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European Journal of Pharmacology

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https://www.readbyqxmd.com/read/28821452/pinocembrin-a-novel-histidine-decarboxylase-inhibitor-with-anti-allergic-potential-in-in-vitro
#1
Hamza Hanieh, Villianur Ibrahim Hairul Islam, Subramanian Saravanan, Muthiah Chellappandian, Kessavane Ragul, Arumugam Durga, Kaliyamoorthy Venugopal, Venugopal Senthilkumar, Palanisamy Senthilkumar, Krishnaraj Thirugnanasambantham
Pinocembrin (5, 7- dihydroxy flavanone) is the most abundant chiral flavonoid found in propolis, exhibiting antioxidant, antimicrobial and anti-inflammatory properties. However, the effect of Pinocembrin on allergic response is unexplored. Thus, current study aimed at investigating the effects of Pinocembrin on IgE-mediated allergic response in vitro. A special emphasis was directed toward histidine decarboxylase (HDC) and other pro-allergic and pro-inflammatory mediators. Preliminary studies, using a microbiological model of Klebsiella pneumoniae, provided first evidences that suggest Pinocembrin as a potential thermal stable inhibitor for HDC...
August 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28821451/5-ht7-receptor-antagonism-sb-269970-attenuates-bleomycin-induced-pulmonary-fibrosis-in-rats-via-downregulating-oxidative-burden-and-inflammatory-cascades-and-ameliorating-collagen-deposition-comparison-to-terguride
#2
Mona K Tawfik, Samy Makary
The neurotransmitter 5-hydroxytryptamine (5-HT) is involved in regulation of local tissue inflammation and repair through a set of receptors (5-HT1-7 receptors), which are expressed in the lung. Considering the protective importance of 5-HT receptor antagonists against development of pulmonary fibrosis, we evaluated whether 5-HT7 receptor antagonist (SB-269970) modulates lung inflammatory and fibrogenic processes in comparison with 5-HT2A/B receptor antagonist (terguride), in bleomycin (BLM)-induced idiopathic pulmonary fibrosis (IPF) model...
August 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28821450/carvedilol-abrogates-hypoxia-induced-oxidative-stress-and-neuroinflammation-in-microglial-bv2-cells
#3
Xiujuan Gao, Bin Wu, Zhijian Fu, Zongwang Zhang, Guangjun Xu
Microglia initially undergo rapid activation in response to injury and stressful stimuli, such as hypoxia. Oxidative stress and the inflammatory response play critical roles in hypoxic-ischemic brain injury. Carvedilol is a β-blocker used to treat high blood pressure and heart failure. In this study, we investigated whether carvedilol had a protective effect against hypoxia-induced oxidative stress and inflammation in microglial BV2 cells. Our results indicate that hypoxic exposure significantly reduced mean cell viability of BV2 microglia, which was significantly restored by carvedilol (10 and 50μM)...
August 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28811128/a-newly-synthesized-ligustrazine-stilbene-derivative-inhibits-pdgf-bb-induced-vascular-smooth-muscle-cell-phenotypic-switch-and-proliferation-via-delaying-cell-cycle-progression
#4
Chunlian Peng, Siming Zhang, Haixin Liu, Yanxiao Jiao, Guifa Su, Yan Zhu
Vascular Smooth muscle cells (VSMCs) possess remarkable phenotype plasticity that allows it to rapidly adapt to fluctuating environmental cues, including the period of development and progression of vascular diseases such as atherosclerosis and restenosis subsequent to vein grafting or coronary intervention. Although VSMC phenotypic switch is an attractive target, there is no effective drug so far. Using rat aortic VSMCs, we investigate the effects of Ligustrazine and its synthetic derivatives on platelet-derived growth factor-BB (PDGF-BB) induced proliferation and phenotypic switch by a cell image-based screening of 60 Ligustrazine stilbene derivatives...
August 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28811127/attenuation-of-sunitinib-induced-cardiotoxicity-through-the-a3-adenosine-receptor-activation
#5
Hardip Sandhu, Samantha Cooper, Afthab Hussain, Christopher Mee, Helen Maddock
Sunitinib is an anti-cancer tyrosine kinase inhibitor associated with severe cardiotoxic adverse effects. Using rat Langendorff heart model and human acute myeloid leukemia 60 (HL60) cell line we detected the involvement of protein kinase C (PKC) α during Sunitinib-induced cardiotoxicity and the effect of Sunitinib on cancer progression. The cardioprotective and anti-cancer properties of the A3 adenosine receptor agonist 2-chloro-N6-(3-iodobenzyl)-adenosine-5'-N-methyluronamide (IB-MECA) were investigated...
