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Specialty: Drugs & Pharmacology
Source: Biochemical Pharmacology

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Total 204 results found since Jan 2013.

Oroxyloside prevents dextran sulfate sodium-induced experimental colitis in mice by inhibiting NF-κB pathway through PPARγ activation.
Abstract Oroxyloside, as a metabolite of oroxylin A, may harbor various beneficial bioactivities which have rarely been reported in the previous studies. Here we established the dextran sulfate sodium (DSS)-induced experimental colitis and evaluated the anti-inflammatory effect of oroxyloside in vivo. As a result, oroxyloside attenuated DSS-induced body weight loss, colon length shortening and colonic pathological damage. Furthermore, oroxyloside inhibited inflammatory cells infiltration and decreased myeloperoxidase (MPO) and inducible nitric oxide synthase (iNOS) activities as well. The production of pro-inflamm...
Source: Biochemical Pharmacology - March 3, 2016 Category: Drugs & Pharmacology Authors: Wang X, Sun Y, Zhao Y, Ding Y, Zhang X, Kong L, Li Z, Guo Q, Zhao L Tags: Biochem Pharmacol Source Type: research

Aryl hydrocarbon receptor (AHR) regulation of L-Type Amino Acid Transporter 1 (LAT-1) expression in MCF-7 and MDA-MB-231 breast cancer cells.
Abstract The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that is regulated by environmental toxicants that function as AHR agonists such as 2,3,7,8 tetrachlorodibenzo-p-dioxin (TCDD). L-Type Amino Acid Transporter 1 (LAT1) is a leucine transporter that is overexpressed in cancer. The regulation of LAT1 by AHR in MCF-7 and MDA-MB-231 breast cancer cells (BCCs) was investigated in this report. Ingenuity pathway analysis (IPA) revealed a significant association between TCDD-regulated genes (TRGs) and molecular transport. Overlapping the TCDD-RNA-Seq dataset obtained in this study with a...
Source: Biochemical Pharmacology - March 1, 2016 Category: Drugs & Pharmacology Authors: Tomblin JK, Arthur S, Primerano DA, Chaudhry AR, Fan J, Denvir J, Salisbury TB Tags: Biochem Pharmacol Source Type: research

The C421A (Q141K) polymorphism enhances the 3'-untranslated region (3'-UTR)-dependent regulation of the ATP-binding cassette transporter ABCG2.
Abstract The impact of the gout-causing C421A (Q141K) single nucleotide polymorphism (SNP) on ABC transporter ABCG2 expression and function has been extensively characterized. However, the influence of the C421A SNP on 3'-UTR-dependent ABCG2 regulation has not been analysed so far. To elucidate this matter, we generated vectors for expression of either the ABCG2 coding sequence (ORF) or the ABCG2 ORF fused to its 3'-UTR, inserted the C421A mutation via site-directed mutagenesis and expressed wild-type and C421A-mutated ABCG2 transcripts in HEK293-Tet-On cells. As shown previously, the C421A SNP significantly reduc...
Source: Biochemical Pharmacology - February 19, 2016 Category: Drugs & Pharmacology Authors: Ripperger A, Benndorf RA Tags: Biochem Pharmacol Source Type: research

Serum- and Glucocorticoid-Inducible Kinase SGK2 Regulates Human Organic Anion Transporters 4 via Ubiquitin Ligase Nedd4-2.
In conclusion, our study demonstrated for the first time that sgk2 stimulated hOAT4 transport activity by abrogating the inhibition effect of Nedd4-2 on the transporter. PMID: 26740304 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - December 28, 2015 Category: Drugs & Pharmacology Authors: Wang H, Xu D, Toh MF, Pao AC, You G Tags: Biochem Pharmacol Source Type: research

Ceramide 1-phosphate regulates cell migration and invasion of human pancreatic cancer cells.
Abstract Pancreatic cancer is an aggressive and devastating disease characterized by invasiveness, rapid progression and profound resistance to treatment. Despite years of intense investigation, the prognosis of this type of cancer is poor and there is no efficacious treatment to overcome the disease. Using human PANC-1 and MIA PaCa-2 cells, we demonstrate that the bioactive sphingolipid ceramide 1-phosphate (C1P) increases pancreatic cancer cell migration and invasion. Treatment of these cells with selective inhibitors of phosphatidylinositol 3-kinase (PI3K), Akt1, or mammalian target of rapamycin 1 (mTOR1), or w...
Source: Biochemical Pharmacology - December 18, 2015 Category: Drugs & Pharmacology Authors: Rivera IG, Ordoñez M, Presa N, Gangoiti P, Gomez-Larrauri A, Trueba M, Fox T, Kester M, Gomez-Muñoz A Tags: Biochem Pharmacol Source Type: research

