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Molecular targets for tivantinib (ARQ 197) and vasculogenic mimicry in human melanoma cells.
Abstract Tivantinib (TivB) was reported previously to target MET and microtubule assembly in different cells resulting in cytotoxicity. However, its other cellular targets remain unknown, especially the proteins involved in focal adhesion and cytoskeletal organization. We studied the effect of TivB on vinculin a focal adhesion protein, and RhoC, a GTPase which promote the reorganization of cytoskeleton. Biomolecules involved in vasculogenic mimicry (VM) previously not reported in melanoma, and their susceptibility to TivB was also evaluated. TivB affects the viability and apoptosis of human melanoma cells dependin...
Source: European Journal of Pharmacology - April 3, 2019 Category: Drugs & Pharmacology Authors: Kumar SR, Gajagowni S, Bryan JN, Bodenhausen HM Tags: Eur J Pharmacol Source Type: research

Vitexin protects against ischemia/reperfusion-induced brain endothelial permeability.
In this study, the effects of Vitexin on endothelial permeability and the underlying mechanisms in human brain microvascular endothelial cells (HBMEc) I/R injury model were investigated. Cell viability, lactate dehydrogenase (LDH), inflammation and apoptosis were detected. The effects of Vitexin on BBB integrity tight junction, matrix metalloproteinases (MMP) were also investigated. The mechanism was confirmed by PI3K inhibitor and NOS inhibitor in normal or eNOS siRNA transfection HBMEc. Vitexin significantly reduced LDH, Caspase 3 level, alleviated inflammation, also could maintain BBB integrity, increased tight junction...
Source: European Journal of Pharmacology - March 11, 2019 Category: Drugs & Pharmacology Authors: Cui YH, Zhang XQ, Wang ND, Zheng MD, Yan J Tags: Eur J Pharmacol Source Type: research

Metformin reduced NLRP3 inflammasome activity in Ox-LDL stimulated macrophages through adenosine monophosphate activated protein kinase and protein phosphatase 2A.
Abstract Metformin has been suggested to have cardiovascular protective effects. Previous researches showed that metformin activates Adenosine Monophosphate Activated Protein Kinase (AMPK) and Protein Phosphatase 2A (PP2A). This research aimed to elucidate whether and how metformin affects NLR Family Pyrin Domain Containing 3 (NLRP3) inflammasome activity in oxidized low-density lipoprotein (ox-LDL) stimulated macrophages. Macrophages were treated with ox-LDL and metformin in a continuous manner, and NLRP3 inflammasome activation was evaluated by detecting IL-1β and caspase-1 p10 release by ELISA and western blot...
Source: European Journal of Pharmacology - March 5, 2019 Category: Drugs & Pharmacology Authors: Zhang L, Lu L, Zhong X, Yue Y, Hong Y, Li Y, Li Y Tags: Eur J Pharmacol Source Type: research

Targeted regulation of Rell2 by microRNA-18a is implicated in the anti-metastatic effect of polyphyllin VI in breast cancer cells.
Abstract Polyphyllin VI (PP-VI) is one of the major saponins present in Paris polyphylla Sm., a medicinal plant primarily used for cancer treatment in China and India. However, its anti-metastatic activity remains largely unknown. The current study thus investigated the anti-metastatic activity of PP-VI in mouse mammary carcinoma 4T1 and human breast cancer MDA-MB-231 cells. The anti-metastatic effect of PP-VI was investigated at a sub-cytotoxic dose in migration and invasion assays in vitro. Experimental metastasis mouse model was used to examine the anti-metastatic effect of PP-VI in vivo. Additionally, target p...
Source: European Journal of Pharmacology - February 24, 2019 Category: Drugs & Pharmacology Authors: Wang P, Yang Q, Du X, Chen Y, Zhang T Tags: Eur J Pharmacol Source Type: research

IPP-1 controls Akt/CREB phosphorylation extension in A2a adenosine receptor signaling cascade in MIN6 Pancreatic β-cell line.
Abstract Signaling through A2a adenosine receptor specifically prevent pancreatic β-cells (PBCs) loses under diabetogenic conditions. However, signaling mediators of this receptor in PBCs remained unidentified. Thus, we aimed to investigate the possible involvement of PKA/Akt/IPP-1/CREB pathway in MIN6 β-cells. In addition, we investigated IPP-1 role in A2a receptor signaling pathway. The expression of A2a receptor in MIN6 cell line was evaluated by RT-PCR and its functionality confirmed by quantification of cAMP in response to the CGS 21680, an A2a receptor agonist. MTT and Brdu assays were used to evaluate cel...
Source: European Journal of Pharmacology - February 14, 2019 Category: Drugs & Pharmacology Authors: Shahrestanaki MK, Arasi FP, Aghaei M Tags: Eur J Pharmacol Source Type: research

