47 results match your criteria mlx gel


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

Cocrystallization as a novel approach to enhance the transdermal administration of meloxicam.

Eur J Pharm Sci 2018 Oct 20;123:184-190. Epub 2018 Jul 20.

Programa de Pós-Graduação em Farmácia, Universidade Federal de Santa Catarina, Florianópolis, SC 88040-970, Brazil. Electronic address:

Despite its large effectiveness, the long-term oral administration of high doses of meloxicam (MLX) may lead to gastrointestinal events such as abdominal pain, diarrhea, dyspepsia, ulceration, hemorrhage, and gastrointestinal perforation. Moreover, the pH-dependent solubility of MLX makes the development of new oral formulations even more challenging. As an alternative to overcome these limitations, the transdermal delivery of this drug has been purposed. Read More

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October 2018

Flexosomes for transdermal delivery of meloxicam: characterization and antiinflammatory activity.

Artif Cells Nanomed Biotechnol 2017 Mar 28;45(2):305-312. Epub 2016 Feb 28.

a Department of Pharmaceutics, College of Pharmacy , King Saud University , Riyadh , Saudi Arabia.

The study aims to investigate the impact of flexosomes (FLs) on transdermal delivery of meloxicam (MLX). FLs are composed of phospholipid, Tween 80, and ethanol which were prepared by film hydration method. The prepared FLs were characterized for particle size, zeta potential, and entrapment efficiency (EE). Read More

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Nanostructured lipid carriers based nanogel for meloxicam delivery: mechanistic, in-vivo and stability evaluation.

Drug Dev Ind Pharm 2015 25;41(8):1368-75. Epub 2014 Aug 25.

Department of Pharmaceutical Sciences, Guru Nanak Dev University , Amritsar, Punjab , India and.

Aim: Our investigation was aimed to investigate the potential suitability of meloxicam-loaded nanostructured lipid carriers (MLX-NLC) gel for topical application.

Main Methods: MLX-NLC gel was prepared and in vivo skin penetration ability of the NLC gel was evaluated using confocal laser scanning microscopy. We studied the effect of MLX-NLC gel on the changes in lipid profile of skin to get an insight into its skin penetration enhancement mechanism. Read More

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Association of the MLXIPL/TBL2 rs17145738 SNP and serum lipid levels in the Guangxi Mulao and Han populations.

Lipids Health Dis 2013 Oct 25;12:156. Epub 2013 Oct 25.

Department of Cardiology, Institute of Cardiovascular Diseases, The First Affiliated Hospital, Guangxi Medical University, 22 Shuangyong Road, Nanning 530021, Guangxi, People's Republic of China.

Background: The rs17145738 single nucleotide polymorphism (SNP) near MLX interacting protein-like/transducin (beta)-like 2 (MLXIPL/TBL2) loci is associated with serum lipid levels, but the results are inconsistent in diverse ethnic/racial groups. The current study was to investigate the association of MLXIPL/TBL2 rs17145738 SNP and several environmental factors with serum lipid profiles in the Guangxi Mulao and Han populations.

Methods: A total of 649 subjects of Mulao nationality and 712 participants of Han nationality aged 16-84 years were randomly selected from our previous stratified randomized samples. Read More

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October 2013

Development and characterization of a novel controlled release drug delivery system based on nanostructured lipid carriers gel for meloxicam.

Life Sci 2013 Nov 7;93(21):763-72. Epub 2013 Oct 7.

Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar 143104, India.

Aim: The main objective of the current investigation was to develop nanostructured lipid carriers (NLC) based gel for the enhancement of transdermal absorption of meloxicam (MLX) to achieve local as well as systemic drug action without concurrent gastrointestinal toxicity.

Main Methods: NLC gel containing MLX was prepared and characterized for particle size, polydispersity, zeta potential, pH, rheology, entrapment efficiency, occlusion factor, and thermal behavior. In vitro drug release, in vitro skin permeation and deposition studies were carried out using Franz diffusion cells. Read More

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November 2013

Preparation and evaluation of solid lipid nanoparticles based nanogel for dermal delivery of meloxicam.

Chem Phys Lipids 2013 Oct-Nov;175-176:65-72. Epub 2013 Aug 28.

Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar 143104, India. Electronic address:

The aim of the current investigation was to prepare and investigate the potential of solid lipid nanoparticles based gel (SLN-gel) for the dermal delivery of meloxicam (MLX). The meloxicam loaded SLN (MLX-SLN) gel was developed and characterized by means of photon correlation spectroscopy, rheometry, and differential scanning calorimetry to determine the physicochemical properties. The behavior of SLN gel on rat skin was evaluated in vitro using Franz diffusion cells to determine the skin permeation and penetration characteristics, in vivo on mice to determine the skin tolerance by histopathological examinations. Read More

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Nanostructured lipid carriers (NLCs) versus solid lipid nanoparticles (SLNs) for topical delivery of meloxicam.

Pharm Dev Technol 2014 May 26;19(3):304-14. Epub 2013 Mar 26.

Department of Pharmaceutical Technology, National Research Center , Cairo , Egypt .

Objective: The aim of this study was to develop nanostructured lipid carriers (NLCs) as well as solid lipid nanoparticles (SLNs) and evaluate their potential in the topical delivery of meloxicam (MLX).

Materials And Methods: The effect of various compositional variations on their physicochemical properties was investigated. Furthermore, MLX-loaded lipid nanoparticles-based hydrogels were formulated and the gels were evaluated as vehicles for topical application. Read More

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Nanoemulsion based gel for transdermal delivery of meloxicam: physico-chemical, mechanistic investigation.

Life Sci 2013 Mar 23;92(6-7):383-92. Epub 2013 Jan 23.

Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar - 143104, India.

Aims: The aim of the present investigation was to develop a nanoemulsion (NE) gel formulation for the transdermal delivery of meloxicam (MLX) in order to ensure maximum controlled and sustained drug release capacity.

Main Methods: The MLX containing NE gel was prepared and characterized for particle size, zeta potential, pH, rheology, in vitro drug release, in vitro skin permeation, and in vitro hemolysis. Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR) of MLX-NE gel treated rat skin was performed to investigate the skin permeation mechanism of meloxicam from NE gel. Read More

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Quantification of dermal and transdermal delivery of meloxicam gels in rabbits.

Drug Dev Ind Pharm 2011 May;37(5):613-7

Division of Pharmaceutical Sciences, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, 75 DeKalb Ave., Brooklyn, NY 11201, USA.

Background: This study was designed to quantify the effects of penetration enhancers on systemic bioavailability of 0.3% meloxicam (MLX) hydroxypropylcellulose gels. Cutaneous microdialysis was also performed to assess dermis availability and to better understand the penetration process. Read More

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Formulation of meloxicam gel for topical application: In vitro and in vivo evaluation.

Acta Pharm 2010 Jun;60(2):153-63

Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga, Mumbai-400019, India.

Skin delivery of NSAIDs offers several advantages over the oral route associated with potential side effects. In the present investigation, topical gel of meloxicam (MLX) was formulated using N-methyl pyrrolidone (NMP) as a solubilizer and Carbopol Ultrez 10® as a gelling polymer. MLX gel was evaluated with respect to different physicochemical parameters such as pH, viscosity and spreadability. Read More

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Hepatic expression of the SPOT 14 (S14) paralog S14-related (Mid1 interacting protein) is regulated by dietary carbohydrate.

Endocrinology 2008 Oct 12;149(10):5155-61. Epub 2008 Jun 12.

Department of Biochemistry, Molecular Biology, and Biophysics, University of Minnesota, Minneapolis, Minnesota 55455, USA.

The Spot 14 (S14) gene is rapidly up-regulated by signals that induce lipogenesis such as enhanced glucose metabolism and thyroid hormone administration. Previous studies in S14 null mice show that S14 is required for normal lipogenesis in the lactating mammary gland, but not the liver. We speculated that the lack of a hepatic phenotype was due to the expression of a compensatory gene. Read More

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October 2008

Effects of penetration enhancers on in vitro permeability of meloxicam gels.

Int J Pharm 2007 Oct 24;343(1-2):26-33. Epub 2007 Apr 24.

Division of Pharmaceutical Sciences, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, 75 DeKalb Ave., Brooklyn, NY 11201, USA.

Meloxicam (MLX) was formulated as a 0.3% hydroxypropylcellulose (Klucel) gel. The effect of four different combinations of co-solvents (ethanol, glycol-PEG-400, propylene glycol, and water) on MLX permeability was determined in vitro throughout isopropyl myristate (IPM)-saturated cellulose membranes. Read More

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October 2007

Sterol regulatory element-binding protein-2 interacts with hepatocyte nuclear factor-4 to enhance sterol isomerase gene expression in hepatocytes.

J Biol Chem 2003 Sep 10;278(38):36176-82. Epub 2003 Jul 10.

Department of Applied Biological Chemistry, Graduate School of Agricultural and Life Sciences, The University of Tokyo, Tokyo 113-8657, Japan.

