Use of microminipigs for unveiling unknown mechanisms of azithromycin-induced cardiovascular death
We examined electropharmacological effects of azithromycin in intravenous doses of 0.3, 3 and 30 mg/kg using microminipigs under the halothane anesthesia (n=4), which provided plasma concentrations of 3.1, 11.2 and 120.4 μg/mL, respectively. The low dose did not alter any of the cardiohemodynamic or electrocardiographic variables. The middle dose significantly shortened QT interval for 10-20 min and QTc for 10-30 min. The high dose significantly decreased mean blood pressure for 5-60 min, prolonged QRS width at 20 min, but shortened QT interval for 15-20 min and QTc for 15-30 min (n=3). Cardiohemodynamic collapse occurr...
Source: Journal of Pharmacological Sciences - October 18, 2018 Category: Drugs & Pharmacology Source Type: research

Maslinic acid protects against pressure overload-induced cardiac hypertrophy in mice
In conclusion, we found that MA protected against cardiac hypertrophy. MA has the potential to become a therapeutic drug for cardiac hypertrophy. (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - October 15, 2018 Category: Drugs & Pharmacology Source Type: research

Anti-angiogenic effects of valproic acid in a mouse model of oxygen-induced retinopathy
Publication date: Available online 14 October 2018Source: Journal of Pharmacological SciencesAuthor(s): Naoto Iizuka, Akane Morita, Chihiro Kawano, Asami Mori, Kenji Sakamoto, Masakazu Kuroyama, Kunio Ishii, Tsutomu NakaharaAbstractPathological retinal angiogenesis contributes to the pathogenesis of several ocular diseases. Valproic acid, a widely used antiepileptic drug, exerts anti-angiogenic effects by inhibiting histone deacetylase (HDAC). Herein, we investigated the effects of valproic acid and vorinostat, a HDAC inhibitor, on pathological retinal angiogenesis in mice with oxygen-induced retinopathy (OIR). OIR was ind...
Source: Journal of Pharmacological Sciences - October 15, 2018 Category: Drugs & Pharmacology Source Type: research

Dual effect of polyphosphate on mineralization of rat osteoblast ROS17/2.8 cells in a dose-dependent manner
Publication date: Available online 13 October 2018Source: Journal of Pharmacological SciencesAuthor(s): Yoshikazu Mikami, Daisuke Omagari, Yusuke Mizutani, Manabu Hayatsu, Tatsuo Ushiki, Hiromasa TsudaAbstractInorganic polyphosphate (polyP), a linear polymer of orthophosphate, is found at high concentrations in osteoblasts. We demonstrated the effects of various polyP concentrations on the mineralization of rat osteoblast ROS17/2.8 cells. Mineralization of ROS17/2.8 was induced by a high polyP concentration (1 mg/mL), which was accompanied by an upregulation of the bone sialoprotein and osteocalcin. In contrast, a low poly...
Source: Journal of Pharmacological Sciences - October 14, 2018 Category: Drugs & Pharmacology Source Type: research

Involvement of 5-HT2A receptor hyperfunction in the anxiety-like behavior induced by doxorubicin and cyclophosphamide combination treatment in rats
We examined whether combination treatment with doxorubicin and cyclophosphamide, a traditional chemotherapy for breast cancer, induced anxiety-like behavior in rats. Furthermore, we evaluated the role of the serotonin (5-HT)2A receptor subtype in the anxiety-like behavior induced by such chemotherapy. Rats were intraperitoneally injected with doxorubicin and cyclophosphamide once a week for 2 weeks. This caused the rats to display anxiety-like behavior during the light-dark test. In addition, we examined the rats’ 5-HT2A receptor-mediated behavioral responses. Combination treatment with doxorubicin and cyclophosphami...
Source: Journal of Pharmacological Sciences - October 10, 2018 Category: Drugs & Pharmacology Source Type: research

