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Biological & Pharmaceutical Bulletin

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https://read.qxmd.com/read/30726781/analysis-of-an-impurity-n-nitrosodimethylamine-in-valsartan-drug-substances-and-associated-products-using-gc-ms
#1
Tomoaki Tsutsumi, Hiroshi Akiyama, Yosuke Demizu, Nahoko Uchiyama, Sayaka Masada, Genichiro Tsuji, Ryoko Arai, Yasuhiro Abe, Takashi Hakamatsuka, Ken-Ichi Izutsu, Yukihiro Goda, Haruhiro Okuda
Valsartan products, commonly used to treat high blood pressure and heart failure, have been recalled in many countries due to the presence of an impurity, N-nitrosodimethylamine (NDMA), in the recalled products. We present and evaluate a GC-MS-based analytical method for the determination of NDMA levels and attempt an investigation of NDMA concentrations in valsartan drug substances and associated products. The limit of detection and limit of quantification for the method were estimated to be 0.1 µg/g and 0...
February 7, 2019: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30713268/effect-of-selective-serotonin-5-ht-2b-receptor-agonist-bw723c86-on-epidermal-growth-factor-transforming-growth-factor-%C3%AE-receptor-tyrosine-kinase-and-ribosomal-p70-s6-kinase-activities-in-primary-cultures-of-adult-rat-hepatocytes
#2
Kota Naito, Kazuki Kurihara, Hajime Moteki, Mitsutoshi Kimura, Hideshi Natsume, Masahiko Ogihara
Serotonin (5-hydroxytryptamine; 5-HT) can induce hepatocyte DNA synthesis and proliferation by autocrine secretion of transforming growth factor (TGF)-α through 5-HT2B receptor/phospholipase C (PLC)/Ca2+ and a signaling pathway involving epidermal growth factor (EGF)/TGF-α receptor tyrosine kinase (RTK)/extracellular signal-regulated kinase 2 (ERK2)/mammalian target of rapamycin (mTOR). In the present study, we investigated whether 5-HT or a selective 5-HT2B receptor agonist BW723C86, would stimulate phosphorylation of TGF-α RTK and ribosomal p70 S6 kinase (p70S6K) in primary cultures of adult rat hepatocytes...
February 1, 2019: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30700647/inhibition-of-mapks-signaling-pathways-prevents-acrolein-induced-neurotoxicity-in-ht22-mouse-hippocampal-cells
#3
Mengting Liu, YingJuan Huang, Jian Qin, YuanYuan Wang, Bin Ke, YuBin Yang
Activation of mitogen-activated protein kinases (MAPKs) in neurons may underlie the pathogenesis of Alzheimer's disease (AD). Acrolein, a ubiquitous pollutant, has been reported to implicate in the etiology of AD. Our previous data showed that acrolein changed the levels of key AD-associated proteins, including advanced glycation end products (RAGE), A-disintegrin and metalloprotease (ADAM-10), and beta-site amyloid-beta peptide cleaving enzyme 1(BACE-1). In this study, we investigated whether acrolein-induced alterations of AD-associated proteins are relevant to MAPKs activation, and strategies to inhibit MAPKs activation yield benefits to acrolein-induced neurotoxicity in HT22 mouse hippocampal cells...
January 29, 2019: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30686807/usp34-regulated-human-pancreatic-cancer-cell-survival-via-akt-and-pkc-pathways
#4
Zhiwei Gu, Changjie Lin, Jian Hu, Jing Xia, Shaohua Wei, Dekang Gao
Pancreatic cancer is known to be a fatal disease, which is difficult to be diagnosed in its early stages. USP34 (Ubiquitin-Specific Protease 34) are closely related to human cancers in the development and progression. However, there are rarely studies about the role of USP34 in pancreatic cancer. Thus, we aimed to investigate the effect of USP34 in human pancreatic cancer. Short-hairpin RNA targeting USP34 (USP34-shRNA) and USP34 overexpression lentivirus were used in the current study. The level of USP34 in human pancreatic cancer (PANC-1) cells were then analyzed by qRT-PCR...
January 26, 2019: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30686806/adjustment-of-conditions-for-combining-oxybutynin-transdermal-patch-with-heparinoid-cream-in-mice-by-analyzing-blood-concentrations-of-oxybutynin-hydrochloride
#5
Yoshihito Murakami, Hidehisa Sekijima, Yutaka Fujisawa, Kazuya Ooi
The combination of skin external preparation and transdermal patch is influenced by drug absorption through the skin. We investigated the effect of heparinoid cream on the transdermal absorption of oxybutynin hydrochloride using an oxybutynin transdermal patch and determined the combined effect of these medications. Normal skin and dry dorsal skin in hairless mice were treated with heparinoid cream, followed by the application of the oxybutynin transdermal patch. A blood sample was collected from the mouse tail vein and the blood concentration of oxybutynin hydrochloride was analyzed by LC-MS/MS...
