Abstract:
:We established a highly sensitive method for evaluating P-glycoprotein activity in Caco-2 cells. Using time-lapse confocal laser-scanning microscopy, we measured the change in fluorescence of residual rhodamine 123 in Caco-2 cells. Horizontal fluorescence images of rhodamine 123 in the apical and central parts of these cells were captured for 90 min. A continuous and significant decrease in the fluorescent intensity of rhodamine 123 in the apical part of the Caco-2 cells occurred during the measurement period, while the decrease in the central part was mild. The decrease in rhodamine 123 intensity in the apical part of Caco-2 cells were abolished in the presence of 10 microM digoxin, but the decrease in the central part was not. The decrease in total rhodamine 123 over whole cells was no significant influence of digoxin was observed. This residual rhodamine 123 assay for evaluating P-glycoprotein in the apical part of Caco-2 cells imaged by confocal laser scanning microscopy is more sensitive than conventional methods and will be a valuable screening tool for studying both the inhibition and induction of P-glycoprotein activity and expression. This method may also be useful for predicting P-glycoprotein-mediated alterations in the intestinal absorption of drugs.
journal_name
Biol Pharm Bulljournal_title
Biological & pharmaceutical bulletinauthors
Wakuda H,Nejime N,Tada Y,Kagota S,Umegaki K,Yamada S,Shinozuka Kdoi
10.1248/bpb.33.1238subject
Has Abstractpub_date
2010-01-01 00:00:00pages
1238-41issue
7eissn
0918-6158issn
1347-5215pii
JST.JSTAGE/bpb/33.1238journal_volume
33pub_type
杂志文章abstract::In this study, the quantitative analysis of saikosaponins from Radix Bupleuri in China was performed by high performance liquid chromatography. Saikosaponin-a and -d were converted completely into saikosaponin-b1 and -b2 by mild acid treatment. Distinctive measuring of these converted diene-saponins provided a rapid a...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.1736
更新日期:2005-09-01 00:00:00
abstract::We earlier reported that collagen synthesis in false aged model rats was stimulated by the administration of a methanol extract from the leaves of Eucommia ulmoides OLIVER. When the methanol extract was fractionated to n-hexane, ethyl acetate, acetone and methanol fractions by silica gel chromatography, we discovered ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.22.582
更新日期:1999-06-01 00:00:00
abstract::The bioassay-guided fractionation of the MeOH extract of Galla Rhois furnished two hepatoprotective compounds, an equilibrium mixture of 3-galloyl-gallic acid and 4-galloyl-gallic acid isomers (3), 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (4), and two inactive phenolic compounds, gallic acid methyl ester (1) and galli...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.2155
更新日期:2005-11-01 00:00:00
abstract::Recently, Banhabackchulchunmatang (HMC05) has been implicated as a preventive and/or therapeutic candidate for cardiovascular diseases due to its inhibition of atherosclerosis lesions and its reduction of neointima formation. Knowledge of the mechanism of HMC05 in smooth muscle cells (SMC) is limited. However, SMC may...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b14-00336
更新日期:2014-01-01 00:00:00
abstract::The effect of pH on the microenvironment surrounding 34Cys in human serum albumin (HSA) has been studied using acrylodan, a Cys-specific fluorescence probe. The reactivity of 34Cys with 5,5'-dithiobis(2-nitro benzoic acid) (DTNB) followed a pseudo-first-order reaction, and the increase in reactivity was dependent on p...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.20.452
更新日期:1997-04-01 00:00:00
abstract::The characteristics of the binding of human lactoferrin (LF) to the cells of a human monocytic leukemia cell line, THP-1, were investigated. 125I-Labeled LF (125I-LF) bound to THP-1 cells, and the binding increased markedly as the cells matured into macrophages (THP-1 macrophages) by stimulation with phorbol 12-myrist...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.19.167
更新日期:1996-02-01 00:00:00
abstract::The extracellular matrix (ECM), which contributes to structural homeostasis as well as to the regulation of cellular function, is enzymatically cleaved by proteases, such as matrix metalloproteinases and cathepsins, in the normal and diseased heart. During the past two decades, matricryptins have been defined as fragm...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
doi:10.1248/bpb.b17-00308
更新日期:2017-01-01 00:00:00
abstract::Bepridil hydrochloride is used for treatment of atrial fibrillation (AF) in Japan. We investigated the relationship between plasma concentrations of bepridil just before dosing (Cbep) and its clinical efficacy in Japanese patients (n=36) with AF. Patients were treated orally with 100, 150 or 200 mg/d bepridil. Cbep we...
