Cellular Pharmacokinetic Aspects of Reversal Effect of Itraconazole on P-Glycoprotein-Mediated Resistance of Anticancer Drugs
スポンサーリンク
概要
- 論文の詳細を見る
The reversla effect of itraconazole on P-glycoprotein (P-gp)-mediated resistance of vinblastine, daunorubicin and doxorubicin was analyzed from a cellular pharmacokinetic point of view, namely by [^3H]azidopine photoaffinity labeling, intracellular accumulation and transcellular transport experiments. The LLC-GA5-COL150 cells, which expressed human P-gp selectively on the apical membrane due to transfection of MDR1 cDNA into the porcine kidney epithelial cells (LLC-PK_1 cells), was used here, since this cell line constructs the monolayer with tight junction, being able to characterize the cellular pharmacokinetics. In LLC-GA5-COL150 cells, itraconazole caused a reversal from resistance as shown by a growth inhibition assay. [^3H]Azidopine photoaffinity labeling demonstrated that itraconazole, vinblastine, daunorubicin and doxorubicin showed higher binding ability for P-gp compared with digoxin, suggesting the following results were via P-gp. The intracellular accumulation of [^3H]vinblastine, [^3H]daunorubicin and [^<14>C]doxorubicin after their application on the basal and apical sides was increased by itraconazole. These changes were similar to the dose modifying factors determined by the growth inhibition assay. However, their basal-to-apical transport was hardly affected by itraconazole, and this was explained by the fact that itraconazole inhibited P-gp, and subsequently increased their intracellular concentration and then the non-P-gp mediated transport from the intracellular space to apical side. The apical-to-basal transport of [^3H]vinblastine, [^3H]daunorubicin and [^<14>C]coxorubicin was increased by itraconazole, and this was reasonably explained by the inhibition of P-gp, and partly also by the increase of their intracellular concentration via the inhibition of P-gp.
- 公益社団法人日本薬学会の論文
- 1999-12-15
著者
-
TANIGAWARA Yusuke
Department of Pharmacy, School of Medicine, Keio University
-
OKUMURA Katsuhiko
Department of Hospital Pharmacy, Kobe University School of Medicine
-
SAKAEDA Toshiyuki
Department of Hospital Pharmacy, Kobe University School of Medicine
-
Kimura T
Kobe University Graduate School Of Medicine
-
Nishiguchi Kohshi
Department of Hospital Pharmacy, School of Medicine, Kobe University
-
Takara Kohji
Department of Hospital Pharmacy, Faculty of Pharmaceutical Sciences, Kyoto Pharmaceutical University
-
Okumura K
Department Of Clinical Evaluation Of Pharmacotherapy Kobe University Graduate School Of Medicine
-
Takara Kohji
Department Of Hospital Pharmacy Faculty Of Pharmaceutical Sciences Kyoto Pharmaceutical University
-
Takara Kohji
Department Of Clinical Pharmacy Faculty Of Pharmaceutical Sciences Kyoto Pharmaceutical University
-
Takara Kohji
Department Of Hospital Pharmacy School Of Medicine Kobe University
-
Sakaeda Toshiyuki
Department Of Hospital Pharmacy Kobe University Hospital
-
KOMADA Fusao
Department of Drug Informatics, Faculty of Pharmaceutical Sciences, Josai University
-
Shirakawa T
Kobe University School Of Medicine
-
Kamiyama Fumio
京都大学再生医科学研究所
-
Kodama Fusao
Cosmed Pharmaceutical Co. Ltd.
