2,655 results match your criteria Journal of Pharmacological Sciences[Journal]


Trimetazidine prevents diabetic cardiomyopathy by inhibiting Nox2/TRPC3-induced oxidative stress.

J Pharmacol Sci 2019 Mar 15. Epub 2019 Mar 15.

Institute of Biomedical & Pharmaceutical Sciences, Guangdong University of Technology, Guangzhou 510006, China. Electronic address:

Diabetic cardiomyopathy (DCM) is characterized by cardiac hypertrophy, fibrosis, oxidative stress and inflammation. Trimetazidine (TMZ), a potent metabolism modulator, has been shown to be cardioprotective in experimental models of ischaemia-reperfusion and type 2 diabetes-induced cardiomyopathy. The present study examined whether TMZ inhibits cardiomyopathy induced by insulin-dependent type 1 diabetes. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.016DOI Listing
March 2019
1 Read

Involvement of sex hormonal regulation of K channels in electrophysiological and contractile functions of muscle tissues.

J Pharmacol Sci 2019 Mar 11. Epub 2019 Mar 11.

Department of Bio-Informational Pharmacology, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka 422-8526, Japan. Electronic address:

Sex hormones, such as testosterone, progesterone, and 17β-estradiol, control various physiological functions. This review focuses on the sex hormonal regulation of K channels and the effects of such regulation on electrophysiological and contractile functions of muscles. In the cardiac tissue, testosterone and progesterone shorten action potential, and estrogen lengthens QT interval, a marker of increased risk of ventricular tachyarrhythmias. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.02.009DOI Listing

Kangxianling decoction prevents renal fibrosis in rats with 5/6 nephrectomy and inhibits Ang II-induced ECM production in glomerular mesangial cells.

J Pharmacol Sci 2019 Mar 14. Epub 2019 Mar 14.

Shanghai University of Traditional Chinese Medicine, Shanghai, 200120, China; Department of Nephrology, Shuguang Hospital Affiliated to Shanghai University of Traditional Chinese Medicine, Shanghai, 200013, China. Electronic address:

Renal fibrosis is a common pathological change in all stages of kidney disease. Kangxianling decoction was widely used in patients with chronic kidney disease, which could improve symptoms such as poor appetite, edema, and fatigue. However, its effect on renal fibrosis remains to be studied. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.03.003DOI Listing

S-allyl-l-cysteine attenuates bleomycin-induced pulmonary fibrosis and inflammation via AKT/NF-κB signaling pathway in mice.

J Pharmacol Sci 2019 Mar 14. Epub 2019 Mar 14.

Department of Basic Medicine, Wuxi School of Medicine, Jiangnan University, Wuxi, Jiangsu, 214122, PR China. Electronic address:

Idiopathic pulmonary fibrosis (IPF) is a progressive and lethal lung disease characterized by inflammation, multifocal fibrotic lesions and excessive collagen deposition with limited therapies. As a major bioactive compound in garlic, S-allyl-l-cysteine (SAC) is a neuroprotective drug candidate to prevent cognitive decline, however, its anti-pulmonary fibrotic activity remains unknown. Here, we investigated whether SAC could attenuate bleomycin (BLM)-induced pulmonary fibrosis and inflammation in mice. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.03.002DOI Listing
March 2019
1 Read

Incidence and types of HIV-1 drug resistance mutation among patients failing first-line antiretroviral therapy.

J Pharmacol Sci 2019 Jan 17. Epub 2019 Jan 17.

The 4th People's Hospital of Nanning, The Infectious Disease Hospital of Nanning Affiliated to Guangxi Medical University, and the AIDS Clinical Treatment Center of Guangxi (Nanning), Nanning, 530023, China.

Objective: This study aims to investigate the prevalence and types of drug resistance mutations among patients failing first-line antiretroviral therapy (ART).

Methods: Plasma samples from 112 patients with human immunodeficiency virus-1 (HIV-1) were collected for virus RNA extract and gene amplification. The mutations related to drug resistance were detected and the incidence was statistically analyzed, and the drug resistance rate against common drugs was also evaluated. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.11.016DOI Listing
January 2019
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Comparative efficacy and safety of thirteen biologic therapies for patients with moderate or severe psoriasis: A network meta-analysis.

J Pharmacol Sci 2018 Dec 27. Epub 2018 Dec 27.

Department of Dermatology, Dongzhimen Hospital, Beijing University of Chinese Medicine, Beijing 100700, China. Electronic address:

Purpose: This network meta-analysis was aimed to enhance the corresponding evidence with respect to the efficacy and safety of biologic treatments.

Methods: PubMed and EMBASE database searches were conducted. Odds ratios were used to evaluate multi-aspect comparisons. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.12.006DOI Listing
December 2018

Pretreatment with Tilianin improves mitochondrial energy metabolism and oxidative stress in rats with myocardial ischemia/reperfusion injury via AMPK/SIRT1/PGC-1 alpha signaling pathway.

J Pharmacol Sci 2019 Mar 8. Epub 2019 Mar 8.

Pharmacy of College, Shihezi University, Xinjiang, 832002, PR China; First Affiliated Hospital of the Medical College, Shihezi University, XinJiang, 832008, PR China. Electronic address:

Mitochondrial energy metabolism and oxidative stress play a crucial role in ameliorating myocardial ischemia/reperfusion injury (MIRI). Tilianin has been reported to have a significant protection for mitochondrion in MIRI. However, the underlying mechanisms remain unknown. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.02.008DOI Listing

Effect of co-administered inducer or inhibitor on omeprazole pharmacokinetics based on CYP2C19 genotype.

