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European Journal of Pharmacology

Qinghong Zhou, Ruoyu Luo, Xiaohong Zhou, Jun Wang, Fang Chen
Cervical cancer (CC) is the fourth most frequent malignancy worldwide. MicroRNAs (miRNAs) can function as potential biomarkers or therapeutic targets in multiple cancers including CC. Our present study aimed to investigate the roles and downstream targets of microRNA-20a (miR-20a) in regulating CC proliferation, apoptosis and autophagy. Here, RT-qPCR assay revealed that miR-20a was highly expressed in CC tissues and cells. Functional analysis showed that the inhibition of miR-20a resulted in reduced proliferation, increased apoptosis and downregulated autophagic activity in CC cells...
December 1, 2018: European Journal of Pharmacology
Li-Li Gong, Song Yang, He Liu, Wen Zhang, Lu-Lu Ren, Fei-Fei Han, Ya-Li Lv, Zi-Rui Wan, Li-Hong Liu
Akebia saponin D, which is originates from Dipsacus asper Wall, has been used as a tonic, an analgesic and anti-inflammatory agent for the therapy of low back pain, rheumatic arthritis, traumatic hematoma, habitual abortion and bone fractures in traditional Chinese medicine. However, the anti-nociceptive and anti-inflammatory activity and mechanism of Akebia saponin D has been rarely reported. The aim of this study was to investigate the anti-nociceptive and anti-inflammatory activity of Akebia saponin D and to assess its possible mechanism...
November 30, 2018: European Journal of Pharmacology
Hitomi Sasamori, Yu Ohmura, Takayuki Yoshida, Mitsuhiro Yoshioka
Higher impulsivity is a risk factor for criminal involvement, substance abuse, and suicide. However, only a few drugs are clinically available for the treatment of deficient impulse control. We recently proposed a strategy for identifying potential drugs to treat such disorders by investigating clinically available drugs that increase extracellular dopamine levels in the medial prefrontal cortex and stimulate dopamine D1 -like receptors without increasing extracellular dopamine levels in the ventral striatum...
November 29, 2018: European Journal of Pharmacology
Zhoufan Xie, Ziyan Guo, Jiachuan Lei, Jianqing Yu
Platinum resistance is a major limitation in the treatment of ovarian cancer. Combination of natural compounds with platinum-based agents is a new strategy for cancer chemotherapy. Recently, we found that scutellarin sensitized the anticancer effect of cisplatin to ovarian cancer cells. How scutellarin interacts with cisplatin and sensitizes its effect is unclear. Here, we found that the combination treatment of scutellarin and cisplatin enhanced apoptosis in ovarian cancer cells via increasing the extent of platinum-DNA adducts and the ratio of Bax/Bcl-2...
November 29, 2018: European Journal of Pharmacology
Silin Gan, Ping Ma, Jie Ma, Weimin Wang, Haohao Han, Li Chen, Xue Li, Feifei Wu, Hui Sun
Leukemia is the most frequent malignancy in children with acute myeloid leukemia (AML) as the second commonest type. Long non-coding RNA zinc finger antisense 1 (ZFAS1) has been widely reported as an oncogenic factor in multiple malignancies including AML. However, the roles and molecular mechanisms of ZFAS1 in the tumorigenesis of AML are poor defined till now. In the present study, RT-qPCR assay showed that ZFAS1 was highly expressed in bone marrow of acute leukemia patients and AML cell lines. Loss-of-function analyses revealed that ZFAS1 knockdown inhibited proliferation and promoted apoptosis in AML cells and curbed AML xenograft growth in vivo...
November 28, 2018: European Journal of Pharmacology
Zhai Li, Jia Yulei, Ji Yaqing, Zou Jinmin, Liu Xinyong, Gao Jing, Liu Min
The aim of our study was to investigate the effects of a new synthetic compound (E) -1- (E) -1- (2- hydroxy -5- chlorophenyl) -3- (3, 5, 6- three methyl pyrazine -2- based) -2- propylene -1 ketone, Z-11, a tetramethylpyrazine analogue, on cerebral ischemia reperfusion injury and the underlying mechanism. 240~260g adult male Wistar rats were subjected to middle cerebral artery occlusion for 2h, followed by 22h of reperfusion. Z-11 (1.7, 3.4 and 6.8mg/kg, i.p.), Edaravone (3mg/kg, i.p.) and DMSO (1‰, i.p.) was administered at 2h after the onset of ischemia...
November 28, 2018: European Journal of Pharmacology
Min Jung Lee, Jun-Hwan Moon, Hyung Keun Lee, Chong Hwan Cho, Sung Hak Choi, Weon-Bin Im
Several antimuscarinics have been commonly used for overactive bladder patients, but dry mouth as a major anticholinergic side effect remains a shortcoming to limit long-term use. The aim of this study was to elucidate the pharmacological properties of DA-8010, a novel muscarinic receptor antagonist selective for urinary bladder over salivary gland. DA-8010 exhibited a high binding affinity for human muscarinic M3 receptor with pKi of 8.81 ± 0.05 and great potencies for human M3 receptor and rat bladder preparation...