In the course of an effort to identify unknown targets genes for sterol regulatory element-binding proteins (SREBPs) by PCR, the gene for ATP citrate-lyase was determined to be one such gene. (Sato, R., Okamoto, A. Read More

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September 2003

Activation of the insulin gene promoter through a direct effect of hepatocyte nuclear factor 4 alpha.

J Biol Chem 2002 Jul 6;277(29):25914-9. Epub 2002 May 6.

Department of Biological Chemistry, Weizmann Institute of Science, Rehovot 76100, Israel.

Maturity onset diabetes of the young, subtype 1 (MODY1), is associated with defective glucose-dependent insulin secretion from pancreatic beta cells. MODY1 is caused by mutation in the transcription factor hepatocyte nuclear factor 4 alpha (HNF4 alpha). To understand better the MODY1 phenotype, we tested whether HNF4 alpha was able to modulate directly the insulin gene promoter. Read More

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Characterization of the human PPARalpha promoter: identification of a functional nuclear receptor response element.

Mol Endocrinol 2002 May;16(5):1013-28

U.545 Institut National de la Santé et de la Recherche Médicale, Département d'Athérosclérose, Institut Pasteur de Lille, 59019 Lille, France.

PPARalpha is a nuclear receptor that controls lipid and glucose metabolism and exerts antiinflammatory activities. The factors regulating human PPARalpha (hPPARalpha) gene expression remain largely unexplored. To study the mechanisms controlling hPPARalpha expression, the hPPARalpha gene promoter was identified and characterized. Read More

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Cloning and characterization of the human factor XI gene promoter: transcription factor hepatocyte nuclear factor 4alpha (HNF-4alpha ) is required for hepatocyte-specific expression of factor XI.

J Biol Chem 2002 May 12;277(21):18510-6. Epub 2002 Mar 12.

Department of Pathology, Vanderbilt University, Nashville, Tennessee 37232-6307, USA.

Factor XI is the zymogen of a plasma protease produced primarily in liver that is required for normal blood coagulation. We cloned approximately 2600 base pairs of the human factor XI gene upstream of exon one, identified transcription start sites, and conducted a functional analysis. Luciferase reporter assays demonstrate that the 381 base pairs upstream of exon one are sufficient for maximum promoter activity in HepG2 hepatocellular carcinoma cells. Read More

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Polyunsaturated fatty acyl coenzyme A suppress the glucose-6-phosphatase promoter activity by modulating the DNA binding of hepatocyte nuclear factor 4 alpha.

J Biol Chem 2002 May 25;277(18):15736-44. Epub 2002 Feb 25.

INSERM U. 449, Faculté de Médecine Laennec, Rue Guillaume Paradin, 69372 Lyon cedex 08, France.

Glucose-6-phosphatase confers on gluconeogenic tissues the capacity to release endogenous glucose in blood. The expression of its gene is modulated by nutritional mechanisms dependent on dietary fatty acids, with specific inhibitory effects of polyunsaturated fatty acids (PUFA). The presence of consensus binding sites of hepatocyte nuclear factor 4 (HNF4) in the -1640/+60 bp region of the rat glucose-6-phosphatase gene has led us to consider the hypothesis that HNF4 alpha could be involved in the regulation of glucose-6-phosphatase gene transcription by long chain fatty acid (LCFA). Read More

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An automated fluorescent single strand conformation polymorphism technique for high throughput mutation screening.

Chin Med J (Engl) 2001 Nov;114(11):1147-50

Department of Endocrinology, First Affiliated Hospital of Sun Yet-San University of Medical Sciences, Guangzhou 510080, China.

Objective: To develop a high throughput mutational detection method by multiple fluorescence-labeled polymerase chain reaction (PCR) products.

Methods: A total of 27 known mutations including 22 substitutions, 3 insertions (1, 2 and 7 bp) and 2 deletions (1 and 2 bp) in the hepatocyte nuclear factor (HNF)-4 alpha, glucokinase and HNF-1 alpha genes were tested. During nested PCR, amplified fragments were labeled with three fluorescent dyes. Read More

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November 2001

Reactivation of liver-specific gene expression in an immortalized human hepatocyte cell line by introduction of the human HNF4alpha2 gene.

Int J Mol Med 2001 Nov;8(5):481-7

Department of Cell Biology, Institute of Molecular and Cellular Biology, Okayama University Medical School, 2-5-1 Shikata, Okayama 700-8558, Japan.