J Pharmacol Sci 2019 Mar 11. Epub 2019 Mar 11.

Department of Clinical Pharmacology and Therapeutics, Hamamatsu University School of Medicine, 1-20-1 Handayama, Hamamatsu, 431-3192, Japan.

Polymorphisms of cytochrome P450 (CYP) enzymes can affect enzymatic activity, drug metabolism and drug interactions. Although the potential for drug interactions is especially important when co-administering drugs with strong inductive or inhibitory potential towards drug-metabolizing enzymes, the relationship between CYP genotypes and the extent of the inductive or inhibitory effects remain poorly understood. We investigated the effects of rifampicin (inductive) and fluvoxamine (inhibitory) on metabolism of omeprazole and CYP2C19 enzymatic activity in 19 healthy Japanese subjects. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.03.001DOI Listing

Collection of biochemical samples with brain-wide electrophysiological recordings from a freely moving rodent.

J Pharmacol Sci 2019 Feb 27. Epub 2019 Feb 27.

Laboratory of Chemical Pharmacology, Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7-3-1 Hongo Bunkyo-ku, Tokyo, 113-0033, Japan; Precursory Research for Embryonic Science and Technology (PRESTO), Japan Science and Technology Agency (JST), 4-1-8 Honcho, Kawaguchi, Saitama, 332-0012, Japan. Electronic address:

Bridging accumulating insights from microscopic and macroscopic studies in neuroscience research requires monitoring of neuronal population dynamics and quantifying specific molecules or genes from the brain of identical animals. To this end, by minimizing the size and weight of an electrode array, we developed a method that records local field potential signals of multiple brain regions from one side of the hemisphere in a freely moving rodent. At the same time, extracellular cerebrospinal fluid for biochemical assays or a small part of brain tissue samples for gene expression assays are collected from the other side of the hemisphere. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.02.006DOI Listing
February 2019
3 Reads

Indomethacin plus minocycline coadministration relieves chemotherapy and antiretroviral drug-induced neuropathic pain in a cannabinoid receptors-dependent manner.

J Pharmacol Sci 2019 Feb 27. Epub 2019 Feb 27.

Department of Pharmacology and Therapeutics, Faculty of Pharmacy, Kuwait University, Kuwait.

Neuropathic pain sometimes occurs during chemotherapy with paclitaxel or HIV/AIDS antiretroviral therapy with nucleoside reverse transcriptase inhibitors (NRTIs). We previously reported that coadministration of indomethacin plus minocycline (IPM) was antihyperalgesic in a cannabinoid type 1 (CB1) receptor-dependent manner in a mouse model of paclitaxel-induced neuropathic pain. We evaluated if IPM combination has antihyperalgesic and antiallodynic activities in animal models of paclitaxel or NRTI (ddC, zalcitabine)-induced neuropathic pain, and whether antagonists of CB1, CB2 receptors or G protein-coupled receptor 55 (GPR55) can inhibit these activities of IPM. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.02.007DOI Listing
February 2019
1 Read

Effect of ASP2205 fumarate, a novel 5-HT receptor agonist, on urethral closure function in rats.

J Pharmacol Sci 2019 Feb 27. Epub 2019 Feb 27.

Institute for Drug Discovery Research, Astellas Pharma Inc, 21, Miyukigaoka, Tsukuba-shi, Ibaraki, 305-8585, Japan.

The pharmacological profile of ASP2205 fumarate (ASP2205), a novel 5-HT receptor agonist, was evaluated in vitro and in vivo. ASP2205 showed potent and selective agonistic activity for the human 5-HT receptor, with an EC of 0.85 nM in the intracellular Ca mobilization assay. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.02.004DOI Listing
February 2019
2 Reads

Combined citicoline and docosahexaenoic acid treatment improves cognitive dysfunction following transient brain ischemia.

J Pharmacol Sci 2019 Feb 20. Epub 2019 Feb 20.

Department of Pharmacology, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Miyagi, 980-8678, Japan. Electronic address:

Phospholipids are structural components of cellular membranes that play important roles as precursors for various signaling pathways in modulating neuronal membrane function and maintenance of the intracellular environment. Phosphatidylcholine (PtdCho) is the most abundant cellular phospholipid. Citicoline and docosahexaenoic acid (DHA) are essential intermediates in the synthesis of PtdCho. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.02.003DOI Listing
February 2019

Apoptotic effect of Aralia echinocaulis extract on fibroblast-like synoviocytes in rats with adjuvant-induced arthritis via inhibiting the Akt/Hif-1α signaling pathway in vitro.

J Pharmacol Sci 2019 Feb 27. Epub 2019 Feb 27.

The Institute of Biology, National Institute of Measurement and Testing Technology, Chengdu, 610056, PR China.

Aralia echinocaulis is used for the treatment of rheumatoid arthritis by Tujia Minority in China. A previous study demonstrated that A. echinocaulis had a significant anti-arthritic effect on adjuvant arthritis (AA) rats in vivo. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.02.005DOI Listing
February 2019

Butyrate suppresses abnormal proliferation in colonic epithelial cells under diabetic state by targeting HMGB1.