journal_title:Biological & pharmaceutical bulletin
pub_type: 临床试验,杂志文章
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更新日期:2012-01-01 00:00:00
abstract::We reported previously that N-linked glycoproteins were accumulated in the cytosol of the normal aging rat brain, and that one protein had been identified as cathepsin D (Mech. Ageing Dev., 127, 771-778 (2006)). In this study, to elucidate the mechanism of cathepsin D accumulation in the cytosol, we examined the effec...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.33.22
更新日期:2010-01-01 00:00:00
abstract::Mucus on the nasal mucosa is translocated to the pharynx by ciliary beating, which is an important nonspecific defense mechanism called mucociliary clearance (MC). MC is one of the important factors determining the rate and extent of drug absorption after nasal application. The purpose of this study is to evaluate MC ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.35.889
更新日期:2012-01-01 00:00:00
abstract::Cloning of polyketide synthase (PKS) gene for amphidinolide biosynthesis was attempted from a dinoflagellate Amphidinium sp. (strain Y-42). Fourteen beta-ketoacyl synthase gene fragments were obtained by Polymerase Chain Reaction (PCR) amplification from degenerated primer sets designed on the basis of the conserved a...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.29.1314
更新日期:2006-07-01 00:00:00
abstract::Dermatan sulfate-proteoglycans (DS-PGs) were extracted from rabbit, rat and bovine defatted livers by magnesium chloride extraction and DEAE-cellulose chromatography, and then submitted successively to Asahipak GS-520 gel filtration chromatography, Asahipak ES-502N anion exchange chromatography, and cellulose acetate ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.16.335
更新日期:1993-04-01 00:00:00
abstract::Sesamin is a major lignan in sesame seeds, and a recent meta-analysis of controlled trials indicated that sesamin intake decreases blood pressure. The antihypertensive effect of sesamin has been suggested to be due to sesamin-mediated suppression of 20-hydroxyeicosatetraenoic acid production catalyzed by CYP4F2. Howev...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b19-00953
更新日期:2020-01-01 00:00:00
abstract::Cannabinoids are the active ingredients in marijuana, which is among the most widely used addictive drugs despite the well-documented harmfulness related to its abuse. The mechanism underlying cannabinoid addiction remains unclear, which is attributed partially to the difficulty in behavioral testing of high-dose cann...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b15-00834
更新日期:2016-05-01 00:00:00
abstract::Studies on drug disposition in inflamed skin are important for safe and effective application of topical drugs. Here, the absorption of flurbiprofen (FP) through inflamed skin was examined in vivo and in a skin-mimicking artificial model system. The model skin system consisted of a silicone membrane acting as a model ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.35.203
更新日期:2012-01-01 00:00:00
abstract::Mouth washing after inhalation of corticosteroids is effective for prevention of local adverse effects such as hoarseness and oropharyngeal candidiasis. To establish an optimal procedure for such mouth washing, we investigated the removal rates of drug residues remaining on the oropharyngeal mucosa using various mouth...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.29.1923
更新日期:2006-09-01 00:00:00
abstract::An accumulating body of evidence indicates that inflammation plays a crucial role in the pathophysiology of myocardial infarction (MI). Nucleotide-binding oligomerization domain-like receptor (NLR) family pyrin domain containing 3 (NLRP3) inflammasome is an intracellular multiprotein complex that regulates caspase-1 a...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章,评审
doi:10.1248/bpb.b18-00369
更新日期:2019-01-01 00:00:00
abstract::Hydroxyproline (Hyp) content in biological fluids is used as a parameter of collagen catabolism, especially bone resorption. In this paper, we examined the relationship between aging and serum free 4-Hyp and proline (Pro) content using a newly introduced analytical technique which is chemiluminescence determination wi...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.23.101
