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Journal of Pharmacological Sciences

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https://www.readbyqxmd.com/read/28645489/effects-of-hypnotic-bromovalerylurea-on-microglial-bv2-cells
#1
Shun Kawasaki, Naoki Abe, Fumito Ohtake, Afsana Islam, Mohammed Emamussalehin Choudhury, Ryo Utsunomiya, Satoshi Kikuchi, Tasuku Nishihara, Jun Kuwabara, Hajime Yano, Yuji Watanabe, Mayuki Aibiki, Toshihiro Yorozuya, Junya Tanaka
An old sedative and hypnotic bromovalerylurea (BU) has anti-inflammatory effects. BU suppressed nitric oxide (NO) release and proinflammatory cytokine expression by lipopolysaccharide (LPS)-treated BV2 cells, a murine microglial cell line. However, BU did not inhibit LPS-induced nuclear translocation of nuclear factor-κB and subsequent transcription. BU suppressed LPS-induced phosphorylation of signal transducer and activator of transcription 1 (STAT1) and expression of interferon regulatory factor 1 (IRF1)...
June 8, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28619445/effects-of-kallidinogenase-on-retinal-edema-and-size-of-non-perfused-areas-in-mice-with-retinal-vein-occlusion
#2
Anri Nishinaka, Shinichiro Fuma, Yuki Inoue, Masamitsu Shimazawa, Hideaki Hara
Kallidinogenase has been used to treat retinal vein occlusion (RVO) in patients, although there are no evidences on the effects of kallidinogenase on the retinal edema and the non-perfused areas in eyes with a RVO. We have established a murine RVO model with retinal edema and non-perfused areas. The purpose of this study was to evaluate the effects of kallidinogenase on the retinal edema and size of the non-perfused areas in the mouse RVO model. We evaluated the thickness of the retinal layers and size of the non-perfused areas, and the blood flow by laser speckle flowgraphy in RVO model...
May 27, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28615142/overexpression-of-kcnj2-in-induced-pluripotent-stem-cell-derived-cardiomyocytes-for-the-assessment-of-qt-prolonging-drugs
#3
Min Li, Yasunari Kanda, Takashi Ashihara, Tetsuo Sasano, Yuji Nakai, Masami Kodama, Erina Hayashi, Yuko Sekino, Tetsushi Furukawa, Junko Kurokawa
Human induced pluripotent stem cell (hiPSC)-derived cardiomyocytes hold great potentials to predict pro-arrhythmic risks in preclinical cardiac safety screening, although the hiPSC cardiomyocytes exhibit rather immature functional and structural characteristics, including spontaneous activity. Our physiological characterization and mathematical simulation showed that low expression of the inward-rectifier potassium (IK1) channel is a determinant of spontaneous activity. To understand impact of the low IK1 expression on the pharmacological properties, we tested if transduction of hiPSC-derived cardiomyocytes with KCNJ2, which encodes the IK1 channel, alters pharmacological response to cardiac repolarization processes...
May 27, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28602541/connexin-43-enhances-bax-activation-via-jnk-activation-in-sunitinib-induced-apoptosis-in-mesothelioma-cells
#4
Miaki Uzu, Hiromi Sato, Ayaka Shimizu, Yukihiro Shibata, Koichi Ueno, Akihiro Hisaka
The constituent protein of gap junctions, connexin (Cx), interacts with various proteins via its C-terminus region, including kinases, cell-adhesion proteins, and a pro-apoptotic protein, Bax. This molecular interaction may affect expression and functioning of the interacting proteins and modulate the cellular physiology. In our previous work, Cx43 was found to interact directly with Bax and in the presence of sunitinib, lead to the Bax-mediated apoptosis in mesothelioma cells. In this study, we investigated the mechanism of how Cx43 promotes Bax-mediated apoptosis using the same cell line...
May 27, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28552584/physiological-functions-of-the-cholinergic-system-in-immune-cells
#5
REVIEW
Takeshi Fujii, Masato Mashimo, Yasuhiro Moriwaki, Hidemi Misawa, Shiro Ono, Kazuhide Horiguchi, Koichiro Kawashima
T and B cells, macrophages and dendritic cells (DCs) all express most of the components necessary for a functional cholinergic system. This includes choline acetyltransferase (ChAT), muscarinic and nicotinic acetylcholine (ACh) receptors (mAChRs and nAChRs, respectively) and acetylcholinesterase (AChE). Immunological activation of T cells up-regulates cholinergic activity, including ChAT and AChE expression. Moreover, toll-like receptor agonists induce ChAT expression in DCs and macrophages, suggesting cholinergic involvement in the regulation of immune function...
