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European Journal of Pharmacology

Yoshifumi Morikawa, Akinobu Shibata, Yasuhide Sasajima, Koichi Suenami, Kiyohito Sato, Yuji Takekoshi, Satoshi Endo, Akira Ikari, Toshiyuki Matsunaga
Sibutramine had been prescribed as an oral anorexiant that reduces dietary intake, but was withdrawn from the market due to frequent occurrence of severe cardiovascular events including hypertension. To elucidate the pathogenic mechanism of hypertension, we here investigated whether sibutramine facilitates damage and contraction of human aortic smooth muscle (HASM) cells or not. Treatment with sibutramine provoked HASM cell apoptosis, which was attributed to production of reactive oxygen species and mitochondria dysfunction...
October 16, 2018: European Journal of Pharmacology
Junkui Wang, Zhiguo Tang, Yong Zhang, Chuan Qiu, Ling Zhu, Na Zhao, Zhongwei Liu
Featured by heart dysfunction, the diabetic cardiomyopathy is causing mortality and morbidity in type 2 diabetes mellitus patients. Matrine was considered as a cardioprotective agent. This study was aimed to investigate the therapeutic effects and molecular mechanisms of matrine on advanced glycation end products (AGEs)- induced cardiac dysfunctions. Rats and isolated primary myocytes were exposed to AGEs. Left ventricular hemodynamic parameters were used to assess the cardiac function. Cell apoptosis was detected with TUNEL assay...
October 16, 2018: European Journal of Pharmacology
Hao Jin, Geom Seog Seo, Sung Hee Lee
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...
October 16, 2018: European Journal of Pharmacology
Regina A Nascimento, José S Possomato-Vieira, Victor H Gonçalves-Rizzi, Gisele F Bonacio, Elen Rizzi, Carlos A Dias-Junior
Preeclampsia is manifested as maternal hypertension and fetal growth restriction. Matrix metalloproteinases (MMPs) are involved in hypertension and doxycycline reduces blood pressure by inhibition of MMPs. Moreover, excessive levels of MMPs and reduced nitric oxide (NO) bioavailability have been related to preeclampsia. We investigated the involvement of MMPs in hypertension in pregnancy induced by Nω-Nitro-L-arginine methyl ester (L-NAME) in rats. To this end, zimography was performed to evaluate the activity of MMPs -2 and -9 in placenta, uterus and thoracic aorta, and systolic blood pressure, feto-placental development and metabolites of NO were evaluated...
October 15, 2018: European Journal of Pharmacology
Charlotte E Pelgrim, Julia D Peterson, Harry R Gosker, Annemie M W J Schols, Ardy van Helvoort, Johan Garssen, Gert Folkerts, Aletta D Kraneveld
COPD is a chronic lung disease characterized by persistent respiratory symptoms and airflow limitation due to airway and/or alveolar abnormalities. Furthermore, COPD is often characterized by extrapulmonary manifestations and comorbidities worsening COPD progression and quality of life. A neglected comorbidity in COPD management is mental health impairment defined by anxiety, depression and cognitive problems. This paper summarizes the evidence for impaired mental health in COPD and focuses on current pharmacological intervention strategies...
October 15, 2018: European Journal of Pharmacology
Ting-Ting Gu, Tian-Yu Chen, Yan-Zi Yang, Xiao-Juan Zhao, Yang Sun, Tu-Shuai Li, Dong-Mei Zhang, Ling-Dong Kong
High dietary fructose is a key causative factor in the development of renal fibrosis. Pterostilbene has anti-fibrotic effect. Understanding the action mechanism of pterostilbene in fructose-induced renal fibrosis remains as a challenge. Here, fructose feeding was found to promote the progress of epithelial-to-mesenchymal transition (EMT) of proximal tubule epithelial cells (PTECs) and collagen deposition in renal cortex of rats with tubulointerstitial fibrosis. Simultaneously, it impaired insulin receptor (IR)/insulin receptor substrate-1 (IRS-1)/protein kinase B (Akt) pathway, and increased transforming growth factor-beta 1 (TGF-β1) and TGF-β type I receptor to enhance phosphorylation of drosophila mothers against decapentaplegic homolog 2 (Smad2) and Smad3, and Smad4 expression in rat kidney cortex...
October 15, 2018: European Journal of Pharmacology
Qing Tang, Ming-Yue Li, Yu-Fei Su, Jia Fu, Zong-Yi Zou, Yi Wang, Shao-Ning Li
Apoptosis of cardiomyocytes and oxidant stress are considered essential processes in the progression of cardiovascular diseases. A hypoxic stress which causes apoptosis of cardiomyocytes is the main problem in ischemic heart disease. The aim of the present study was to explore the functional role and potential mechanisms of miR-223-3p in hypoxia-induced cardiomyocyte apoptosis and oxidative stress. Here, we observed a increment of miR-223-3p level accompanied by the decrease of Krüppel-like zinc-finger transcription factor 15 (KLF15) expression in response to hypoxia...