An immortalized human hepatocyte cell line (OUMS-29) was established from fetal liver by transfection with the SV-40 large T antigen gene that has certain liver-specific functions such as albumin production and enzyme activities of CYP1A1, 1A2, and 2E1. To make OUMS-29 cells express other liver-specific functions, the human hepatocyte nuclear factor 4alpha2 (HNF4alpha2) gene was introduced into the cells, because this gene was found to be markedly down-regulated. The transduced HNF4alpha2 was overexpressed in the nuclei of the transfected cells, and its DNA-binding activity was also detected. Read More

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November 2001

Co-operative regulation of the transcription of human dihydrodiol dehydrogenase (DD)4/aldo-keto reductase (AKR)1C4 gene by hepatocyte nuclear factor (HNF)-4alpha/gamma and HNF-1alpha.

Biochem J 2001 Apr;355(Pt 2):537-44

Laboratory of Drug Metabolism, Hokkaido University Graduate School of Pharmaceutical Sciences, Sapporo, Hokkaido 060-0812, Japan.

Human dihydrodiol dehydrogenase (DD) 4/aldo-keto reductase (AKR) 1C4 is a major isoform of hepatic DD that oxidizes trans-dihydrodiols of polycyclic aromatic hydrocarbons to reactive and redox-active o-quinones and that reduces several ketone-containing drugs. To investigate the mechanism of transcriptional regulation of the human DD4 gene, the 5'-flanking region of the gene was fused to the luciferase gene. The results of luciferase assays using HepG2 cells and of 1,10-phenanthroline-copper footprinting indicated that two positive regulatory regions were located in regions from -701 to -684 and from -682 to -666. Read More

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Triethoxysilyl-substituted aminoethanethiol ligands for zinc and cadmium complexes and aminoethanethiol-modified silica gel. Evaluation of the corresponding supported molecular trap for metallic pollutant uptake (Cd2+, Hg2+ and Pb2+).

J Environ Monit 2000 Jun;2(3):240-7

Laboratoire de Chimie Inorganique, Université P. Sabatier, Toulouse, France.

The reaction of 2-[3-(triethoxysilyl)propylamino]ethanethiol (LH, a) and 1-methyl-2-[3-(triethoxysilyl)propylamino]ethanethiol (LH, b) with ZnX2 and CdX2 (X = Cl, Br, I, NO3) in tetrahydrofuran (THF) or CH2Cl2 gives several complexes depending on the experimental conditions. Elemental analyses, IR, Raman, 13C[1H], 1H NMR and mass spectroscopies indicated the formation of mononuclear and dinuclear complexes. In the absence of NEt3 as proton quencher, the protonated ligands react in their zwitterionic form giving dinuclear [M(LH)X2]2 [M = Zn (1), Cd (2); LH = a, b; X = Cl, Br, I] or mononuclear M(NO3)2(LH)2 [M = Zn (5), Cd (6); LH = a] complexes. Read More

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Synergistic activation of the Atlantic salmon hepatocyte nuclear factor (HNF) 1 promoter by the orphan nuclear receptors HNF4 and chicken ovalbumin upstream promoter transcription factor I (COUP-TFI).

Biochem J 2000 Dec;352 Pt 2:557-64

National Diagnostics Centre, University College Galway, Ireland.

Hepatocyte nuclear factor 1 (HNF1) is a liver-enriched transcription factor that plays an important role in transcriptional networks involved in liver function. The promoters of mammalian HNF1 genes contains a single binding site for another liver-enriched transcription factor, the nuclear hormone receptor HNF4. A transcriptional hierarchy involving HNF4-mediated activation of the HNF1 promoter has been proposed to be of crucial importance in maintaining the differentiated hepatocyte phenotype. Read More

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December 2000

Identification of retinoic acid-responsive elements on the HNF1alpha and HNF4alpha genes.

Biochem Biophys Res Commun 2000 Oct;276(3):837-42

Department of Pathology, Harbor-UCLA Medical Center, Torrance, California, 90509, USA.

Hepatocyte nuclear factor 1alpha (HNF1alpha) and HNF4alpha are liver-selective transcription factors and are essential for hepatocyte differentiation. This study demonstrates that HNF1alpha as well as HNF4alpha genes contain a direct repeat with a space of one nucleotide (DR1)-retinoic acid (RA) response element that can be bound and regulated by RA and retinoid x receptor alpha (RXRalpha) complex. Transient transfection experiments showed that RA increased the promoter activity of the HNF1alpha and HNF4alpha genes in Hep3B cells. Read More

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October 2000

HNF-4 plays a pivotal role in the liver-specific transcription of the chipmunk HP-25 gene.

