Abstract：
PURPOSE:The purpose of this study was to clarify the localization and function of the ATP-binding cassette transporter G2 (ABCG2; BCRP/MXR/ABCP) in retinal capillary endothelial cells, which form the inner blood-retinal barrier, as an efflux transport system. METHODS:The expression was determined by reverse transcriptase polymerase chain reaction and Western blotting. The localization was identified by immunostaining. The transport function of ABCG2 was measured by flow cytometry. RESULTS:Western blotting indicated that ABCG2 was expressed as a glycosylated disulfide-linked complex in the mouse retina and in peripheral tissues, including liver, kidney, and small intestine. Double immunolabeling of ABCG2 and glucose transporter 1 suggested that ABCG2 was localized on the luminal membrane of mouse retinal capillary endothelial cells. ABCG2 mRNA and protein were found to be expressed in a conditionally immortalized rat retinal capillary endothelial cell line, TR-iBRB, and rat retina. Treatment with Ko143, an ABCG2 inhibitor, restored the accumulation of pheophorbide a and protoporphyrin IX in TR-iBRB cells. CONCLUSION:ABCG2 is expressed on the luminal membrane of retinal capillary endothelial cells, where ABCG2 acts as the efflux transporter for photosensitive toxins such as pheophorbide a and protoporphyrin IX. ABCG2 could play an important role at the inner blood-retinal barrier in restricting the distribution of phototoxins and xenobiotics in retinal tissue.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Asashima T,Hori S,Ohtsuki S,Tachikawa M,Watanabe M,Mukai C,Kitagaki S,Miyakoshi N,Terasaki Tdoi
10.1007/s11095-006-0067-2subject
Has Abstractpub_date
2006-06-01 00:00:00pages
1235-42issue
6eissn
0724-8741issn
1573-904Xjournal_volume
23pub_type
杂志文章abstract：PURPOSE:To characterize the electrochemical behavior of the photodegradation product of nifedipine, i.e., 2,6-dimethyl-4-(2-nitrosophenyl)-3,5-pyridine-carboxylic acid dimethyl ester (NPD) in different electrolytic media. We also evaluated the interaction between free radicals generated from NPD and xeno/endobiotics. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015112216360
更新日期：2002-04-01 00:00:00
abstract：:Defined size fractions of polyethyleneglycol powder (MW = 10,000) were mixed with defined size fractions of alpha-lactose monohydrate in order to study the effect of compaction as a function of the weight ratios of the two excipients. For a precise control of the compression cycle, tablets were compressed on a Univers...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015864415693
更新日期：1990-02-01 00:00:00
abstract：PURPOSE:The purpose of the present study was to explore the involvement of indoxyl sulfate (IS) in nephrotoxicity and central nervous system (CNS) toxicity in cisplatin (CDDP)-treated rats. MATERIALS AND METHODS:Renal function was evaluated by serum creatinine and BUN levels. The IS levels in the serum, brain and kidn...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9183-2
更新日期：2007-04-01 00:00:00
abstract：PURPOSE:We compared cationic, polyamine-coated microparticles (MPs) and anionic, protein-coated MPs with respect to their phagocytosis and phagosomal fate in dendritic cells (DCs) and macrophages (Mphi). METHODS:Polystyrene MPs were surface modified by covalent coupling with fluorescein isothiocyanate-labeled polyamin...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1022271020390
更新日期：2003-02-01 00:00:00
abstract：PURPOSE:Since a previous qualitative study carried out by us showed the existence of an important influence of the particle size on the percolation thresholds and taking into account that the existing theoretical models can only provide qualitative explanation to this influence, the purpose of this work is to carry out...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016088424993
更新日期：1996-03-01 00:00:00
abstract：PURPOSE:The combination of morphine and gabapentin seems promising for the treatment of postoperative and neuropathic pain. Despite the well characterised pharmacodynamic interaction, little is known about possible pharmacokinetic interactions. The aim of this study was to evaluate whether co-administration of the two ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1988-z
更新日期：2016-11-01 00:00:00
abstract：PURPOSE:The purpose of this study was to evaluate an effect of the proteolytic enzyme papain on permeation of low molecular weight heparin (LMWH) in vitro and in vivo. MATERIALS AND METHODS:In vitro permeation studies were performed using rat small intestine as permeation barrier. In order to determine the ratio of pa...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9226-8
更新日期：2007-05-01 00:00:00