-
Tanigawara Yusuke
Department Of Clinical Pharmacokinetics And Pharmacodynamics School Of Medicine Keio University
-
Nishiguchi K
Department Of Hospital Pharmacy Kobe University School Of Medicine
-
Nishiguchi Kohshi
Department Of Clinical Pharmacy Faculty Of Pharmaceutical Sciences Kyoto Pharmaceutical University
-
Nishiguchi Kohshi
Department Of Hospital Pharmacy School Of Medicine Kobe University
-
Okumura Katsuhiko
Department Of Hospital Pharmacy School Of Medicine Kobe University
-
Okumura Katsuhiko
Department Of Clinical Evaluation Of Pharmacotherapy Kobe University Graduate School Of Medicine
-
Okumura Katsuhiko
Department Of Hospital Pharmacy Kyoto Pharmaceutical University:department Of Hospital Pharmacy Kobe
-
Komada F
Department Of Pharmacy Kobe University School Of Medicine
-
Nakamura Takeshi
Department Of Gastroenterological Surgery Kobe University Graduate School Of Medical Sciences
-
Sakai T
Department Of Internal Medicine And Gastrointestinal Endoscopy Saga Medical School
-
Nagahiro Kazumi
Department Of Hospital Pharmacy Kobe University School Of Medicine
-
Koishi Tomokazu
Department Of Hospital Pharmacy Faculty Of Pharmaceutical Sciences Kyoto Pharmaceutical University
関連論文
- 高血圧症患者におけるオルメサルタン及びアゼルニジピンの比較薬力学 : 母集団薬物動態 / 薬力学解析
- S22-3 Pharmaco-proteomics and metabolomics for personalized medicine(FIP joint conference S22 International Conference Supported by FIP and JSPHCS Individualized Medicine: Bridging between Scientific and Clinical Studies)
- Effects of 19 Herbal Extracts on the Sensitivity to Paclitaxel or 5-Fluorouracil in HeLa Cells(Biopharmacy)
- Association of Cumulative Cyclosporine Dose with Its Irreversible Nephrotoxicity in Japanese Patients with Pediatric-Onset Autoimmune Diseases(Biopharmacy)
- Phase I Study of Intravenous PSC-833 and Doxorubicin: Reversal of Multidrug Resistance
- Pharmacokinetics-based optimal dose-exploration of mycophenolate mofetil in allogeneic hematopoietic stem cell transplantation
- MEAN RESIDENCE TIME IN ORGANS IN TOXICOKINETIC STUDIES
- Antitumor Effect of Gemcitabine on Orthotopically Inoculated Human Gallbladder Cancer Cells in Nude Mice
- Correlation between expression of major histocompatibility complex class I and that of antigen presenting machineries in carcinoma cell lines of the pancreas, biliary tract and colon
- Change in Pharmacokinetics of Model Compounds with Different Elimination Processes in Rats during Hypothermia
- 健康成人における塩酸ランジオロールの母集団薬物動態モデルの構築
- Reversal Effects of Ca2+ Antagonists on Multidrug Resistance via Down-regulation of MDR1 mRNA
- Three-Dimensional, but not Two-Dimensional, Culture Results in Tumor Growth Enhancement after Exposure to Anticancer Drugs
- Knock-down of Sorcin Induces Up-regulation of MDR1 in HeLa Cells(Molecular and Cell Biology)
- Effect of Rabeprazole on MDR1-Mediated Transport of Rhodamine 123 in Caco-2 and Hvr100-6 Cells(Biopharmacy)
- Effects of Reactive Oxygen Species on Cell Proliferation and Death in HeLa Cells and Its MDR1-Overexpressing Derivative Cell Line
- Effects of carvedilol on MDR1-mediated multidrug resistance : comparison with verapamil
- Effects of St John's Wort and Hypericin on Cytotoxicity of Anticancer Drugs
- Cytotoxic Effects of 27 Anticancer Drugs in HeLa and MDR1-Overexpressing Derivative Cell Lines
- Antiproliferative Activity of Rhinacanthus nasutus (L.) KURZ Extracts and the Active Moiety, Rhinacanthin C(Pharmacology)
- High Expression of Thymidylate Synthase Leads to Resistance to 5-Fluorouracil in Biliary Tract Carcinoma in vitro
- MDR1 T-129C Polymorphism can be Predictive of Differentiation, and Thereby Prognosis of Colorectal Adenocarcinomas in Japanese(Biopharmacy)
- MDR1, MRP1 and MRP2 Genotypes and In Vitro Chemosensitivity in Japanese Patients with Colorectal Adenocarcinomas
