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Specialty: Drugs & Pharmacology
Source: European Journal of Pharmacology

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Total 212 results found since Jan 2013.

Guggulsterone sensitized drug-resistant human hepatocarcinoma cells to doxorubicin through a Cox-2/P-gp dependent pathway.
Abstract Previous researches indicated that cyclooxygenase-2 (Cox-2) might be involved in P-glycoprotein (P-gp)-mediated multidrug resistance in hepatocellular carcinoma cells. Doxorubicin-resistant hepatocellular carcinoma PLC/PRF/5 cells (PLC/PRF/5R) and HepG2 (HepG2R) cells were developed in the present study. The modulatory effect of guggulsterone on Cox-2 and P-gp in PLC/PRF/5R and HepG2R cells was investigated. Cells proliferation, Cox-2 and P-gp expression, and prostaglandin E2 release were examined using MTT, flow cytometry, western blot and ELISA assays. Small interfering RNA (siRNA) targeted against Cox-...
Source: European Journal of Pharmacology - March 23, 2017 Category: Drugs & Pharmacology Authors: Xu HB, Fu J, Huang F, Yu J Tags: Eur J Pharmacol Source Type: research

Targeted inhibition of HDAC8 increases the doxorubicin sensitivity of neuroblastoma cells via up regulation of miR-137.
Abstract Histone deacetylases (HDACs) have been suggested to be potential therapeutic targets for cancer treatment. Recent studies revealed that HDAC8 expression was associated with poor prognostic markers and poor overall survival rate of neuroblastoma (NB). Our present study revealed that among the four members of class I HDACs, HDAC8 is significantly over expressed in NB cells as compared with the normal fibroblast 3T3 cells or primary normal human astrocytes (NHA) cells. Targeted inhibition of HDAC8 by its specific siRNA (si-HDAC8) can inhibit the in vitro growth of NB cells. Furthermore, si-HDAC8 significantl...
Source: European Journal of Pharmacology - February 17, 2017 Category: Drugs & Pharmacology Authors: Zhao G, Wang G, Bai H, Li T, Gong F, Yang H, Wen J, Wang W Tags: Eur J Pharmacol Source Type: research

Sodium influx through cerebral sodium-glucose transporter type 1 exacerbates the development of cerebral ischemic neuronal damage.
Abstract We recently reported that cerebral sodium-glucose transporter type 1 (SGLT-1) plays a role in exacerbation of cerebral ischemia. However, the mechanism by which cerebral SGLT-1 acts remains unclear. Here we demonstrated that sodium influx through cerebral SGLT-1 exacerbates cerebral ischemic neuronal damage. SGLT-specific sodium ion influx was induced using α-methyl-D-glucopyranoside (α-MG). Intracellular sodium concentrations in primary cortical neurons were estimated using sodium-binding benzofuran isophthalate fluorescence. SGLT-1 knockdown in primary cortical neurons and mice was achieved using SGLT...
Source: European Journal of Pharmacology - February 3, 2017 Category: Drugs & Pharmacology Authors: Yamazaki Y, Harada S, Wada T, Hagiwara T, Yoshida S, Tokuyama S Tags: Eur J Pharmacol Source Type: research

TLR4/NF- κB/Ceramide signaling contributes to Ox-LDL-induced calcification of human vascular smooth muscle cells.
In conclusion, these findings suggest that TLR4 regulates VSMC calcification induced by Ox-LDL through activation of NK-κB, highlighting the critical role of TLR4/NK-κB signaling in vascular calcification. PMID: 27876618 [PubMed - as supplied by publisher]
Source: European Journal of Pharmacology - November 18, 2016 Category: Drugs & Pharmacology Authors: Song Y, Hou M, Li Z, Luo C, Ou JS, Yu H, Yan J, Lu L Tags: Eur J Pharmacol Source Type: research

Antidepressant effects of TBE-31 and MCE-1, the novel Nrf2 activators, in an inflammation model of depression.
Abstract The Nuclear factor (erythroid 2-derived)-like 2 (Nrf2) plays a key role in inflammation which is implicated in the pathophysiology of depression. The Nrf2 activators have antidepressant effects in animal models of depression. The present study was undertaken to examine whether TBE-31 [(±)-(4bS,8aR,10aS)-10a-ethynyl-4b,8,8-trimethyl-3,7-dioxo-3,4b,7,8,8a,9,10,10a-octahydrophenanthrene-2,6-dicarbonitrile] and MCE-1 [(±)-3-ethynyl-3-methyl-6-oxocyclohexa-1,4-dienecarbonitrile], the novel Nrf2 activator, could show antidepressant effects in inflammation model of depression. We found that TBE-31 and MCE-1 si...
Source: European Journal of Pharmacology - October 31, 2016 Category: Drugs & Pharmacology Authors: Yao W, Zhang JC, Ishima T, Ren Q, Yang C, Dong C, Ma M, Saito A, Honda T, Hashimoto K Tags: Eur J Pharmacol Source Type: research

