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Specialty: Drugs & Pharmacology
Source: European Journal of Pharmacology

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Total 212 results found since Jan 2013.

Baicalin inhibiting cerebral ischemia /hypoxia-induced neuronal apoptosis via MRTF-A-mediated transactivity.
Abstract Baicalin has been shown to provide the neuroprotective effect by alleviating cerebral ischemia injury. However, little's known about the underlying mechanism. Here, a cerebral artery occlusion (MACO)/reperfusion rat model and rat primary cortical neuron culture exposed to hydrogen peroxide (H2O2) were established to evaluate the effect of baicalin on ischemia-induced neuronal apoptosis. We found baicalin can significantly less neurological deficit and reduced infarct volume in vivo. And it efficiently inhibited neuronal apoptosis in vivo and vitro, which was especially characterized by the enhancing of tr...
Source: European Journal of Pharmacology - October 17, 2015 Category: Drugs & Pharmacology Authors: Zheng WX, Cao XL, Wang F, Wu FJ, Wang J, Ying TZ, Xiao W, Zhang Y, Xing H, Dong W, Xu SQ, Min ZL, Hu XM Tags: Eur J Pharmacol Source Type: research

Thrombin-induced IL-8/CXCL8 release is mediated by CK2, MSK1, and NF-κB pathways in Human lung epithelial cells.
In this study, we further investigated the role of casein kinase 2 (CK2)/mitogen stress-activated protein kinase 1 (MSK1)-dependent p65 phosphorylation in thrombin-induced NF-κB activation and IL-8/CXCL8 release. Thrombin-induced IL-8/CXCL8 release was inhibited by CK2 inhibitors (apigenin and tetrabromobenzotriazole, TBB), small interfering RNA of CK2β (CK2β siRNA), and MSK1 siRNA. Treatment of cells with thrombin caused increases in CK2β phosphorylation at Ser209, which was inhibited by a protein kinase C α (PKCα) inhibitor (Ro-32-0432). Thrombin-induced MSK1 phosphorylation at Ser581 and Akt phosphorylation at Ser...
Source: European Journal of Pharmacology - October 10, 2015 Category: Drugs & Pharmacology Authors: Lin CH, Shih CH, Chen BC Tags: Eur J Pharmacol Source Type: research

Subcellular localization and internalization of the vasopressin V1B receptor.
Abstract Only limited information is available on agonist-dependent changes in the subcellular localization of vasopressin V1B receptors. Our radioligand binding study of membrane preparations and intact cells revealed that a large fraction of the V1B receptor is located in the cytoplasm in unstimulated CHO cells, which is in contrast to the plasma membrane localization of the V1A and V2 receptors. Moreover, when the affinity of radiolabeled arginine-vasopressin ([(3)H]AVP) was compared between membrane preparations and intact cells, the affinity of [(3)H]AVP to the cell surface V1B receptors, but not the V1A rece...
Source: European Journal of Pharmacology - August 26, 2015 Category: Drugs & Pharmacology Authors: Kashiwazaki A, Fujiwara Y, Tsuchiya H, Sakai N, Shibata K, Koshimizu TA Tags: Eur J Pharmacol Source Type: research

Blockade of autophagy enhances proapoptotic potential of BI-69A11, a novel Akt inhibitor, in colon carcinoma.
Abstract BI-69A11, novel Akt inhibitor, is currently drawing much attention due to its intriguing effect in inducing apoptosis in melanoma, breast, prostate and colon cancer. However, earlier reports reveal that PI3K/Akt/ mTOR inhibitors promote autophagy at the early stage as a survival mechanism that might affect its apoptotic potential. It is necessary to investigate whether BI-69A11 mediated apoptosis is associated with autophagy for enhancing its therapeutic efficacy. Here, we found that BI-69A11 induced autophagy at earlier time point through the inhibition of Akt/mTOR/p70S6kinase pathway. Dose-dependent and...
Source: European Journal of Pharmacology - August 22, 2015 Category: Drugs & Pharmacology Authors: Pal I, Parida S, Prashanth Kumar BN, Banik P, Kumar Dey K, Chakraborty S, Bhutia SK, Mandal M Tags: Eur J Pharmacol Source Type: research

A functional tandem between transient receptor potential canonical channels 6 and calcium-dependent chloride channels in Human epithelial cells.
In conclusion, we show that TRPC6 channel is pivotal for the activation of CaCC by guanabenz through a α2-adrenergic-independent pathway in human airway epithelial cells. We suggest propose a functional coupling between TRPC6 and CaCC and guanabenz as a potential TRPC6 activator for exploring TRPC6 and CaCC channel functions and corresponding channelopathies. PMID: 26265544 [PubMed - as supplied by publisher]
Source: European Journal of Pharmacology - August 8, 2015 Category: Drugs & Pharmacology Authors: Bertrand J, Dannhoffer L, Antigny F, Vachel L, Jayle C, Vandebrouck C, Becq F, Norez C Tags: Eur J Pharmacol Source Type: research