J Pharmacol Sci 2018 Aug 31. Epub 2018 Aug 31.

Department of Gastroenterology, Sun Yat-Sen Memorial Hospital, Sun Yat-Sen University, 107 Yan Jiang Xi Road, Guangzhou, Guangdong, 510120, People's Republic of China. Electronic address:

Butyrate 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 mice and non-cancerous NCM460 colon cells. Proliferation and the expression of HMGB1 and RAGE were increased and could be partially reversed by butyrate treatment in the colon of db/db mice, which were consistent in NCM460 cells under a high glucose state. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.07.012DOI Listing

Plasma concentration and efficacy of tolvaptan in cirrhotic patients with refractory ascites.

J Pharmacol Sci 2019 Feb 27. Epub 2019 Feb 27.

Department of Gastroenterology, Juntendo University Nerima Hospital, Tokyo, Japan.

To investigate the relationship between the exposure and efficacy of tolvaptan, we measured pharmacokinetics of total drug at 7 days after repeated doses of 3.75 mg/day tolvaptan in 16 patients with hepatic edema. Nine patients (56. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.015DOI Listing
February 2019
2 Reads
2.360 Impact Factor

Cucurbitacin B induces inhibitory effects via the CIP2A/PP2A/C-KIT signaling axis in t(8;21) acute myeloid leukemia.

J Pharmacol Sci 2019 Feb 19. Epub 2019 Feb 19.

Laboratory of Molecular Target Therapy of Cancer, Institute of Basic Medical Sciences, Hubei University of Medicine, Shiyan, Hubei, 442000, China; Laboratory of Molecular Target Therapy of Cancer, Biomedical Research Institute, Hubei University of Medicine, Shiyan, Hubei, 442000, China. Electronic address:

Acute myeloid leukemia (AML) is the most common subtype of hematological malignancy in humans, and its incidence increases with age. The treatment of AML still faces challenges. Therefore, there is an urgent need to develop more effective targeted therapies. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.12.010DOI Listing
February 2019
4 Reads

Effect of miR-132 on bupivacaine-induced neurotoxicity in human neuroblastoma cell line.

J Pharmacol Sci 2019 Mar 19;139(3):186-192. Epub 2019 Feb 19.

Department of Anesthesiology, BenQ Medical Center, The Affiliated BenQ Hospital of Nanjing Medical University, Nanjing, Jiangsu, 210019, PR China. Electronic address:

Background: Local anesthetics (LAs) may generate neurotoxicity in neurons. In the current study, we explored the mechanisms by which microRNA-132 (miR-132) regulated the neurotoxicity of human neuroblastoma cells (SH-SY5Y) induced by bupivacaine (BUP).

Methods: CCK-8, flow cytometry, EdU detection, qRT-PCR and western blotting were used to explore the cell viability, apoptosis and gene expression, respectively. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.014DOI Listing

Inhibition of microRNA-17-5p reduces the inflammation and lipid accumulation, and up-regulates ATP-binding cassette transporterA1 in atherosclerosis.

J Pharmacol Sci 2018 Dec 6. Epub 2018 Dec 6.

Department of Cardiology, The Second Affiliated Hospital of Shenyang Medical College, Shenyang 110035, People's Republic of China.

Atherosclerosis (AS) is a chronic inflammatory disease of the arterial wall. Macrophages are considered to be closely associated with the development and progression of AS. However, the precise mechanism of miR-17-5p in the macrophages under AS remains incompletely clarified. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S13478613183021
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http://dx.doi.org/10.1016/j.jphs.2018.11.012DOI Listing
December 2018
5 Reads

Boron delivery for boron neutron capture therapy targeting a cancer-upregulated oligopeptide transporter.

J Pharmacol Sci 2019 Mar 18;139(3):215-222. Epub 2019 Feb 18.

Department of Bio-system Pharmacology, Graduate School of Medicine, Osaka University, 2-2 Yamadaoka, Suita, Osaka 565-0871, Japan. Electronic address:

Boron neutron capture therapy (BNCT) is a radiotherapy utilizing the neutron capture and nuclear fission reaction of B taken up into tumor cells. The most commonly used boron agent in BNCT, p-borono-l-phenylalanine (BPA), is accumulated in tumors by amino acid transporters upregulated in tumor cells. Here, by using dipeptides of BPA and tyrosine (BPA-Tyr and Tyr-BPA), we propose a novel strategy of selective boron delivery into tumor cells via oligopeptide transporter PEPT1 upregulated in various cancers. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.012DOI Listing
March 2019
1 Read

Protective effect of T3 peptide, an active fragment of tumstatin, against ischemia/reperfusion injury in rat heart.

J Pharmacol Sci 2019 Mar 10;139(3):193-200. Epub 2019 Feb 10.

Laboratory of Veterinary Pharmacology, School of Veterinary Medicine, Kitasato University, Higashi 23 Bancho 35-1, Towada City, Aomori, 034-8628, Japan.

Ischemia/reperfusion (I/R)-induced oxidative stress is a serious clinical problem in the reperfusion therapy for ischemic diseases. Tumstatin is an endogenous bioactive peptide cleaved from type IV collagen α3 chain. We previously reported that T3 peptide, an active subfragment of tumstatin, exerts cytoprotective effects on HO-induced apoptosis through the inhibition of intracellular reactive oxygen species (ROS) production in H9c2 cardiomyoblasts. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.010DOI Listing

Mechanisms underlying the cardio-protection of total ginsenosides against myocardial ischemia in rats in vivo and in vitro: Possible involvement of L-type Ca channels, contractility and Ca homeostasis.