Pioglitazone, a PPARγ agonist, attenuates PDGF-induced vascular smooth muscle cell proliferation through AMPK-dependent and AMPK-independent inhibition of mTOR/p70S6K and ERK signaling.
Abstract Pioglitazone (PIO), a PPARγ agonist that improves glycemic control in type 2 diabetes through its insulin-sensitizing action, has been shown to exhibit beneficial effects in the vessel wall. For instance, it inhibits vascular smooth muscle cell (VSMC) proliferation, a major event in atherosclerosis and restenosis after angioplasty. Although PPARγ-dependent and PPARγ-independent mechanisms have been attributed to its vasoprotective effects, the signaling events associated with PIO action in VSMCs are not fully understood. To date, the likely intermediary role of AMP-activated protein kinase (AMPK) towar...
Source: Biochemical Pharmacology - November 28, 2015 Category: Drugs & Pharmacology Authors: Osman I, Segar L Tags: Biochem Pharmacol Source Type: research

A crucial role for ATR in the regulation of deoxycytidine kinase activity.
Abstract Deoxycytidine kinase (dCK) (EC 2.7.1.74) is a key enzyme for salvage of deoxynucleosides and activation of numerous anticancer and antiviral nucleoside analogs. dCK activity is enhanced in response to several genotoxic treatments, which has been correlated with an increase of dCK phosphorylation at Ser-74. ATM was recently identified as the kinase responsible for Ser-74 phosphorylation and dCK activation after ionizing radiation (IR). Here, we investigated the role of ATM and the related kinase ATR in dCK activation induced by other types of DNA damage. Using ATM-deficient cells or the ATM inhibitor KU-60...
Source: Biochemical Pharmacology - November 24, 2015 Category: Drugs & Pharmacology Authors: Beyaert M, Starczewska E, Neste EV, Bontemps F Tags: Biochem Pharmacol Source Type: research

Involvement of Pregnane X Receptor in the Impaired Glucose Utilization Induced by Atorvastatin in Hepatocytes.
In conclusion, atorvastatin impaired glucose utilization in hepatocytes via repressing GLUT2 and GCK expressions, which may be partly due to PXR activation. PMID: 26616219 [PubMed - as supplied by publisher]
Source: Biochemical Pharmacology - November 23, 2015 Category: Drugs & Pharmacology Authors: Ling Z, Shu N, Xu P, Wang F, Zhong Z, Sun B, Li F, Zhang M, Zhao K, Tang X, Wang Z, Zhu L, Liu L, Liu X Tags: Biochem Pharmacol Source Type: research

Inhibition of Kv Channel Expression by NSAIDs Depolarizes Membrane Potential and Inhibits Cell Migration by Disrupting Calpain Signaling.
Abstract Clinical use of non-steroidal anti-inflammatory drugs (NSAIDs) is well known to cause gastrointestinal ulcer formation via several mechanisms that include inhibiting epithelial cell migration and mucosal restitution. The drug-affected signaling pathways that contribute to inhibition of migration by NSAIDs are poorly understood, though previous studies have shown that NSAIDs depolarize membrane potential and suppress expression of calpain proteases and voltage-gated potassium (Kv) channel subunits. Kv channels play significant roles in cell migration and are targets of NSAID activity in white blood cells, ...
Source: Biochemical Pharmacology - November 5, 2015 Category: Drugs & Pharmacology Authors: Silver K, Littlejohn A, Thomas L, Marsh E, Lillich JD Tags: Biochem Pharmacol Source Type: research

Autophagy exacerbates caspase-dependent apoptotic cell death after short times of starvation.
Abstract Autophagy is generally regarded as a mechanism to promote cell survival. However, autophagy can occasionally be the mechanism responsible of cell demise. We have found that a concomitant depletion of glucose, nutrients and growth factors provoked cell death in a variety of cell lines. This death process was contingent upon caspase activation and was mediated by BAX/BAK proteins, thus indicating its apoptotic nature and the engagement of an intrinsic pathway. In order to abrogate autophagy, 3-methyladenine (3-MA), BECLIN-1 siRNA and Atg5 knock-out (Tet-Off type) approaches were alternatively employed. Irre...
Source: Biochemical Pharmacology - October 3, 2015 Category: Drugs & Pharmacology Authors: Mattiolo P, Yuste VJ, Boix J, Ribas J Tags: Biochem Pharmacol Source Type: research

