Membrane Transporters Contributing to PGE2 Distribution in Central Nervous System.
Abstract Prostaglandin (PG) E2 is a well-established lipid mediator that plays a role in diverse functions and diseases of the brain. Cyclooxygenase and PGE synthase have been extensively studied as molecular determinants of extracellular concentration of PGE2 near prostanoid E receptors since the brain has limited capacity of PG metabolism. There is accumulating evidence that several members of the solute carrier (SLC) and ATP-binding cassette (ABC) superfamilies regulate PGE2 distribution in brain capillary endothelial cells, choroid plexus (CP) and arachnoid epithelium, and different parenchyma cells such as ne...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Nakamura Y, Nakanishi T, Tamai I Tags: Biol Pharm Bull Source Type: research

Molecular State of Active Pharmaceutical Ingredients in Ketoprofen Dermal Patches Characterized by Pharmaceutical Evaluation.
Abstract The molecular states of ketoprofen and the interaction between ketoprofen and other pharmaceutical excipients in the matrix layer were examined to determine their effect on the pharmaceutical properties of original and generic ketoprofen dermal patches (generic patches A and B). Molecular states of ketoprofen were evaluated using polarized light microscopy, Raman spectroscopy and powder X-ray diffraction. For the original ketoprofen patch, crystalline components were not observed in the matrix layer. However, crystalline ketoprofen was observed in the two generic ketoprofen patches. Moreover, the ketoprof...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Azuma M, Fujii M, Inoue M, Hisada H, Koide T, Kemper M, Yamamoto Y, Suzuki N, Suzuki T, Fukami T Tags: Biol Pharm Bull Source Type: research

Piceatannol-Induced Apoptosis Is Reversed by N-Acetyl-L-cysteine through Restoration of XIAP Expression.
Abstract Piceatannol, a naturally occurring stilbene derivative mainly found in grapes, possesses apoptotic activity in various cancer cell lines, in addition to potent antioxidant activity. In the current study, we showed that piceatannol exhibits potent cytotoxic effects in all tested leukemia cell lines (THP-1, HL-60, U937, and K562). These effects were accompanied by induction of DNA damage, an increase in the proportion of cells in the sub-G1 phase of the cell cycle, and inhibition of reactive oxygen species (ROS) generation. However, N-acetyl-L-cysteine (NAC), a strong ROS scavenger, significantly inhibited ...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Jin CY, Molagoda IMN, Park C, Kwon TK, Yun SJ, Kim WJ, Kim GY, Choi YH Tags: Biol Pharm Bull Source Type: research

High-Glucose Conditions Promote Anchorage-Independent Colony Growth in Human Breast Cancer MCF-7 Cells.
Abstract Previous studies have shown that hyperglycemia is connected to the malignant progression of breast cancer; however, the effects of hyperglycemia on tumorigenic potential in breast cancer cells are largely unknown. Here, we demonstrated that the ability of the human breast cancer cell line MCF-7 to undertake anchorage-independent colony growth was significantly enhanced when cultured under high-glucose conditions compared with that under physiological glucose conditions. The high-glucose conditions also promoted phosphorylation of Akt, suggesting that MCF-7 cells cultured in these conditions acquired an in...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Matsui C, Takatani-Nakase T, Maeda S, Takahashi K Tags: Biol Pharm Bull Source Type: research

Multiple Cellular Transport and Binding Processes of Unesterified Docosahexaenoic Acid in Outer Blood-Retinal Barrier Retinal Pigment Epithelial Cells.
Abstract Docosahexaenoic acid (DHA, 22 : 6) is an essential omega-3 long-chain polyunsaturated fatty acid that plays a pivotal role in vision. The purpose of this study was to clarify the cellular uptake and binding processes of free and protein-bound unesterified DHA in retinal pigment epithelial cell (RPE) line ARPE-19 as a model of the human outer blood-retinal barrier and isolated porcine RPE cell fractions. Uptake of free [14C]DHA by ARPE-19 cells was saturable with a Michaelis-Menten constant of 283 µM, and was significantly inhibited by eicosapentaenoic acid, arachidonic acid, and...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Tachikawa M, Akanuma SI, Imai T, Okayasu S, Tomohiro T, Hatanaka Y, Hosoya KI Tags: Biol Pharm Bull Source Type: research

Reduction of Thermotolerance by Heat Shock Protein 90 Inhibitors in Murine Erythroleukemia Cells.
Abstract Cells induce heat shock proteins (HSPs) against various stress. However, murine erythroleukemia (MEL) cells do not express HSP72, a heat-inducible member of HSP70 family. So, it is of interest to examine how MEL cells respond to heat stress (44°C, 30 min). Heat stress-induced apoptosis was suppressed by pretreatment of heat shock (44°C, 10 min). Such suppressive effects were maximal at 6 h after heat shock and remained up to 12 h. Interestingly, such effects of heat shock were abrogated by specific inhibitors of HSP90 such as 17-allylamino-17-demethoxygeldanamycin (17-A...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Uehara Y, Temma K, Kobayashi Y, Irie N, Yamaguchi T Tags: Biol Pharm Bull Source Type: research