August 12, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28802717/chronic-d609-treatment-interferes-with-cell-cycle-and-targets-the-expression-of-olig2-in-glioma-stem-like-cells
#6
Haviryaji S G Kalluri, John S Kuo, Robert J Dempsey
Glioma Stem-like Cells (GSCs) isolated from patient derived tumors have high metabolic activity and survive in the absence of exogenous growth factors. We recently demonstrated that acute D609 (Tricyclodecan-9-yl-xanthogenate), a PC-PLC inhibitor with anti-oxidative property, can decrease the ATP content & GADD45β protein in GSCs cultured without growth factors, but not in the presence of growth factors. In this study we examined the effect of chronic D609 treatment on GSCs cultured in complete medium containing growth factors...
August 10, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28802718/curcumin-ameliorates-cardiac-dysfunction-induced-by-mechanical-trauma
#7
Xintao Li, Tingting Cao, Shuo Ma, Zehao Jing, Yue Bi, Jicheng Zhou, Chong Chen, Deqin Yu, Liang Zhu, Shuzhuang Li
Curcumin, a phytochemical component derived from turmeric (Carcuma longa), has been extensively investigated because of its anti-inflammatory and anti-oxidative properties. Inflammation and oxidative stress play critical roles in posttraumatic cardiomyocyte apoptosis, which contributes to secondary cardiac dysfunction. This research was designed to identify the protective effect of curcumin on posttraumatic cardiac dysfunction and investigate its underlying mechanism. Noble-Collip drum was used to prepare a mechanical trauma (MT) model of rats, and the hemodynamic responses of traumatised rats were observed by ventricular intubation 12h after trauma...
August 9, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28800884/ionic-mechanisms-of-the-action-of-anaesthetics-on-sinoatrial-node-automaticity
#8
REVIEW
Akiko Kojima, Hiroshi Matsuura
Although various general anaesthetics affect the heart rate in clinical settings, their precise mechanisms remain to be fully elucidated. Because the heart rate is determined by automaticity of the cardiac pacemaker sinoatrial node and its regulation by autonomic nervous system, it is important to clarify the effect of anaesthetics on sinoatrial node automaticity. The spontaneous electrical activity of sinoatrial node is generated by a complex but coordinated interaction of multiple ionic currents, such as the hyperpolarisation-activated cation current (If), T-type and L-type Ca(2+) currents (ICa,T and ICa,L), Na(+)/Ca(2+) exchange current (INCX), and rapidly and slowly activating delayed rectifier K(+) currents (IKr and IKs)...
August 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28800883/gene-expression-profiling-and-pathway-network-analysis-of-anti-tumor-activity-by-jaridon-6-in-esophageal-cancer
#9
Ling Fu, Yu-Qing Wang, Bing-Kai Han, Xiao-Rui Li, Xiao-Jing Shi, Fen Yin, Jun-Wei Wang, Pei-Rong Zhao, Yu Ke, Hong-Min Liu
Jaridon 6, a novel ent-kaurene diterpenoid derived from Rabdosia rubescens (Hemsl.) Hara, possesses strong anti-tumor activity in esophageal cancer cells. In this study, we explored the underlying molecular events of the anti-tumor activity of Jaridon 6. Cell viability and apoptosis results obtained by flow cytometry confirmed the tumor inhibitory effect of Jaridon 6 in esophageal cancer cells. A cDNA microarray was performed and the observations were validated using quantitative reverse transcription polymerase chain reaction...
August 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28800882/salvianolic-acid-b-inhibits-intermittent-high-glucose-induced-ins-1-cell-apoptosis-through-regulation-of-bcl-2-proteins-and-mitochondrial-membrane-potential
#10
Shanjun Tao, Younan Ren, Haowen Zheng, Mengqiu Zhao, Xu Zhang, Yuanmei Zhu, Jieren Yang, Shuguo Zheng
Blood glucose fluctuations, also referred to as intermittent high glucose, have been validated to be more harmful than sustained high glucose in exacerbating pancreatic dysfunction by inducing β cell apoptosis. Salvianolic acid B (Sal B), an aqueous component of Salvia miltiorrhiza, has been proved beneficial to pancreatic islet function in diabetes, but the underlying mechanisms remain to be elucidated. The present study investigated the protective effect of Sal B on INS-1 cells exposed to intermittent high glucose and the possible mechanisms implicated...