November 28, 2018: European Journal of Pharmacology
Surabhi Chandra, David J R Fulton, Ruth B Caldwell, R William Caldwell, Haroldo A Toque
Diabetes-induced vascular endothelial dysfunction has been reported to involve hyperglycemia-induced increases in arginase activity. However, upstream mediators of this effect are not clear. Here, we have tested involvement of Rho kinase, ERK1/2 and p38 MAPK pathways in this process. Studies were performed with aortas isolated from wild type or hemizygous arginase 1 knockout (Arg1+/- ) mice and bovine aortic endothelial cells exposed to high glucose (HG, 25mmol/l) or normal glucose (NG, 5.5mmol/l) conditions for different times...
November 28, 2018: European Journal of Pharmacology
Dan Wang, Xing Xu, Yue Wu, Yong Lin, Minhui Gao, Peili Hu, Dongjian Chen, Xu Lu, Zhuo Chen, Hui Wang, Chao Huang
This study was designed to examine the potency of SMIP004, an inhibitor of S-phase kinase-associated protein 2 (Skp2), to exert antidepressant-like properties in mouse models following acute or chronic administration to C57BL6/J mice. To this end, the tail suspension test (TST), forced swim test (FST), and sucrose preference test (SPT) were utilized and the antidepressant-like activity of SMIP004 at different concentrations or time points in mice with or without chronic unpredictable stress (CUS) treatment were evaluated...
November 28, 2018: European Journal of Pharmacology
Xin Zhao, Fang Shu, Xiaoqiang Wang, Fang Wang, Li Wu, Lu Li, Haigang Lv
Excessive exposure to commonly used anesthetic agents, such as ketamine, may induce permanent damage to immature human brains. In this work, we used a human embryonic stem cell (hESC)-derived neuron model to assess the expression and function of human microRNA 735 (hsa-miR-375) in regulating ketamine-induced neural cell death and neural toxicity in vitro. In the in vitro culture, hESC-derived neurons were incubated with ketamine for 72h. After that, cell viability, reactive oxygen species activity, neural apoptosis, neurite degeneration, and hsa-miR-375 gene expression were assessed, respectively...
November 27, 2018: European Journal of Pharmacology
H S Nandini, Prakash Ramachandra Naik
Diabetes mellitus is the most common endocrine disorder characterized by hyperglycemia resulting from defects in insulin secretion or insulin action. The present study was designed to investigate the antidiabetic effects of vincamine, one of the monoterpenoid indole alkaloid, in streptozotocin-induced diabetic rat model. Diabetes was induced in rats by an intraperitoneal injection of streptozotocin (40mg/kg bw). Vincamine 20 and 30mg/ were administrated orally as a single dose per day to the diabetic rats for 30 days...
November 26, 2018: European Journal of Pharmacology
Lei Wang, Jian Cheng, Zhen Hua, Mingming Liu, Haiyan Xu, Yong Ma, Guicheng Huang, Guoqing Mao
α-melanocyte stimulating hormone (α-MSH) is a member of the melanocortin family, that has displayed important biological functions in diverse cells and tissues. The purpose of this study is to test the effect of α-MSH on the differentiation and mineralization of osteoblast cells. The expression of the α-MSH membrane receptor MC1R but not MC2R, MC3R, or MC4R increased distinctively during the osteogenic differentiation from 3, 7 to 14 d. Treatment with α-MSH promoted the differentiation and mineralization of MC3T3-E1 cells by increasing the activity of ALP, enhancing Alizarin Red S staining, and stimulating the expression of osteogenic genes, including ALP1, osteocalcin (Bglap2), and osterix (Sp7)...
November 26, 2018: European Journal of Pharmacology
Xiaoming Fa, Junyan Tao, Yulin Zhou, Yunhe Hou, Yiyu Wang, Danshan Gu, Yanmei Su, Yanping Jiang, Shude Li
Insulin resistance is a major pathophysiological feature in the development of type 2 diabetes. The liver is an important organ responsible for the development of insulin resistance, and exploring liver glucose metabolism is important to study insulin resistance. We first established the model of insulin resistance in HepG2 cells and then treated them with different concentrations of ginsenoside-Rg1. The results showed that ginsenoside-Rg1 is not toxic to HepG2 cells. In addition, ginsenoside-Rg1 relieved the insulin-induced insulin resistance in HepG2 cells...
