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Discovery of a novel chalcone derivative inhibiting CFTR chloride channel via AMPK activation and its anti-diarrheal application
This study aimed to identify novel chalcone derivatives with improved potency and explore their mechanism of action. Screening of 27 chalcone derivatives identified CHAL-025 as the most potent chalcone analog that reversibly inhibited CFTR-mediated Cl- secretion in T84 cells with an IC50 of ∼1.5 μM. As analyzed by electrophysiological and biochemical analyses, the mechanism of CFTR inhibition by CHAL-025 is through AMP-activated protein kinase (AMPK), a negative regulator of CFTR activity. Furthermore, western blot analyses and molecular dynamics (MD) results suggest that CHAL-025 activates AMPK by binding at the allost...
Source: Journal of Pharmacological Sciences - August 2, 2019 Category: Drugs & Pharmacology Source Type: research

Effects of geldanamycin on neurite outgrowth-related proteins and kinases in nerve growth factor-differentiated pheochromocytoma 12 cells
Publication date: Available online 30 July 2019Source: Journal of Pharmacological SciencesAuthor(s): Keisuke Migita, Taichi Matsumoto, Kazuki Terada, Kazuhiko Ono, Shuji HaraAbstractHeat shock protein 90 (HSP90) antagonists are currently being evaluated as potential anticancer drugs. However, adverse effects related to these drugs, such as fatigue and pain, suggest that they affect neurons. Therefore, to understand the influence of HSP90 inhibitors on neurons, we investigated the effects of geldanamycin, an HSP90 antagonist, on nerve growth factor (NGF)-differentiated pheochromocytoma 12 (PC12) cells, particularly, on the ...
Source: Journal of Pharmacological Sciences - July 31, 2019 Category: Drugs & Pharmacology Source Type: research

Genetic deletion of Cav3.2 T-type calcium channels abolishes H2S-dependent somatic and visceral pain signaling in C57BL/6 mice
Publication date: Available online 30 July 2019Source: Journal of Pharmacological SciencesAuthor(s): Kazuki Matsui, Maho Tsubota, Saaya Fukushi, Nene Koike, Hiroshi Masuda, Yoshihito Kasanami, Takaya Miyazaki, Fumiko Sekiguchi, Tsuyako Ohkubo, Shigeru Yoshida, Yutaro Mukai, Akira Oita, Mitsutaka Takada, Atsufumi KawabataAbstractWe tested whether genetic deletion of Cav3.2 T-type Ca2+ channels abolishes hydrogen sulfide (H2S)-mediated pain signals in mice. In Cav3.2-expressing HEK293 cells, Na2S, an H2S donor, at 100 μM clearly increased Ba2+ currents, as assessed by whole-cell patch-clamp recordings. In wild-type C57BL/6 ...
Source: Journal of Pharmacological Sciences - July 30, 2019 Category: Drugs & Pharmacology Source Type: research

Retinoic acid promotes barrier functions in human iPSC-derived intestinal epithelial monolayers
Publication date: Available online 26 July 2019Source: Journal of Pharmacological SciencesAuthor(s): Shigeru Yamada, Yasunari KandaAbstractVitamin A (VA) is a fat-soluble micronutrient that plays essential roles in various biological processes, including cell growth, differentiation, and apoptosis. In the intestine, VA are known to promote mucosal homeostasis and immunity. However, the effect of VA in intestinal development has not been well elucidated. In the present study, we generated human intestine organoids from human induced pluripotent stem cells (iPSCs), and investigated the effect of the VA active metabolite all-...
Source: Journal of Pharmacological Sciences - July 27, 2019 Category: Drugs & Pharmacology Source Type: research

Paracetamol inhibits Ca2+ permeant ion channels and Ca2+ sensitization resulting in relaxation of precontracted airway smooth muscle
Publication date: Available online 24 July 2019Source: Journal of Pharmacological SciencesAuthor(s): Yuan-Yuan Chen, Meng-Fei Yu, Xiao-Xue Zhao, Jinhua Shen, Yong-Bo Peng, Ping Zhao, Lu Xue, Weiwei Chen, Li-Qun Ma, Gangjian Qin, Jiapei Dai, Qing-Hua LiuAbstrctThe purpose of this study was to screen a bronchodilator from old drugs and elucidate the underlying mechanism. Paracetamol (acetaminophen) is a widely used analgesic and antipyretic drug. It has been reported that it inhibits the generation of prostaglandin and histamine, which play roles in asthma. These findings led us to explore whether paracetamol could be a pote...
Source: Journal of Pharmacological Sciences - July 25, 2019 Category: Drugs & Pharmacology Source Type: research

