Abstract:
:Proteasome inhibitors are a novel class of molecular-targeted anti-cancer drugs that suppress the degradation of malfolded proteins, trigger endoplasmic reticulum (ER) stress, and activate apoptosis signals. Glucose-regulated protein 78 (GRP78), a major ER chaperone, is one of the most important molecules for transduction of unfolded protein response (UPR) signals. In accordance with past findings that expression of GRP78 is elevated in cancer cells and helps to resist stress-induced apoptosis, GRP78 knockdown could be effective in anticancer therapy. We tested this hypothesis and found that transfection of small interfering RNA (siRNA) targeting GRP78 inhibited the growth of RENCA renal carcinoma cells, in association with elevated gene expression of UPR downstream signaling molecules (CHOP, EDEM1, and ERdj4 mRNA). In addition, the combinatorial effect of GRP78 siRNA with ER stress inducers (tunicamycin, MG132, and 2-deoxyglucose) on survival was measured. Combination of GRP78 siRNA and the ER stress inducers more extensively reduced cell viability than combination with scrambled siRNA. Besides RENCA, B16BL6 melanoma cells were also shown to be sensitive to GRP78 siRNA. These results suggest that GRP78 knockdown might be an effective strategy for cancer therapy targeting UPR-induced apoptosis.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Matsumura K,Sakai C,Kawakami S,Yamashita F,Hashida Mdoi
10.1248/bpb.b13-00930subject
Has Abstractpub_date
2014-01-01 00:00:00pages
648-53issue
4eissn
0918-6158issn
1347-5215pii
DN/JST.JSTAGE/bpb/b13-00930journal_volume
37pub_type
杂志文章abstract::The quantification of tenofovir, a nucleoside reverse transcriptase inhibitor prescribed once daily, in human plasma is important due to a recent increase in its use. HPLC, however, can not easily detect and quantify tenofovir because of interfering peaks. Therefore, we developed a rapid and conventional LC-MS method,...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.30.1784
更新日期:2007-09-01 00:00:00
abstract::Several neurological disorders such as Alzheimer's and Parkinson's diseases have been attributed to gamma-aminobutyric acid (GABA) depletion in the brain. In order to provide a pharmacological basis for the neuroprotective actions of the enhanced accumulation of GABA in mulberry leaves (ML) against cerebral ischemia i...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.29.270
更新日期:2006-02-01 00:00:00
abstract::Lysosomal trapping was investigated in the retinal capillary endothelial cells that are responsible for the inner blood-retinal barrier (BRB) using LysoTracker(®) Red (LTR). Using confocal microscopy on TR-iBRB2 cells, an in vitro model of the inner BRB, the presence of lysosomal trapping in retinal capillary endothel...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b16-00140
更新日期:2016-01-01 00:00:00
abstract::We investigated whether endogenous nitric oxide (NO) has a role as an inhibitory modulator of norepinephrine (NE)- and angiotensin II (Ang II)-induced renal effects in anesthetized dogs. Intrarenal arterial infusion of NE (100 ng/kg/min) or Ang II (10 ng/kg/min) decreased renal blood flow (RBF), glomerular filtration ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.18.496
更新日期:1995-04-01 00:00:00
abstract::Four lavandulyl flavanones, (2S)-2'-methoxykurarinone (1), sophoraflavanone G (2), leachianone A (3), and (-)-kurarinone (4), which are isolated from the roots of Sophora flavescens have been tested for in vitro antimalarial activity against Plasmodium falciparum. Compounds 1-3 showed moderate antimalarial activities ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.27.748
更新日期:2004-05-01 00:00:00
abstract::Aconitine administered intraperitoneally (i.p.) produces bradycardia mainly by a central muscarinic action. The involvement of hypothalamic regions in the occurrence of aconitine-induced bradycardia was investigated in hypothalamus-lesioned mice. The lesions were made by passing a direct current (1.5 mA, 13 s) through...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.20.856
更新日期:1997-08-01 00:00:00
abstract::The availability and applicability of the combination of paramagnetic nitroxyl contrast agent and T(1)-weighted gradient echo (GE)-based dynamic magnetic resonance imaging (MRI) measurement for redox imaging are described. The time courses of T(1)-weighted GE MRI signal intensities according to first-order paramagneti...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.711
更新日期:2009-04-01 00:00:00