A Rho-kinase inhibitor reverses learning and memory deficits in a Rat model of chronic cerebral ischemia by altering Bcl-2/Bax-NMDAR signaling in the cerebral cortex
Publication date: Available online 22 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Ming Ni, Jigang Zhang, Lin Huang, Gaolin Liu, Qin LiAbstractThe current study investigated whether a Rho-kinase inhibitor alleviated impairments in a rat model of chronic cerebral ischemia and examined the specific pathological mechanisms by which Rho-kinase impacts neuronal damage and cognitive dysfunction. Adult Sprague–Dawley rats underwent permanent bilateral carotid artery occlusion (BCAO) to establish our chronic cerebral ischemia model. Chronic Y27632 administration reversed the abnormal behaviors of BCAO-...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Na+, K+-ATPase inhibition induces neuronal cell death in rat hippocampal slice cultures: Association with GLAST and glial cell abnormalities
Publication date: Available online 22 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Yuki Kurauchi, Kazuki Noma, Akinori Hisatsune, Takahiro Seki, Hiroshi KatsukiAbstractNa+, K+-ATPase is a highly expressed membrane protein. Dysfunction of Na+, K+-ATPase has been implicated in the pathophysiology of several neurodegenerative and psychiatric disorders, however, the underlying mechanism of neuronal cell death resulting from Na+, K+-ATPase dysfunction is poorly understood. Here, we investigated the mechanism of neurotoxicity due to Na+, K+-ATPase inhibition using rat organotypic hippocampal slice cultures...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Relationship between the fluorescence intensity of rhodamine-labeled orexin A and the calcium responses in cortical neurons: An in vivo two-photon calcium imaging study
Publication date: Available online 22 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Saori Ohtani, Satoshi Fujita, Koki Hasegawa, Hiromasa Tsuda, Morio Tonogi, Masayuki KobayashiAbstractNeural responses to a ligand vary widely between neurons; however, the mechanisms underlying this variation remain unclear. One possible mechanism is a variation in the number of receptors expressed in each neural membrane. Here, we synthesized a rhodamine-labeled orexin A compound, enabling us to quantify the amount of orexin binding to its receptors, OX1 and OX2, which principally couple to the Gq/11 protein. The rhod...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Interleukin-6 induced by YAP in hepatocellular carcinoma cells recruits tumor-associated macrophages
Publication date: Available online 22 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Tian-yi Zhou, Yu-lu Zhou, Mei-jia Qian, Yi-zheng Fang, Song Ye, Wen-xiu Xin, Xiao-chun Yang, Hong-hai WuAbstractTumor-associated macrophages (TAMs) has been regarded as the most prominent component in tumor microenvironment. The correlation between TAM density and poor prognosis in Hepatocellular carcinoma (HCC) patients suggests a supportive role for TAMs in tumor progression. Here we employed a co-culture system to interrogate the molecular link between Yes-Associated Protein (YAP) and TAMs chemotaxis in HCC cells. W...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Anti-tumor activity of Escherichia coli Shiga toxin A subunit delivered by SF9 insect cells
In conclusion, this method can be used as a safe alternative for anticancer drug delivery inside cancer cells. (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Resolvin E3 attenuates lipopolysaccharide-induced depression-like behavior in mice
Publication date: Available online 26 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Satoshi Deyama, Kento Shimoda, Hiroyuki Ikeda, Hayato Fukuda, Satoshi Shuto, Masabumi MinamiAbstractEicosapentaenoic acid (EPA)-derived resolvin E1 (RvE1) and E2 (RvE2) have antidepressant effects. Here, we investigated the antidepressant effects of resolvin E3 (RvE3) in a mouse model of lipopolysaccharide (LPS)-induced depression. We observed that LPS (0.8 mg/kg, i.p.) significantly increased immobility time on the tail suspension test, and this depression-like behavior was dose-dependently attenuated by intracer...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Mogroside IIIE attenuates gestational diabetes mellitus through activating of AMPK signaling pathway in mice
Publication date: Available online 26 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Cuili Zou, Qiaoqin Zhang, Shenghong ZhangAbstractAs one kind of complications of pregnancy, gestational diabetes mellitus (GDM) can influence the health of maternal-child in clinical practice. The C57 BL/KsJdb/+(db/+) mice, genetic GDM model, and C57 BL/KsJ+/+ (wild-type) mice were purchased and classified into three groups: normal pregnancy (C57 BL/KsJ+/+), GDM (C57 BL/KsJdb/+), and GDM plus Mogroside IIIE (20.0 mg/kg) group. GDM symptoms (maternal body weight, serum glucose, and insulin levels), glucose and insulin t...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Prolonged stimulation of β2-adrenergic receptor with β2-agonists impairs insulin actions in H9c2 cells
In this study, we demonstrate that chronic treatment with salbutamol, salmeterol, and formoterol inhibited insulin-induced glucose uptake and GLUT4 synthesis in H9c2 myoblast cells. Sustained β2AR stimulation also attenuated GLUT4 translocation to the plasma membrane, whereas short-term stimulation had no effect. In HBSM cells, prolonged treatment with β2-agonists had no effect on insulin-induced glucose uptake and did not alter insulin-induced expressions of GLUT1, GLUT4, and GLUT10. In addition, genetic polymorphisms at amino acid position 16 and 27 of β2AR are linked to insulin resistance by significant s...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Effects of Derinat on ischemia-reperfusion-induced pressure ulcer mouse model
Publication date: Available online 27 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Jiadai Liu, Elena G. Rybakina, Eelena A. Korneva, Mami NodaAbstractSodium salt of deoxyribonucleic acid (DNA), Derinat, isolated from the soft roes of Russian sturgeon, has been utilized as an immunomodulator for the treatment of reactive oxygen species (ROS)-associated diseases in clinics. Here we show that treatment with Derinat has an anti-inflammatory and anti-oxidative effects on cutaneous ischemia-reperfusion (IR) injury in pressure ulcer (PU) model mice. Dorsal skin damage and dermal edema in mild PU model mice ...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