Factors Predicting the Therapeutic Response to Methotrexate in Japanese Patients with Rheumatoid Arthritis: A Hospital-Based Cohort Study.
This study showed that the therapeutic response to MTX in Japanese RA patients was associated with the genetic polymorphisms of SLC19A1 80G>A and GGH 16T>C in actual clinical practice. PMID: 30175777 [PubMed - in process] (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Hakamata J, Kaneko Y, Shimizu M, Yamaoka K, Maruyama J, Takeuchi T, Mochizuki M, Hashiguchi M Tags: Biol Pharm Bull Source Type: research

Effect of Royal Jelly and Brazilian Green Propolis on the Signaling for Histamine H1 Receptor and Interleukin-9 Gene Expressions Responsible for the Pathogenesis of the Allergic Rhinitis.
Abstract The significant correlation between nasal symptom scores and level of histamine H1 receptor (H1R) mRNA in nasal mucosa was observed in patients with pollinosis, suggesting that H1R gene is an allergic disease sensitive gene. We demonstrated that H1R and interleukin (IL)-9 gene are the allergic rhinitis (AR)-sensitive genes and protein kinase Cδ (PKCδ) signaling and nuclear factor of activated T-cells (NFAT) signaling are involved in their expressions, respectively. Honey bee products have been used to treat allergic diseases. However, their pathological mechanism remains to be elucidated. In t...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Shaha A, Mizuguchi H, Kitamura Y, Fujino H, Yabumoto M, Takeda N, Fukui H Tags: Biol Pharm Bull Source Type: research

Investigation of Intracellular Delivery of NuBCP-9 by Conjugation with Oligoarginines Peptides in MDA-MB-231 Cells.
In this study, we conjugated NuBCP-9 with various Rn (n=8, 10, 12, 14) to investigate and compare their cellular uptake characteristics. In addition, their non-specific cytotoxicity and apoptosis-inducing abilities were evaluated. We found that NuBCP-9 conjugated with Rn enhanced cellular uptake mainly through clathrin-mediated endocytosis and macropinocytosis, and that the uptake pathways were not different from those used by unconjugated Rn. However, the cytotoxicity study showed that NuBCP-9-R12 and NuBCP-9-R14 conjugates enhanced non-specific cytotoxicity. We found that NuBCP-9-R10 conjugate had the highest uptake effi...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Wang W, Suga T, Hagimori M, Kuroda N, Fuchigami Y, Kawakami S Tags: Biol Pharm Bull Source Type: research

Effects of Supplementary Seleno-L-methionine on Atopic Dermatitis-Like Skin Lesions in Mice.
Abstract Effects of selenium supplementation on atopic dermatitis (AD) were investigated by administering seleno-L-methionine (SeMet) using a mouse model of AD caused by repeated application of 2,4,6-trinitrochlorobenzene (TNCB). BALB/c mice were sensitized with TNCB to the abdomen on day -7; then, TNCB was applied repeatedly to each ear three times a week from days 0 to 23. SeMet was orally administered to the mice from days 0 to 23. The efficacy of SeMet on AD was assessed by measuring ear thickness, histologic evaluation, serum total immunoglobulin (Ig) E levels, and expression of interleukin (IL)-4 in the ear ...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Arakawa T, Sugiyama T, Matsuura H, Okuno T, Ogino H, Sakazaki F, Ueno H Tags: Biol Pharm Bull Source Type: research

Functional Modulation of Nav1.2 Voltage-Gated Sodium Channels Induced by Escitalopram.
In this study, we investigated the effect of escitalopram in Nav1.2 voltage-gated sodium channels (VGSCs) transfected HEK293 cells. Nav1.2 VGSCs current decreased by approximately 50.7±8.3% under treatment with 100 µM escitalopram. The IC50 of escitalopram against Nav1.2 VGSCs was 114.17 µM. Moreover, the treatment with 100 µM escitalopram changed the voltage-dependence of inactivation and the voltage at half-maximal inactivation shifted significantly from -50.3±3.7 to -56.7±6.0 mV toward negative potential under treatment with 100 µM escitalop...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Nakatani Y, Amano T Tags: Biol Pharm Bull Source Type: research

Acquired Resistance to Shiga Toxin-Induced Apoptosis by Loss of CD77 Expression in Human Myelogenous Leukemia Cell Line, THP-1.
In this study, we isolated resistant clones to Stx-induced apoptosis from highly sensitive THP-1 cells by continuous exposure with lethal dose of Stx. All of the ten resistant clones lost the expression of CD77 as a consequence of the reduction in CD77 synthase mRNA expression. These results suggest that downregulation of CD77 or CD77 synthase expression could be a novel approach to suppress the fatal toxicity of Stx in EHEC infected patient. PMID: 30175782 [PubMed - in process] (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Hattori T, Watanabe-Takahashi M, Nishikawa K, Naito M Tags: Biol Pharm Bull Source Type: research