J Pharmacol Sci 2019 Mar 14;139(3):240-248. Epub 2019 Feb 14.

School of Pharmacy, Hebei University of Chinese Medicine, Shijiazhuang 050200, Hebei, China; Hebei Key Laboratory of Integrative Medicine on Liver-Kidney Patterns, Shijiazhuang 050200, Hebei, China. Electronic address:

Here we aimed to observe the effects of total ginsenosides (TG) against isoproterenol (ISO) induced myocardial ischemia (MI) and to explore its underlying mechanisms based on L-type Ca current (I), intracellular Ca ([Ca]) and contraction in isolated rat myocytes. Rat model of MI was induced by subcutaneously injection of ISO (85 mg/kg) for 2 consecutive days. J-point elevation, heart rate, serum levels of creatine kinase (CK) and lactated dehydrogenase (LDH), and heart morphology changes were observed. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.02.001DOI Listing
March 2019
4 Reads

Calcilytics inhibit the proliferation and migration of human prostate cancer PC-3 cells.

J Pharmacol Sci 2019 Mar 10;139(3):254-257. Epub 2019 Feb 10.

Department of Physiology, Aichi Medical University, 1-1 Yazakokarimata, Nagakute, Aichi, 480-1195, Japan.

The carcinogenesis and development of prostate cancer are mediated by enhanced Ca signaling. In the present study, the pharmacological profile of the Ca-sensing receptor (CaSR) antagonists (calcilytics) was examined in human prostate cancer PC-3 cells. NPS2143 and Calhex 231 blocked extracellular Ca-induced increases in cytosolic [Ca]. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.008DOI Listing

Glypican-3 gene silencing for ovarian cancer using siRNA-PLGA hybrid micelles in a murine peritoneal dissemination model.

J Pharmacol Sci 2019 Mar 10;139(3):231-239. Epub 2019 Feb 10.

Department of Immunological and Molecular Pharmacology, Faculty of Pharmaceutical Sciences, Fukuoka University, Fukuoka, Japan.

Small interfering RNA (siRNA) has received much attention and for possible therapeutic applications to treat incurable chronic and genetic diseases, including cancer. However, the development of safe and efficient carriers for siRNA delivery still remains formidable hurdles for in vivo. The purpose of this study is to prepare siRNA-PLGA hybrid micelles to deliver the siRNA into the ovarian cancer cells and to evaluate of gene silencing effects in mice model. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.009DOI Listing
March 2019
1 Read

Ginsenoside compound K attenuates cognitive deficits in vascular dementia rats by reducing the Aβ deposition.

J Pharmacol Sci 2019 Mar 13;139(3):223-230. Epub 2019 Feb 13.

Department of Clinical Pharmacology, Xiangya Hospital, Central South University, Changsha, 410008, People's Republic of China; Institute of Clinical Pharmacology, Hunan Key Laboratory of Pharmacogenetics, Central South University, Changsha, 410078, People's Republic of China; Hunan Key Laboratory for Bioanalysis of Complex Matrix Samples, Changsha, Hunan, 410000, People's Republic of China. Electronic address:

Ginsenoside compound K (CK) is the main metabolite of protopanaxadiol-type ginsenosides and has been demonstrated to exert neuroprotective and cognition-enhancing effects. The effects of CK on cognitive function in vascular dementia (VD) has not been elucidated. Therefore, the present study aims to elucidate the effects of CK on memory function as well as its potential mechanism in VD rats. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.013DOI Listing
March 2019
1 Read

Influence of genetic polymorphisms and habitual caffeine intake on the changes in blood pressure, pulse rate, and calculation speed after caffeine intake: A prospective, double blind, randomized trial in healthy volunteers.

J Pharmacol Sci 2019 Mar 1;139(3):209-214. Epub 2019 Feb 1.

Department of Clinical Pharmacology, Faculty of Medical Sciences, Kyushu University, Maidashi 3-1-1, Higashi-ku, Fukuoka, 812-8582, Japan.

The aim of this study was to investigate the contribution of gene polymorphisms, in combination with habitual caffeine consumption, to the effect of caffeine intake on hemodynamic and psychoactive parameters. A double-blind, prospective study was conducted with 201 healthy volunteers randomly allocated 2:1 to the caffeinated group (150 mL decaffeinated coffee with additional 200 mg caffeine) or decaffeinated group (150 mL decaffeinated coffee). We measured the changes in blood pressure (BP) and calculation speed upon coffee intake, stratifying with gene polymorphisms, e. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.006DOI Listing

Anti-inflammatory and anti-hyperplastic effect of Bazhengsan in a male rat model of chronic nonbacterial prostatitis.

J Pharmacol Sci 2019 Mar 2;139(3):201-208. Epub 2019 Feb 2.

Department of Pharmacy, School of Life and Health Science, Anhui Science and Technology University, Fengyang, Anhui, People's Republic of China. Electronic address:

Objectives: The therapeutic potentiality of Bazhengsan on the chronic nonbacterial prostatitis was investigated.