A delta opioid receptor agonist, KNT-127, in the prelimbic medial prefrontal cortex attenuates glial glutamate transporter blocker-induced anxiety-like behavior in mice
Publication date: Available online 27 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Akiyoshi Saitoh, Akinobu Soda, Shuhei Kayashima, Kazumi Yoshizawa, Jun-Ichiro Oka, Hiroshi Nagase, Mitsuhiko YamadaAbstractWe previously reported that systemic administration of a delta opioid receptor (DOP) agonist, KNT-127, produced a potent anxiolytic-like effect in rats. Interestingly, DOPs are highly distributed in the prelimbic medial prefrontal cortex (PL-PFC). In the present study, we investigated the effect of KNT-127 co-perfusion in the PL-PFC on anxiety-like behavior in mice, induced by a glial glutamate tra...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Artesunate enhances radiosensitivity of esophageal cancer cells by inhibiting the repair of DNA damage
Publication date: Available online 29 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Zhenhua Fei, Wenyue Gu, Raoying Xie, Huafang Su, Yiyan JiangAbstractRadiotherapy plays an important therapeutic role in esophageal cancer (EC). However, acquired radioresistance impairs the efficacy of radiotherapy, often leading to treatment failure. Therefore, it is important to develop novel radiosensitizers to enhance the clinical treatment of EC. The purpose of this study was to investigate the role of artesunate (ART) on radiosensitivity of human EC cell line TE-1. We found that ART inhibited the proliferation of...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Lipid-modulate activity of Cichorium glandulosum Boiss.et Huet polysaccharide in nonalcoholic fatty liver disease larval zebrafish model
In this study, extraction and purification of CG polysaccharides (CGP) was performed, and the lipid regulation effect of CGP was investigated on NAFLD zebrafish model. The results showed that CGP significantly decreased the levels of TC, TG, and decreased the mRNA expression of srebf-1, and fas, increased the expression of pparab. The findings suggest that the lipid-lowering effects of CGP mainly depend on facilitation of lipolysis (mainly beta-oxidation) or inhibition of lipogenesis. Furthermore, CGP could prevent and causes the regression of steatosis in NAFLD via its lipid metabolism regulation effect. (Source: Journal ...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

Improved endogenous epoxyeicosatrienoic acid production mends heart function via increased PGC 1α-mitochondrial functions in metabolic syndrome
Publication date: Available online 4 October 2018Source: Journal of Pharmacological SciencesAuthor(s): Lu Liu, Xin Huang, Jinliao Gao, Yusong Guo, Yanqi Di, Shasha Sun, Xinli Deng, Jian CaoAbstractMetabolic syndrome (MS) is a combination of symptoms characterized by central obesity, hypertension, hyperglycemia, and hyperlipidemia, which together increase the risk of heart disease, stroke and diabetes. In our study, we hypothesized that an EET-agonist (AUDA) would increase expression of PGC 1α and improve mitochondrial and endothelial functions, resulting in improved heart function in a rat model of MS. To investigate...
Source: Journal of Pharmacological Sciences - October 5, 2018 Category: Drugs & Pharmacology Source Type: research

FM1-Editorial Board
Publication date: August 2018Source: Journal of Pharmacological Sciences, Volume 137, Issue 4Author(s): (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - September 20, 2018 Category: Drugs & Pharmacology Source Type: research