October 15, 2018: European Journal of Pharmacology
Longhua Guo, Ling Zhao, Pinghong Ming, Ling Hong, Aisheng Liu, Rukai Li
Sumatriptan, a selective serotonin 5-HT1 receptor agonist, is an effective therapeutic for migraine attacks. However, the molecular mechanisms underlying sumatriptan migraine relief are still not fully understood. Here, we found that acid-sensing ion channels (ASICs), pH sensors, are peripheral targets of sumatriptan against migraine. Sumatriptan can inhibit the electrophysiological activity of ASICs in the trigeminal ganglion (TG) neurons. In the present study, sumatriptan decreased proton-gated currents mediated by ASICs in a concentration-dependent manner...
October 15, 2018: European Journal of Pharmacology
Zhen Liu, Rui Li, Cheng Jiang, Sha Zhao, Weishan Li, Xiaobo Tang
To the clinical cognitive impairment following intracerebral hemorrhage, comprehensive neuropsychological assessments and efficacious interventions have rarely been conducted. Lithium chloride, a classical treatment for bipolar disorder, has shown neuroprotective effects through glycogen synthase kinase-3β inhibition in a variety of central nervous system diseases, including stroke. Since neurons that contain glutamate play crucial roles in psychological functions, such as learning and memory, the glutamate-mediated excitotoxicity and consequent neuronal death and cognitive impairment in hippocampus may co-determine the clinical course of intracerebral hemorrhage...
October 15, 2018: European Journal of Pharmacology
Farshad Homayouni Moghadam, Mehrnaz Mesbah-Ardakani, Mohammad Hossein Nasr-Esfahani
Ferulic Acid (FA) is a phenolic compound with anti-apoptotic and anti-oxidative properties. There are reports regarding its neuro-protective, neuro-proliferative and neuro-differentiative effects. However, effect of FA on neuronal differentiation and its effective neuro-protective and neuro-differentiative concentrations are unknown. Also the role of sirtuin molecules in neuroprotective effects of FA were not reported. We used PC12 and mouse neural stem cells (mNSCs) in our experiments. Intact and apoptotic (H2 O2 -exposed) cells were treated with different concentrations of FA, and then they were evaluated by MTT, quantitative real-time RT-PCR and immunostaining assays...
October 14, 2018: European Journal of Pharmacology
Jianbin Su, Meixue Huang
Glaucoma is a common heterogeneous eye disorder that may lead to irreversible blindness. In the present study, we examined whether etidronate, a member of bisphosphonates, may have neuroprotective effects in in vivo and in vitro rat model of glaucoma. In an in vivo setting, chronic ocular hypertension (COH) was induced in adult rat retina. We discovered that systemic injection of etidronate reduced COH-induced retinal oxidative stress, including caspase-3 activity and MDA level, as well as promoted retinal ganglion cell survival...
October 13, 2018: European Journal of Pharmacology
Diego Romário Silva, Janaína de Cássia Orlandi Sardi, Irlan Almeida Freires, Andréa Cristina Barbosa Silva, Pedro Luiz Rosalen
Candida species are opportunistic pathogens which can cause conditions ranging from simple mucocutaneous infections to fungemia and death in immunosuppressed and hospitalized patients. Candida albicans is considered to be the species mostly associated with fungal infections in humans and, therefore, the mostly studied yeast. This microorganism has survival and virulence factors which, allied to a decreased host immunity response, make infection more difficult to control. Today, the current limited antifungal arsenal and a dramatic increase in fungal resistance have driven the need for the synthesis of drugs with novel mechanisms of action...
October 13, 2018: European Journal of Pharmacology
Malavika Srikanth, Wee Siong Chew, Tatsuma Hind, Siew Mon Lim, Nicholas Wei Jie Hay, Jasmine Hui Min Lee, Rich Rivera, Jerold Chun, Wei-Yi Ong, Deron R Herr
Lysophosphatidic acid receptor 1 (LPA1 ) is one of six G protein-coupled receptors (GPCRs) activated by the bioactive lipid, lysophosphatidic acid (LPA). Previous studies have shown that LPA1 signaling plays a major role in the pathophysiology of neuropathic pain. It has also been shown that the inhibition of phospholipase A2 , an enzyme upstream of LPA synthesis, reduces mechanical allodynia in experimental inflammatory orofacial pain. This suggests that the LPA-LPA1 axis may mediate inflammatory pain in addition to its known role in neuropathic pain, but this activity has not been reported...
October 12, 2018: European Journal of Pharmacology
Hao Jin, Hak Sung Kim, Geom Seog Seo, Sung Hee Lee
Chalcone (1,3-diphenyl-2-propen-1-one) derivatives exert anti-cancer activity by targeting key molecules that can lead to carcinogenesis. We synthesized the chalcone derivative 3-phenyl-1-(2,4,6-tris(methoxymethoxy)phenyl)prop-2-yn-1-one (KB-34) and previously reported its anti-inflammatory activity in macrophages. In this study, we examined the anti-metastatic activity of KB-34 against human colorectal cancer (CRC) cells and elucidated its underlying molecular mechanisms. KB-34 treatment significantly inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced migration, as well as the invasion and proliferation of CRC cells (HT-29 and SW620)...