Globo-A Binds to the Recombinant Natural Cytotoxicity Receptor NKp44.
In this study, we investigated the binding between NCRs and glycolipids. The possible binding of glycolipids to NCRs was screened by microarray, using the recombinant extracellular domain of NKp46, NKp44 and NKp30 tagged with 6×His (rNKp46, rNKp44 and rNKp30). We found that rNKp44 binds to Globo-A. However, we did not detect the interaction between rNKp46 or rNKp30 and any of the glycolipids investigated. Direct binding assays supported the results of the microarray screening. Therefore, we concluded that Globo-A is a novel ligand for NKp44 but not NKp46 and NKp30, and showed differences in the ligand selectivity of ...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Ito K, Shiraishi R, Higai K Tags: Biol Pharm Bull Source Type: research

Daisaikoto Inhibits Pancreatic Lipase Activity and Decreases Serum Triglyceride Levels in Mice.
In conclusion, Daisaikoto represents a natural medicine, in particular SR, capable of inhibiting pancreatic lipase and lipid absorption. PMID: 30175784 [PubMed - in process] (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Matsuo Y, Matsumoto K, Inaba N, Mimaki Y Tags: Biol Pharm Bull Source Type: research

Durable Transgene Expression Driven by CpG-Free and -Containing Promoters in Plasmid DNA with CpG-Free Backbone.
Abstract The duration of transgene expression from plasmid DNAs is important for gene therapy with nonviral vectors. In the present study, various cytosine-phosphate-guanine (CpG)-free and CpG-containing transcription regulatory sequences were introduced into plasmid DNAs with a CpG-free backbone. The transgenes encoding mouse secreted alkaline phosphatase and Gaussia princeps luciferase, which are both apparently non-immunogenic, were used as reporters. The plasmid DNAs were injected by the hydrodynamics-based method, and the expression was monitored for 28 d. All transcription regulatory sequences achieve...
Source: Biological and Pharmaceutical Bulletin - September 5, 2018 Category: Drugs & Pharmacology Authors: Suzuki T, Goda T, Kamiya H Tags: Biol Pharm Bull Source Type: research

Analysis of Glycoforms and Amino Acids in Infliximab and a Biosimilar Product using New Method with LC/TOF-MS.
In conclusion, our analytical method can analyze not only amino acids but also carbohydrate chains of therapeutic antibodies, and will provide a useful strategy to evaluate bio-medicines including biosimilar antibodies. PMID: 30158337 [PubMed - as supplied by publisher] (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - August 30, 2018 Category: Drugs & Pharmacology Authors: Tsuda M, Otani Y, Yonezawa A, Masui S, Ikemi Y, Denda M, Sato Y, Nakagawa S, Omura T, Imai S, Nakagawa T, Hayakari M, Matsubara K Tags: Biol Pharm Bull Source Type: research

The Wakan-yaku Universe: A useful authorized traditional concept for developing novel therapeutic categories and medicinal drugs.
Abstract This review article mentions about the following points, and proposes its importance and positive thinking. 1) Wakan-yaku (Japanese oriental medicines) is covered by the national health insurance system in Japan as therapeutic drugs to be actively used in medical practice to treat illness. 2) Applications of Wakan-yaku is accomplished based on the reliable own theories which are established with long histories. 3) Promotion of studies based on these theories will be highly expected to find novel view points which breaks conventional concepts and to novel standards for developing new medicinal drugs. Altho...
Source: Biological and Pharmaceutical Bulletin - August 28, 2018 Category: Drugs & Pharmacology Authors: Tohda M, Watanabe H Tags: Biol Pharm Bull Source Type: research

Ginsenoside Rg1 protects against non-alcoholic fatty liver disease by ameliorating lipid peroxidation, endoplasmic reticulum stress, and inflammasome activation.
Abstract Nonalcoholic fatty liver disease (NAFLD) is increasingly prevalent and represents a growing challenge in terms of prevention and treatment. The purpose of this study is to investigate the protective effects of ginsenoside Rg1 (Rg1), an active ingredient of a natural medicine, and further clarify its protective mechanisms, in a mouse model of NAFLD induced by a high-fat diet. Rg1 significantly reduced liver weight, serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), triglyceride (TG), liver free fatty acids (FFAs) and malondialdehyde (MDA) levels, and increased superoxide dismutase (SOD...
Source: Biological and Pharmaceutical Bulletin - August 21, 2018 Category: Drugs & Pharmacology Authors: Xu Y, Yang C, Zhang S, Li J, Xiao Q, Huang W Tags: Biol Pharm Bull Source Type: research

The Role of Exosomes/Extracellular Vesicles in Neural Signal Transduction.
Abstract Exosomes, in a broad sense extracellular vesicles (EVs), are secreted from several cells and also exist in cerebrospinal fluid (CSF); they contribute to signal transduction not only between neural cells but also among hematopoietic cells. In addition to the peripheral nervous system, the association of regeneration and EVs has also been reported in the central nervous system, for example, following a spinal cord injury. Furthermore, it has become clear that major causative factors of neurodegenerative diseases are transmitted by EVs; thus, EVs are involved in the pathogenesis of neurodegenerative diseases...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Kawahara H, Hanayama R Tags: Biol Pharm Bull Source Type: research