January 25, 2019: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30674757/a-novel-animal-model-of-induced-breast-precancerous-lesion-in-tree-shrew
#6
Maojian Chen, Chao Ou, Chun Yang, Weiping Yang, Qinghong Qin, Wei Jiang, Qixing Tan, Anyun Mao, Xiaoli Liao, Xinqing Ye, Changyuan Wei
Chinese tree shrew, an animal exhibited closer evolutionary relationship with humans compared to rodents, is getting increasingly attentions as an appealing experimental animal model for human diseases. However, a high-efficiency and stable method to establish tree shrew breast precancerous lesions model has not been clearly elucidated. Thus, the current study aimed to explore the way of establishing breast precancerous model in tree shrew and investigate the pathologic characteristics of induced breast precancerous lesions...
January 24, 2019: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30626802/curcumin-down-regulates-toll-like-receptor-2-gene-expression-and-function-in-human-cystic-fibrosis-bronchial-epithelial-cells
#7
Niraj Chaudhary, Keiko Ueno-Shuto, Tomomi Ono, Yuko Ohira, Kenji Watanabe, Aoi Nasu, Haruka Fujikawa, Ryunosuke Nakashima, Noriki Takahashi, Mary Ann Suico, Hirofumi Kai, Tsuyoshi Shuto
Cystic fibrosis (CF), the most common lethal inherited disorder caused by mutation in the gene encoding the CF transmembrane regulator (CFTR), is characterized by chronic inflammation that ultimately leads to death from respiratory failure. In CF patients, up-regulation of toll-like receptor-2 (TLR2), a pattern recognition receptor that senses CF-pathogenic bacteria Staphylococcus aureus peptidoglycan (PGN), in airway epithelial cells is observed, and enhanced proinflammatory responses towards PGN may result in detrimental effects in CF patients...
January 10, 2019: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30626801/histone-deacetylase-inhibitor-saha-treatment-prevents-the-development-of-heart-failure-after-myocardial-infarction-via-an-induction-of-heat-shock-proteins-in-rats
#8
Shiho Nagata, Tetsuro Marunouchi, Kouichi Tanonaka
Protein quality control (PQC) in the heart plays an important role to maintain cellular protein homeostasis. Impairment of PQC may cause the development of heart failure. It is well known that histone deacetylase 6 (HDAC6) is an essential enzyme for regulating the cellular PQC response. In this study, we aimed at examining the association between HDAC6 and the chaperone system and the effects of HDAC6 inhibition in the development of heart failure following myocardial infarction (MI). MI was induced by coronary artery ligation...
January 10, 2019: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30626800/expression-and-characterization-of-the-human-intestinal-bacterial-enzyme-which-cleaves-the-c-glycosidic-bond-in-3-oxo-puerarin
#9
Kenichi Nakamura, Shu Zhu, Katsuko Komatsu, Masao Hattori, Makoto Iwashima
Puerarin (daidzein 8-C-glucoside) is an isoflavone C-glucoside contained in the roots of Pueraria lobata Ohwi. We have previously isolated the human intestinal bacterium, strain PUE, which metabolizes puerarin to daidzein, though the enzyme which cleaves C-glycosidic bond has not been clarified. Here, we identified one of the intermediates of enzymatic puerarin C-deglycosylation reaction as 3″-oxo-puerarin (1): C-3 in the glucose moiety connecting to hydroxyl is oxidized to ketone group. 1 was easily isomerized to the mixture of 1, 2"-oxo-puerarin (2a) and cyclic acetal (2b) of 2a in non-enzymatic condition...
January 10, 2019: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30606896/juglone-inhibits-proliferation-of-hpv-positive-cervical-cancer-cells-specifically
#10
Xingyu Zhao, Xiaoxing Song, Jierui Zhao, Wenhe Zhu, Jiangcheng Hou, Yanchun Wang, Wei Zhang
Human papillomaviruses (HPVs), such as HPV 16 and HPV 18 are related to cervical cancer. Therefore, it is important to inhibit HPV-positive cervical cancer for treating cervical cancer. This study is aiming at investigating the proposed molecular mechanism, which underlies the antineoplastic potential of the aqueous extract of juglone of HPV-positive cervical cancer cells. According to the results, it is showed that, juglone prohibited HPV positive cervical cancer cells' growth through dose-dependent way. Nevertheless, when pin 1 was knocked down, the proliferation inhibition reduced...