更新日期:2000-01-01 00:00:00
abstract::UDP-N-acetylglucosaminyl transferase (OGT) resides in both cytosolic and nuclear compartments and catalyzes O-linked glycosylation of various proteins. In the current study, we have extracted protein from nuclear DNA (chromatin protein) using 0.2% NP-40 detergent. Addition of chromatin protein to either cytosolic or n...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.27.1293
更新日期:2004-08-01 00:00:00
abstract::B-type natriuretic peptide (BNP) is one peptide hormone released in response to myocyte stretch, whose functions play significant roles in health and disease. Its physiologic effects result in improved loading conditions and have led to the development of recombinant BNP as a therapeutic agent for heart failure. Previ...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.32.1545
更新日期:2009-09-01 00:00:00
abstract::Lutein is a carotenoid and it has antioxidant effects. Lutein may have a protective effect on ischemia reperfusion (I/R) injury induced by free radical species. However, little is known about the protective effect of lutein on I/R injury in vivo. The present study was undertaken to clarify the protective effects of lu...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.29.1764
更新日期:2006-08-01 00:00:00
abstract::The intestinal expression of the CYP3A subfamily was investigated in female rats, and the intestinal metabolism of two CYP3A substrates, testosterone and rifabutin, was examined and compared between males and females. CYP3A1/23 and CYP3A2 intestinal expression was barely detected in male and female rats. Although CYP3...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.28.311
更新日期:2005-02-01 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::The promoting effect of d-limonene and l-menthol on the percutaneous absorption of nonionized and ionized diclofenac (DF) was investigated employing a pretreatment method. After the pretreatment of hairless rat skin with an ethanol buffer solution containing terpenes, the permeation study was performed in vitro. The p...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.16.312
更新日期:1993-03-01 00:00:00
abstract::The immunoreactivity (specific binding) of three Gly(A1)-sulfobenzoxadiazole-labeled insulins which have different spacer groups, Gly(A1)-[3-(4-sulfobenzoxadiazol-7-ylthio)propanoyl]-insulin , Gly(A1)-[2-(4-sulfobenzoxadiazol-7-ylthio)acetyl]-insulin, Gly(A1)-[3-carboxy-2(or 3)-(4-sulfobenzoxadiazol-7-ylthio)propanoyl...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.16.516
更新日期:1993-05-01 00:00:00
abstract::Plasma hyaluronan-binding protein (PHBP), a serine protease that can activate coagulation factor VII and prourokinase, circulates in a single-chain form (pro-PHBP) and autoproteolytically converts to an active two-chain form with the aid of an effector such as spermidine and heparin. It has been postulated that PHBP p...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.34.462
更新日期:2011-01-01 00:00:00
abstract::Eight new diterpenoids (1-8) have been isolated from the wood of Excoecaria agallocha (Euphorbiaceae) and their inhibitory effects on the induction of Epstein-Barr virus early antigen (EBV-EA) in Raji cells were examined to search for potent anti-tumor-promoters from natural resources. Of these compounds, the secolabd...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.24.1440
更新日期:2001-12-01 00:00:00
abstract::The tumor microenvironment is one of the key factors contributing to the efficiency of drug delivery to a tumor. It has been reported that lymphangiogenesis is induced in certain tumors. Because the lymphatic system functions as a drainage one, it is possible that tumor lymphatic vessels alter not only the tumor micro...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.b17-00730
更新日期:2018-01-01 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::Ointments of the skin depigmentation agent hydroquinone (HQ) have been prepared by extemporaneous nonsterile compounding in our hospital. The HQ ointments were highly effective in the treatment of various types of skin pigmentations; however, various problems have emerged including chromatic aberration of the ointment...
journal_title:Biological & pharmaceutical bulletin
pub_type: 杂志文章
doi:10.1248/bpb.26.1365
更新日期:2003-09-01 00:00:00