Foreword.
PMID: 30068859 [PubMed - in process] (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Ohya S Tags: Biol Pharm Bull Source Type: research

Involvement of Voltage-Gated Calcium Channels in Inflammation and Inflammatory Pain.
Abstract Voltage-gated calcium channels (VGCCs) are classified into high-voltage-activated (HVA) channels and low-voltage-activated channels consisting of Cav3.1-3.3, known as T ("transient")-type VGCC. There is evidence that certain types of HVA channels are involved in neurogenic inflammation and inflammatory pain, in agreement with reports indicating the therapeutic effectiveness of gabapentinoids, ligands for the α2δ subunit of HVA, in treating not only neuropathic, but also inflammatory, pain. Among the Cav3 family members, Cav3.2 is abundantly expressed in the primary afferents, regulat...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Sekiguchi F, Tsubota M, Kawabata A Tags: Biol Pharm Bull Source Type: research

Role of Thermo-Sensitive Transient Receptor Potential Channels in Brown Adipose Tissue.
Abstract Brown and beige adipocytes are a major site of mammalian non-shivering thermogenesis and energy dissipation. Obesity is caused by an imbalance between energy intake and expenditure and has become a worldwide health problem. Therefore modulation of thermogenesis in brown and beige adipocytes could be an important application for body weight control and obesity prevention. Over the last few decades, the involvement of thermo-sensitive transient receptor potential (TRP) channels (including TRPV1, TRPV2, TRPV3, TRPV4, TRPM4, TRPM8, TRPC5, and TRPA1) in energy metabolism and adipogenesis in adipocytes has been...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Uchida K, Sun W, Yamazaki J, Tominaga M Tags: Biol Pharm Bull Source Type: research

Physiological and Pathological Functions of Cl- Channels in Chondrocytes.
Abstract Articular chondrocytes are embedded in the cartilage of diarthrodial joints and responsible for the synthesis and secretion of extracellular matrix. The extracellular matrix mainly contains collagens and proteoglycans, and covers the articular cartilage to protect from mechanical and biochemical stresses. In mammalian chondrocytes, various types of ion channels have been identified: e.g., voltage-dependent K+ channels, Ca2+-activated K+ channels, ATP-sensitive K+ channels, two-pore domain K+ channels, voltage-dependent Ca2+ channels, store-operated Ca2+ channels, epithelial Na+ channels, acid-sensing ion ...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Yamamura H, Suzuki Y, Imaizumi Y Tags: Biol Pharm Bull Source Type: research

Physiological and Pathophysiological Roles of Transient Receptor Potential Channels in Microglia-Related CNS Inflammatory Diseases.
Abstract Central nervous system (CNS) inflammation is a potential therapeutic target for neurodegenerative diseases. In recent years, a number of studies have focused on the links between neurodegenerative diseases and CNS glial cells, especially microglia. Microglia are the main resident immune cells in the CNS and represent approximately 10-15% of all CNS cells. Microglia play an important role in maintaining brain homeostasis at rest by surveying the environment, and engulfing apoptotic cells and debris in the healthy brain. However, under certain pathological conditions, microglia can generate neurotoxic facto...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Shirakawa H, Kaneko S Tags: Biol Pharm Bull Source Type: research

Ca2+-Activated K+ Channel KCa3.1 as a Therapeutic Target for Immune Disorders.
Abstract In lymphoid and myeloid cells, membrane hyperpolarization by the opening of K+ channels increases the activity of Ca2+ release-activated Ca2+ (CRAC) channels and transient receptor potential (TRP) Ca2+ channels. The intermediate-conductance Ca2+-activated K+ channel KCa3.1 plays an important role in cell proliferation, differentiation, migration, and cytokine production in innate and adaptive immune systems. KCa3.1 is therefore an attractive therapeutic target for allergic, inflammatory, and autoimmune disorders. In the past several years, studies have provided new insights into 1) KCa3.1 pharmacology and...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Ohya S, Kito H Tags: Biol Pharm Bull Source Type: research

Testosterone and Mast Cell Interactions in the Development of Kidney Fibrosis after Unilateral Ureteral Obstruction in Rats.
va LB Abstract Mast cell and testosterone interactions involved in renal fibrosis in rats subjected to unilateral ureteral obstruction (UUO) were investigated. Orchiectomized (ORX) and nonorchiectomized Wistar rats were subjected to UUO, and a nonorchiectomized group was sham-operated (control: SO). Animals from the UUO group were treated with saline or sodium cromoglycate (CG). Some ORX rats from the saline or CG groups also received testosterone propionate replacement (TR). Kidneys and blood were collected 14 d after UUO or SO. Kidney sections were stained with toluidine blue to quantify mast cells, and p...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Oliveira-Silva GL, Morais IBM, Fortunato-Silva J, Alvarez MMP, França-Silva N, Galo JA, Hiraki KRN, Balbi APC, Bispo-da-Silva LB Tags: Biol Pharm Bull Source Type: research