FM3-Aims & Scope
Publication date: August 2018Source: Journal of Pharmacological Sciences, Volume 137, Issue 4Author(s): (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - September 20, 2018 Category: Drugs & Pharmacology Source Type: research

Administration of cinnamaldehyde promotes osteogenesis in ovariectomized rats and differentiation of osteoblast in vitro
Publication date: Available online 11 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Zongyi Wu, Sheji Weng, Deyi Yan, Zhongjie Xie, Qiang Zhou, Hang Li, Bingli Bai, Viraj Boodhun, Zijian Shen, Jiahao Tang, Lingling Zhou, Zhoushan Tao, Lei YangAbstractTo explore the effect of cinnamaldehyde on the distal femur in ovariectomized rats and its influence on osteoblast in vitro.Female Sprague-Dawley rats which underwent either bilateral ovariectomy or sham operation were divided into five groups randomly:group OVX(OVX,N=10) and group sham(SHAM,N=10) received normal saline(NS) by gavage at a dose of 50 ml/Kg&...
Source: Journal of Pharmacological Sciences - September 12, 2018 Category: Drugs & Pharmacology Source Type: research

Effects of irradiation with narrowband-ultraviolet B on up-regulation of histamine H1 receptor mRNA and induction of apoptosis in HeLa cells and nasal mucosa of rats
Publication date: Available online 10 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Tatsuya Fujii, Yoshiaki Kitamura, Hiroyuki Mizuguchi, Kentaro Okamoto, Nanae Sanada, Takuya Yamada, Manabu Sugiyama, Shotaro Michinaga, Mika Kitayama, Hiroyuki Fukui, Noriaki TakedaAbstractNarrowband-ultraviolet B (NB-UVB) phototherapy is used for the treatment of atopic dermatitis. Previously, we reported that irradiation with 200 mJ/cm2 of 310 nm NB-UVB suppressed phorbol-12-myristate-13-acetate (PMA)-induced up-regulation of histamine H1 receptor (H1R) gene expression without induction of apoptosis in HeLa cells. Ho...
Source: Journal of Pharmacological Sciences - September 10, 2018 Category: Drugs & Pharmacology Source Type: research

Probing the benzofuroquinolinium derivative as a potent antibacterial agent through the inhibition of FtsZ activity
Publication date: Available online 10 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Ning Sun, Li Ban, Ming Li, Zhiyuan Fang, Xiaomei Li, Wenxia Yao, Jinghui Pan, Yujing Lu, Zhihua Liu, Wing-Leung WongAbstractA benzofuroquinolinium derivative that exhibits excellent cell division inhibitory effect was discovered through cell-based screening approach. This compound possesses potent antimicrobial activity against both Gram-positive and Gram-negative bacteria including the drug-resistant strains. In addition, this compound is able to restore MRSA susceptibility to beta-lactam antibiotics. The biochemical ...
Source: Journal of Pharmacological Sciences - September 10, 2018 Category: Drugs & Pharmacology Source Type: research

Icariside II attenuates cardiac remodeling via AMPKα2/mTORC1 in vivo and in vitro
Publication date: Available online 4 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Xiao-Yu Liu, Hai-han Liao, Hong Feng, Nan Zhang, Jing-jing Yang, Wen-jing Li, Si Chen, Wei Deng, Qi-Zhu TangAbstractIcariside II (ICA II), a flavonoid derived from Epimediumbrevicormum Maxin in, has multiple biological activities in Chinese traditional medicine. Our study aimed to investigate the potential activity of ICA II against cardiac remodeling and the underlying mechanism. Mice received aorta banding (AB) or sham surgery, and then were randomly divided into ICA II or vehicle (veh) group for 6 weeks. After echoca...
Source: Journal of Pharmacological Sciences - September 9, 2018 Category: Drugs & Pharmacology Source Type: research

Polydatin alleviated alcoholic liver injury in zebrafish larvae through ameliorating lipid metabolism and oxidative stress
In conclusion, polydatin may improve the liver function of zebrafish with acute alcoholic liver injury through attenuating hepatic fat accumulation, ameliorating lipid and ethanol metabolism and reducing oxidative stress and DNA damage.Graphical abstract (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - September 8, 2018 Category: Drugs & Pharmacology Source Type: research

