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European Journal of Pharmacology

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https://www.readbyqxmd.com/read/28089921/penehyclidine-hydrochloride-prevents-anoxia-reoxygenation-injury-and-induces-h9c2-cardiomyocyte-apoptosis-via-a-mitochondrial-pathway
#1
Zhaoqi Wang, Duomao Lin, Liang Zhang, Wenjun Liu, Hongbao Tan, Jun Ma
Penehyclidine hydrochloride (PHC) is an anticholinergic drug that has been widely used in the clinic for years, evaluating for anesthetic premedication, anti-muscarinic, or improving microcirculation. However, very little is known about its protective effects against anoxia/reoxygenation (A/R) injury in myocardiocytes. The aim of our study was to investigate the protective effects of PHC pretreatment on A/R injury, as well as the underlying mechanisms involved. To investigate apoptosis, we used the cell viability assay, Annexin-V/PI assay, and lactate dehydrogenase (LDH) and creatine kinase (CK) activity measurements...
January 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28089920/g-protein-coupled-estrogen-receptor-mediated-non-genomic-facilitatory-effect-of-estrogen-on-cooling-induced-reduction-of-skin-blood-flow-in-mice
#2
Izumi Serizawa, Nozomi Iwasaki, Hirotake Ishida, Shin-Ya Saito, Tomohisa Ishikawa
An enhanced vasoconstrictor activity of cutaneous arteries participates in the reduction of skin blood flow induced by cooling stimulation. Raynaud's phenomenon, which is characterized by intense cooling-induced constriction of cutaneous arteries, is more common in women during the period from menarche to menopause. We thus investigated the effect of 17β-estradiol (E2) on cooling-induced reduction of plantar skin blood flow (PSBF) in mouse in vivo. Ovariectomized female ddY mice, anaesthetized with pentobarbital, were treated with tetrodotoxin for eliminating the sympathetic nerve tone and artificially ventilated...
January 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28089919/an-orally-active-geranyl-acetophenone-attenuates-airway-remodeling-in-a-murine-model-of-chronic-asthma
#3
Yu Zhao Lee, Khozirah Shaari, Manraj Singh Cheema, Chau Ling Tham, Mohd Roslan Sulaiman, Daud Ahmad Israf
2,4,6-trihydroxy-3-geranyl acetophenone (tHGA) is a synthetic compound that is naturally found in Melicope ptelefolia. We had previously demonstrated that parenteral administration of tHGA reduces pulmonary inflammation in OVA-sensitized mice. In this study, we evaluated the effect of orally administered tHGA upon airway remodeling in a murine model of chronic asthma. Female BALB/C mice were sensitized intraperitoneally with ovalbumin (OVA) on day 0, 7 and 14, followed by aerosolized 1% OVA 3 times per week for 6 weeks...
January 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28089918/cardiovascular-and-respiratory-activity-of-pk20-opioid-and-neurotensin-hybrid-peptide-in-anesthetized-and-awake-rats
#4
Katarzyna Kaczyńska, Piotr Wojciechowski, Monika Jampolska, Andrzej W Lipkowski, Patrycja Kleczkowska
AIM: Chimeric compound - PK20 despite its therapeutic activity on nociceptive and inflammatory processes may affect respiration and blood pressure. Our objective was to evaluate influence of the hybrid composed of endomorphin-2 and neurotensin fragments on ventilation, heart rate and blood pressure in anesthetized and awake rats. METHODS: The effects of PK20 (1mg/kg) were studied either after its intravenous administration in anesthetized rats or intraperitoneal injection in awake state...