December 28, 2018: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30606895/circulating-concentrations-of-insulin-resistance-associated-hepatokines-selenoprotein-p-and-leukocyte-cell-derived-chemotaxin-2-during-an-oral-glucose-tolerance-test-in-humans
#11
Kensuke Mohri, Hirofumi Misu, Hiroaki Takayama, Kiyo-Aki Ishii, Akihiro Kikuchi, Fei Lan, Yasufumi Enyama, Yumie Takeshita, Yoshiro Saito, Shuichi Kaneko, Toshinari Takamura
A hepatokine is a collective term for liver-derived secretory factors whose previously-unrecognized functions have been recently elucidated. We have rediscovered selenoprotein P (SeP) and leukocyte cell-derived chemotaxin 2 (LECT2) as hepatokines that are involved in the development of insulin resistance and hyperglycemia. The aim of this study was to determine whether and, if so, how oral glucose loading alters the two hepatokines in humans. We measured concentrations of serum SeP and plasma LECT2 during 75g oral glucose tolerance test (OGTT) (n = 20) in people with various degrees of glucose tolerance...
December 28, 2018: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30587670/hyperbaric-oxygen-combined-with-5-aminolevulinic-acid-photodynamic-therapy-inhibited-human-squamous-cell-proliferation
#12
Li-Hong Mei, Gao Yang, Fang Fang
The photodynamic therapy (PDT) depends on the presence of molecular oxygen. Thus, the efficiency of PDT is limited in anoxic regions of tumor tissue and vascular shutdown. It is reported the use of hyperbaric oxygen (HBO) may enhance the efficiency of PDT. However, there are rarely studies about utilizing HBO plus PDT for treatment with human squamous cell carcinoma (SCC). Therefore, this study aimed to investigate and compare the therapeutic effect of combined therapy and PDT alone treatment. Multiple cellular and molecular biology techniques were used in the current study such as CCK-8, western blotting, flow cytometry, MDC staining and immunofluorescence assay...
December 27, 2018: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30587668/panax-notoginseng-saponins-attenuate-oxygen-glucose-deprivation-reoxygenation-induced-injury-in-human-sh-sy5y-cells-by-regulating-the-expression-of-inflammatory-factors-through-mir-155
#13
Lanqing Meng, Jun Lin, Qing Huang, Ping Liang, Jianmin Huang, Chongdong Jian, Chong Lin, Xuebin Li
Panax notoginseng saponins (PNS) have been widely used in China to treat stroke. Accumulating evidence has found that miR-155 plays critical roles in the pathology of ischemic stroke. Here we investigated whether PNS plays a protective effect against oxygen-glucose deprivation/reoxygenation (OGD/R)-induced focal inflammation and injury in SH-SY5Y cells by regulating miR-155 expression. Treatment with PNS at a concentration less than 160 µg/mL had no effect on the proliferation of SH-SY5Y cell. In OGD/R-induced SH-SY5Y cells, 160 µg/mL PNS treatment promoted cell proliferation and cell cycle progression, as well as decreased inhibited apoptosis and miR-155 expression...
December 26, 2018: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30568106/evaluation-of-in-vitro-bactericidal-activity-of-1-5-olanexidine-gluconate-a-novel-biguanide-antiseptic-agent
#14
Shoji Seyama, Hisae Nishioka, Hidemasa Nakaminami, Keisuke Nakase, Takeaki Wajima, Akifumi Hagi, Norihisa Noguchi
Recently, 1.5% olanexidine gluconate, a biguanide compounds, was launched as a new antiseptic agent in Japan. However, the comprehensive bactericidal spectrum of olanexidine gluconate is still unknown. In this study, we evaluated in vitro bactericidal activity of olanexidine gluconate using time-kill assay against various bacteria, mycobacteria, and fungi. With the exception of Burkholderia cepacia and Mycobacterium spp., 1.5% olanexidine gluconate exhibited fast-acting (<60 s) bactericidal activity against all tested gram-positive and gram-negative bacteria, including vancomycin-resistant Enterococcus faecalis, methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, extended spectrum β-lactamase producing Klebsiella pneumoniae, and multidrug-resistant Pseudomonas aeruginosa...
December 20, 2018: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30531092/the-yeast-minichromosome-system-consisting-of-highly-positioned-nucleosomes-in-vivo
#15
Tomohiro Fuse, Akio Yanagida, Mitsuhiro Shimizu
In eukaryotic genomes, the nucleosome is the structural and functional unit, and its position and dynamics are important for gene expression control and epigenetic regulation. Epigenetics is an important mechanism in development and homeostasis, and aberrant epigenetics is a common feature in cancer. Although understanding the mechanistic basis that determines nucleosome positioning in vivo is important for elucidating chromatin function and epigenetic regulation, a suitable experimental system to examine such mechanisms is still being developed...