Complement C3a receptor antagonist attenuates tau hyperphosphorylation via glycogen synthase kinase 3 β signaling pathways.
In this study, we found that exposure of SH-SY5Y cells to okadaic acid (OA) decreased cell viabilities and induced tau hyperphosphorylation. These effects were alleviated by C3a receptor antagonist SB290157 and were further validated by C3a receptor siRNA in OA-treated SH-SY5Y cells. In addition, our results demonstrated that SB290157 markedly inhibited the activities of glycogen synthase kinase 3β (GSK3β), but had no effect on protein phosphatase 2AC subunit (PP2Ac) and cyclin-dependent kinases 5 (CDK5). Our findings here indicate the unique role of the C3a receptor in regulating tau phosphorylation via GSK3β signaling...
Source: European Journal of Pharmacology - February 13, 2019 Category: Drugs & Pharmacology Authors: Hu J, Yang Y, Wang M, Yao Y, Chang Y, He Q, Ma R, Li G Tags: Eur J Pharmacol Source Type: research

Inhibition of microRNA-155 attenuates sympathetic neural remodeling following myocardial infarction via reducing M1 macrophage polarization and inflammatory responses in mice.
In conclusion, miR-155 inhibition downregulated NGF expression via decreasing M1 macrophage polarization and inflammatory responses dependent on the SOCS1/NF-κB pathway, subsequently diminishing MI-induced sympathetic neural remodeling and ventricular arrhythmias (VAs). PMID: 30721702 [PubMed - as supplied by publisher]
Source: European Journal of Pharmacology - February 2, 2019 Category: Drugs & Pharmacology Authors: Hu J, Huang CX, Rao PP, Zhou JP, Wang X, Tang L, Liu MX, Zhang GG Tags: Eur J Pharmacol Source Type: research

Levobupivacaine-induced vasoconstriction involves caldesmon phosphorylation mediated by tyrosine kinase-induced ERK phosphorylation.
Abstract The goals of this study were to examine the cellular signaling pathways associated with the phosphorylation of caldesmon, the phosphorylation-dependent inhibitory protein of myosin phosphatase (CPI-17), and the 20-kDa regulatory light chain of myosin (MLC20) induced by levobupivacaine in isolated rat aortas. The effects of genistein, tyrphostin 23, GF109203X, PD98059, Y-27632, 1-butanol, and ML-7 HCl on levobupivacaine-induced contraction were assessed. The effect of genistein on the simultaneous calcium-tension curves induced by levobupivacaine was examined. The effects of GF109203X, genistein, PD98059 a...
Source: European Journal of Pharmacology - November 1, 2018 Category: Drugs & Pharmacology Authors: Lee SH, Kwon SC, Ok SH, Hong JM, Kim JY, Ahn SH, Il Bae S, Shin Y, Sohn JT Tags: Eur J Pharmacol Source Type: research

Xanthatin induces apoptosis by activating endoplasmic reticulum stress in hepatoma cells.
Abstract Hepatocellular carcinoma (HCC) has high incidence and mortality in patients with chronic liver diseases worldwide. However, there are limited chemotherapeutic agents for HCC in clinic. Xanthatin, a natural sesquiterpene lactone, has significant antitumor activity against a variety of cancers, but little is known about its effects on HCC and the underlying mechanism. Here, we evaluated the antitumor effects of xanthatin on human hepatoma cells. We found that xanthatin caused morphological changes and reduced cell viability in three HCC cell lines in concentration- and time-dependent manners. Xanthatin at 1...
Source: European Journal of Pharmacology - October 30, 2018 Category: Drugs & Pharmacology Authors: Shi TL, Zhang L, Yu JS, Cheng QR, Liu J, Shen YJ, Feng XJ, Shen YX Tags: Eur J Pharmacol Source Type: research

Calcitonin gene-related peptide inhibits the cardiac fibroblasts senescence in cardiac fibrosis via up-regulating klotho expression.
Abstract It has been documented cardiac fibroblasts as the predominant cell population undergoing senescence in heart. Calcitonin gene-related peptide (CGRP) exhibits a wide range of cardiovascular protective effects. Whether CGRP protects against cardiac fibroblasts senescence in cardiac fibrosis remains unknown. Here, we detected the down-regulation of CGRP concomitant with senescence in fibrotic myocardium, both hypertension- induced left ventricular fibrosis in SHR rats and hypoxia-induced right ventricular fibrosis in pulmonary artery hypertension rats. Exogenous CGRP inhibited the cardiac fibroblasts senesce...
Source: European Journal of Pharmacology - October 20, 2018 Category: Drugs & Pharmacology Authors: Li WQ, Tan SL, Li XH, Sun TL, Li D, Du J, Wei SS, Li YJ, Zhang BK Tags: Eur J Pharmacol Source Type: research