January 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28088387/sirt2-mediated-antitumour-effects-of-shikonin-on-metastatic-colorectal-cancer
#5
Li-Li Zhang, Lin Zhan, Yong-Dong Jin, Zhen-Li Min, Can Wei, Qiang Wang, Ya-Jun Chen, Qing-Ming Wu, Xia-Min Hu, Qiong Yuan
SIRT2 is involved in the development of a variety of cancers. Shikonin is a natural compound that is known to have antitumour effects. This study aims to assess the effects of shikonin on the development and metastatic progression of colorectal cancer (CRC) through regulation of SIRT2 expression and whether this effect is related to the phosphorylation of extracellular signal-regulated kinases (ERKs). The results demonstrated that SIRT2 is downregulated in CRC biopsy samples (n = 31) compared with the adjacent non-cancerous tissues (ANCT, n = 26)...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28088386/trypsin-induces-biphasic-muscle-contraction-and-relaxation-via-transient-receptor-potential-vanilloid-1-and-neurokinin-receptors-1-2-in-porcine-esophageal-body
#6
Bai Xiaopeng, Yoshimasa Tanaka, Eikichi Ihara, Katsuya Hirano, Kayoko Nakano, Mayumi Hirano, Yoshinao Oda, Kazuhiko Nakamura
Duodenal reflux of fluids containing trypsin relates to refractory gastroesophageal reflux disease (GERD). Esophageal peristalsis and clearance are important factors in GERD pathogenesis. However, the function of trypsin in esophageal body contractility is not fully understood. In this study, effects of trypsin on circular smooth muscle (CSM) and longitudinal smooth muscle (LSM) of the porcine esophageal body were examined. Trypsin elicited a concentration dependent biphasic response, a major contraction and a subsequent relaxation only in CSM...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28088385/flavonoid-derivative-fla-cn-inhibited-adipocyte-differentiation-via-activating-ampk-and-up-regulating-microrna-27-in-3t3-l1-cells
#7
Chun-Chun Gan, Tian-Wen Ni, Yang Yu, Nan Qin, Ying Chen, Mei-Na Jin, Hong-Quan Duan
Fla-CN (3-O-[(E)-4-(4-cyanophenyl)-2-oxobut-3-en-1-yl] kaempferol) is a semi-synthesized flavonoid derivative of tiliroside which exhibited anti-diabetic effect in vivo. Our previous study revealed the role of Fla-CN in anti-obesity and anti-diabetes in vivo, but the underlying mechanism remained to be addressed. The present study aimed to investigate the mechanism of anti-adipogenesis in vitro. Fla-CN markedly inhibited intracellular lipid accumulation in a dose-dependent manner, and the inhibitory effect was mainly limited to the early stage of adipocyte differentiation in vitro...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28088384/the-signalling-mechanisms-of-a-novel-mitochondrial-complex-i-inhibitor-prevent-lipid-accumulation-and-attenuate-tnf-%C3%AE-induced-insulin-resistance-in-vitro
#8
Siobhán Leonard, Laura M Tobin, John B C Findlay
RTC-1 has recently been identified as a member of a new class of anti-diabetic compounds acting through the inhibition of complex I of the mitochondrial respiratory chain (NADH:ubiquinone oxidoreductase) to improve glucose handling and inhibit weight gain in mice fed a high-fat diet (HFD). The exact mechanism by which the reduced activity of NADH:ubiquinone oxidoreductase, in response to RTC-1, promotes these improved metabolic parameters remains to be established. Through extensive in vitro analysis, new molecular insights into these downstream signalling pathways have been obtained...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28088383/evaluating-the-role-of-astrocytes-on-%C3%AE-estradiol-effect-on-seizures-of-pilocarpine-epileptic-model
#9
Masoumeh Sarfi, Mahmoud Elahdadi Salmani, Iran Goudarzi, Taghi Lashkar Boluki, Kataneh Abrari
Epilepsy with periodic and unpredictable seizures is associated with hippocampal glutamate toxicity and tissue reorganization. Astrocytes play an important role in mediating the neuroprotective effects of estradiol and reducing seizure severity. Accordingly, the protective effects of low and high doses of estradiol on behavioral, astrocytic involvement and neuronal survival aspects of Pilocarpine-induced epilepsy were investigated. Lithium- Pilocarpine (30mg/kg) model was used to provoke epilepsy. Βeta-estradiol (2,40μg/ µl) was injected subcutaneously from 48 before to 48h after seizure induction...
January 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28087255/unknown-face-of-known-drugs-what-else-can-we-expect-from-angiotensin-converting-enzyme-inhibitors
#10
REVIEW
Anna Wzgarda, Robert Kleszcz, Monika Prokop, Katarzyna Regulska, Milosz Regulski, Jaroslaw Paluszczak, Beata J Stanisz
The renin-angiotensin system (RAS) is one of important systems among homeostatic mechanisms that controls the function of cardiovascular, renal and adrenal systems. As RAS has a very complex nature, it has been also found as related to the control of cell migration and apoptosis. Angiotensin-converting enzyme inhibitors (ACEI) are drugs most commonly used in the modulation of RAS activity. ACEI have been extensively described as effective in the treatment of hypertension among adults, but also as drugs delaying progression in diabetic nephropathy and reducing mortality in left ventricular dysfunction and congestive heart failure...