Methods: Prostatitis was induced by subcutaneous injection of the 17-beta-estradiol (E) and dihydrotestosterone in male rat, and treated with Bazhengsan. After 8 weeks, prostatic fluid was collected for counting lecithin corpuscle density (LCD) and the organs were removed from animals and used for measuring prostate viscera coefficient (PVC). Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.007DOI Listing
March 2019
1 Read

The effect of honokiol on pulmonary artery endothelium cell autophagy mediated by cyclophilin A in hypoxic pulmonary arterial hypertension.

J Pharmacol Sci 2019 Mar 1;139(3):158-165. Epub 2019 Feb 1.

Department of Pharmaceutical Analysis and Analytical Chemistry, College of Pharmacy, Harbin Medical University, Harbin 150081, Heilongjiang Province, China. Electronic address:

Abnormal autophagy plays critical roles in the structure and function of the pulmonary vasculature. Cyclophilin A (CyPA) can be secreted from cells in response to hypoxia and oxidative stress, which are involved in inducing autophagy and regulating the function of endothelial cells in pulmonary arterial hypertension. Honokiol is a small molecule natural compound; it has many bioactivities, such as antitumor, anti-inflammatory, antioxidant and antiangiogenic properties, but how honokiol mediates autophagy in pulmonary arterial hypertension is unclear. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.005DOI Listing
March 2019
2 Reads
2.360 Impact Factor

Electropharmacological effects of intracellular Ca handling modulator caldaret on the heart assessed in the halothane-anesthetized dogs.

J Pharmacol Sci 2019 Mar 24;139(3):180-185. Epub 2019 Jan 24.

Department of Pharmacology, Faculty of Medicine, Toho University, 5-21-16 Omori-nishi, Ota-ku, Tokyo 143-8540, Japan; Department of Pharmacology, Toho University Graduate School of Medicine, 5-21-16 Omori-nishi, Ota-ku, Tokyo 143-8540, Japan.

We analyzed how the enhancement of net sarcoplasmic reticulum (SR) Ca uptake may affect cardiac electrophysiological properties in vivo by using caldaret which can decrease SR diastolic Ca leak, enhance SR Ca reuptake and inhibit reverse-mode Na/Ca exchanger. Caldaret in doses of 0.5, 5 and 50 μg/kg was intravenously administered over 10 min to the halothane-anesthetized beagle dogs (n = 5), attaining pharmacologically active plasma concentration. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S13478613193000
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http://dx.doi.org/10.1016/j.jphs.2019.01.004DOI Listing
March 2019
8 Reads

Coumarins ameliorate diabetogenic action of dexamethasone via Akt activation and AMPK signaling in skeletal muscle.

J Pharmacol Sci 2019 Mar 23;139(3):151-157. Epub 2019 Jan 23.

Institute of Pharmacology, Zhejiang University of Technology, Hangzhou 310014, People's Republic of China; Section of Endocrinology, School of Medicine, Yale University, New Haven 06520, USA. Electronic address:

Glucocorticoids are widely prescribed for lots of pathological conditions, however, can produce 'Cushingoid' side effects including central obesity, glucose intolerance, insulin resistance and so forth. Our study is intended to investigate the improving effects of coumarins on diabetogenic action of dexamethasone in vivo and in vitro and elucidate potential mechanisms. ICR mice treated with dexamethasone for 21 days exhibited decreased body weight, increased blood glucose and impaired glucose tolerance, which were prevented by fraxetin (40 mg/kg/day), esculin (40 mg/kg/day) and osthole (20 mg/kg/day), respectively. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.001DOI Listing
March 2019
2 Reads

Fetal neural stem cells from a mouse model of 15q11-13 duplication syndrome exhibit altered differentiation into neurons and astrocytes.

J Pharmacol Sci 2019 Mar 28;139(3):249-253. Epub 2018 Dec 28.

Department of Pharmacology, College of Medicine, Seoul National University, 103 Daehakro, Jongro-gu, Seoul, 110-799, Republic of Korea; Department of Biomedical Sciences, College of Medicine, Seoul National University, 103 Daehakro, Jongro-gu, Seoul, 110-799, Republic of Korea; Seoul National University Bundang Hospital, Seongnam, 463-707, South Korea; Neuroscience Research Institute, College of Medicine, Seoul National University, 103 Daehakro, Jongro-gu, Seoul, 110-799, Republic of Korea. Electronic address:

The duplication of human chromosome 15q11-13 is known to be associated with an estimated 1.1% of autism cases. Here, we investigated whether differentiation into neurons and astrocytes is altered in fetal neural stem cells (FNSCs) isolated from the mouse model of 15q11-13 duplication syndrome (patDp/+ mice). Read More

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http://dx.doi.org/10.1016/j.jphs.2018.12.007DOI Listing
March 2019
1 Read

Qingnao dripping pills mediate immune-inflammatory response and MAPK signaling pathway after acute ischemic stroke in rats.

J Pharmacol Sci 2019 Mar 22;139(3):143-150. Epub 2019 Jan 22.

Central Laboratory, Dongfang Hospital, Beijing University of Chinese Medicine, 6 Zone One of Fangxingyuan, Fang Zhuang, Feng Tai District, Beijing, 100078, China. Electronic address:

The aim of the present study was to examine the neuroprotective effect of Qingnao dripping pills (QNDP), especially the infiltration of neutrophils and macrophages, as well as the mitogen-activated protein kinase (MAPK) signal pathway. Adult male Sprague-Dawley rats were randomized to three groups: sham, MCAO, and QNDP. After 24 h of ischemia and reperfusion, neurological deficit scores and infarct volume were measured. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.12.009DOI Listing
March 2019
1 Read
2.360 Impact Factor

Oxyresveratrol protects human lens epithelial cells against hydrogen peroxide-induced oxidative stress and apoptosis by activation of Akt/HO-1 pathway.