Generation and Characterization of Anti-phenyl Sulfate Monoclonal Antibodies and a Potential Use for Phenyl Sulfate Analysis in Human Blood.
In this study, we produced anti-PS monoclonal antibodies (mAbs) and characterized their cross-reactivity to structural PS analogs. To induce PS-specific mAbs, we synthesized 4-mercaptophenyl sulfate with a sulfhydryl group at the para-position of PS and conjugated it to carrier proteins via bifunctional linkers. Using these PS conjugates as immunogens and as antigens for enzyme-linked immunosorbent assay (ELISA) screening, we produced by a hybridoma method two novel mAbs (YK33.1 and YKS19.2) that react with PS conjugates independent of carrier and linker structures. Although all of the PS analogs tested, with the exception...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Kanemitsu Y, Tsukamoto H, Matsumoto Y, Nozawa-Kumada K, Kondo Y, Abe T, Tomioka Y Tags: Biol Pharm Bull Source Type: research

Qiliqiangxin Protects against Renal Injury in Rat with Cardiorenal Syndrome Type I through Regulating the Inflammatory and Oxidative Stress Signaling.
Abstract Cardiorenal syndrome (CRS) is a frequently encountered clinical condition when the dysfunction of either the heart or kidneys amplifies the failure progression of the other organ. CRS remains a major global health problem. Qiliqiangxin (QLQX) is a traditional Chinese herbs medication, which can improve cardiac function, urine volume, and subjective symptoms in patients with chronic heart failure. In the present study, we aim to investigate the role of QLQX in the treatment of CRS type I and the possible mechanism through establishment of a rat model of myocardial infarction. Rats in CRS-Q group were orall...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Duan X, Yan F, Hu H, Liu H, Wu Q, Sun S, Ming X, Bu X, He Y, Zhu H Tags: Biol Pharm Bull Source Type: research

The Major Lysosomal Membrane Proteins LAMP-1 and LAMP-2 Participate in Differentiation of C2C12 Myoblasts.
In this study, to understand the role of LAMP proteins in the course of differentiation of myoblasts into myotubes, we used C2C12 myoblasts and found that the protein and mRNA levels of LAMP-1 and LAMP-2 were increased in the course of differentiation of C2C12 myoblasts into myotubes. Then, we investigated the effects of LAMP-1 or LAMP-2 knockdown on C2C12 myotube formation, and found that LAMP-1 or LAMP-2 depletion impaired the differentiation of C2C12 myoblasts and reduced the diameter of C2C12 myotubes. LAMP-2 knockdown more severely impaired C2C12 myotube formation compared with LAMP-1 knockdown, and knockdown of LAMP-...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Sakane H, Akasaki K Tags: Biol Pharm Bull Source Type: research

Molybdate Attenuates Lipid Accumulation in the Livers of Mice Fed a Diet Deficient in Methionine and Choline.
Abstract Both lipid accumulation and oxidative stress are major pathologic contributors to the development of hepatic steatosis. Treatment with molybdate reduces hepatic levels of lipids in diabetic rats. Potential activities of molybdate as an antioxidant have also been demonstrated in various animal models. In the present study, we evaluated the effects of sodium molybdate dihydrate (SM) on hepatic steatosis and associated disturbances in a widely used mouse model of the metabolic disease. Male C57Bl/6 mice at 10 weeks of age were fed a diet deficient in methionine and choline (MCD) and bottled water containing ...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Lee S, Nam KH, Seong JK, Ryu DY Tags: Biol Pharm Bull Source Type: research

Dysregulation of BSEP and MRP2 May Play an Important Role in Isoniazid-Induced Liver Injury via the SIRT1/FXR Pathway in Rats and HepG2 Cells.
Abstract To explore the role of the abnormal expression of the bile salt export pump (BSEP) and multidrug resistance protein 2 (MRP2) in isoniazid (INH)-induced liver injury, we assessed the liver injury induced by INH in rats and HepG2 cells in vitro. The regulatory pathways via Sirtuin 1 (SIRT1) and farnesoid X receptor (FXR) were also determined. Rat liver injury was assessed by histopathological and biochemical analysis and HepG2 cytotoxicity was assessed by a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) test. The levels of protein were determined by Western blot. The results indicated th...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Qu X, Zhang Y, Zhang S, Zhai J, Gao H, Tao L, Song Y Tags: Biol Pharm Bull Source Type: research

O-Methylbulbocapnine and Dicentrine Suppress LPS-Induced Inflammatory Response by Blocking NF- κB and AP-1 Activation through Inhibiting MAPKs and Akt Signaling in RAW264.7 Macrophages.
In this study, we investigated anti-inflammatory effect of CN analogs including OMP, DC, THP, and NTHP in RAW264.7 macrophages. The pre-treatment of macrophages with CN, OMP and DC suppressed lipopolysaccharide (LPS)-induced pro-inflammatory cytokines and mediators including interleukin-6 (IL-6), tumor necrosis factor alpha, prostaglandin E2 and nitric oxide, in which the rank-order of inhibitory potency was DC>CN≥OMP. Whereas, high dose THP (30-40 µg/mL) reduced LPS-induced IL-6 production in RAW264.7 cells but NTHP did not effect. Moreover, CN, OMP and DC inhibited the LPS-induced expression of inducib...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Yodkeeree S, Ooppachai C, Pompimon W, Limtrakul Dejkriengkraikul P Tags: Biol Pharm Bull Source Type: research