May 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28532624/tyrphostin-ag-related-compounds-attenuate-h2o2-induced-trpm2-dependent-and-independent-cellular-responses
#6
Shinichiro Yamamoto, Takahiro Toda, Ryo Yonezawa, Takaharu Negoro, Shunichi Shimizu
PURPOSE: TRPM2 is a Ca(2+)-permeable channel that is activated by H2O2. TRPM2-mediated Ca(2+) signaling has been implicated in the aggravation of inflammatory diseases. Therefore, the development of TRPM2 inhibitors to prevent the aggravation of these diseases is expected. We recently reported that some Tyrphostin AG-related compounds inhibited the H2O2-induced activation of TRPM2 by scavenging the intracellular hydroxyl radical. In the present study, we examined the effects of AG-related compounds on H2O2-induced cellular responses in human monocytic U937 cells, which functionally express TRPM2...
May 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28522217/celastrol-inhibits-chondrosarcoma-proliferation-migration-and-invasion-through-suppression-cip2a-c-myc-signaling-pathway
#7
Jinhui Wu, Muchen Ding, Ningfang Mao, Yungang Wu, Chao Wang, Jiabin Yuan, Xiong Miao, Jingfeng Li, Zhicai Shi
Chondrosarcomas (CS) is the second most frequent tumors of cartilage origin. A small compound extracted from Thunder God Vine (Tripterygium wilfordii Hook. F.) called celastrol can directly bound CIP2A protein and effectively inhibit cell proliferation and induce apoptosis in several cancer cells. However, little knowledge is concern about the important role of CIP2A in CS patients and the therapeutic value of celastrol on CS. Our results showed that CIP2A and c-MYC were verified to be oncoproteins by detecting their mRNA and protein expression in 10 human CS tissues by qRT-PCR and Western blots...
May 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28506595/plumbagin-suppresses-the-migration-and-invasion-of-glioma-cells-via-downregulation-of-mmp-2-9-expression-and-inaction-of-pi3k-akt-signaling-pathway-in%C3%A2-vitro
#8
Guanghui Chen, Yan Yue, Jun Qin, Xinping Xiao, Qing Ren, Bin Xiao
Plumbagin is a natural naphthoquinone constituent isolated from the roots of medicinal plant Plumbago zeylanica L., and has demonstrated anti-proliferative and anti-invasion activities in various cancer cells. However, its effect on the migration and invasion of glioma cells has not been elucidated. Therefore, human glioma U87 and U251 cells were treated with plumbagin at 1.0 and 2.0 μM for 24 h, and cell migration and invasion were assessed with scratch wound healing and invasion assays. The results showed that plumbagin significantly inhibited the migration and invasion of U87 and U251 cells, suppressed the activity and expression of MMP-2/-9, and inhibited the nuclear translocation of transcription factors Sp1 in the U87 and U251 cells...
May 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28499726/inhibitory-effect-of-donepezil-on-bradykinin-induced-increase-in-the-intracellular-calcium-concentration-in-cultured-cortical-astrocytes
#9
Kouki Makitani, Shota Nakagawa, Yasuhiko Izumi, Akinori Akaike, Toshiaki Kume
Donepezil is a potent and selective acetylcholinesterase inhibitor developed for the treatment of Alzheimer's disease. In the present study, we investigated the responses of astrocytes to bradykinin, an inflammatory mediator, and the effect of donepezil on these responses using cultured cortical astrocytes. Bradykinin induced a transient increase of intracellular calcium concentration ([Ca(2+)]i) in cultured astrocytes. Bradykinin-induced [Ca(2+)]i increase was inhibited by the exposure to thapsigargin, which depletes Ca(2+) stores on endoplasmic reticulum, but not by the exclusion of extracellular Ca(2+)...
May 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28479222/effects-of-a-spleen-tyrosine-kinase-inhibitor-on-progression-of-the-lupus-nephritis-in-mice
#10
Maki Kitai, Noboru Fukuda, Takahiro Ueno, Morito Endo, Takashi Maruyama, Masanori Abe, Kazuyoshi Okada, Masayoshi Soma, Koichi Matsumoto
The Fc receptors (FcR) have pivotal roles in the pathogenesis of the autoimmune glomerulonephritis. We therefore investigated the effects of a Syk inhibitor on the progression of lupus nephritis and SH3 domain binding protein 2 and p38MAP kinase signalings in mice. NZB/W F1 mice, a model of lupus nephritis, received a Syk inhibitor R406. Western blotting and immunohistochemistry revealed that R406 treatment significantly delayed the appearance of proteinuria, histologically improved their glomerulosclerosis and inhibited the increased the expression of MCP-1 and TGF-β1 mRNAs and the nephrin and podocin proteins in the kidney...