November 25, 2018: European Journal of Pharmacology
Francieli Vuolo, Soraia C Abreu, Monique Michels, Débora G Xisto, Natália G Blanco, Jaime Ec Hallak, Antonio W Zuardi, José A Crippa, Cardine Reis, Marina Bahl, Emílio Pizzichinni, Rosemeri Maurici, Marcia M M Pizzichinni, Patricia R M Rocco, Felipe Dal-Pizzol
Asthma is characterized by chronic lung inflammation and airway hyperresponsiveness. Asthma remains a major public health problem and, at present, there are no effective interventions capable of reversing airway remodelling. Cannabidiol (CBD) is known to exert immunomodulatory effects through the activation of cannabinoid-1 and -2 (CB1 and CB2 ) receptors located in the central nervous system and immune cells, respectively. However, as the role of CBD on airway remodelling and the mechanisms of CB1 and CB2 aren't fully elucidated, this study was designed to evaluate the effects of cannabidiol in this scenario...
November 24, 2018: European Journal of Pharmacology
Ke Zhang, Jianqiu Liu, Cuilin Li, Xiaowei Peng, Hui Li, Zhi Li
Thyroid cancer (TC) is one of the most common endocrine malignancies, and the incidence of TC has almost tripled over the past three decades. This increase may partially own to overdiagnosis and approximately 15% to 30% of cytological indeterminate thyroid nodules cannot be evaluated by means of fine-needle aspiration. The present study aimed to identify potential crucial genes of PTC and provide new sights into improving the diagnosis of thyroid lesions for future study. We adopted an integrated analysis of Gene expression profiles of PTC patients and adjacent normal controls and data from The Cancer Genome Atlas databases (TCGA)...
November 22, 2018: European Journal of Pharmacology
Yan Cheng, Qing Chang, Bo Zheng, Jing Xu, Hongsong Li, Ruoxin Wang
Accumulating evidence demonstrated that abnormal expression of long non-coding RNAs (lncRNAs) was closely associated with cancer development including retinoblastoma (RB). LncRNA X inactive specific transcript (XIST) has been found to function as an oncogene or a tumor suppressor in several cancers. However, the role and underlying mechanism of XIST in RB have not been clarified. The expression of XIST, microRNA (miR)-101, zinc finger E-box binding homeobox (ZEB) 1, and ZEB2 was detected in human RB tissues and cell lines...
November 22, 2018: European Journal of Pharmacology
Haruna Sasaki-Iwaoka, Katsunari Taguchi, Yohei Okada, Emiko Imamura, Satoshi Kubo, Shigetada Furukawa, Tatsuaki Morokata
Interleukin (IL)-23 is thought to be critical in the pathogenesis of psoriasis, and anti-IL-23 monoclonal antibodies (mAbs) have been approved for the treatment of psoriasis. We speculated that an anti-IL-23 receptor mAb might have greater efficacy than an anti-IL-23 mAb in the treatment of local inflamed lesions with high IL-23 levels. We previously generated an anti-human IL-23 receptor mAb, AS2762900-00, which potently blocked IL-23-induced cell proliferation, regardless of the concentration of IL-23. Here, we evaluated the therapeutic potential of AS2762900-00 in the treatment of psoriasis...
November 22, 2018: European Journal of Pharmacology
Yong Li, Daorong Hou, Xuguan Chen, Jingfeng Zhu, Ruyi Zhang, Wei Sun, Peng Li, Yunfan Tian, Xiangqing Kong
In this study, we investigated whether hydralazine could reduce renal ischemia and reperfusion (I/R) injury in rats. Renal I/R was induced by a 70-min occlusion of the bilateral renal arteries and a 24-h reperfusion, which was confirmed by the increased the mortality, the levels of blood urea nitrogen (BUN), blood creatinine (Cr), renal tissue NO and the visible histological damage of the kidneys. Apoptosis was evaluated by terminal deoxynucleotidyltransferase-mediated dUTP nick-end labeling (TUNEL) staining...
November 22, 2018: European Journal of Pharmacology
Daili Chen, Xiaofei Qi, Renkun Zhuang, Jun Cao, Yang Xu, Xiaolei Huang, Yuantao Li
The impacts of prenatal propofol on cognition and emotion of offspring remain elusive. In the present study, pregnant rats in the second trimester were anesthetized with propofol. Neuronal apoptosis and proliferation was determined in fetuses and postnatal rats by detecting caspase-3 and BrdU expression. The offspring were subjected to several behavior tests. Then the pyramidal neurons in hippocampus and the expression of NR1, NR2A, and NR2B subunits of NMDA receptor and PSD-95 in frontal cortex were examined...
November 22, 2018: European Journal of Pharmacology
Weijie Liang, Taibing Fan, Lin Liu, Lianzhong Zhang
Endothelial cells injury and autophagy dysfunction play vital roles in the development of atherosclerosis. Long noncoding RNAs (lncRNAs) have been identified to participate in the pathogenesis of atherosclerosis. However, it remains largely undefined whether lncRNA growth-arrest specific transcript 5 (GAS5) could influence ox-LDL-induced autophagy dysfunction in endothelial cells. The expression levels of GAS5 and miR-26a were detected in the plasma samples of patients with atherosclerosis and oxidized low-density lipoprotein (ox-LDL)-treated human aortic endothelial cells (HAECs) by quantitative real-time PCR (qRT-PCR)...
November 20, 2018: European Journal of Pharmacology
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