Eur J Biochem 2000 Aug;267(15):4635-41

Hibernation Control Project, Kanagawa Academy of Science and Technology, Mitsubishi Kasei Institute of Life Sciences, Machida, Tokyo, Japan.

The gene for chipmunk hibernation-specific protein HP-25 is expressed specifically in the liver. To understand the transcriptional regulation of HP-25 gene expression, we isolated its genomic clones, and characterized its structural organization and 5' flanking region. The gene spans approximately 7 kb and consists of three exons. Read More

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Identification and characterization of a 315-base pair enhancer, located more than 55 kilobases 5' of the apolipoprotein B gene, that confers expression in the intestine.

J Biol Chem 2000 Aug;275(34):26637-48

Research Institute, Palo Alto Medical Foundation, Palo Alto, California 94301, USA.

We recently reported that an 8-kilobase (kb) region, spanning from -54 to -62 kb 5' of the human apolipoprotein B (apoB) gene, contains intestine-specific regulatory elements that control apoB expression in the intestines of transgenic mice. In this study, we further localized the apoB intestinal control region to a 3-kb segment (-54 to -57 kb). DNaseI hypersensitivity studies uncovered a prominent DNaseI hypersensitivity site, located within a 315-base pair (bp) fragment at the 5'-end of the 3-kb segment, in transcriptionally active CaCo-2 cells but not in transcriptionally inactive HeLa cells. Read More

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Identification and characterization of cis-acting elements conferring insulin responsiveness on hamster cholesterol 7alpha-hydroxylase gene promoter.

Biochem J 2000 Apr;347 Pt 1:147-54

Institute of Pharmacological Sciences, School of Pharmacy, University of Milan, Via Balzaretti 9, I-20133 Milano, Italy.

Bile acid biosynthesis occurs primarily through a pathway initiated by the 7alpha-hydroxylation of cholesterol, catalysed by cholesterol 7alpha-hydroxylase (encoded by CYP7A1). Insulin down-regulates CYP7A1 transcription. The aim of our study was to characterize the sequences of hamster CYP7A1 promoter, mediating the response to insulin. Read More

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Identification of new mutations in the hepatocyte nuclear factor 4alpha gene among families with early onset Type 2 diabetes mellitus.

Diabet Med 1999 Mar;16(3):193-200

Research Division, Joslin Diabetes Center, Boston, Massachusetts 02215-5397, USA.

Aims: Mutations in hepatocyte nuclear factor (HNF)-4alpha gene located on chromosome 20q have been found to be responsible for the development of early onset Type 2 diabetes mellitus (DM). Through a national campaign, 53 families with autosomal dominant, early onset Type 2 DM (n=654) were assembled to determine the frequency of mutations in the HNF-4alpha gene and their contribution to the development of diabetes.

Methods: Twelve exons and the promoter region of the HNF-4alpha gene were screened in probands of the families by a double gradient, denaturing gradient gel electrophoresis (DG-DGGE) protocol combined with automated bi-directional sequencing of the PCR products of all heterozygous individuals. Read More

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Orphan receptor hepatocyte nuclear factor-4 antagonizes estrogen receptor alpha-mediated induction of human coagulation factor XII gene.

Endocrinology 1998 Nov;139(11):4581-9

Molecular Oncogenesis Laboratory, Regina Elena Cancer Institute, and University of Rome La Sapienza, Italy.

Factor XII (FXII) is a liver-specific zymogen involved in the regulation of hemostasis, particularly in the activation of fibrinolysis. Transcription of the FXII gene is stimulated by estrogens through specific interaction of the estrogen receptor alpha (ER alpha) with an estrogen response element present on FXII promoter. Interestingly, the magnitude of ER alpha induction in liver HepG2 cells is much lower than in NIH3T3 fibroblasts, suggesting that cell-specific factors may modulate ER alpha-dependent trans-activation. Read More

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November 1998

Retinoic acid mediates down-regulation of the alpha-fetoprotein gene through decreased expression of hepatocyte nuclear factors.

J Biol Chem 1998 Nov;273(45):30024-32

Department of Pathology, Harbor-UCLA Medical Center, Torrance, California 90509, USA.

alpha-Fetoprotein (AFP), a protein highly induced during fetal liver development, is down-regulated by retinoids in the human hepatoma cell line Hep3B, in contrast to up-regulation observed in other cell types. Previously, we have documented that such up-regulation involves direct effects through cis-retinoid X receptor-binding sites in the AFP enhancer. In this report, we show a distinctive effect of all-trans-retinoic acid (RA) in Hep3B cells. Read More

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November 1998