- Intradermal Concentration of Hydroquinone after Application of Hydroquinone Ointments Is Higher than Its Cytotoxic Concentration(Biopharmacy)
- Different Contribution of CYP2C19 in the in Vitro Metabolism of Three Proton Pump Inhibitors
- MDR1 Haplotype Frequencies in Japanese and Caucasian, and in Japanese Patients with Colorectal Cancer and Esophageal Cancer
- MDR1 C3435T Polymorphism Is Predictive of Later Onset of Ulcerative Colitis in Japanese(Biopharmacy)
- Reversal Effects of Antifungal Drugs on Multidrug Resistance in MDR1-Overexpressing HeLa Cells
- IL-1β Genotype-Related Effect of Prednisolone on IL-1β Production in Human Peripheral Blood Mononuclear Cells under Acute Inflammation(Pharmacology)
- Genetic polymorphisms associated with adverse events and elimination of methotrexate in childhood acute lymphoblastic leukemia and malignant lymphoma
- Effect of Therapeutic Moderate Hypothermia on Multi-drug Resistance Protein 1-Mediated Transepithelial Transport of Drugs
- Comparison of Synthetic DNA Templates with Authentic cDNA Templates in Terms of Quantification by Real-Time Quantitative Reverse Transcription Polymerase Chain Reaction(Analytical Biochemistry)
- 電流検出方式DNAチップを用いた複数遺伝子型同時判定法のMDR1遺伝子への応用
- Comparative Study of Superoxide Dismutase in Normal and Hereditary Cataract (UPL) Rats
- Single-institute phase 2 study of thalidomide treatment for refractory or relapsed multiple myeloma : Prognostic factors and unique toxicity profile
- MDR1 Genotype-related Pharmacokinetics : Fact or Fiction?
- Effects of Polymorphisms of MDR1, MRP1, and MRP2 Genes on Their mRNA Expression Levels in Duodenal Enterocytes of Healthy Japanese Subjects(Biopharmacy)
- MDR1-Mediated Interaction of Digoxin with Antiarrhythmic or Antianginal Drugs
- Factors Influencing the Prediction of Steady State Concentrations of Digoxin
- Interaction of Docetaxel ("Taxotere") with Human P-Glycoprotein
- Cellular Pharmacokinetic Aspects of Reversal Effect of Itraconazole on P-Glycoprotein-Mediated Resistance of Anticancer Drugs
- Inhibitory Effects of a Cyclosporin Derivative, SDZ PSC 833, on Transport of Doxorubicin and Vinblastine via Human P-Glycoprotein
- Thalidomide for the Treatment of Refractory Multiple Myeloma : Association of Plasma Concentrations of Thalidomide and Angiogenic Growth Factors with Clinical Outcome
- Kidney- and Site-Selective Delivery of 5-Fluorouracil Utilizing the Absorption on the Kidney Surface in Rats
- P-gp誘導 Caco-2 細胞 : P-gp高感度 Assay System の構築
- URINARY EXCRETION AND DIURETIC RESPONSE TO FUROSEMIDE IN RATS AND HUMANS WITH RENAL INSUFFICIENCY
- FATE OF PORCINE AND HUMAN INSULIN AT THE SUBCUTANEOUS INJECTION SITE. II. IN VITRO DEGRADATION OF INSULINS IN THE SUBCUTANEOUS TISSUE OF THE RAT
- FATE OF PORCINE AND HUMAN INSULIN AT THE SUBCUTANEOUS INJECTION SITE. I. DEGRADATION AND ABSORPTION OF INSULINS IN THE RAT
- FATE OF PORCINE AND HUMAN INSULIN IN SUBCUTANEOUSLY ADMINISTERED SITE
- Pharmacokinetics of Pirarubicin in Pediatric Patients
- Determining the Optimum Dose for the Intravenous Administration of Nicardipine in the Treatment of Acute Heart Failure : A Multicenter Study
- N-Acetyltransferase2 Genotype Correlated with Isoniazid Acetylation in Japanese Tuberculous Patients
- Effects of Secretable SOD Delivered by Genetically Modified Cells on Xanthine/Xanthine Oxidase and Paraquat-Induced Cytotoxicity in Vitro
- Effects of Cu, Zn-Superoxide Dismutase Delivered by Genetically Modified Skin Fibroblasts on Cold-Induced Skin Edema in Rats
- Protective Effect of Transfection with Secretable Superoxide Dismutase (SOD) (a Signal Sequence-SOD Fusion Protein Coding cDNA) Expression Vector on Superoxide Anion-Induced Cytotoxicity in Vitro)