Distinct roles of transforming growth factor-β signaling and transforming growth factor-β receptor inhibitor SB431542 in the regulation of p21 expression.
Abstract Transforming growth factor-β (TGF-β) has both tumor suppressive and oncogenic activities. Autocrine TGF-β signaling supports tumor survival and growth in certain types of cancer, and the TGF-β signaling pathway is a potential therapeutic target for these types of cancer. TGF-β induces p21 expression, and p21 is considered as an oncogene as well as a tumor suppressor, due to its anti-apoptotic activity. Thus, we hypothesized that autocrine TGF-β signaling maintains the expression of p21 at levels that can support cell growth. To verify this hypothesis, we sought to examine p21 expression and cell gro...
Source: European Journal of Pharmacology - July 14, 2015 Category: Drugs & Pharmacology Authors: Koo BH, Kim Y, Je Cho Y, Kim DS Tags: Eur J Pharmacol Source Type: research

Modulation of osteoblast differentiation and bone mass by 5-HT2A receptor signaling in mice.
Abstract Recent studies reported that serotonin (5-hydroxytryptamine, 5-HT) may be an endogenous paracrine and/or autocrine factor that is used for intercellular communication in bone cells and between multiple organs regulating bone homeostasis. In the present study, we showed that the administration of MDL11939, a selective 5-HT2A receptor antagonist, reduced bone mass in mice. The loss of bone mass in MDL11939-treated mice was associated with impaired bone formation in vivo, as demonstrated by the lower expression of osterix (Osx) and osteocalcin than that in vehicle-treated mice. On the other hand, no signific...
Source: European Journal of Pharmacology - May 27, 2015 Category: Drugs & Pharmacology Authors: Tanaka K, Hirai T, Ishibashi Y, Izumo N, Togari A Tags: Eur J Pharmacol Source Type: research

Acanthoic acid ameliorates lipopolysaccharide-induced acute lung injury.
In conclusion, our results suggested that the protective effect of acanthoic acid on LPS-induced ALI was due to its ability to activate LXRα, thereby inhibiting LPS-induced inflammatory response. PMID: 25620130 [PubMed - as supplied by publisher]
Source: European Journal of Pharmacology - January 22, 2015 Category: Drugs & Pharmacology Authors: Qiushi W, Guanghua L, Guangquan X Tags: Eur J Pharmacol Source Type: research

Cyclophilin D-mediated apoptosis attributes to sorafenib-induced cytotoxicity in clear cell -renal cell carcinoma.
In conclusion, our results suggested that CypD may represent a new therapeutic target for the treatment of ccRCC. Sorafenib induced apoptosis in ccRCC through CypD upregulation and this effect was related to the inhibition of p-ERK. PMID: 25614335 [PubMed - as supplied by publisher]
Source: European Journal of Pharmacology - January 19, 2015 Category: Drugs & Pharmacology Authors: Hu W, Yuan Q, Liu XH, Zhu HC, Lv SQ, Wang XH Tags: Eur J Pharmacol Source Type: research

Inhibition of P2Y6 receptor-mediated phospholipase C activation and Ca(2+) signalling by prostaglandin E2 in J774 murine macrophages.
In this study, we examined the mechanism of PGE2 inhibitory effects on P2Y6 receptor-mediated function in J774 cells. The P2Y6 receptor agonist UDP induced a sustained elevation of [Ca(2+)]i by stimulating the phospholipase C (PLC) signalling pathway. PGE2 inhibited [Ca(2+)]i elevation and phosphatidylinositol (PI) hydrolysis in a concentration-dependent manner. J774 cells highly expressed the E-type prostanoid 2 (EP2) receptor subtype, a Gs-coupled receptor. PGE2 and a selective EP2 receptor agonist caused cyclic AMP (cAMP) accumulation in J774 cells. The inhibitory effects of PGE2 on P2Y6 receptor-mediated responses were...
Source: European Journal of Pharmacology - January 19, 2015 Category: Drugs & Pharmacology Authors: Ito MA, Matsuoka I Tags: Eur J Pharmacol Source Type: research