Dibenzoylmethane, a Component of Licorice, Suppresses Monocyte-to-Macrophage Differentiation and Inflammatory Responses in Human Monocytes and Mouse Macrophages.
The objective of this study was to investigate the effect of dibenzoylmethane (DBM) on monocyte-to-macrophage differentiation, the inflammatory response, and the resulting signaling in human monocytes and murine macrophage. DBM effectively inhibited the monocyte-to-macrophage differentiation induced by phorbol 12-myristate 13-acetate (PMA) through a reduction in adhesion of THP-1 cells. Cluster of differentiation molecule β (CD11β) and CD36, which are surface markers of macrophage differentiation, were downregulated by 80 and 74%, respectively. DBM also significantly inhibited lipopolysaccharide (LPS)-induced nit...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Kang B, Kim JH, Kim CY, Hong J, Choi HS Tags: Biol Pharm Bull Source Type: research

miR-22-Notch Signaling Pathway Is Involved in the Regulation of the Apoptosis and Autophagy in Human Ovarian Cancer Cells.
This study is designed to investigate the mechanisms of miR-22-Notch signaling pathway in apoptosis and autophagy of human ovarian cancer cells. After over-expressing miR-22 in human ovarian cancer cell lines OVCAR-3 and SKOV3, cell viability is determined by 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) method, cell apoptosis is observed by Flow cytometry (FCM), mRNA expression of miR-22 is measured by RNA preparation and RT-PCR, protein expression of Notch1, Hes1, Beclin1 and LC3B-II is analyzed by Western blot. It is suggested that miR-22 expression is heavily decreased in human ovarian ...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Li Y, Gu Y, Tang N, Liu Y, Zhao Z Tags: Biol Pharm Bull Source Type: research

Celastrol Suppresses Tryptophan Catabolism in Human Colon Cancer Cells as Revealed by Metabolic Profiling and Targeted Metabolite Analysis.
This study provided scientific basis for further development of celastrol on treating colon cancer. PMID: 30068874 [PubMed - in process] (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Qi Y, Wang R, Zhao L, Lv L, Zhou F, Zhang T, Lu F, Yan H, Duan G Tags: Biol Pharm Bull Source Type: research

Anti-inflammatory Effect of the Water-Soluble Portion of Porcine Placental Extract in Lipopolysaccharide-Stimulated RAW264.7 Murine Macrophage Cells.
Abstract Porcine placental extract (PPE) is used as a nonprescription drug for analeptics and in health foods and cosmetics in Japan, Korea and China. It was reported that PPE has anti-oxidative and anti-inflammatory activities; however, the mechanisms and the responsible molecules involved in these activities are still unclear. Here, we investigated how enzymatically prepared PPE affects proinflammatory factors such as interleukin (IL)-1β, IL-6, and tumor necrosis factor (TNF)-α in a cultured macrophage cell line, RAW264.7, when co-stimulated with lipopolysaccharide (LPS). Enhanced production of IL-1&b...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Tebakari M, Daigo Y, Ishikawa H, Nakamura M, Kawashima J, Takano F Tags: Biol Pharm Bull Source Type: research

Romaine Lettuce/Skullcap Mixture Improves Sleep Behavior in Vertebrate Models.
Abstract The aim of this study is to investigate the effects of romaine lettuce leaves extract (RE), skullcap root extract (SE) and their mixture on sleep behaviors in vertebrate models. HPLC analysis showed that RE contains lactucopicrin (0.02±0.01 mg/g extract), chlorogenic acid (4.05±0.03 mg/g extract), caffeic acid (2.38±0.03 mg/g extract), and chicoric acid (7.02±0.32 mg/g extract) as main phenolic compounds, while SE includes baicalin (99.4±0.5 mg/g extract), baicalein (8.28±0.21 mg/g extract), and wogonin (3.09±0.32&t...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Hong KB, Han SH, Park Y, Suh HJ, Choi HS Tags: Biol Pharm Bull Source Type: research

Effects of Cultivation Month and Genetic Background on Phenolic Content of Citrus tachibana Peel.
This study evaluated the phenolic and flavonoid contents of C. tachibana and C. unshiu in an effort to provide new insights into herbal medicines for further study and utilization. PMID: 30068877 [PubMed - in process] (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Yamaguchi M, Shigeyama K, Yoshikawa M, Matsumoto T, Yonezawa Y, Shiota H, Ueyama T, Sakaguchi I Tags: Biol Pharm Bull Source Type: research