May 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28461003/ginsenoside-rg3-exerts-anti-depressive-effect-on-an-nmda-treated-cell-model-and-a-chronic-mild-stress-animal-model
#11
Hualin Zhang, Zhongliu Zhou, Ziming Chen, Zhiyong Zhong, Zhong Li
Depression is a common mental disorder and a leading cause of disability. At its most severe, it can lead to suicide. Recently, there has been growing interest in the application of natural herbs for the prevention and treatment of depression. In this report, we found that the ginsenoside active component Rg3 has an apparent antidepressant effect. In N-methyl-d-aspartic acid (NMDA)-treated HT22 murine hippocampal neuronal cells, Rg3 recovered proliferation and inhibited apoptosis by altering the cell cycle...
May 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28456375/rolipram-improves-facilitation-of-contextual-fear-extinction-in-the-1-methyl-4-phenyl-1-2-3-6-tetrahydropyridine-induced-mouse-model-of-parkinson-s-disease
#12
Ken-Ichi Kinoshita, Yoshikage Muroi, Toshihiro Unno, Toshiaki Ishii
Cognitive impairment often occurs in Parkinson's disease (PD), but the mechanism of onset remains unknown. Recently, we reported that PD model mice produced by 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) show facilitation of hippocampal memory extinction, which may be the cause of cognitive impairment in PD. When we examined the cAMP/CREB signaling in the hippocampus, decreased levels of cAMP and phosphorylated CREB were observed in the dentate gyrus (DG) of MPTP-treated mice. Administration of rolipram improved the memory deficits with concomitant recovery of cAMP and phosphorylated CREB levels, suggesting that reduced cAMP/CREB signaling in the DG leads to cognitive impairment in MPTP-treated mice...
May 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28434657/corrigendum-to-human-grin2b-variants-in-neurodevelopmental-disorders-j-pharmacol-sci-132-2-115-121
#13
Chun Hu, Wenjuan Chen, Scott J Myers, Hongjie Yuan, Stephen F Traynelis
No abstract text is available yet for this article.
April 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28433566/%C3%AE-aminoisobutyric-acid-ameliorates-the-renal-fibrosis-in-mouse-obstructed-kidneys-via-inhibition-of-renal-fibroblast-activation-and-fibrosis
#14
Huijuan Wang, Jun Qian, Xiufen Zhao, Changing Xing, Bin Sun
Renal fibrosis is a hallmark feature of chronic kidney disease, which is reflected by proliferation and migration of interstitial fibroblasts and extracellular matrix (ECM) accumulation. β-Aminoisobutyric acid (BAIBA) is recently demonstrated to exert a protective role from metabolic diseases. However, whether and how BAIBA on fibroblast activation and renal fibrosis response to angiotensin II (Ang II) remains largely obscure. Herein, we showed that BAIBA significantly depressed the proliferation and migration of NRK-49F cells in vitro...
April 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28433565/inhibitory-effects-of-pine-nodule-extract-and-its-component-sj-2-on-acetylcholine-induced-catecholamine-secretion-and-synthesis-in-bovine-adrenal-medullary-cells
#15
Xiaojia Li, Takafumi Horishita, Yumiko Toyohira, Hui Shao, Jie Bai, Haixia Bo, Xinbo Song, Shin Ishikane, Yukari Yoshinaga, Noriaki Satoh, Masato Tsutsui, Nobuyuki Yanagihara
Extract of pine nodules (matsufushi) formed by bark proliferation on the surface of trees of Pinus tabulaeformis or Pinus massoniana has been used as an analgesic for joint pain, rheumatism, neuralgia, dysmenorrhea and other complaints in Chinese traditional medicine. Here we report the effects of matsufushi extract and its components on catecholamine secretion and synthesis in cultured bovine adrenal medullary cells. We found that matsufushi extract (0.0003-0.005%) and its component, SJ-2 (5-hydroxy-3-methoxy-trans-stilbene) (0...