Estrogen receptor mediates simvastatin-stimulated osteogenic effects in bone marrow mesenchymal stem cells.
In this study, we hypothesize that the estrogen receptor (ER) mediates simvastatin-induced osteogenic differentiation. ER antagonists and siRNA were used to determine the involvement of the ER in simvastatin-induced osteogenesis in mouse bone marrow mesenchymal stem cells (D1 cells). Osteogenesis was evaluated by mRNA expression, protein level/activity of osteogenic markers, and mineralization. The estrogen response element (ERE) promoter activity and the ER-simvastatin binding affinity were examined. Our results showed that the simvastatin-induced osteogenic effects were decreased by treatment with ERα antagonists and ER...
Source: Biochemical Pharmacology - September 24, 2015 Category: Drugs & Pharmacology Authors: Chuang SC, Chen CH, Fu YC, Tai IC, Li CJ, Chang LF, Ho ML, Chang JK Tags: Biochem Pharmacol Source Type: research

PKC-δ/PKC-α activity balance regulates the lethal effects of cisplatin.
Abstract Cisplatin is commonly employed in therapy of mesothelioma but its efficacy is limited and the mechanisms by which induces its effects are not clearly understood. PKCs can regulate cisplatin sensitivity. PKCs effects on cellular sensitivity/resistance depend on the pattern of active PKC isozymes as well as on cellular context. The present study was undertaken to determine if specific PKC isoforms regulate cisplatin-induced apoptosis in the human mesothelioma ZL55 cells. Cells were treated with cisplatin at various concentrations and for different incubation periods. Cytotoxicity assays and Western blotting...
Source: Biochemical Pharmacology - August 20, 2015 Category: Drugs & Pharmacology Authors: Muscella A, Vetrugno C, Antonaci G, Cossa LG, Marsigliante S Tags: Biochem Pharmacol Source Type: research

Berberine induces GLP-1 secretion through activation of bitter taste receptor pathways.
This study was designed to ascertain whether berberine-induced secretion of GLP-1 was related with activation of bitter taste receptors expressed in gastrointestinal tract. Western blotting results showed that TAS2R38, a subtype of bitter taste receptor, was expressed on human enteroendocrine NCI-H716 cells. GLP-1 secretion induced by berberine from NCI-H716 cells was inhibited by incubation with anti-TAS2R38 antibody. We further performed gene silencing using siRNA to knockdown TAS2R38 from NCI-H716 cells, which showed that siRNA knockdown of the TAS2R38 reduced berberine-mediated GLP-1 secretion. We adopted inhibitors of...
Source: Biochemical Pharmacology - July 20, 2015 Category: Drugs & Pharmacology Authors: Yu Y, Hao G, Zhang Q, Hua W, Wang M, Zhou W, Zong S, Huang M, Wen X Tags: Biochem Pharmacol Source Type: research

JAK1/STAT3 activation directly inhibits IL-12 production in dendritic cells by preventing CDK9/P-TEFb recruitment to the p35 promoter.
Abstract Inhibition of Janus-activated kinase-1 (JAK1) is a promising clinical concept for post-transplant immunosuppression and autoimmunity. However, it also raises concerns regarding possible immunosuppressive side effects. Our study investigates JAK1 signalling in the context of CD40L and bacterially activated human MoDC using siRNA and biological inhibitors. We demonstrate that strong stimuli (e.g. intact E. coli or LPS in addition to IL-1β) induce IL-12p70 via a ROS/RELA/CDK9 pathway that is inhibited by simultaneous JAK1/STAT3 signalling. Transcription is effective if RELA recruits the positive transcripti...
Source: Biochemical Pharmacology - April 27, 2015 Category: Drugs & Pharmacology Authors: Wagner AH, Conzelmann M, Fitzer F, Giese T, Gülow K, Falk CS, Krämer OH, Dietrich S, Hecker M, Luft T Tags: Biochem Pharmacol Source Type: research

Ascorbic acid reduces HMGB1 secretion in lipopolysaccharide-activated RAW 264.7 cells and improves survival rate in septic mice by activation of Nrf2/HO-1 signals.
Abstract High mobility group box 1 (HMGB1) is now recognized as a late mediator of sepsis. We tested hypothesis that ascorbic acid (AscA) induces heme oxygenase (HO)-1 which inhibits HMGB1 release in lipopolysaccharide (LPS)-stimulated cells and increases survival of septic mice. AscA increased HO-1 protein expression in a concentration- and time-dependent manner via Nrf2 activation in RAW 264.7 cells. HO-1 induction by AscA was significantly reduced by Nrf2 siRNA-transfected cells. Mutation of cysteine to serine of keap-1 proteins (C151S, C273S, and C288S) lost the ability of HO-1 induction by AscA, due to failur...
Source: Biochemical Pharmacology - April 17, 2015 Category: Drugs & Pharmacology Authors: Kim SR, Ha YM, Kim YM, Park EJ, Kim JW, Park SW, Kim HJ, Chung HT, Chang KC Tags: Biochem Pharmacol Source Type: research