abstract::4-Acetyltropolone, a minor component of Thujopsis dolabrata SIEB. et Zucc. hondai MAKINO, showed antimicrobial activity against various microorganisms including wood-rotting fungi, a phytogrowth-inhibitory effect with chlorophyll biosynthesis inhibition, cytotoxic effect and inhibitory activity on metalloproteases. Th...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.25.981
更新日期:2002-08-01 00:00:00
abstract::The effects of various surfactants and protease inhibitors on the nasal absorption of recombinant human granulocyte colony-stimulating factor (rhG-CSF) were examined in rats. No effects of bile salts and acids such as sodium glycocholate or taurocholic acid, amphoteric surfactants such as lauryldimethyl betaine, or an...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.1375
更新日期:1994-10-01 00:00:00
abstract::The effects of ketoconazole (KCZ) on secretion of progesterone and cAMP in Leydig cells were investigated in vitro. MA-10 mouse Leydig tumor cells were used to conduct the experiments. KCZ significantly inhibited the progesterone production from MA-10 cells in a dose dependent fashion between 2 and 20 microM among 1, ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.25.794
更新日期:2002-06-01 00:00:00
abstract::Mast cells are critical for initiating innate immune and inflammatory responses by releasing a number of pro-inflammatory mediators. The potential immunomodulatory properties of hydrogenated aromatic hydrocarbons have been the subject of extensive investigation, as the immune system is a sensitive target for hydrogena...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.25.1165
更新日期:2002-09-01 00:00:00
abstract::The purpose of this research is improvement of therapeutic treatment for periodontitis by using lipophilic and/or hydrophilic zinc materials. The sample suspension injections were prepared from zinc octanate (C8Zn), zinc stearate (C18Zn), zinc sulfate hepta-hydrate (ZnSO4) and tricalcium phosphate (ZnTCP) containing 6...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b12-00218
更新日期:2012-01-01 00:00:00
abstract::A pharmacokinetic analysis program based on a tank-in-series model, MULTI(TIS), was developed for the evaluation of dose-dependency in the local disposition of a drug. The program written in FORTRAN was constructed by expanding MULTI(RUNGE). The reliability of MULTI(TIS) was verified by analyzing the experimental data...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.21.1338
更新日期:1998-12-01 00:00:00
abstract::The anti-inflammatory effects of 1,6-anhydro-3,4-dideoxy-2-furfuryl-beta-D-threo-3-enopyranose (MT2221) were investigated using animal models and compared with the effects of dexamethasone (DEX) and cyclosporin A (CYA). MT2221 inhibited carrageenan-induced acute inflammation and adjuvant arthritis in rats, as well as ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.17.1070
更新日期:1994-08-01 00:00:00
abstract::In vivo redox reactions of nitroxyl contrast agents in bile and blood under an oxidative atmosphere were investigated using normal healthy Wistar rats. Differences in intracellular and extracellular volumes in redox environments are discussed. Pharmacokinetic profiles of two nitroxyl contrast agents, 3-carbamoyl-2,2,5...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.535
更新日期:2009-04-01 00:00:00
abstract::R(-)-Apomorphine is a dopamine agonist used for rescue management of motor function impairment associated with levodopa therapy in Parkinson's disease patients. The aim of this study was to examine the role of proton-coupled organic cation antiporter in uptake of R(-)-apomorphine and its S-enantiomer in human brain, u...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b13-00773
更新日期:2014-01-01 00:00:00
abstract::Rapamycin (Rap) has been demonstrated to affect lipid metabolism through stimulating lipolysis, inhibiting de novo lipogenesis and reducing adiposity. In the present study, we investigated rapamycin exposure's influence on adipose tissue browning in high-fat diet-induced fatty mice. Four-week old C57BL/6J mice were fe...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b16-00946
更新日期:2017-01-01 00:00:00
abstract::Povidone-iodine (PVP-I), an antibacterial medicine, was infiltrated in sepiolite (SPL). The available iodine content in this new pharmaceutical product, a sepiolite preparation containing povidone-iodine (PVP-I-SPL), was retained at 98.9 and 98.3% during storage at 40 degrees C for 3 and 6 months, respectively. The ef...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.22.42
更新日期:1999-01-01 00:00:00
abstract::In the present study, we evaluated the effect of the novel acid pump antagonist 7-(4-fluorobenzyloxy)-2,3-dimethyl-1-{[(1S,2S)-2-methylcyclopropyl]methyl}-1H-pyrrolo[2,3-d]pyridazine (CS-526) on the intragastric acidity of cynomolgus monkeys. The study was performed in a crossover manner with five male animals. CS-526...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.2010