abstract：PURPOSE:The aim of this study was to develop a labile sphingosine-based liposome for intramuscular gene delivery. METHODS:Sphingosine-based liposomes were formulated in a range of solutions with phosphatidylcholine, then were associated to DNA. The physico-chemical characteristics of the sphingosine/EPC liposomes and ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1019894008885
更新日期：2002-08-01 00:00:00
abstract：:Unsymmetrical aryl(heteroaryl)methyl isopropyl ester analogues of nifedipine, in which the 2-nitrophenyl group at C-4 is replaced by a 2- or 3-pyridyl substituent, were synthesized and evaluated as calcium-channel antagonists using guinea pig ileal longitudinal smooth muscle. The point of attachment of the C-4 pyridyl...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015941706008
更新日期：1990-09-01 00:00:00
abstract：PURPOSE:To investigate the effect of polyelectrolytes on the formation and physicochemical properties of chitosan nanoparticles (CS-NPs) used for the delivery of an anticancer drug, doxorubicin (DOX). METHOD:Three DOX-loaded CS-NPs were formulated with tripolyphosphate (CS-TP/DOX NPs), dextran sulfate (CS-DS/DOX NPs),...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1251-9
更新日期：2014-05-01 00:00:00
abstract：PURPOSE:The purpose of this study was to use a replicate designed trial to assess the overall, intra- and inter-subject variabilities in pharmacokinetic parameters of CGP 33101 after oral administration of tablets relative to that of powder suspended in water, and to determine the relative proportion of the intra-subje...
journal_title：Pharmaceutical research
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1023/a:1016275402723
更新日期：1995-12-01 00:00:00
abstract：PURPOSE:The United States Pharmacopoeia (USP) imposes strict requirements on the geometry and operating conditions of the USP Dissolution Testing Apparatus II. A previously validated Computational Fluid Dynamics (CFD) approach was used here to study the hydrodynamics of USP Apparatus II when the impeller was placed at ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9477-z
更新日期：2008-02-01 00:00:00
abstract：PURPOSE:The purpose of this human intestinal perfusion study was to investigate the transport and metabolism of R/S-verapamil in the human jejunum (in vivo). METHODS:A regional single-pass perfusion of the jejunum was performed using a Loc-I-Gut perfusion tube in 12 healthy volunteers. Each perfusion lasted for 200 mi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011916329863
更新日期：1998-06-01 00:00:00
abstract：PURPOSE:Long-acting injectables (LAIs) are increasingly recognized as an effective therapeutic approach for treating chronic conditions. Many LAIs are formulated to create a poorly soluble depot from which the active agent is delivered over time. This long residing depot can cause localized chronic-active inflammation ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1308-4
更新日期：2014-08-01 00:00:00
abstract：PURPOSE:The aim of this study was to investigate whether biodegradable nanocapsules could be obtained by the emulsification-diffusion technique. METHODS:This technique consists of emulsifying an organic solution containing an oil, a polymer, and a drug in an aqueous solution of a stabilizing agent. The subsequent addi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011934328471
更新日期：1998-07-01 00:00:00
abstract：PURPOSE:The aim of this work was to develop a quantitative, flow cytometric method for tracking the endolysosomal escape of a fluorescently labelled saporin toxin. METHODS:Flow cytometric measurements of fluorescent pulse width and height were used to track the endocytic uptake into Daudi cells of a fluorescently labe...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2725-1
更新日期：2019-12-23 00:00:00
abstract：PURPOSE:Melanoma is an aggressive neoplasm with a propensity for metastases and resistance to therapy. Previously, we showed that (-)-epigallocatechin-3-gallate (EGCG), the major polyphenolic antioxidant present in green tea, resulted in a significant decrease in the viability and growth of melanoma and induction of ap...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-010-0054-5
更新日期：2010-06-01 00:00:00
abstract：PURPOSE:To study the role of unsaturated fatty acid ester substituents in the autoxidation of polysorbate 80 using quantitative kinetics. METHODS:Oxidation kinetics were monitored at 40 degrees C in aqueous solution by tracking head space oxygen consumption using a fiber optic oxygen sensor with phase shift fluorescen...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9946-7
更新日期：2009-10-01 00:00:00
abstract：PURPOSE:We aimed to assess the fate of β-arteether lipid-based drug delivery systems (AE-LBDDS) in terms of resistance to lipolysis and permeation across intestinal cells. METHODS:AE-LBDDS contained Tween 80 or Cremophor EL as surfactants, ethanol, Maisine 35-1 and vegetable oil. The solubilization behavior of AE was ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1094-4