Schisandra Chinensis Acidic Polysaccharide Partialy Reverses Acetaminophen-Induced Liver Injury in mice
In conclusion, we speculated that the protective activities of SCAP on the APAP-induced mouse model of acute liver injury might be related to its antioxidation, anti-inflammation and anti-apoptosis properties. (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - July 25, 2019 Category: Drugs & Pharmacology Source Type: research

Donepezil ameliorates oxaliplatin-induced peripheral neuropathy via a neuroprotective effect
Publication date: Available online 19 July 2019Source: Journal of Pharmacological SciencesAuthor(s): Takehiro Kawashiri, Shiori Shimizu, Nao Shigematsu, Daisuke Kobayashi, Takao ShimazoeAbstractOxaliplatin induces severe peripheral neuropathy. The effect of donepezil, a drug used for treatment of Alzheimer’s disease, on oxaliplatin-induced peripheral neuropathy was investigated using both in vivo and in vitro models. Donepezil effectively attenuated oxaliplatin- and cisplatin-induced inhibition of neurite outgrowth in cultured PC12 cells. In a rat model, repeated oral administration of donepezil (5 times/week for 4 weeks...
Source: Journal of Pharmacological Sciences - July 20, 2019 Category: Drugs & Pharmacology Source Type: research

Engeletin inhibits Lipopolysaccharide/D-galactosamine-induced liver injury in mice through activating PPAR-γ
Publication date: Available online 19 July 2019Source: Journal of Pharmacological SciencesAuthor(s): Qing Tian, Guijie Wang, Yamin Zhang, Fubo Zhang, Long Yang, Zirong Liu, Zhongyang ShenAbstractLiver injury is a serious clinical syndrome that characterized by inflammatory response. Engeletin is known to have anti-inflammatory activity. However, the effects of engeletin on liver injury remain unclear. We aimed to assess the protective effect of engeletin on Lipopolysaccharide (LPS)/D-galactosamine (D-gal)-induced liver injury in mice. Engeletin was administered intraperitoneally 1 h before and 12 h after LPS/D-gal treatmen...
Source: Journal of Pharmacological Sciences - July 20, 2019 Category: Drugs & Pharmacology Source Type: research

Analysis of electro-mechanical relationship in human iPS cell-derived cardiomyocytes sheets under proarrhythmic condition assessed by simultaneous field potential and motion vector recordings
Publication date: Available online 19 July 2019Source: Journal of Pharmacological SciencesAuthor(s): Atsushi Sugiyama, Mihoko Hagiwara-Nagasawa, Ryuichi Kambayashi, Ai Goto, Koki Chiba, Atsuhiko T. Naito, Yasunari Kanda, Akio Matsumoto, Hiroko Izumi-NakasekoAbstractWe investigated the electro-mechanical relationship of human iPS cell-derived cardiomyocyte sheets under arrhythmic condition, which was induced by digitalis intoxication along with the electrical train stimulation (n=4). We adopted motion vector analysis by high-speed video microscopy and extracellular field potential recording by 64-microelectrode array system...
Source: Journal of Pharmacological Sciences - July 20, 2019 Category: Drugs & Pharmacology Source Type: research

Transplantation of cardiac Sca-1-positive cells rather than c-Kit-positive cells preserves mitochondrial oxygen consumption of the viable myocardium following myocardial infarction in rats
In this study, we compared the effect of transplantation of isolated Sca-1+ cells and c-Kit+ cells with that of the crude CDCs (CrCDCs). Focusing on the differences in the ability for secretion of paracrine factors among 3 types of cells, we determined the effects of transplantation of these cells on cardiac intracellular signaling and mitochondrial function in rats with permanently ligated coronary arteries. We showed that the transplantation of these cells resulted in a preservation of the cardiac pump function and mitochondrial respiration at the 8th week after myocardial infarction. However, mitochondrial function in t...
Source: Journal of Pharmacological Sciences - July 20, 2019 Category: Drugs & Pharmacology Source Type: research