更新日期:2009-12-01 00:00:00
abstract::To improve bioavailability of pueraria flavones (PF), a self-microemulsifying drug delivery system (SMEDDS) dropping pills composed of PF, Crodamol GTCC, Maisine 35-1, Cremophor RH 40, 1,2-propylene glycol and polyethylene glycol 6000 (PEG6000) was developed. Particle size, zeta potential, morphology and in vitro drug...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b15-00854
更新日期:2016-05-01 00:00:00
abstract::The gas phase of cigarette smoke is important from the viewpoint of human health, because it can pass through alveolar epithelium and enter the circulation. There is no standard method for the preparation of a gas phase extract of cigarette smoke (CSE), although CSE is widely used for research instead of whole cigaret...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
doi:10.1248/bpb.b16-00062
更新日期:2016-01-01 00:00:00
abstract::Immediate early genes (IEG) are rapidly but transiently induced directly by intracellular signaling cascades to alter patterns of gene expression. It has been proposed that histone modifications could be the key to the quick alteration of chromatin structure, as this spread occurs too rapidly to be the consequence of ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
doi:10.1248/bpb.27.606
更新日期:2004-05-01 00:00:00
abstract::Cancer is one of the leading causes of death in the world. The triterpenoid compound asiatic acid derived from the tropical medicinal plant Centella asiatica displays cytotoxic activity on fibroblast cells and several other kinds of cells. The present work studies asiatic acid-mediated growth inhibition of cancer cell...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.1399
更新日期:2009-08-01 00:00:00
abstract::The anti-herpes simplex virus type 1 (HSV-1) activity of 15 oleanan-type triterpenoides including glycyrrhizin and its sapogenol was examined and their structure-activity relationships were discussed. Although glycyrrhizin which exhibited in vivo efficacy against HSV-1 replication showed moderate in vitro anti-HSV-1 a...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.1779
更新日期:2005-09-01 00:00:00
abstract::Cry j 1 is one of the major allergens in Japanese cedar pollen. We attempt high throughput analysis and comprehensive identification of the linear IgE epitopes of Cry j 1. A series of overlapping synthetic Cry j 1 peptides chemically spotted on cellulose membrane was probed with sera from patients in Japan and United ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.1496
更新日期:2005-08-01 00:00:00
abstract::Microvessels are composed of endothelial cells that cover the luminal surface and pericytes that wrap around and along endothelial cells. In the present study, we investigated the regulation of fibrinolysis in cultured human brain microvascular pericytes and endothelial cells after exposure to thrombin. It was found t...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.208
更新日期:2005-02-01 00:00:00
abstract::Cynanchum wilfordii is one of most widely used medicinal plants in Oriental medicine for the treatment of various conditions. In the present study, we isolated cynandione A (CA) from an extract of Cynanchum wilfordii roots (CWE) and investigated the effects of CA on the expression of inducible nitric oxide synthase (i...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b13-00939
更新日期:2014-01-01 00:00:00
abstract::Tumor necrosis factor-alpha (TNF-α) plays an important role in the developing process of inflammatory bowel disease. Tight junction protein zonula occludens-1 (ZO-1), one of epithelial junctional proteins, maintains the permeability of intestinal barrier. The objective of this study was to investigate the mechanism of...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b16-00789
更新日期:2017-04-01 00:00:00
abstract::The purpose of this study was to determine the high-density lipoprotein (HDL)-associated alpha-tocopherol (alpha-tocopherol-HDL) transport and clarify the contribution of scavenger receptor class B, type I (SR-BI) to the uptake in the human retinal pigment epithelial cell line (ARPE-19 cells). [(3)H]alpha-Tocopherol-H...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.1131
更新日期:2009-06-01 00:00:00
abstract::We investigated whether poly-L-arginine (PLA) could improve permeation of the hydrophilic compounds, FITC-labeled dextran (MW 3800, FD-4) and pyridoxamine, through ocular surface tissues. Samples of cornea, conjunctiva, or conjunctiva/sclera composite from Japanese white rabbits were mounted in Ussing chambers to meas...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.29.155
更新日期:2006-01-01 00:00:00