更新日期：2013-10-01 00:00:00
abstract：PURPOSE:The purpose of this study is to investigate the characteristics of pGlu-L-Dopa-Pro as a prodrug of L-Dopa. METHODS:pGlu-L-Dopa-Pro and L-Dopa-Pro were synthesized using the standard procedures of peptide synthesis. The conversion of pGlu-L-Dopa-Pro to L-Dopa was studied using pyroglutamyl aminopeptidase I and ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016239321494
更新日期：1995-07-01 00:00:00
abstract：PURPOSE:Recently identified organic solute transporter (Ost) alpha and beta are located on the basolateral membrane of enterocytes and may be responsible for the intestinal absorption of many substrates including bile acids. In the present study, the mechanism governing the transcriptional regulation of their expressio...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9163-6
更新日期：2007-02-01 00:00:00
abstract：PURPOSE:To assess the effects of selective lipid extraction and tape stripping on transepidermal water loss (TEWL) at three body regions in the pig. METHODS:Lipids were extracted from the abdominal, inguinal. and back regions using three different solvent extraction procedures or cellophane tape stripping (15x) on Yor...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1010944529387
更新日期：2001-07-01 00:00:00
abstract：PURPOSE:For the assessment of bioequivalence it is assumed that drug clearance in each subject on each of the study days is the same and any observed differences in AUC and/or Cmax between a brand and generic formulation are due to differences in bioavailability. We hypothesized that this assumption was invalid for hig...
journal_title：Pharmaceutical research
pub_type： 临床试验,杂志文章
doi：10.1023/a:1016040825844
更新日期：1996-06-01 00:00:00
abstract：:Diltiazem (DTZ) is a calcium channel blocker widely used in the treatment of angina and hypertension. DTZ undergoes extensive metabolism yielding several metabolites, some of which are active like N-desmethyldiltiazem (MA), desacetyldiltiazem (M1) and N-desmethyl,desacetyldiltiazem (M2). Due to the nature of its biotr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016226601988
更新日期：1995-04-01 00:00:00
abstract：PURPOSE:Penetration enhancers (PEs) enhancing efficacy depends on two processes: PEs release from patches and action on skin. Compared with their action on skin, PEs release process was poorly understood. Therefore, the purpose of this study was to make a mechanistic understanding of PEs release from acrylic pressure-s...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02901-0
更新日期：2020-08-13 00:00:00
abstract：PURPOSE:The purpose of the study was to examine the suitability of using laser diffraction to measure the fine particle fraction (FPF) of drugs emitted from carrier-free dry powder aerosol formulations. MATERIALS AND METHODS:Particle size distribution of terbutaline sulphate from Bricanyl Turbohaler, which contained l...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-006-9056-8
更新日期：2006-09-01 00:00:00
abstract：PURPOSE:To study the PK interaction of L-dopa/benserazide in rats. METHODS:Male rats received a single oral dose of 80 mg/kg L-dopa or 20 mg/kg benserazide or 80/20 mg/kg L-dopa/benserazide. Based on plasma concentrations the kinetics of L-dopa, 3-O-methyldopa (3-OMD), benserazide, and its metabolite Ro 04-5127 were c...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1010935228654
更新日期：2001-08-01 00:00:00
abstract：:The pharmacokinetics of trilostane and one of its metabolites ketotrilostane are described and characterized in the rat following the separate intravenous administration of trilostane and ketotrilostane. It was noted during these studies that the parent compound and its metabolite undergo metabolic interconversion-tri...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015828027060
更新日期：1992-04-01 00:00:00
abstract：PURPOSE:Excipients are added to lyophilized protein drug formulations to protect the protein during processing and storage, but the mechanisms are poorly understood. Here, hydrogen/deuterium (H/D) exchange with mass spectrometry was used to assess protein conformation and excipient interactions in lyophilized solids. ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9365-6
更新日期：2008-02-01 00:00:00
abstract：PURPOSE:Type I collagen accumulates during liver fibrosis primarily because α-complex protein-2 (αCP(2)), encoded by the poly(rC) binding protein 2 (PCBP2) gene, binds to the 3' end of the collagen mRNA and increases its half-life. This study aimed to reverse the pro-fibrogenic effect of alcohol on hepatic stellate cel...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0475-9
更新日期：2011-12-01 00:00:00