August 8, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28789934/targeting-calpains-a-novel-immunomodulatory-approach-for-microbial-infections
#11
REVIEW
Vijay Kumar, Ahmad Ali
Calpains are a family of Ca(2+) dependent cytosolic non-lysosomal proteases with well conserved cysteine-rich domains for enzymatic activity. Due to their functional dependency on Ca(2+) concentrations, they are involved in various cellular processes that are regulated by intracellular ca(2+) concentration (i.e. embryo development, cell development and migration, maintenance of cellular architecture and structure etc.). Calpains are widely studied proteases in mammalian (i.e. mouse and human) physiology and pathophysiology due to their ubiquitous presence...
August 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28780058/endothelial-nitric-oxide-synthase-and-cyclooxygenase-are-activated-by-hydrogen-peroxide-in-renal-hypertensive-rat-aorta
#12
B R Silva, L Pernomian, T D De Paula, M D Grando, L M Bendhack
In this work, we hypothesized that cyclooxygenase (COX) activity can be regulated by nitric oxide (NO) and hydrogen peroxide (H2O2). In the renal hypertension (2K-1C), phenylephrine (PE)-induced contraction was lower than in normotensive (2K) rat aortas. This impaired contraction is due to NO/H2O2- induced vasodilation. We evaluated the effects of H2O2 on the activity of COX and endothelial NO-Synthase (eNOS) in 2K-1C rat aortas stimulated with PE. Responses for PE or H2O2 were evaluated in 2K-1C and 2K rat aortas, without or with inhibitors for COX (Indomethacin) or eNOS (L-NAME)...
August 2, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28768146/diosmin-prevents-left-ventricular-hypertrophy-adenosine-triphosphatases-dysfunction-and-electrolyte-imbalance-in-experimentally-induced-myocardial-infarcted-rats
#13
Sharmila Queenthy Sabarimuthu, Stanely Mainzen Prince Ponnian, Babu John
Currently, there has been an increased interest globally to identify natural compounds that are pharmacologically potent and have low or no adverse effects for use in preventive medicine. Myocardial infarction is a vital pathological feature resulting in high levels of mortality and morbidity. Left ventricular hypertrophy (LVH), adenosine triphosphatases (ATPases) dysfunction and electrolyte imbalance play a vital role in the pathogenesis of myocardial infarction. This study aims to evaluate the preventive effects of diosmin on LVH, ATPases dysfunction and electrolyte imbalance in isoproterenol induced myocardial infarcted rats...
July 30, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28757324/silicon-containing-ibuprofen-derivatives-with-antioxidant-and-anti-inflammatory-activities-an-in-vivo-and-in-silico-study
#14
David J Pérez, M Irene Díaz-Reval, Fernando Obledo-Benicio, Uzma I Zakai, Zeferino Gómez-Sandoval, Rodrigo Said Razo-Hernández, Robert West, María Teresa Sumaya-Martínez, Kayim Pineda-Urbina, Ángel Ramos-Organillo
There are many chronic diseases related with inflammation. The chronic inflammation can produce other problems as cancer. Therefore, it is necessary to design drugs with better anti-inflammatory activity than those in the clinic. Likewise, these could be used in chronic treatments with minimum adverse effects. The amide or ester functionality in combination with the insertion of a silyl alkyl moiety is able to improve some drug properties. In this context, the evaluation of a group of silicon containing ibuprofen derivatives (SCIDs) as antioxidants and anti-inflammatory agents is reported...
July 28, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28755986/investigating-the-involvement-of-glycogen-synthase-kinase-3%C3%AE-and-gap-junction-signaling-in-trpv1-and-remote-hind-preconditioning-induced-cardioprotection
#15
Puneet Kaur Randhawa, Amteshwar Singh Jaggi
Remote ischemic preconditioning (RIPC) is the phenomenon that harnesses the body's endogenous protective mechanisms against prolonged ischemia-reperfusion-induced injury. The present study aimed to explore the involvement of glycogen synthase kinase-3β and gap junction signaling in TRPV1 and remote hind preconditioning-induced cardioprotection. In the present study, four consecutive cycles (5min of ischemia-reperfusion) of remote hind limb preconditioning stimulus were delivered using a blood pressure cuff fastened at the inguinal level of the rat...