Role of eukaryotic translation initiation factor 3a in bleomycin-induced pulmonary fibrosis.
Abstract Eukaryotic translation initiation factor 3a (eIF3a) is a multifunctional protein and plays an important role in regulation of cellular function including proliferation and differentiation. In the present study, we tested the function of eIF3a in pulmonary fibrosis. Pulmonary fibrosis was induced by intratracheal instillation of bleomycin (5mg/kg) in rats. Primary pulmonary fibroblasts were cultured for proliferation investigation by BrdU incorporation method and flow cytometry. The expression/level of eIF3a, TGF-β1, ERK1/2 and α-SMA were analyzed by ELISA, real-time PCR or western blot. Results showed t...
Source: European Journal of Pharmacology - January 12, 2015 Category: Drugs & Pharmacology Authors: Li XW, Wu YH, Li XH, Li D, Du J, Hu CP, Li YJ Tags: Eur J Pharmacol Source Type: research

Aspirin may influence cellular energy status.
Abstract In our previous findings, we have demonstrated that aspirin/acetyl salicylic acid (ASA) might induce sirtuins via aryl hydrocarbon receptor (Ah receptor). Induction effects included an increase in cellular paraoxonase 1 (PON1) activity and apolipoprotein A1 (ApoA1) gene expression. As predicted, ASA and salicylic acid (SA) treatment resulted in generation of H2O2, which is known to be an inducer of mitochondrial gene Sirt4 and other downstream target genes of Sirt1. Our current mass spectroscopic studies further confirm the metabolism of the drugs ASA and SA. Our studies show that HepG2 cells readily conv...
Source: European Journal of Pharmacology - December 31, 2014 Category: Drugs & Pharmacology Authors: Kamble P, Litvinov D, Aluganti Narasimhulu C, Jiang X, Parthasarathy S Tags: Eur J Pharmacol Source Type: research

The inhibition of activated hepatic stellate cells proliferation by arctigenin through G0/G1 phase cell cycle arrest: Persistent p27(Kip1) induction by interfering with PI3K/Akt/FOXO3a signaling pathway.
In this study, we describe that arctigenin (ATG), a major bioactive component of Fructus Arctii, exhibited selective cytotoxic activity via inhibiting platelet-derived growth factor-BB (PDGF-BB)-activated HSCs proliferation and arrested cell cycle at G0/G1 phase, which could not be observed in normal human hepatocytes in vitro. The n-dependent kinase (CDK) 4/6 activities could be strongly inhibited by ATG through down-regulation of cyclin D1 and CDK4/6 expression in early G1 phase arrest. In the ATG-treated HSCs, the expression level of p27(Kip1) and the formation of CDK2-p27(Kip1) complex were also increased. p27(Kip1) si...
Source: European Journal of Pharmacology - December 10, 2014 Category: Drugs & Pharmacology Authors: Li A, Wang J, Wu M, Zhang X, Zhang H Tags: Eur J Pharmacol Source Type: research

Angiotensin II limits NO production by upregulating arginase through a p38 MAPK-ATF-2 pathway.
In this study we explored the signaling pathway leading to increased arginase expression/activity in response to Ang II in bovine aortic endothelial cells (BAEC). Our previous studies indicate involvement of p38 mitogen activated protein kinase (MAPK) in Ang II-induced arginase upregulation and reduced NO production. In this study, we further investigated the Ang II-transcriptional regulation of arginase 1 in endothelial cells. Our results indicate the involvement of ATF-2 transcription factor of the AP1 family in arginase 1 upregulation and in limiting NO production. Using small interfering RNA (siRNA) targeting ATF-2, we...
Source: European Journal of Pharmacology - October 30, 2014 Category: Drugs & Pharmacology Authors: Shatanawi A, Lemtalsi T, Yao L, Patel C, Caldwell RB, Caldwell RW Tags: Eur J Pharmacol Source Type: research

Anesthetic agent propofol inhibits myeloid differentiation factor 88-dependent and independent signaling and mitigates lipopolysaccharide-mediated reactive oxygen species production in human neutrophils in vitro.
This study aimed to investigate the influence of PPF on lipopolysaccharide (LPS)-induced reactive oxygen species production in human neutrophils. We isolated neutrophils from the peripheral blood of 10 healthy male donors. Neither 1µg/ml LPS nor 10-150μmol/L PPF influenced the rate of neutrophil apoptosis, but PPF significantly inhibited LPS-mediated reactive oxygen species production in a dose-dependent manner. PPF inhibited LPS-induced expression of MyD88, tumor necrosis factor receptor-associated factor 6, and TRIF, but not the expression of interferon regulatory factor 3 or phosphorylation of p47(phox), p38-mitogen-a...
Source: European Journal of Pharmacology - October 28, 2014 Category: Drugs & Pharmacology Authors: Ren X, Lv F, Fang B, Liu S, Lv H, He G, Ma H, Cao Y, Wang Y Tags: Eur J Pharmacol Source Type: research