October 12, 2018: European Journal of Pharmacology
Roksana SoukhakLari, Leila Moezi, Fatema Pirsalami, Nahid Ashjazadeh, Maryam Moosavi
The loss of cholinergic neurons has been a major issue in researches on Alzheimer's disease (AD) for about 40 years. Therefore, the scopolamine model of amnesia has been widely used in AD researches. Recently, it was reported that the early stage amnesia of AD is related to memory retrieval deficit. Curcumin, as the main ingredient of turmeric, has been suggested to decrease the prevalence of AD in human population. This study was conducted to assess if curcumin prevents retrieval deficit induced by scopolamine in passive avoidance task...
October 12, 2018: European Journal of Pharmacology
Davood Bashash, Mahda Delshad, Niknam Riyahi, Ava Safaroghli-Azar, Atieh Pourbagheri-Sigaroodi, Majid Momeny
The latest molecular investigations leading to the discovery of the brand-new mechanisms associated to immortalized nature of cancer cells have questioned the efficacy of the conventional therapies and have increased the demand for more influential approaches, especially in the context of synergistic strategies. In an effort to enhance the effectiveness of acute promyelocytic leukemia (APL) treatment and to investigate the potential therapeutic value of Phosphoinositide 3-kinase (PI3K) inhibition synergism with chemotherapy, we designed experiments to evaluate the effect of Arsenic trioxide (ATO) in combination with BKM120 for the treatment of APL-derived NB4 cells...
October 11, 2018: European Journal of Pharmacology
Sirichat Kaowinn, Chutima Kaewpiboon, Ji Eun Kim, Mi Rim Lee, Dae Youn Hwang, Young Whan Choi, Hong Won Kim, Jin Kyoon Park, Kyung-Mo Song, Nam Hyouck Lee, Jin-Soo Maeng, Young-Hwa Chung
Dietary garlic has been suggested to possess anticancer properties, and several attempts have been made to isolate the anticancer compounds. In this study, we efficiently synthesized N-benzyl-N-methyl-dodecan-1-amine (BMDA) by the reductive amination method. We evaluated the potential anticancer activities of BMDA against A549 lung cancer cells with cancer stem cell-like phenotypes due to the overexpression of cancer upregulated gene (CUG)2. N-Benzyl-N-methyl-dodecan-1-amine treatment sensitized A549 cells overexpressing CUG2 (A549-CUG2) to apoptosis and autophagy compared with those of the control cells...
October 1, 2018: European Journal of Pharmacology
Fleur McLeary, Arie Davis, Santosh Rudrawar, Anthony Perkins, Shailendra Anoopkumar-Dukie
This review demonstrates the importance of uncovering the mechanisms that underlie chemotherapy-induced neuroinflammation. It builds upon the well-established connection between chemotherapeutic-agents and neurotoxicity along with widespread peripheral toxicities. This article summarises the major studies which have linked chemotherapy-induced neurodegeneration with direct evidence of neuroinflammation. Cancer and chemotherapy-related adverse effects impact a large proportion of the population. A better understanding of the link between chemotherapy, neurotoxicity and specifically the mechanisms of neuroinflammation, will allow the development of strategies to improve the management of side effects, and overall to reduce the burden on cancer patients receiving chemotherapy...
October 1, 2018: European Journal of Pharmacology
Chen-Li Cheng, Wei-Ting Chao, Yu-Hsuan Li, Yen-Chuan Ou, Shian-Shiang Wang, Kun-Yuan Chiu, Sheau-Yun Yuan
Escin (β-escin) is used as traditional folk medicine. The anti-tumour effects of escin have been demonstrated in vitro in certain cell lines, but its effect on bladder cancer has not been well investigated. In this study, the apoptotic activity of escin dissolved in dimethyl sulfoxide (DMSO) in bladder cancer cells and normal peripheral blood mononuclear cells (PBMC) and SV-HUC1 cells (controls) was determined. Cell cytotoxicity was assessed using the MTT assay. Cell cycle, Reactive oxygen species (ROS) generation, annexin V-FITC staining (for detecting early apoptosis), and changes in mitochondrial membrane potential were evaluated using flow cytometry...
October 1, 2018: European Journal of Pharmacology
Mara Yone Dias Fernandes, Marta Regina Santos do Carmo, Analu Aragão Fonteles, Julliana Catharina de Sousa Neves, Ana Thaís Araújo da Silva, Juliana Fernandes Pereira, Emerson de Oliveira Ferreira, Neila Maria Rocha de Lima, Kelly Rose Tavares Neves, Geanne Matos de Andrade
The pathophysiology of ischemic stroke involves multiple events such as inflammation and oxidative stress which will lead to neuronal death and cognitive deficits. The (-)-α-bisabolol is a monocyclic sesquiterpene alcohol found in various plants and mainly in Matricaria chamomilla, which exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. The aim of this work was to investigate the neuroprotective effects of (-)-α-bisabolol in mice underwent permanent occlusion of the middle cerebral artery (pMCAO)...
October 1, 2018: European Journal of Pharmacology
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