Low Molecular-Weight Curdlan, (1 →3)-β-Glucan Suppresses TLR2-Induced RANKL-Dependent Bone Resorption.
Low Molecular-Weight Curdlan, (1→3)-β-Glucan Suppresses TLR2-Induced RANKL-Dependent Bone Resorption. Biol Pharm Bull. 2018;41(8):1282-1285 Authors: Aizawa M, Watanabe K, Tominari T, Matsumoto C, Hirata M, Grundler FMW, Inada M, Miyaura C Abstract Fungal β-glucan is a potent immunological stimulator, and that it activates both the innate immune system and adaptive immunity. Curdlan is (1→3)-β-glucan, a linear form of β-glucan with a high molecular weight; it modulates the immune response. However, its role in bone tissue is controversial, and the effects of curdlan on bon...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Aizawa M, Watanabe K, Tominari T, Matsumoto C, Hirata M, Grundler FMW, Inada M, Miyaura C Tags: Biol Pharm Bull Source Type: research

Clozapine-Induced Acute Hyperglycemia Is Accompanied with Elevated Serum Concentrations of Adrenaline and Glucagon in Rats.
In conclusion, a single administration of clozapine increased the serum concentration of glucose in rats, and adrenaline and/or glucagon would be associated with clozapine-induced acute hyperglycemia. PMID: 30068879 [PubMed - in process] (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Nagata M, Kimura Y, Ishiwata Y, Takahashi H, Yasuhara M Tags: Biol Pharm Bull Source Type: research

Development of an Alcohol Dilution-Lyophilization Method for Preparing Lipid Nanoparticles Containing Encapsulated siRNA.
In this study, we report on the development of an "alcohol dilution-lyophilization method" for preparing siRNA-encapsulating LNPs. This method involves the use of a freeze-drying (lyophilization) method to remove the residual alcohol and to simultaneously concentrate the preparation. At first, the compositions of cryoprotectants and polyethylene glycol (PEG)-lipids that were used were optimized from the point of view of particle stabilization. A combination of sucrose and 1-(monomethoxy polyethyleneglycol5000)-2,3-dimyristoylglycerol (DMG-PEG5000) was found to have the most efficient cryoprotective activity for t...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Shirane D, Tanaka H, Nakai Y, Yoshioka H, Akita H Tags: Biol Pharm Bull Source Type: research

Direct Activation of the Large-Conductance Calcium-Activated Potassium Channel by Flavonoids Isolated from Sophora flavescens.
Abstract In our recent study, we reported that kurarinone, one of the most abundant flavonoids found in the dry root of Sophora flavescens (Kushen), is a potent activator of the large-conductance Ca2+-activated K+ (BKCa) channel. Herein, we isolated and characterized other flavonoid components from Kushen. Among the 13 compounds tested, six flavonoids were found to activate the BKCa channel, three of which, 7,4'-dihydroxy-5-methoxy-8-(γ,γ-dimethylallyl)-flavanone, kuraridin, and kuraridinol, are new activators of the BKCa channel. PMID: 30068881 [PubMed - in process] (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Lee S, Choi JS, Park CS Tags: Biol Pharm Bull Source Type: research

In Vivo Antifungal Activity of Monolaurin against Candida albicans Biofilms.
Abstract Monolaurin is a natural compound that has been known for its broad antimicrobial activities. We evaluate the antifungal activity of monolaurin against Candida albicans biofilms in vivo using a novel bioluminescent model to longitudinally monitor oral fungal infection. Oral fungal infection in vivo was performed using bioluminescent engineered C. albicans (SKCa23-ActgLUC) biofilms on Balb/c mice. The antifungal activity of monolaurin was determined by comparing three groups of mice (n=5/group): monolaurin, vehicle control, and positive control (nystatin). All mice were immunosuppressed with cortisone aceta...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Seleem D, Freitas-Blanco VS, Noguti J, Zancope BR, Pardi V, Murata RM Tags: Biol Pharm Bull Source Type: research

Improved On-Site Protocol for the DNA-Based Species Identification of Cannabis sativa by Loop-Mediated Isothermal Amplification.
In this study, we report an on-site protocol that can be completed in 30 min for C. sativa identification based on a modified LAMP system. Under optimal conditions, the LAMP reaction started at approximately 10 min and was completed within 20 min at 63°C. It had high sensitivity (10 pg of purified DNA). Its specificity for C. sativa was confirmed by examining 20 strains of C. sativa and 50 other species samples. With a simple DNA extraction method, the entire procedure from DNA extraction to detection required only 30 min. Using the protocol, we were able to identify C. sativa from va...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Kitamura M, Aragane M, Nakamura K, Adachi T, Watanabe K, Sasaki Y Tags: Biol Pharm Bull Source Type: research