July 27, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28755985/peripheral-and-central-sites-of-action-for-anti-allodynic-activity-induced-by-the-bifunctional-opioid-npff-receptors-agonist-bn-9-in-inflammatory-pain-model
#16
Run Zhang, Biao Xu, Meng-Na Zhang, Ting Zhang, Zi-Long Wang, Geng Zhao, Guang-Hai Zhao, Ning Li, Quan Fang, Rui Wang
The activation of opioid and neuropeptide FF (NPFF) receptors plays important roles to modulate nociceptive signal in inflammatory pain states. Recently, BN-9 (Tyr-D.Ala-Gly-Phe-Gln-Pro-Gln-Arg-Phe-NH2) was pharmacologically characterized as a novel bifunctional agonist at both opioid and NPFF receptors. In the present study, the anti-allodynic activity and site(s) of action of BN-9 were assessed in a mouse model of carrageenan-induced inflammatory pain. In mice, BN-9 induced a dose-dependent anti-allodinic effect through opioid receptor at supraspinal or spinal level, and this effect was augmented by pretreatment with the NPFF receptor antagonist at the same level...
July 26, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28755984/penehyclidine-hydrochloride-preconditioning-provides-cardiac-protection-in-a-rat-model-of-myocardial-ischemia-reperfusion-injury-via-the-mechanism-of-mitochondrial-dynamics-mechanism
#17
Yanli Yang, Liyun Zhao, Jun Ma
To investigate that penehyclidine hydrochloride (PHC) plays a cardiac protection role in myocardial ischemia/reperfusion injury (IRI) through mitochondrial dynamics mechanism. Rat model of myocardial I/R injury was established by the ligation of left anterior descending coronary artery for 30min followed by 3h perfusion. Before I/R, the rats were pretreated with or without PHC. Cardiac function was measured by echocardiography. The activities/levels of myocardial enzymes, oxidants and antioxidant enzymes were detected...
July 26, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28754379/%C3%AE-2-adrenoceptor-induced-modulation-of-transglutaminase-2-transamidase-activity-in-cardiomyoblasts
#18
Falguni S Vyas, Carl P Nelson, Fiona Freeman, David J Boocock, Alan J Hargreaves, John M Dickenson
Tissue transglutaminase 2 (TG2) is modulated by protein kinase A (PKA) mediated phosphorylation: however, the precise mechanism(s) of its modulation by G-protein coupled receptors coupled to PKA activation are not fully understood. In the current study we investigated the potential regulation of TG2 activity by the β2-adrenoceptor in rat H9c2 cardiomyoblasts. Transglutaminase transamidation activity was assessed using amine-incorporating and protein cross-linking assays. TG2 phosphorylation was determined via immunoprecipitation and Western blotting...
July 25, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28743391/valporic-acid-enhances-the-atrial-natriuretic-peptide-anp-mediated-anti-hypertrophic-activity-by-modulating-the-npr1-gene-transcription-in-h9c2-cells-in-vitro
#19
Senthamizharasi Manivasagam, Tamilselvi Velusamy, Boopathi Sowndharajan, Navvi Chandrasekar, Suresh Dhanusu, Elangovan Vellaichamy
The present study was aimed to determine whether stimulating Npr1 gene activity using Valporic acid (VA), a small short chain fatty acid molecule can enhance ANP mediated anti-hypertrophic activity in isoproterenol (ISO) - treated H9c2 cells in vitro. H9c2 cells were treated with ISO (10(-5) M) and co-treated with VA (10(-5) M) in the presence and absence of ANP (10(-8)M), for 48h. ATRA (10(-5) M) was used as a positive inducer of Npr1 gene transcription. The mRNA expression of Npr1 and PKG-I genes, proto-oncogenes (c-fos, c-jun and c-myc) and hypertrophic markers (ANP, BNP, α-sk and β-MyHC), genes were determined by quantitative PCR (qPCR)...
July 22, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28743390/baicalin-attenuates-in-vivo-and-in-vitro-hyperglycemia-exacerbated-ischemia-reperfusion-injury-by-regulating-mitochondrial-function-in-a-manner-dependent-on-ampk
#20
Shanshan Li, Xiaoxu Sun, Lixing Xu, Ruoxi Sun, Zhanqiang Ma, Xueyang Deng, Baolin Liu, Qiang Fu, Rong Qu, Shiping Ma
Cerebral ischemia/reperfusion (I/R) is a lethal and disabling disease. Studies have suggested that hyperglycemia is a risk factor for cerebral I/R. Baicalin is a natural bioactive flavonoid extracted from Scutellaria baicalensis Georgi with neuroprotective activity. In the present study, we investigated the effects of baicalin on hyperglycemia-exacerbated cerebral I/R injury. Streptozotocin (STZ) injection aggravated the brain damage induced by middle cerebral artery occlusion (MCAO) surgery, while baicalin administration reduced blood glucose, relieved neurological deficit and decreased infarct volume...
July 22, 2017: European Journal of Pharmacology
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