J Pharmacol Sci 2019 Mar 22;139(3):166-173. Epub 2019 Jan 22.

Department of Ophtalmology, Huaihe Hospital of Henan University, Kaifeng 475000, PR China.

Oxidative stress induced by hydrogen peroxide (HO) triggers human lens epithelial cell (HLEC) apoptosis and initiates cataract formation. Oxyresveratrol (Oxy) was reported to possess antioxidant and free radical scavenging activities. Herein, we investigated the effects of Oxy on HO-induced oxidative stress and apoptosis in HLECs and the associated mechanisms. Read More

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https://linkinghub.elsevier.com/retrieve/pii/S13478613193000
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http://dx.doi.org/10.1016/j.jphs.2019.01.003DOI Listing
March 2019
6 Reads

Systemic administration of a delta opioid receptor agonist, KNT-127, facilitates extinction learning of fear memory in rats.

J Pharmacol Sci 2019 Mar 17;139(3):174-179. Epub 2019 Jan 17.

Department of Neuropsychopharmacology, National Institute of Mental Health, National Center of Neurology and Psychiatry, 4-1-1 Ogawahigashimachi, Kodaira, Tokyo 187-8553, Japan. Electronic address:

Strategies to facilitate extinction of fear memory have attracted increasing attention for enhancing the effectiveness of exposure therapy for anxiety disorders. Previously, we demonstrated that systemic administration of a delta opioid receptor agonist, KNT-127, has clear anxiolytic-like effects in rats, without impairing memory. These observations led us to hypothesize that KNT-127 might be an appropriate therapeutic agent for anxiety disorders when combined with exposure therapy. Read More

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http://dx.doi.org/10.1016/j.jphs.2019.01.002DOI Listing
March 2019
1 Read

Post-treatment with JP-1302 protects against renal ischemia/reperfusion-induced acute kidney injury in rats.

J Pharmacol Sci 2019 Mar 31;139(3):137-142. Epub 2018 Dec 31.

Laboratory of Clinical Pharmacology, Faculty of Pharmacy, Osaka Ohtani University, 3-11-1 Nishikiori-kita, Tondabayashi, Osaka, 584-8540, Japan.

Ischemia/reperfusion injury is the most common cause of acute kidney injury. We previously revealed that pre-treatment with yohimbine or JP-1302 attenuated renal ischemia/reperfusion injury by inhibition of α2C-adrenoceptor antagonist. The aim of the present study is to investigate the effects of post-treatment with JP-1302 on renal ischemia/reperfusion injury in rats. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.12.008DOI Listing
March 2019
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Chotosan ameliorates cognitive impairment and hippocampus neuronal loss in experimental vascular dementia via activating the Nrf2-mediated antioxidant pathway.

J Pharmacol Sci 2019 Feb 22;139(2):105-111. Epub 2018 Dec 22.

Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 211198, People's Republic of China; Key Laboratory of Biomedical Functional Materials, China Pharmaceutical University, Nanjing, 211198, People's Republic of China. Electronic address:

Recent studies suggested that Chotosan has ameliorative effects on vascular dementia through antioxidative pathways. Nevertheless, no systematic pharmacological research was conducted to evaluate the contribution of nuclear factor-E2-related factor 2 (Nrf2), a crucial regulator of antioxidative system, on Chotosan-induced neuroprotection invascular dementia. The present study aimed to investigate the neuroprotective effect of Chotosan on vascular dementia and reveal the possible molecular mechanism involving Nrf2. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.12.003DOI Listing
February 2019
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Probucol ameliorates hepatic stellate cell activation and autophagy is associated with farnesoid X receptor.

J Pharmacol Sci 2019 Feb 21;139(2):120-128. Epub 2018 Dec 21.

Department of Pharmacology, College of Medicine and Health, Lishui University, Lishui, 323000, China. Electronic address:

Probucol has antioxidant effects and inhibits inflammation. Farnesoid X receptor (FXR) is a nuclear receptor that regulates autophagy, which is regarded as the key cause of the activation of hepatic stellate cell (HSC). In this study, the effects of probucol on HSC activation and autophagy in vitro and vivo and the role of FXR in this progress were investigated. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.12.005DOI Listing
February 2019
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A dipeptidyl peptidase-4 (DPP-4) inhibitor, linagliptin, attenuates cardiac dysfunction after myocardial infarction independently of DPP-4.

J Pharmacol Sci 2019 Feb 18;139(2):112-119. Epub 2018 Dec 18.

Department of Pharmacology, Osaka City University Graduate School of Medicine, Osaka, Japan; Department of Internal Medicine, Takaishikamo Hospital, Osaka, Japan. Electronic address:

Dipeptidyl peptidase-4 (DPP-4) inhibitors not only improve impaired glucose tolerance in diabetes, but also have pleiotropic extra-pancreatic effects such as preconditioning effect for myocardial ischemia-reperfusion injury. Here, we investigated the anti-remodeling effects of linagliptin, a DPP-4 inhibitor, by use of DPP-4-deficient rats. After the induction of myocardial infarction (MI), Fischer 344 rats with inactivating mutation of DPP-4 were orally administrated with a DPP-4 inhibitor, linagliptin (5 mg kg·day), or vehicle in drinking water for 4 weeks. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.12.004DOI Listing
February 2019
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5-HT deletion protects against Clozapine-induced hyperglycemia.