Screening of Euphorbiaceae Plant Extracts for Anti-5 α-reductase.
Screening of Euphorbiaceae Plant Extracts for Anti-5α-reductase. Biol Pharm Bull. 2018;41(8):1307-1310 Authors: Kamei H, Noguchi K, Matsuda H, Murata K Abstract In our research program to find novel agents for alopecia from natural plant resources, we screened Euphorbiaceae plant extracts using an anti-5α-reductase assay. Among the samples tested, the extract of Phyllanthus urinaria showed the most potent activity with 24.3 and 64.6% inhibition at 50 and 200 µg/mL against the enzyme, respectively. The extract also suppressed the androgen activity of dihydrotestosterone in LNCa...
Source: Biological and Pharmaceutical Bulletin - August 3, 2018 Category: Drugs & Pharmacology Authors: Kamei H, Noguchi K, Matsuda H, Murata K Tags: Biol Pharm Bull Source Type: research

Dynamic characteristics of sequential acute exacerbations and risk windows in AECOPD rats induced by cigarette-smoke and exposure to Klebsiella pneumoniae.
Abstract The risk-window (RW) of chronic obstructive pulmonary disease (COPD) is a period after an acute exacerbation (AE) but before the following stable phase, in which exacerbations are easy to relapse. We established a sequential COPD-AE-RW rat model by cigarette-smoke and bacterial exposures in the first 8 weeks, and was challenged with Klebsiella pneumonia to mimic an AE on Day 1 of week 9, and found that body temperature, white blood cell, neutrophils, serum amyloid A (SAA) and C-reactive protein (CRP) increased in AECOPD rats 24 hours after challenge, and declined in 3 ~ 6 days, while lung function decline...
Source: Biological and Pharmaceutical Bulletin - July 28, 2018 Category: Drugs & Pharmacology Authors: Li J, Li Y, Lu X, Wang H, Wang Y, Li H, Wu Z Tags: Biol Pharm Bull Source Type: research

TRPV4 channel-regulated ATP release contributes to γ-irradiation-induced production of IL-6 and IL-8 in epidermal keratinocytes.
TRPV4 channel-regulated ATP release contributes to γ-irradiation-induced production of IL-6 and IL-8 in epidermal keratinocytes. Biol Pharm Bull. 2018 Jul 19;: Authors: Ohsaki A, Tanuma SI, Tsukimoto M Abstract External stimuli, such as radiation, induce inflammatory cytokine and chemokine production in skin, but the mechanisms involved are not completely understood. We previously showed that the P2Y11 nucleotide receptor, p38 MAPK and NF-κB all participate in IL-6 production induced by γ-irradiation. Here, we focused on the transient receptor potential V4 (TRPV4) channel, which is e...
Source: Biological and Pharmaceutical Bulletin - July 19, 2018 Category: Drugs & Pharmacology Authors: Ohsaki A, Tanuma SI, Tsukimoto M Tags: Biol Pharm Bull Source Type: research

Characteristics of Bone Strength and Metabolism in Type 2 Diabetic Model Nagoya Shibata Yasuda Mice.
Abstract We evaluated the suitability of Nagoya Shibata Yasuda (NSY) mice as an animal model for examining the influence of a glucose metabolism disorder on bone integrity, using Institute of Cancer Research (ICR) mice as controls. We selected six NSY and ICR mice each that were matched for weight, and measured serum glucose levels, serum insulin levels, and conducted an oral glucose tolerance test. Histological sections of the femurs of both mouse lines were prepared, and the bone strength, mass, and microstructure of the femur were compared, along with bone metabolism. Serum glucose levels were significantly hig...
Source: Biological and Pharmaceutical Bulletin - July 13, 2018 Category: Drugs & Pharmacology Authors: Tanaka H, Miura T, Yamashita T, Yoneda M, Takagi S Tags: Biol Pharm Bull Source Type: research

Mechanism for decreased gene expression of β4-galactosyltransferase 5 upon differentiation of 3T3-L1 mouse preadipocytes to adipocytes.
Mechanism for decreased gene expression of β4-galactosyltransferase 5 upon differentiation of 3T3-L1 mouse preadipocytes to adipocytes. Biol Pharm Bull. 2018 Jul 07;: Authors: Ishii T, Miyauchi K, Nitta Y, Kaneko K, Maruyama T, Sato T Abstract Upon differentiation of cells, remarkable changes in the structures of glycans linked to lipids on cell surface have been observed. Lactosylceramide (Lac-Cer) serves as a common precursor for a series of glycosphingolipids with diverse structures. In the present study, we examined the underlying mechanism for the biosynthesis of Lac-Cer upon differentiation...
Source: Biological and Pharmaceutical Bulletin - July 7, 2018 Category: Drugs & Pharmacology Authors: Ishii T, Miyauchi K, Nitta Y, Kaneko K, Maruyama T, Sato T Tags: Biol Pharm Bull Source Type: research

Mechanisms of Yangjing capsule in Leydig cell apoptosis and testosterone synthesis via promoting StAR expression.
In conclusion, our results suggested that YC might suppress the apoptosis of MLTC-1 cells and enhance the production of testosterone through regulating the expression of StAR. PMID: 29984732 [PubMed - as supplied by publisher] (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - July 6, 2018 Category: Drugs & Pharmacology Authors: Sun D, Dong W, Jin B, Chen G, Cai B, Deng W, Cui Y, Jin Y Tags: Biol Pharm Bull Source Type: research