January 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28087254/anti-diabetic-drug-metformin-dilates-retinal-blood-vessels-through-activation-of-amp-activated-protein-kinase-in-rats
#11
Asami Mori, Eriko Ishikawa, Tomoyo Amano, Kenji Sakamoto, Tsutomu Nakahara
The aim of this study was to examine whether metformin, a biguanide anti-hyperglycemic drug, dilates retinal blood vessels in rats. Ocular fundus images were captured with an original high-resolution digital fundus camera in vivo and diameters of retinal blood vessels were measured. Both systemic blood pressure and heart rate were continuously recorded. Metformin (0.01-0.3mg/kg/min) increased diameters of retinal blood vessels in a dose-dependent manner. This retinal vasodilator effect of metformin was abolished by compound C, an inhibitor of AMP-activated protein kinase (AMPK), and N(G)-nitro-L-arginine methyl ester, an inhibitor of nitric oxide (NO) synthase...
January 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28057491/mefloquine-inhibits-voltage-dependent-nav1-4-channel-by-overlapping-the-local-anaesthetic-binding-site
#12
Bertin Paiz-Candia, Angel A Islas, Alfredo Sánchez-Solano, Claudia Mancilla-Simbro, Thomas Scior, Lourdes Millan-PerezPeña, Eduardo M Salinas-Stefanon
Mefloquine constitutes a multitarget antimalaric that inhibits cation currents. However, the effect and the binding site of this compound on Na(+) channels is unknown. To address the mechanism of action of mefloquine, we employed two-electrode voltage clamp recordings on Xenopus laevis oocytes, site-directed mutagenesis of the rat Na(+) channel, and a combined in silico approach using Molecular Dynamics and docking protocols. We found that mefloquine: i) inhibited Nav1.4 currents (IC50 =60μM), ii) significantly delayed fast inactivation but did not affect recovery from inactivation, iii) markedly the shifted steady-state inactivation curve to more hyperpolarized potentials...
January 3, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28057490/blockade-of-patch-based-%C3%AE-opioid-receptors-in-the-striatum-attenuates-methamphetamine-induced-conditioned-place-preference-and-reduces-activation-of-the-patch-compartment
#13
Kristen A Horner, Mary Caroline Logan, Trevor J Fisher, Jordan B Logue
The behavioral effects of methamphetamine (METH) are mediated by the striatum, which is divided into the patch compartment, which mediates limbic and reward functions, and the matrix compartment, which mediates sensorimotor tasks. METH treatment results in repetitive behavior that is related to enhanced relative activation of the patch versus the matrix compartment. The patch, but not the matrix compartment contains a high density of μ opioid receptors, and localized blockade of patch-based μ opioid receptors attenuates METH-induced patch-enhanced activity and repetitive behaviors...
January 3, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28024945/mc37-a-new-mono-carbonyl-curcumin-analog-induces-g2-m-cell-cycle-arrest-and-mitochondria-mediated-apoptosis-in-human-colorectal-cancer-cells
#14
Baoxia Liang, Ziyi Liu, Yingnan Cao, Cuige Zhu, Yinglin Zuo, Lei Huang, Gesi Wen, Nana Shang, Yu Chen, Xin Yue, Jun Du, Baojian Li, Binhua Zhou, Xianzhang Bu
(E)-1-(3'-fluoro-[1,1'-biphenyl-3-yl)-3-(3-hydroxy-4-methoxyphenyl)prop-2-en-1-one) (MC37), a novel mono-carbonyl curcumin analog, was previously synthesized in our laboratory as a nuclear factor kappa B (NF-κB) inhibitor with excellent cytotoxicity against several cancer cell lines. In this study, our further investigations showed that the potent growth inhibitory activity of MC37 in human colorectal cancer cells was associated with the arrest of cell cycle progression and the induction of apoptosis. As a multi-targeted agent, MC37 inhibited the intracellular microtubule assembly, altered the expression of cyclin-dependent kinase 1 (CDK1), and ultimately induced G2/M cell cycle arrest...
December 23, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28017829/12-chloracetyl-ppd-a-novel-dammarane-derivative-shows-anti-cancer-activity-via-delay-the-progression-of-cell-cycle-g2-m-phase-and-reactive-oxygen-species-mediate-cell-apoptosis
#15
Xu De Wang, Yuan Yuan Sun, Chen Zhao, Fan Zhi Qu, Yu Qing Zhao
(20R)-Dammarane-3β, 12β, 20, 25-tetrol (25-OH-PPD) is a ginsenoside isolated from Panax ginseng (C. A. Meyer). This compound exhibits anti-cancer activities on many human cancer cell lines. In this study, we investigated anti-cancer mechanisms of 12β-O-(L-Chloracetyl)-dammar-20(22)-ene-3β,25-diol(12-Chloracetyl-PPD), a modified 25-OH-PPD. We found that compound 12-Chloracetyl-PPD resulted in a concentration-dependent inhibition of viability in prostate, breast, and gastric cancer cells, without affecting the viability of normal cell (human gastric epithelial cell line-GES-1, hair follicle dermal papilla cell line-HHDPC and rat myocardial cell line-H9C2)...