J Pharmacol Sci 2019 Feb 18;139(2):133-135. Epub 2018 Dec 18.

National Centre for Biological Sciences, TIFR, GKVK Campus, Bellary Road, Bengaluru, India; Department of Physiology and Biophysics, School of Medicine, University of California, Irvine, CA, USA. Electronic address:

Clozapine is an antipsychotic known for its superior efficacy in treating drug-resistant Schizophrenia. However, Clozapine induces various side effects such as hyperglycemia, agranulocytosis, weight gain etc. The mechanisms of these Clozapine-induced side effects have remained largely elusive though an important role is ascribed to 5-HT (Serotonin receptor subtype-2A). Read More

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http://dx.doi.org/10.1016/j.jphs.2018.11.015DOI Listing
February 2019
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Alzheimer's disease therapeutic candidate SAK3 is an enhancer of T-type calcium channels.

J Pharmacol Sci 2019 Feb 18;139(2):51-58. Epub 2018 Dec 18.

Institute of Pharmacology and Toxicology and Biochemical Pharmaceutics, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.

Low-threshold Ca spikes are mediated by T-type Ca channels, which have electrophysiological properties of fast inactivation and slow deactivation kinetics. A low membrane potential of approximately -60 mV is sufficient to trigger channel opening. We recently introduced a novel T-type Ca channel enhancer that improves cognition and inhibits amyloid beta aggregation in an Alzheimer's disease (AD) mouse model. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.11.014DOI Listing
February 2019
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Fibroblast growth factor 2 modulates extracellular purine metabolism by upregulating ecto-5'-nucleotidase and adenosine deaminase in cultured rat spinal cord astrocytes.

J Pharmacol Sci 2019 Feb 14;139(2):98-104. Epub 2018 Dec 14.

Laboratory of Pharmacology, Department of Basic Veterinary Sciences, Faculty of Veterinary Medicine, Hokkaido University, Kita 18, Nishi 9, Kita-ku, Sapporo 060-0818, Japan. Electronic address:

Purinergic signaling via ATP and adenosine produced by astrocytes is one pathway underlying neuron-glia interactions in the central nervous system (CNS). In production of purines, extracellular metabolism of released purines via ecto-enzymes is important. The expression and activities of these enzymes are altered under pathological conditions. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.12.002DOI Listing
February 2019
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Daphnetin inhibits high glucose-induced extracellular matrix accumulation, oxidative stress and inflammation in human glomerular mesangial cells.

J Pharmacol Sci 2019 Feb 7;139(2):91-97. Epub 2018 Dec 7.

Department of Nephrology, Xinxiang Central Hospital, Xinxiang 453000, Henan, China.

Diabetic nephropathy (DN) is one of the most common causes of end-stage renal disease (ESRD). Oxidative stress and inflammation have been documented to play important roles in the pathogenesis of DN. Daphnetin, a natural coumarin compound, possesses antioxidant and anti-inflammatory activities. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.11.013DOI Listing
February 2019
3 Reads

A current perspective of canstatin, a fragment of type IV collagen alpha 2 chain.

J Pharmacol Sci 2019 Feb 10;139(2):59-64. Epub 2018 Dec 10.

Laboratory of Veterinary Pharmacology, School of Veterinary Medicine, Kitasato University, Higashi 23 Bancho 35-1, Towada City, Aomori 034-8628, Japan.

Type IV collagen is a main component of basement membrane extracellular matrix. Canstatin, a non-collagenous C-terminal fragment of type IV collagen α2 chain, was firstly identified as an endogenous anti-angiogenic and anti-tumor factor, which also has an anti-lymphangiogenic effect. Then, canstatin has been widely investigated as a novel target molecule for cancer therapy. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.12.001DOI Listing
February 2019
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Carteolol hydrochloride reduces visible light-induced retinal damage in vivo and BSO/glutamate-induced oxidative stress in vitro.

J Pharmacol Sci 2019 Feb 6;139(2):84-90. Epub 2018 Dec 6.

Department of Ophthalmology, Shimane University Faculty of Medicine, Izumo, Japan. Electronic address:

The purpose of this study was to determine whether carteolol eye drops, a β-adrenoceptor antagonist used as an intraocular hypotensive agent, has protective effects against the light-induced oxidative stress in retina. Dark-adapted pigmented rats were pre-treated with topical carteolol ophthalmic solution or saline and then exposed to visible light. The effects on electroretinogram (ERG), morphology, oxidative stress, and expression of mRNAs in the retinas were determined. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.11.010DOI Listing
February 2019
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Role of neurosteroid allopregnanolone on age-related differences in exercise-induced hypoalgesia in rats.

J Pharmacol Sci 2019 Feb 30;139(2):77-83. Epub 2018 Nov 30.

Department of Anesthesiology and Intensive Care Medicine, Kochi Medical School, Nankoku, Kochi, Japan.

