developed for oral sustained release in this study. Doxycycline hydrochloride (DOXY) and meloxicam (MLX) were used as hydrophilic and hydrophobic model drug, respectively. Two systems were added with different additives, that is, gelucire 39/01, PEG 1000 and Tween 80 to adjust their melting point and release profiles. Read More

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December 2020

Effects of Mlx-8, a phospholipase A from Brazilian coralsnake venom, on muscarinic acetylcholine receptors in rat hippocampus.

J Venom Anim Toxins Incl Trop Dis 2020 27;26:e20190041. Epub 2020 Jan 27.

Laboratory of Pharmacology, Butantan Institute, São Paulo, SP, Brazil.

Background: Here, we described the presence of a neurotoxin with phospholipase A activity isolated from venom (Mlx-8) with affinity for muscarinic acetylcholine receptors (mAChRs).

Methods: The purification, molecular mass determination, partial amino acid sequencing, phospholipase A activity determination, inhibition of the binding of the selective muscarinic ligand [H]QNB and inhibition of the total [H]inositol phosphate accumulation in rat hippocampus of the Mlx-8 were determined.

Results: Thirty-one fractions were collected from HPLC chromatography, and the Mlx-8 toxin was used in this work. Read More

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January 2020

Development and validation of a novel immune-related prognostic model in hepatocellular carcinoma.

J Transl Med 2020 02 11;18(1):67. Epub 2020 Feb 11.

Department of Infectious Diseases, Qilu Hospital, Shandong University, Wenhua Xi Road 107, Jinan, 250012, Shandong, China.

Background: Growing evidence has suggested that immune-related genes play crucial roles in the development and progression of hepatocellular carcinoma (HCC). Nevertheless, the utility of immune-related genes for evaluating the prognosis of HCC patients are still lacking. The study aimed to explore gene signatures and prognostic values of immune-related genes in HCC. Read More

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February 2020

Partitioning of MLX-Family Transcription Factors to Lipid Droplets Regulates Metabolic Gene Expression.

Mol Cell 2020 03 4;77(6):1251-1264.e9. Epub 2020 Feb 4.

Department of Molecular Metabolism, Harvard T.H. Chan School of Public Health, Boston, MA 02115, USA; Department of Cell Biology, Harvard Medical School, Boston, MA 02115, USA; Howard Hughes Medical Institute, Boston, MA 02115, USA; Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA. Electronic address:

Lipid droplets (LDs) store lipids for energy and are central to cellular lipid homeostasis. The mechanisms coordinating lipid storage in LDs with cellular metabolism are unclear but relevant to obesity-related diseases. Here we utilized genome-wide screening to identify genes that modulate lipid storage in macrophages, a cell type involved in metabolic diseases. Read More

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Glucose-6-Phosphate Upregulates Txnip Expression by Interacting With MondoA.

Front Mol Biosci 2019 9;6:147. Epub 2020 Jan 9.

Department of Biochemistry, School of Medicine, Cancer Institute of the Second Affiliated Hospital, Zhejiang University, Hangzhou, China.

The major metabolic fates of glucose in cells are glycolysis and the pentose phosphate pathway, and they share the first step: converting glucose to glucose-6-phosphate (G6P). Here, we show that G6P can be sensed by the transcription factor MondoA/Mlx to modulate Txnip expression. Endogenous knockdown and EMSA (gel migration assay) analyses both confirmed that G6P is the metabolic intermediate that activates the heterocomplex MondoA/Mlx to elicit the expression of Txnip. Read More

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January 2020

ameliorates insulin secretion failure through Chrebp/Txnip signaling via modulating PKA/PP2A activities.

Nutr Metab (Lond) 2020 14;17. Epub 2020 Jan 14.

1Research Center for Nutrition and Food Safety, Institute of Military Preventive Medicine, Third Military Medical University, Chongqing, 400038 People's Republic of China.