December 7, 2018: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30518742/zhongfenggao-protects-brain-microvascular-endothelial-cells-from-oxygen-glucose-deprivation-reoxygenation-induced-injury-by-angiogenesis
#16
Shenghui Huang, Ting Gong, Tengfei Zhang, Xinfeng Wang, Qianqian Cheng, Yanyi Li
Zhongfenggao (ZFG) is prescribed for the treatment of cerebrovascular diseases in critical projects of the State Administration of Traditional Chinese Medicine. ZFG has been found to nourish qi, activate blood circulation, remove blood stasis, dredge collaterals, and strengthen the brain and mind. The present study investigated the effects of ZFG on oxygen-glucose deprivation/reoxygenation (OGD/R) induced injury to brain microvascular endothelial cells (BMECs), and the mechanisms underlying such effects. BMECs are essential target cells of ischemic stroke...
December 5, 2018: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30504641/the-comparison-of-surface-free-energy-of-human-yucatan-micropig-and-hairless-mouse-skins-and-influence-of-surfactant-on-surface-free-energy-of-the-skin
#17
Makiko Fujii, Kiku Kato, Miko Imai, Hiroki Kuwabara, Minori Awano, Kaname Hashizaki, Hiroyuki Taguchi
Surface free energy (SFE) is an important factor for evaluation of wettability or adhesion. Thus, the SFE of a Yucatan micropig (YMP) skin and a hairless mouse (HM) skin, which are commonly used in skin permeation studies instead of human skin, were compared with the human skin. Contact angles of water and 1-bromo naphthalene to skin were measured and the SFE was calculated using the Owens-Wendt equation. The SFE of the human abdominal skin was 40 mN/m and its polar component σs p was as low as 2 mN/m, which was similar to that of the low sebum skin reported previously...
December 1, 2018: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30504654/a-new-series-of-salicylic-acid-derivatives-as-non-saccharide-%C3%AE-glucosidase-inhibitors-and-antioxidants
#18
Jiangang Chen, Wenfang Lu, Hao Chen, Xiaoli Bian, Guangde Yang
In this study, a series of salicylic acid derivatives were designed and synthesized as novel non-saccharide α-glucosidase inhibitors. Biological evaluation indicated that when compared to acarbose, compounds T9, T10, and T32 exhibited a higher potency of α-glucosidase inhibitory activity with IC50 values of 0.15 ± 0.01 mM, 0.086 ± 0.01 mM and 0.32 ± 0.02 mM, respectively. Evaluation of the inhibition kinetics indicated that T9, T10, T32, and acarbose interacted with α-glucosidase in a mixed non-competitive inhibitory manner...
November 30, 2018: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30464092/triterpenoid-saponins-from-ardisia-gigantifolia-stapf-and-mechanism-on-inhibiting-proliferation-of-mda-mb-231-cells
#19
Li-Hua Mu, Hong Yan, Yu-Ning Wang, Teng-Fei Yu, Ping Liu
Seventeen 13, 28-epoxy triterpenoid saponins obtained from Ardisia gigantifolia stapf. were evaluated their anti-proliferative activities on MCF-7 cells. The structure-activity relationship analysis indicated that CH3 group at C-30, four saccharide units with L-rhamnose at R6 in the sugar units are crucial for the cytotoxic activity on MCF-7. Compounds 1, 2, 6, 7, 12, 14 were selected to identify the anti-proliferative activity on the other three breast cancer cell lines (T47D, MDA-MB-231 and SK-BR-3). Compounds (2, 6, 7) with good activity on MCF-7 also showed activity on T47D, MDA-MB-231 and SK-BR-3...
November 21, 2018: Biological & Pharmaceutical Bulletin
https://read.qxmd.com/read/30713260/inhibition-of-the-inflammatory-pathway-enhances-both-the-in-vitro-and-in-vivo-transfection-activity-of-exogenous-in-vitro-transcribed-mrnas-delivered-by-lipid-nanoparticles
#20
Takara Ohto, Manami Konishi, Hiroki Tanaka, Koji Onomoto, Mitsutoshi Yoneyama, Yuta Nakai, Kota Tange, Hiroki Yoshioka, Hidetaka Akita
While the use of in vitro-transcribed mRNA (IVT-mRNA) in therapeutics is a rapidly expanding area, the transfection of the exogenous IVT-mRNA is accompanied by a risk of immune activation. This immunological defense mechanism suppresses cellular translation process and can reduce transfection efficiency to a considerable extent. In the present study, we investigated the in vitro effects of Integrated Stress Response Inhibitor (ISRIB), and dexamethasone, a steroidal anti-inflammatory drug, on the transfection activity of a lipid nanoparticle (LNP) that was composed of ionizable lipids and IVT-mRNA...
2019: Biological & Pharmaceutical Bulletin
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