The beneficial effects of physical activity for pain are denominated exercise-induced hypoalgesia (EIH). Here, we examined the age-related change and potential role of the neurosteroid allopregnanolone (ALLO) on EIH in rats. Adult and aged rats were randomly divided into one of three groups; non-exercise control, Low-exercise, and High-exercise. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.11.009DOI Listing
February 2019
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Reduced variability in tacrolimus pharmacokinetics following intramuscular injection compared to oral administration in cynomolgus monkeys: Investigating optimal dosing regimens.

J Pharmacol Sci 2019 Feb 11;139(2):65-71. Epub 2018 Dec 11.

Department of Surgery, Samsung Medical Center, Sungkyunkwan University School of Medicine, Seoul, South Korea. Electronic address:

Tacrolimus is one of the most commonly used immunosuppressive agents in animal models of transplantation. However, in these models, oral administration is often problematic due to the lowered compliance associated with highly invasive surgery and due to malabsorption in the intestinal tract. Therefore, we carried out a study to determine the pharmacokinetics of tacrolimus after intramuscular (IM) injection and to determine the optimal IM dosing regimens in primate models. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.05.013DOI Listing
February 2019
3 Reads

PPARγ overexpression regulates cholesterol metabolism in human L02 hepatocytes.

J Pharmacol Sci 2019 Jan 30;139(1):1-8. Epub 2018 Nov 30.

Department of General Surgery, The First Affiliated Hospital of Nanjing Medical University, Nanjing, 210000, Jiangsu, China. Electronic address:

Peroxisome proliferator-activator receptor (PPAR) γ is a nuclear hormone receptor that regulates glucose homeostasis, lipid metabolism, and adipocyte function. It has been shown that activation of PPARγ can reduce the incidence of gallstone. Herein we aimed to clarify the role of PPARγ in the reduction of gallstones. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.09.013DOI Listing
January 2019
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The novel small-molecule antagonist of PAC1 receptor attenuates formalin-induced inflammatory pain behaviors in mice.

J Pharmacol Sci 2019 Feb 1;139(2):129-132. Epub 2018 Dec 1.

Department of Pharmacology, Graduate School of Medical and Dental Sciences, Kagoshima University, Kagoshima, Japan.

We recently developed PA-8, a novel small-molecule antagonist of PACAP type 1 (PAC1) receptor. In the present study, we examined whether PA-8 was effective against formalin-induced inflammatory pain in mice. Both intrathecal and oral administration of PA-8 resulted in the dose-dependent attenuation of the second phase of formalin-induced nociceptive responses. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.11.011DOI Listing
February 2019
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Kamiuntanto increases prefrontal extracellular serotonin levels and ameliorates depression-like behaviors in mice.

J Pharmacol Sci 2019 Feb 30;139(2):72-76. Epub 2018 Nov 30.

Laboratory of Functional Biomolecules and Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Setsunan University, 45-1 Nagaotoge-cho, Hirakata, Osaka 573-0101, Japan. Electronic address:

Kamiuntanto (KUT; Jia Wei Wen Dan Tang in Pinyin) is a traditional Japanese Kampo medicine that is used to treat psychological dysfunction. However, the mechanisms of action of KUT are not understood. To investigate the mechanisms underlying the ameliorative properties of KUT, the effects of KUT on abnormal behaviors of isolation-reared mice and on the prefrontal monoaminergic system were examined. Read More

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February 2019
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Pioglitazone improves visceral sensation and colonic permeability in a rat model of irritable bowel syndrome.

J Pharmacol Sci 2019 Jan 24;139(1):46-49. Epub 2018 Nov 24.

Division of Gastroenterology and Hematology/Oncology, Department of Medicine, Asahikawa Medical University, 2-1-1-1 Midorigaoka-Higashi, Asahikawa, Hokkaido 078-8510, Japan; Department of General Medicine, Asahikawa Medical University, 2-1-1-1 Midorigaoka-Higashi, Asahikawa, Hokkaido 078-8510, Japan.

Visceral hypersensitivity and impaired gut barrier with minor inflammation are considered to play an important role in the pathophysiology of irritable bowel syndrome (IBS). Since pioglitazone is known to have anti-inflammatory property, we hypothesized that pioglitazone is beneficial for treating IBS. In this study, the effect was tested in rat IBS models such as lipopolysaccharide or repeated water avoidance stress-induced visceral allodynia and increased colonic permeability. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.11.006DOI Listing
January 2019
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SKF-10047, a prototype Sigma-1 receptor agonist, augmented the membrane trafficking and uptake activity of the serotonin transporter and its C-terminus-deleted mutant via a Sigma-1 receptor-independent mechanism.

J Pharmacol Sci 2019 Jan 24;139(1):29-36. Epub 2018 Nov 24.

Department of Molecular and Pharmacological Neuroscience, Graduate School of Biomedical & Health Sciences, Hiroshima University, 1-2-3 Kausmi, Minami-ku, Hiroshima 734-8551, Japan. Electronic address:

The serotonin transporter (SERT) is functionally regulated via membrane trafficking. Our previous studies have demonstrated that the SERT C-terminal deletion mutant (SERTΔCT) showed a robust decrease in its membrane trafficking and was retained in the endoplasmic reticulum (ER), suggesting that SERTΔCT is an unfolded protein that may cause ER stress. The Sigma-1 receptor (SigR1) has been reported to attenuate ER stress via its chaperone activity. Read More

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http://dx.doi.org/10.1016/j.jphs.2018.11.005DOI Listing
January 2019
2 Reads