The therapeutic effects of Jaceosidin on lipopolysaccharide-induced acute lung injury in mice
Publication date: Available online 18 July 2019Source: Journal of Pharmacological SciencesAuthor(s): Xiao-lei Huang, Xiao-chen Wei, Leng-qiu Guo, Lei Zhao, Xi-hua Chen, Ya-dong Cui, Jie Yuan, Dao-feng Chen, Jian ZhangAbstractAcute lung injury (ALI) results from various factors including uncontrolled pulmonary inflammation, oxidative damage and the over-activated complement with high mortality rates. Jaceosidin was a flavonoid compound with significant anti-complement activity. We aimed to investigate the therapeutic effects of Jaceosidin on ALI induced by lipopolysaccharide (LPS). Mice were orally administrated with Jaceos...
Source: Journal of Pharmacological Sciences - July 18, 2019 Category: Drugs & Pharmacology Source Type: research

DNA methylation was involved in Total glucosides of Paeony regulating ERα for the treatment of female Systemic lupus erythematosus mice
In this study, we found that TGP treatment significantly decreased the expression of ERα by up-regulating ERα promoter methylation levels. Further investigation revealed that treatment with TGP increased the expression of DNMT in lupus mice. We also used DNA methyltransferase inhibitors to verify whether DNA methylation was involved in these process. HE staining results showed that TGP can reduce renal injury in SLE mice. Moreover, cytokines including IFN-γ, IL6 and IL12 expression and dsDNA levels in serum were inhibited by TGP treatment. These findings indicate that TGP inhibits autoimmunity in SLE mice possibly by do...
Source: Journal of Pharmacological Sciences - July 11, 2019 Category: Drugs & Pharmacology Source Type: research

IRR is involved in glucose-induced endocytosis after insulin secretion
Publication date: Available online 5 July 2019Source: Journal of Pharmacological SciencesAuthor(s): Mami Yamaokax, Takeshi Terabayashi, Tomoki Nishioka, Kozo Kaibuchi, Tomohisa Ishikawa, Toshimasa Ishizaki, Toshihide KimuraAbstractEndocytosis after insulin secretion plays a pivotal role in the regulation of insulin secretion in pancreatic β-cells. Our recent study suggested that EPI64, a GTPase activating protein for Rab27a, contributes to the regulation of glucose-induced endocytosis, which is mediated by the GDP-bound form of Rab27a. Here, we identified insulin receptor-related receptor (IRR) as an EPI64-interacting pro...
Source: Journal of Pharmacological Sciences - July 6, 2019 Category: Drugs & Pharmacology Source Type: research

Establishment of Enzyme-linked Immunosorbent Facilitated Antigen Binding as a Biomarker Assay for Japanese Cedar Pollen Allergy Immunotherapy
Conclusion; The JC pollen ELIFAB assay represents a simple, cell-free biomarker assay for monitoring the development of IgE-blocking antibody activity during JC pollen AIT. (Source: Journal of Pharmacological Sciences)
Source: Journal of Pharmacological Sciences - July 5, 2019 Category: Drugs & Pharmacology Source Type: research

Possible biased analgesic of hydromorphone through the G protein-over β-arrestin-mediated pathway: cAMP, CellKeyTM, and receptor internalization analyses
Publication date: Available online 2 July 2019Source: Journal of Pharmacological SciencesAuthor(s): Sei Manabe, Kanako Miyano, Yuriko Fujii, Kaori Ohshima, Yuki Yoshida, Miki Nonaka, Miaki Uzu, Yoshikazu Matsuoka, Tetsufumi Sato, Yasuhito Uezono, Hiroshi MorimatsuAbstractMorphine, fentanyl, and oxycodone are widely used as analgesics, and recently hydromorphone has been approved in Japan. Although all of these are selective for μ-opioid receptors (MORs) and have similar structures, their analgesic potencies and adverse effects (AEs) are diverse. Recent molecular analyses of MOR signaling revealed that the G protein-mediat...
Source: Journal of Pharmacological Sciences - July 3, 2019 Category: Drugs & Pharmacology Source Type: research