Inhibitory effect of the gut microbial linoleic acid metabolites, 10-oxo-trans-11-octadecenoic acid and 10-hydroxy-cis-12-octadecenoic acid, on BV-2 microglial cell activation
In this study, we aimed to investigate the effects of these fatty acids on lipopolysaccharide (LPS)-induced inflammatory processes in mouse microglial cells (BV-2 cells). KetoC and HYA inhibited LPS-induced nitric oxide (NO) production and suppressed the expression of inducible NO synthase in BV-2 cells. NO changes in these inhibitory effects were observed with AH7614, a G-protein coupled receptor 120 antagonist, or the peroxisome proliferator-activated receptors antagonists, GW6471 and GW9662. In addition, KetoC and HYA did not inhibit translocation of p65, a subunit of NF-κB, or IκB degradation. Similarly, no...
Source: Journal of Pharmacological Sciences - September 6, 2018 Category: Drugs & Pharmacology Source Type: research

Icariside II attenuates cardiac remodeling via AMPKα2/mTORC1 in vivo and in vitro
Publication date: Available online 4 September 2018Source: Journal of Pharmacological SciencesAuthor(s): Xiao-Yu Liu, Hai-han Liao, Hong Feng, Nan Zhang, Yang Jing-jing, Wen-jing Li, Si Chen, Wei Deng, Qi-Zhu TangAbstractIcariside II (ICA II), a flavonoid derived from Epimediumbrevicormum Maxinin, has multiple biological activities in Chinese traditional medicine. Our study aimed to investigate the potential activity of ICA II against cardiac remodeling and the underlying mechanism. Mice received aorta banding (AB) or sham surgery, and then were randomly divided into ICA II or vehicle (veh) group for 6 weeks. After echocar...
Source: Journal of Pharmacological Sciences - September 5, 2018 Category: Drugs & Pharmacology Source Type: research

Butyrate suppresses abnormal proliferation in colonic epithelial cells under diabetic state by targeting HMGB1
Publication date: Available online 31 August 2018Source: Journal of Pharmacological SciencesAuthor(s): Si-Yi Wang, Jie-Yao Li, Ji-Hao Xu, Zhong-Sheng Xia, Di Cheng, Wa Zhong, Yu Lai, Tao Yu, Qi-Kui ChenAbstractButyrate is widely accepted as a proliferation inhibitor in colon cancer but less thoroughly characterized in the colonic epithelium of objects with type 2 diabetes mellitus. The present study investigated the regulatory effect of butyrate on proliferation, the related molecule high-mobility group box 1 (HMGB1) and the receptor for advanced glycation end products (RAGE) in the colon of db/db type 2 diabetic model mic...
Source: Journal of Pharmacological Sciences - September 1, 2018 Category: Drugs & Pharmacology Source Type: research

C-terminal Site-specific PEGylated Exendin-4 Analog: A Long-Acting Glucagon Like Peptide-1 Receptor Agonist, on Glycemic Control and Beta Cell Function in Diabetic db/db Mice
Publication date: Available online 31 August 2018Source: Journal of Pharmacological SciencesAuthor(s): Daoqi Tang, Hong Tian, Jicheng Wu, Jiaxiao Cheng, Cheng Luo, Wenbo Sai, Xiaoda Song, Xiangdong Gao, Wenbing YaoAbstractPEG modification is a common clinical strategy for prolonging the half-life of therapeutic proteins or polypeptides. In a previous work, we have successfully synthesized PEG-modified Exendin-4 (PE) by conjugating a 20 kDa PEG to the C-terminal of Exendin-4. Then, we introduced an integrative characterization for PE to evaluate its hypoglycemic activity and pharmacokinetic properties. The normoglycemic eff...
Source: Journal of Pharmacological Sciences - September 1, 2018 Category: Drugs & Pharmacology Source Type: research

Neuroprotective effects of pramipexole transdermal patch in the MPTP-induced mouse model of Parkinson's disease
In conclusion, our studies demonstrated that the long-acting pramipexole patch exerts its neuroprotective effects, at least in part, by inhibiting oxidative stress and mitochondrial apoptosis pathway and holds promise as a candidate drug. (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - August 27, 2018 Category: Drugs & Pharmacology Source Type: research