April 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28410967/involvement-of-alpha-and-beta-adrenoceptors-in-the-automaticity-of-the-isolated-guinea-pig-pulmonary-vein-myocardium
#16
Masahiko Irie, Yayoi Tsuneoka, Mariko Shimobayashi, Nao Hasegawa, Yusuke Tanaka, Soh Mochizuki, Sho Ichige, Shogo Hamaguchi, Iyuki Namekata, Hikaru Tanaka
We examined the involvement of adrenoceptors in the automaticity of the pulmonary vein myocardium, which probably plays a crucial role in the generation of atrial fibrillation. The automatic activity of the myocardium in guinea pig pulmonary vein tissue preparations were monitored by contractile force or membrane potential measurement. In quiescent preparations, application of noradrenaline induced an automatic activity. The firing frequency was reduced by prazosin or atenolol. Methoxamine induced an automatic activity of low frequency, which was accelerated by further application of isoproterenol...
April 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28410966/vincristine-induced-peripheral-neuropathic-pain-and-expression-of-transient-receptor-potential-vanilloid-1-in-rat
#17
Terumasa Chiba, Yusuke Oka, Hiroya Sashida, Toshie Kanbe, Kenji Abe, Iku Utsunomiya, Kyoji Taguchi
The clinical anti-cancer efficacy of vincristine is limited by the development of dose-dependent peripheral neuropathy. Up-regulation of transient receptor potential vanilloid 1 (TRPV1) is correlated with peripheral neuropathy following anti-cancer drug treatment. To analyze the contribution of TRPV1 to the development of vincristine-induced mechanical allodynia/hyperalgesia, TRPV1 expression in the rat dorsal root ganglion (DRG) was analyzed after vincristine treatment. Mechanical allodynia/hyperalgesia was tested with von Frey filaments 14 days after intraperitoneal administration of 0...
April 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28410965/permissive-role-of-reduced-inwardly-rectifying-potassium-current-density-in-the-automaticity-of-the-guinea-pig-pulmonary-vein-myocardium
#18
Yayoi Tsuneoka, Masahiko Irie, Yusuke Tanaka, Takahiko Sugimoto, Yuka Kobayashi, Taichi Kusakabe, Keisuke Kato, Shogo Hamaguchi, Iyuki Namekata, Hikaru Tanaka
The electrophysiological properties underlying the automaticity of the guinea pig pulmonary vein myocardium were studied. About 30% of the isolated pulmonary vein tissue preparations showed spontaneous electrical activity, as shown by glass microelectrode recordings from their myocardial layer. The remaining quiescent preparations had a resting membrane potential less negative than that in the left atria. Blockade of the acetylcholine activated potassium current (IK-ACh) by tertiapin induced a depolarizing shift of the resting membrane potential and automatic electrical activity in the pulmonary vein, but not in the atria...
April 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28408165/alterations-in-protein-phosphorylation-in-the-amygdala-of-the-5xfamilial-alzheimer-s-disease-animal-model
#19
Eun-Jeong Yang, Usman Mahmood, Hyunju Kim, Moonseok Choi, Yunjung Choi, Jean-Pyo Lee, Moon-Jeong Chang, Hye-Sun Kim
Alzheimer's disease is the most common disease underlying dementia in humans. Two major neuropathological hallmarks of AD are neuritic plaques primarily composed of amyloid beta peptide and neurofibrillary tangles primarily composed of hyperphosphorylated tau. In addition to impaired memory function, AD patients often display neuropsychiatric symptoms and abnormal emotional states such as confusion, delusion, manic/depressive episodes and altered fear status. Brains from AD patients show atrophy of the amygdala which is involved in fear expression and emotional processing as well as hippocampal atrophy...
April 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28391996/molecular-mechanisms-underlying-pimaric-acid-induced-modulation-of-voltage-gated-k-channels
#20
Kazuho Sakamoto, Yoshiaki Suzuki, Hisao Yamamura, Susumu Ohya, Katsuhiko Muraki, Yuji Imaizumi
Voltage-gated K(+) (KV) channels, which control firing and shape of action potentials in excitable cells, are supposed to be potential therapeutic targets in many types of diseases. Pimaric acid (PiMA) is a unique opener of large conductance Ca(2+)-activated K(+) channel. Here, we report that PiMA modulates recombinant rodent KV channel activity. The enhancement was significant at low potentials (<0 mV) but not at more positive potentials. Application of PiMA significantly shifted the voltage-activation relationships (V1/2) of rodent KV1...
April 2017: Journal of Pharmacological Sciences
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