MicroRNA-127 is a tumor suppressor in human esophageal squamous cell carcinoma through the regulation of oncogene FMNL3.
In this study, we investigated the expression patterns and functional roles of microRNA 127 (miR-127) and its target gene Formin-Like 3 (FMNL3) in human esophageal squamous cell carcinoma (ESCC). Quantitative RT-PCR (qRT-PCR) was used to compare miR-127 expression between ESCC cell lines and normal esophageal epithelium cell line, as well as paired ESCC tumors and adjacent normal esophageal tissues in 33 patients. We found miR-127 was aberrantly downregulated in both ESCC cell lines and human ESCC tumors. In ESCC cell lines TE-1 and ECA109 cells, lentiviral-induced miR-127 upregulation markedly inhibited cancer proliferati...
Source: European Journal of Pharmacology - September 15, 2016 Category: Drugs & Pharmacology Authors: Gao X, Wang X, Cai K, Wang W, Ju Q, Yang X, Wu H, Wang H Tags: Eur J Pharmacol Source Type: research

Activation of AMPK α2 inhibits airway smooth muscle cells proliferation.
Abstract The aims of the present study were to examine the effect of adenosine monophosphate-activated protein kinase (AMPK) activation on airway smooth muscle cells (ASMCs) proliferation and to address its potential mechanisms. Platelet derived growth factor (PDGF) activated phosphatidylinositol 3-kinase (PI3K)/protein kinase B (Akt)/mammalian target of rapamycin (mTOR) signaling pathway, and this in turn up-regulated S-phase kinase-associated protein 2 (Skp2) and consequently reduced cyclin dependent kinase inhibitor 1B (p27) leading to ASMCs proliferation. Pre-incubation of cells with metformin, an AMPK activat...
Source: European Journal of Pharmacology - September 2, 2016 Category: Drugs & Pharmacology Authors: Liu L, Pan Y, Song Y, Su X, Ke R, Yang L, Gao L, Li M Tags: Eur J Pharmacol Source Type: research

HNF-4 α regulated miR-122 contributes to development of gluconeogenesis and lipid metabolism disorders in Type 2 diabetic mice and in palmitate-treated HepG2 cells.
We examined how HNF-4α regulated gluconeogenesis and lipid metabolism through miR-122 in vivo and in vitro. Expression of miR-122, HNF-4α, phosphoenolpyruvate carboxykinase (PEPCK), glucose-6-phosphatase (G6Pase), sterol response elementary binding protein-1 (SREBP-1), fatty acid synthase-1 (FAS-1), carnitine palmitoyltransferase-1 (CPT-1) and acetyl Coenzyme A carboxylase alpha (ACCα) were determined in livers of Type 2 diabetic mice and in insulin resistant palmitate-treated HepG2 cells. CPT-1 and phosphorylated ACCα expression were significantly decreased in livers of Type 2 diabetic mice and in palmitated-treated H...
Source: European Journal of Pharmacology - August 30, 2016 Category: Drugs & Pharmacology Authors: Wei S, Zhang M, Yu Y, Xue H, Lan X, Liu S, Hatch G, Chen L Tags: Eur J Pharmacol Source Type: research

Aromatic malononitriles stimulate the resistance of insulin-producing beta- cells to oxidants and inflammatory cytokines.
We presently report that treatment with tyrphostin AG-126 (2-(3-hydroxy-4-nitrobenzylidene)malononitrile) and ten other aromatic malononitrile compounds (AMN) improves the resistance of insulin-producing βTC6, RIN-5AH, and MIN6 cells to oxidative stress and pro-inflammatory cytokines. On the molecular level AMN compounds promote nuclear accumulation of the Nrf2 transcription factor and expression of the cytoprotective genes heme ogygenase 1 (HO-1) and NAD(P)H/quinone oxidoreductase 1 (NQO1), inhibit cytokine-dependent inducible nitric oxide synthase (iNOS) induction, suppress intracellular production of reactive oxygen sp...
Source: European Journal of Pharmacology - May 9, 2016 Category: Drugs & Pharmacology Authors: Turpaev K, Welsh N Tags: Eur J Pharmacol Source Type: research

Targeting the 19S proteasomal subunit, Rpt4, for the treatment of colon cancer.
Abstract Deregulation of the ubiquitin-proteasome pathway has been frequently observed in a number of malignancies. Using quantitative Western blotting of normal and matched tumour tissue, we here identified a significant increase in the 19S proteasome subunit Rpt4 in response to chemoradiation in locally advanced rectal cancer patients with unfavourable outcome. We therefore explored the potential of Rpt4 reduction as a therapeutic strategy in colorectal cancer (CRC). Utilizing siRNA to down regulate Rpt4 expression, we show that silencing of Rpt4 reduced proteasomal activity and induced endoplasmic reticulum str...
Source: European Journal of Pharmacology - March 16, 2016 Category: Drugs & Pharmacology Authors: Boland K, Flanagan L, McCawley N, Pabari R, Kay EW, McNamara DA, Murray F, Byrne AT, Ramtoola Z, Concannon CG, Prehn JH Tags: Eur J Pharmacol Source Type: research