Chrysophanol attenuates nitrosative/oxidative stress injury in a mouse model of focal cerebral ischemia/reperfusion
Publication date: Available online 25 August 2018Source: Journal of Pharmacological SciencesAuthor(s): Yongmei Zhao, Yuyou Huang, Yalan Fang, Haiping Zhao, Wenjuan Shi, Jincheng Li, Yunxia Duan, Yuwei Sun, Li Gao, Yumin LuoAbstractNitrosative/oxidative stress plays an important role in neuronal death following cerebral ischemia/reperfusion (I/R). Chrysophanol (CHR) has been shown to afford significant neuroprotection on ischemic stroke, however, whether its mechanism is related to attenuating nitrosative/oxidative stress is not clear. In the present study, we investigated the effect of CHR on neuronal injury related to nit...
Source: Journal of Pharmacological Sciences - August 25, 2018 Category: Drugs & Pharmacology Source Type: research

Resveratrol-loaded nanoemulsion prevents cognitive decline after abdominal surgery in aged rats
Publication date: Available online 25 August 2018Source: Journal of Pharmacological SciencesAuthor(s): Fabricio M. Locatelli, Takashi Kawano, Hideki Iwata, Bun Aoyama, Satoru Eguchi, Atsushi Nishigaki, Daiki Yamanaka, Hiroki Tateiwa, Marie Shigematsu-Locatelli, Masataka YokoyamaAbstractThe maladaptive response of aged microglia to surgery and consequent neuroinflammation plays a key pathogenic role in postoperative cognitive dysfunction (POCD). Here, we assessed the preventive effect of resveratrol (RESV) for POCD in aged rats. The emulsified form of RESV (e-RESV) was selected to improve its oral and brain bioavailability....
Source: Journal of Pharmacological Sciences - August 25, 2018 Category: Drugs & Pharmacology Source Type: research

MicroRNA-370 inhibits the proliferation, invasion and EMT of gastric cancer cells by directly targeting PAQR4
Publication date: Available online 25 August 2018Source: Journal of Pharmacological SciencesAuthor(s): Ye Feng, Tao Sun, Yabo Yu, Yongjian Gao, Xuefeng Wang, Zhi ChenAbstractIt has been reported that PAQR4 (Progestin and AdipoQ Receptor 4) expression is closely associated with progression of many cancers and microRNA (miRNA) processing. However, the effects and its precise mechanisms of PAQR4 in gastric cancer (GC) have not been well clarified. Our study aimed to explore the interaction between PAQR4 and miR-370 in GC. In our study, we found that the miR-370 level was significantly down-regulated in GC tissues and cell lin...
Source: Journal of Pharmacological Sciences - August 25, 2018 Category: Drugs & Pharmacology Source Type: research

Glycine mitigates renal oxidative stress by suppressing Nox4 expression in rats with streptozotocin-induced diabetes
In this study, we investigated the effects of glycine on diabetic renal injury and oxidative stress by adding 1% glycine in the drinking water of rats with streptozotocin-induced diabetes for 20 weeks. Glycine levels decreased in the plasma and kidney homogenates of diabetic rats but were restored by oral glycine administration. In these diabetic rats, glycine attenuated renal damage, as evidenced by the decreased mesangial expansion, tubular interstitial fibrosis, and neutrophil gelatinase-associated lipocalin (NGAL) expression. Glycine also ameliorated the raise in urinary malondialdehyde (MDA) levels and partially resto...
Source: Journal of Pharmacological Sciences - August 25, 2018 Category: Drugs & Pharmacology Source Type: research

Valproic acid attenuates immunosuppressive function of myeloid-derived suppressor cells
In this study, we focus on the anticonvulsant drug valproic acid (VPA), which has additional activities including anticancer and immunoregulation by inhibition of histone deacetylases. We showed that VPA decreased the proportion of polymorphonuclear (PMN)-MDSCs in vitro and showed for the first time that VPA greatly attenuated the immunosuppressive function of MDSCs in a dose-dependent manner. Moreover, we demonstrated that in vitro differentiated VPA-conditioned MDSCs exhibited impaired ability to stimulate tumor progression in vivo. We also showed the possible involvement of several mechanisms in the VPA-induced attenuat...
Source: Journal of Pharmacological Sciences - August 24, 2018 Category: Drugs & Pharmacology Source Type: research

FM3-Aims & Scope
Publication date: July 2018Source: Journal of Pharmacological Sciences, Volume 137, Issue 3Author(s): (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - August 23, 2018 Category: Drugs & Pharmacology Source Type: research

FM1-Editorial Board
Publication date: July 2018Source: Journal of Pharmacological Sciences, Volume 137, Issue 3Author(s): (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - August 23, 2018 Category: Drugs & Pharmacology Source Type: research