December 22, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28017828/effect-of-dezocine-on-il-12-and-il-10-secretion-and-lymphocyte-activation-by-culturing-dendritic-cells-from-human-umbilical-cord-blood
#16
Chang Feng, Man Feng, Ran Jiao, Dongyi Liu, Yanwu Jin, Xin Zhao, Ruixue Xiao
Dezocine has been generally utilized for pain therapy and auxiliary anesthesia. Although it has some advantages on the prevention of some anesthesia related complications, its effect on immune responses remains unclear. Our study investigated the effects of Dezocine on IL-10 and IL-12 secretion and lymphocytes activation by culturing dendritic cells (DCs), and revealed the underlying mechanism. Mononuclear cells were divided into negative control group (GN), positive control group (GP), experimental group (GD; GD5, D7, D9)...
December 22, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28012974/the-surge-of-flavonoids-as-novel-fine-regulators-of-cardiovascular-cav-channels
#17
REVIEW
Fabio Fusi, Ottavia Spiga, Alfonso Trezza, Giampietro Sgaragli, Simona Saponara
Ion channels underlie a wide variety of physiological processes that involve rapid changes in cell dynamics, such as cardiac and vascular smooth muscle contraction. Overexpression or dysfunction of these membrane proteins are the basis of many cardiovascular diseases that represent the leading cause of morbidity and mortality for human beings. In the last few years, flavonoids, widely distributed in the plant kingdom, have attracted the interest of many laboratories as an emerging class of fine ion, in particular Cav, channels modulators...
December 22, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28012971/effects-of-a-human-recombinant-alkaline-phosphatase-during-impaired-mitochondrial-function-in-human-renal-proximal-tubule-epithelial-cells
#18
Esther Peters, Tom Schirris, Alexander H van Asbeck, Jelle Gerretsen, Jennifer Eymael, Angel Ashikov, Merel J W Adjobo-Hermans, Frans Russel, Peter Pickkers, Rosalinde Masereeuw
Sepsis-associated acute kidney injury is a multifactorial syndrome in which inflammation and renal microcirculatory dysfunction play a profound role. Subsequently, renal tubule mitochondria reprioritize cellular functions to prevent further damage. Here, we investigated the putative protective effects of human recombinant alkaline phosphatase (recAP) during inhibition of mitochondrial respiration in conditionally immortalized human proximal tubule epithelial cells (ciPTEC). Full inhibition of mitochondrial oxygen consumption was obtained after 24h antimycin A treatment, which did not affect cell viability...
December 22, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28012973/methotrexate-prevents-epidural-fibrosis-through-endoplasmic-reticulum-stress-signalling-pathway
#19
Hui Chen, Lianqi Yan, Jingcheng Wang, Yu Sun, Xiaolei Li, Shuai Zhao, Daxin Wang, Gengyao Zhu, Yuan Liang
Lumbar laminectomy is one of the most common treatments for lumbar disc herniation and other lumbar disorders with serious complications, such as failed back surgery syndrome, mainly caused by epidural fibrosis (EF). The developing fibrosis causes radicular pain after the laminectomy or discectomy. Methotrexate (MTX) is a folic acid antagonist that has shown anti-proliferative effects in previous studies. The aim of our experiment is to study whether MTX has positive effects on the outcome of the laminectomy in rats...
December 21, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28012972/a-novel-peptide-9r-p201-strongly-inhibits-the-viability-proliferation-and-migration-of-liver-cancer-hepg2-cells-and-induces-apoptosis-by-down-regulation-of-foxm1-expression
#20
Zhenfei Bi, Wenrong Liu, Ruofang Ding, Yiran Wu, Rongkun Dou, Wenwen Zhang, Xue Yuan, Xinrong Liu, Lili Xiong, Zhiyun Guo, Canquan Mao
Overexpression of FoxM1 was closely related to the proliferation, metastasis, chemo-resistance and poor prognosis of various cancers. FoxM1 was regarded as the Achilles' heel of cancer and a potential target for anti-cancer drug discovery. We previously obtained several high affinity peptides from the phage random library against the DNA binding domain of FoxM1c (FoxM1c-DBD) protein. Here in this paper, we found that 9R-P201, one of the novel peptides, showed stronger inhibition to HepG2 cancer cells than those of DU145, HUVEC and L-02 cells with an IC50 of 43...
December 21, 2016: European Journal of Pharmacology
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