Sphingosine-1-phosphate receptor 2 mediates endothelial cells dysfunction by PI3K-Akt pathway under high glucose condition.
In conclusion, S1P/S1PR2 mediated endothelial dysfunction partly by inhibiting PI3K/Akt signaling pathway under high glucose condition. S1PR2 blockage could ameliorate endothelial dysfunction which might provide a potential therapeutic strategy for diabetic vascular complications. PMID: 26921757 [PubMed - as supplied by publisher]
Source: European Journal of Pharmacology - February 24, 2016 Category: Drugs & Pharmacology Authors: Liu W, Liu B, Liu S, Zhang J, Lin S Tags: Eur J Pharmacol Source Type: research

Novel effects of FTY720 on perinuclear reorganization of keratin network induced by sphingosylphosphorylcholine: Involvement of PP2A and G-protein-coupled receptor-12.
Abstract Sphingosylphosphorylcholine (SPC) evokes perinuclear reorganization of keratin 8 (K8) filaments and regulates the viscoelasticity of metastatic cancer cells leading to enhanced migration. Few studies have addressed the compounds modulating the viscoelasticity of metastatic cancer cells. We studied the effects of sphingosine (SPH), sphingosine 1-phosphate (S1P), FTY720 and FTY720-phosphate (FTY720P) on SPC-induced K8 phosphorylation and reorganization using Western blot and confocal microscopy, and also evaluated the elasticity of PANC-1 cells by atomic force microscopy. FTY720, FTY720P, SPH, and S1P conce...
Source: European Journal of Pharmacology - February 9, 2016 Category: Drugs & Pharmacology Authors: Park MK, Park S, Kim HJ, Kim EJ, Kim SY, Kang GJ, Byun HJ, Kim SH, Lee H, Lee CH Tags: Eur J Pharmacol Source Type: research

Increase of human prostate cancer cell (DU145) apoptosis by telmisartan through PPAR-delta pathway.
In conclusion, telmisartan induces prostate cancer DU145 cells apoptosis through the up-regulation of PPAR-delta protein expression. Pharmacological inhibition or genetic silencing of PPAR-delta activity can both reverse the telmisartan-induced apoptotic effect. Thus the PPAR-delta pathway might be a potential target for the treatment of prostate cancer. PMID: 26852954 [PubMed - as supplied by publisher]
Source: European Journal of Pharmacology - February 4, 2016 Category: Drugs & Pharmacology Authors: Wu TT, Niu HS, Chen LJ, Cheng JT, Tong YC Tags: Eur J Pharmacol Source Type: research

Insulin-like growth factor 1 specifically up-regulates expression of modifier subunit of glutamate-cysteine ligase and enhances glutathione synthesis in SH-SY5Y cells.
Abstract Glutathione is a key regulator of oxidative balance in all mammals, especially in the central nervous system. The first step of glutathione synthesis is catalyzed by glutamate-cysteine ligase (GCL), which is composed of catalytic and modifier subunits (GCLC and GCLM, respectively). In non-neural cells and tissues, insulin and insulin-like growth factor 1 (IGF-1) have been found to stimulate transcription of GCLC gene. Here we found that treatment of human neuroblastoma SH-SY5Y cells with insulin or IGF-1 increased mRNA level of GCLM, but not of GCLC, in a concentration- and time-dependent manner. In contr...
Source: European Journal of Pharmacology - December 11, 2015 Category: Drugs & Pharmacology Authors: Takahashi S, Hisatsune A, Kurauchi Y, Seki T, Katsuki H Tags: Eur J Pharmacol Source Type: research

Effect of vasopressin on Na(+)-K(+)-2Cl(-) cotransporter (NKCC) and the signaling mechanisms on the murine late distal colon.
Abstract It has been demonstrated that the antidiuretic hormone vasopressin is able to regulate the expression of Na-K-Cl cotransporters (NKCC1 and NKCC2) in the kidney. The present study investigated the effects of long- and short-term administration of vasopressin on NKCC and the possible signaling mechanism of vasopressin in the mouse distal colon using the siRNA, real-time PCR, western blotting and Ussing chambers method. The results showed the presence of NKCC2 expression in the colon, which was verified with a siRNA technique. The mRNA and protein expression level of NKCC2 significantly increased by about 40...
Source: European Journal of Pharmacology - December 4, 2015 Category: Drugs & Pharmacology Authors: Xue H, Tang X Tags: Eur J Pharmacol Source Type: research