Lentivirus-mediated knockdown of FcγRI (CD64) attenuated lupus nephritis via inhibition of NF-κB regulating NLRP3 inflammasome activation in MRL/lpr mice
We reported that the administration of FcγRI-RNAi lentivirus (1) mainly inhibited FcγRI expression on macrophage of the kidneys, lowered the levels of urinary protein and serum anti-dsDNA antibody and prevented the impairment of renal function; (2) reduced the renal inflammatory cytokines (IL-1β and IL-18); (3) decreased NF-κB p65 nuclear migration, suppressed NOD-like receptor protein 3 (NLRP3) inflammasome activation, and finally inhibited renal inflammation. Together, these results showed the role of FcγRI on macrophages to involve in renal inflammatory response, potentially via regulating t...
Source: Journal of Pharmacological Sciences - August 19, 2018 Category: Drugs & Pharmacology Source Type: research

Differentiated HASTR/ci35 cells: A promising in vitro human astrocyte model for facilitating CNS drug development studies
In this study, in order to further increase their chances to contribute to various astrocyte studies, we report on the development of a culture method that improves HASTR/ci35 cell differentiation status and provide several proofs related to their astrocyte characteristics. The culture method is based on the simultaneous elimination of serum effects and immortalization signals. The results of qPCR showed that the culture method significantly enhanced several astrocyte marker gene expression levels. Using the differentiated HASTR/ci35, we examined their response profiles to nucleotide treatment and inflammatory stimuli...
Source: Journal of Pharmacological Sciences - August 14, 2018 Category: Drugs & Pharmacology Source Type: research

α1L-adrenoceptors mediate contraction of human erectile tissue
Publication date: Available online 9 August 2018Source: Journal of Pharmacological SciencesAuthor(s): Beverley J. Davis, Christopher R. Chapple, Donna J. Sellers, Alistair L. Naylor, David Sillar, Alistair Campbell, Russ Chess-WilliamsAbstractα1-adrenoceptor antagonists can impact upon sexual function and have potential in the treatment of erectile dysfunction. Human erectile tissue contains predominantly α1A-adrenoceptors, and here we examined whether contractions of this tissue are mediated by the functional phenotype, the α1L-adrenoceptor. Functional experiments using subtype selective agonists and ant...
Source: Journal of Pharmacological Sciences - August 10, 2018 Category: Drugs & Pharmacology Source Type: research

Differentiated HASTR/ci35 cells: a promising in vitro human astrocyte model for facilitating CNS drug development studies
In this study, in order to further increase their chances to contribute to various astrocyte studies, we report on the development of a culture method that improves HASTR/ci35 cell differentiation status and provide several proofs related to their astrocyte characteristics. The culture method is based on the simultaneous elimination of serum effects and immortalization signals. The results of qPCR showed that the culture method significantly enhanced several astrocyte marker gene expression levels. Using the differentiated HASTR/ci35, we examined their response profiles to nucleotide treatment and inflammatory stimuli, alo...
Source: Journal of Pharmacological Sciences - August 9, 2018 Category: Drugs & Pharmacology Source Type: research

Possible anti-inflammatory role of Zingiberis processum rhizoma, one component of the Kampo formula daikenchuto, against neutrophil infiltration through muscarinic acetylcholine receptor activation
In this study, we orally administered individual herbal components of DKT to mice four times before and after intestinal manipulation (IM). The anti-inflammatory action of each crude drug was evaluated by histochemical analysis of relevant molecules. The results showed that treatment with all herbal components of DKT significantly inhibits neutrophil infiltration. This inhibition of neutrophil infiltration by ZPR was significantly reduced in 5-hydroxytryptamine receptor 4 (5-HT4R) knockout (KO) mice but not in alpha-7 nicotinic acetylcholine receptor (α7nAChR) KO mice. Also, transient receptor potential ankyrin 1 (TR...
Source: Journal of Pharmacological Sciences - August 7, 2018 Category: Drugs & Pharmacology Source Type: research

Diallyl trisulfide regulates rat colonic smooth muscle contractions by inhibiting L-type calcium channel currents
Publication date: Available online 30 July 2018Source: Journal of Pharmacological SciencesAuthor(s): Qincai Tang, Haixia Ren, Lin Yan, Xiaojing Quan, Hong Xia, Hesheng LuoAbstractDiallyl trisulfide (DATS) is an active organosulfide component of allicin and has several beneficial effects, including antimicrobial, antioxidant, cardioprotective and anticancer effects. Few studies have shown the modulatory effect of DATS on L-type calcium channels in rat colonic smooth muscle cells and colonic motility. To investigate the modulatory effect of DATS on L-type calcium channels in rat colonic smooth muscle and colonic contraction,...
Source: Journal of Pharmacological Sciences - August 4, 2018 Category: Drugs & Pharmacology Source Type: research