Resveratrol attenuates high fat diet-induced mouse cardiomyopathy through upregulation of estrogen related receptor- α.
Resveratrol attenuates high fat diet-induced mouse cardiomyopathy through upregulation of estrogen related receptor-α. Eur J Pharmacol. 2018 Oct 17;: Authors: Lu Y, Lu X, Wang L, Yang W Abstract Resveratrol reportedly promotes the improvement of cardiac dysfunction and other cardiovascular diseases. Studies demonstrate resveratrol exhibits a set of benefits, including anti-oxidative property, anti-apoptosis and anti-inflammation. However, the molecular mediators of resveratrol-induced cardiac benefits are still not fully disclosed. Present study aims to investigate whether estrogen-related receptor (...
Source: European Journal of Pharmacology - October 17, 2018 Category: Drugs & Pharmacology Authors: Lu Y, Lu X, Wang L, Yang W Tags: Eur J Pharmacol Source Type: research

Isoliquiritigenin-mediated p62/SQSTM1 induction regulates apoptotic potential through attenuation of caspase-8 activation in colorectal cancer cells.
Abstract Isoliquiritigenin (ISL) is a natural flavonoid that exhibits anticancer properties in various carcinoma cell types. However, the precise mechanism responsible for its anticancer activity has not been elucidated fully. In the present study, we examined ISL-mediated apoptotic mechanisms in colorectal cancer (CRC) cells. ISL induced apoptosis in human HCT-116 cells and caused marked induction of p62/SQSTM1 mRNA and protein expression. Similarly, ISL potently inhibited in vivo tumor growth and induced p62/SQSTM1 expression in xenograft tumor tissues. In a p62/SQSTM1 siRNA transfection study, ISL-induced p62/S...
Source: European Journal of Pharmacology - October 16, 2018 Category: Drugs & Pharmacology Authors: Jin H, Seo GS, Lee SH Tags: Eur J Pharmacol Source Type: research

Isoliquiritigenin inhibits mouse S180 tumors with a new mechanism that regulates autophagy by GSK-3 β/TNF-α pathway.
In this study, the pharmacokinetic properties and stability of isoliquiritigenin (ILQ) in microsomes were evaluated. The data showed ILQ administrated by i.h had high absorption degree (absolute bioavailability> 90%), and strong elimination ability (average t1/2≈ 67min). ILQ in rat tissues could reach peak at 0.25h, and be detected in almost all tissues. In vitro, stability of ILQ in four species liver microsomes were rat > beagle dog > monkey > human > mouse. On the basis of pharmacokinetic (PK) profiles, mechanism of ILQ against S180 was explored. ILQ could not inhibit S180 growth directly in vitro. Howe...
Source: European Journal of Pharmacology - August 29, 2018 Category: Drugs & Pharmacology Authors: Yushan R, Ying Y, Yujun T, Jingchun Y, Dongguang L, Lihong P, Pingping W, Lili Z, Fanhui Z, Zhong L, Guimin Z, Jie L Tags: Eur J Pharmacol Source Type: research

Betulinic acid alleviates myocardial hypoxia/reoxygenation injury via inducing Nrf2/HO-1 and inhibiting p38 and JNK pathways.
Abstract Myocardial ischemia reperfusion injury (I/RI) can lead to acute myocardial infarction (MI), which is a common cardiovascular disease (CVD) leading to morbidity and mortality worldwide. Betulinic acid exerts protective effect on myocardial I/RI in rats; however, the mechanism remains unknown. The aim of the current study was to evaluate the effect of betulinic acid on myocardial I/RI in vitro and further investigate the underlying mechanism. Our results showed that betulinic acid increased cell viability and decreased lactate dehydrogenase (LDH) release in H9c2 cells exposed to H/R. Betulinic acid was foun...
Source: European Journal of Pharmacology - August 17, 2018 Category: Drugs & Pharmacology Authors: Wang D, Chen T, Liu F Tags: Eur J Pharmacol Source Type: research

Hepatoprotective effect of rhein against methotrexate-induced liver toxicity.
Abstract The purpose of this study was to investigate the protective effect of rhein, a major metabolite of diacerein, on methotrexate (MTX)-induced hepatotoxicity and clarify the pharmacological mechanism. Rhein significantly reduced the elevation of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) caused by MTX in rat serum and improved liver morphological damage induced by MTX. Moreover, rhein increased the cell survival rate and reduced the number of apoptosis cells in MTX-treated normal human hepatocyte (L02 cells). Rhein treatment in rats up-regulated nuclear factor erythroid 2-related fac...
Source: European Journal of Pharmacology - July 19, 2018 Category: Drugs & Pharmacology Authors: Bu T, Wang C, Meng Q, Huo X, Sun H, Sun P, Zheng S, Ma X, Liu Z, Liu K Tags: Eur J Pharmacol Source Type: research

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