Background: , produced from daidzein by gut microbiota, has been suggested as an potential anti-diabetic agent, but the underlying mechanisms remain unclear. Recent evidences demonstrated that carbohydrate response element-binding protein (Chrebp)/Thioredoxin-interacting protein (Txnip) signaling played central roles on diabetes progression, particularly in relation to the function maintenance and apoptosis of pancreatic β-cell. Here, we investigated the effects of on β-cell function and Chrebp/Txnip signaling

Methods: Zucker diabetic fatty rats were treated with racemic (120 mg/kg. Read More

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January 2020

The MNT transcription factor autoregulates its expression and supports proliferation in MYC-associated factor X (MAX)-deficient cells.

J Biol Chem 2020 02 9;295(7):2001-2017. Epub 2020 Jan 9.

Instituto de Biomedicina y Biotecnología de Cantabria (IBBTEC), Universidad de Cantabria-CSIC, and Department of Molecular Biology, Universidad de Cantabria, 39005 Santander, Spain. Electronic address:

The MAX network transcriptional repressor (MNT) is an MXD family transcription factor of the basic helix-loop-helix (bHLH) family. MNT dimerizes with another transcriptional regulator, MYC-associated factor X (MAX), and down-regulates genes by binding to E-boxes. MAX also dimerizes with MYC, an oncogenic bHLH transcription factor. Read More

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February 2020

A Screen for Gene Paralogies Delineating Evolutionary Branching Order of Early Metazoa.

G3 (Bethesda) 2020 02 6;10(2):811-826. Epub 2020 Feb 6.

Department of Biology, University of Iowa, Iowa City, IA, 52242

The evolutionary diversification of animals is one of Earth's greatest marvels, yet its earliest steps are shrouded in mystery. Animals, the monophyletic clade known as Metazoa, evolved wildly divergent multicellular life strategies featuring ciliated sensory epithelia. In many lineages epithelial sensoria became coupled to increasingly complex nervous systems. Read More

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February 2020

Improving solubility and dissolution of meloxicam by solid dispersion using hydroxypropyl methylcellulose 2910 3 cps and nicotinamide.

J Basic Clin Physiol Pharmacol 2019 Dec 14;30(6). Epub 2019 Dec 14.

Faculty of Pharmacy, Airlangga University, Department of Pharmaceutics, Nanizar Zaman Joenoes Bldg, Campus C Mulyorejo, Airlangga University Surabaya, Indonesia.

Background Solid dispersion (SD) represents a good method for enhancing the solubility of poorly water-soluble drugs. Meloxicam (MLX), a nonsteroidal anti-inflammatory drug has poor solubility in water. Hydroxypropyl methylcellulose (HPMC) 2910 3 cps, a hydrophilic carrier and nicotinamide (NC), a hydrotropic agent can be used as matrix of SD. Read More

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December 2019

Ternary solid dispersion to improve solubility and dissolution of meloxicam.

J Basic Clin Physiol Pharmacol 2019 Dec 14;30(6). Epub 2019 Dec 14.

Department of Pharmaceutics, Faculty of Pharmacy, Universitas Airlangga, Mulyorejo-60115, Surabaya, Indonesia.

Background Meloxicam (MLX) is a potent non-steroidal anti-inflammatory drug with poor solubility. Solid dispersion (SD) is an effective formulation strategy to improve the dissolution rate of poorly water-soluble compounds. Hydroxy propyl methyl cellulose (HPMC) as an inert polymer carrier and nicotinic acid (NA) as disturbance can be used as a matrix of SD. Read More

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December 2019

Expression and pathophysiological significance of carbohydrate response element binding protein (ChREBP) in the renal tubules of diabetic kidney.

Endocr J 2020 Mar 7;67(3):335-345. Epub 2019 Dec 7.

Department of Molecular Endocrinology, Tohoku University Graduate School of Medicine, Sendai 980-8575, Japan.

Carbohydrate response element binding protein (ChREBP), a glucose responsive transcription factor, mainly regulates expression of genes involved in glucose metabolism and lipogenesis. Recently, ChREBP is speculated to be involved in the onset and progression of diabetic nephropathy (DN). However, there exists no report regarding the localization and function of ChREBP in the kidney. Read More

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