Intravitreal aflibercept protects photoreceptors of mice against excessive light exposure
Publication date: Available online 4 August 2018Source: Journal of Pharmacological SciencesAuthor(s): Yoshiki Kuse, Kei Takahasi, Yuki Inoue, Hiroshi Izawa, Shinsuke Nakamura, Masamitsu Shimazawa, Hideaki HaraAbstractOur previous studies found that an anti-placental growth factor (PlGF) antibody protected the retina in light-induced retinal damage model, a model of non-exudative age-related macular degeneration (AMD). Aflibercept is an inhibitor of vascular endothelial growth factor (VEGF) and PlGF. In present study, we revealed that the intravitreal injection of aflibercept lessens light-induced retinal damage, while anti...
Source: Journal of Pharmacological Sciences - August 4, 2018 Category: Drugs & Pharmacology Source Type: research

Application of human induced pluripotent stem cell-derived cardiomyocytes sheets with microelectrode array system to estimate antiarrhythmic properties of multi-ion channel blockers
We examined electrophysiological indices of human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) sheets in order to quantitatively estimate Na+, K+ and Ca2+ channel blocking actions of bepridil and amiodarone using microelectrode array system in comparison with that of E-4031. We analyzed the field potential duration, effective refractory period, current threshold and conduction property using a programmed electrical stimulation protocol to obtain the post repolarization refractoriness and coefficient a of the relationship between the pacing cycle length and field potential duration. Electropharmacologica...
Source: Journal of Pharmacological Sciences - August 4, 2018 Category: Drugs & Pharmacology Source Type: research

FM1-Editorial Board
Publication date: June 2018Source: Journal of Pharmacological Sciences, Volume 137, Issue 2Author(s): (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - August 1, 2018 Category: Drugs & Pharmacology Source Type: research

FM3-Aims & Scope
Publication date: June 2018Source: Journal of Pharmacological Sciences, Volume 137, Issue 2Author(s): (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - August 1, 2018 Category: Drugs & Pharmacology Source Type: research

Diallyl trisulfide regulates rat colonic smooth muscle contractions by inhibiting L-type calcium channel currents
In conclusion, DATS has an inhibitory effect on the contractions of colonic muscle strips that is related to its regulation of L-type calcium channels. (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - July 30, 2018 Category: Drugs & Pharmacology Source Type: research

Polyphyllin I inhibits growth and invasion of cisplatin-resistant gastric cancer cells by partially inhibiting CIP2A/PP2A/Akt signaling axis
Publication date: Available online 26 July 2018Source: Journal of Pharmacological SciencesAuthor(s): Yunfei Zhang, Ping Huang, Xuewen Liu, Yuchen Xiang, Te Zhang, Yezi Wu, Jiaxin Xu, Zhiting Sun, Weiguo Zhen, Liang Zhang, Yuan Si, Ying LiuAbstractThe aberrant expression of cancerous inhibitor of protein phosphatase 2A (CIP2A) indicates poor prognosis and promotes EMT and metastasis. EMT, a crucial cellular process that occurs during cancer progression and metastasis, has been reported to promote drug resistance in several previous studies. Consequently, ongoing research has been focused on exploring therapeutic options for...
Source: Journal of Pharmacological Sciences - July 27, 2018 Category: Drugs & Pharmacology Source Type: research

Osthole inhibits pancreatic cancer progression by directly exerting negative effects on cancer cells and attenuating tumor-infiltrating M2 macrophages
In this study, we aimed to explore the anti-tumor and immunomodulatory effects of osthole on pancreatic cancer. We found that osthole suppressed Panc 02 cell migration and proliferation and induced apoptosis as shown in vitro. Osthole also attenuated the development of pancreatic cancer in mice by inhibiting tumor-infiltrating M2 macrophages in our study. Additionally, osthole inhibited the polarization of primary bone marrow cells into M2 macrophages and inhibited the expression of MRC1, CCL22 and TGF-β in the M2 polarization process in vitro. Detection of the related signaling pathways revealed that osthole exerted ...
Source: Journal of Pharmacological Sciences - July 26, 2018 Category: Drugs & Pharmacology Source Type: research