- Effect of Transfection with a Superoxide Dismutase Expression Plasmid on Xanthine/Xanthine Oxidase-Induced Cytotoxicity in Cultured Rat Lung Cells
- Pharmaceutical Studies for Gene Therapy : Expression of Human Cu, Zn-Superoxide Dismutase Gene Transfected by Lipofection in Rat Skin Fibroblasts
- Effect of Clarithromycin on the Bioavailability of Cyclosporin in Rats
- Effect of Transfection with Superoxide Dismutase Expression Plasmid on Superoxide Anion Induced Cytotoxicity in Cultured Rat Lung Cells
- Pharmacokinetics of Zonisamide ; Saturable Distribution into Human and Rat Erythrocytes and into Rat Brain
- Improvement in Wound Healing by Epidermal Growth Factor (EGF) Ointment. II. Effect of Protease Inhibitor, Nafamostat, on Stabilization and Efficacy of EGF in Burn
- A Novel Method for Preparation of Animal Models of Liver Damage: Liver Targeting of Carbon Tetrachloride in Rats
- Biodistribution and Pharmacokinetics of O-Palmitoyl Tilisolol, a Lipophilic Prodrug of Tilisolol, after Intravenous Administration in Rats
- Effects of Various Storage Conditions and Alterations of Antioxidant Contents on Chromatic Aberration of Hydroquinone Ointment(Biopharmacy)
- Effect of Serum Triglyceride Concentration on the Fluctuation of Whole Blood Concentration of Cyclosporin A in Patients
- Pharmacodynamic analysis of vancomycin effect alone and with serum proteins : using a novel in vitro model
- Proapoptotic Effect of a Dietary Supplement : Water Soluble Chitosan Activates Caspase-8 and Modulating Death Receptor Expression
- N-Acetyltransferase 2 Genotype-Related Sulfapyridine Acetylation and Its Adverse Events
- Optimal Dose of Omeprazole for CYP2C19 Extensive Metabolizers in Anti-Helicobacter pylori Therapy : Pharmacokinetic Considerations
- N-Acetyltransferase 2 Genotype Correlates with Sulfasarazine Pharmacokinetics after Multiple Dosing in Healthy Japanese Subjects
- Sufficient effect of 1-week omeprazole and amoxicillin dual treatment for Helicobacter pylori eradication in cytochrome P450 2C19 poor metabolizers
- ミカファンギンの小児適応のためのポピュレーションPK解析
- Linear Pharmacokinetics of Micafungin and Its Active Metabolites in Japanese Pediatric Patients with Fungal Infections(Biopharmacy)
- Pharmaceutical and Clinical Assessment of Hydroquinone Ointment Prepared by Extemporaneous Nonsterile Compounding
- INFLUENCE OF ACUTE RENAL FAILURE ON PHARMACOKINETICS OF PHENOLSULFONPHTHALEIN IN RATS : A COMPARATIVE STUDY IN VIVO AND IN THE SIMULTANEOUS PERFUSION SYSTEM OF LIVER AND KIDNEY
- INCREASED AVAILABILITY OF PROPRANOLOL IN RATS WITH URANYL NITRATE-INDUCED ACUTE RENAL FAILURE
- A novel proteomic approach to determine possible biomarkers for acute rejection after small bowel transplantation
- Discovery of new biomarkers for acute rejection and therapeutic effect of immunosuppressive drugs in the rat liver transplantation : a comprehensive gene expression analysis
- Molecular and Pharmacokinetic Properties of 222 Commercially Available Oral Drugs in Humans
- A major influence of CYP2C19 genotype on the steady-state concentration of N-desmethylclobazam
- Influence of N-Terminal Peptide and Oligosaccharide on the Clearance of t-PA
- PHARMACOKINETICS AND PHARMACODYNAMICS OF AJMALINE IN DISEASE STATES
- DISPOSITION OF SECRETIN IN RAT STOMACH AND PANCREAS
- A NONLINEAR MULTIPLE REGERSSION PROGRAM, MULTI2 (BAYES), BASED ON BAYESIAN ALGORITHM FOR MICROCOMPUTERS
- The Novel Anticancer Drug KRN5500 Interacts with, but is Hardly Transported by, Human P-Glycoprotein
- Influence of Sugar Chain on Fibrin Affinity of Recombinat t-PA
- New biomarkers for acute rejection and therapeutic effect of immunosuppressive drugs in the rat cardiac transplantation by cDNA microarray analysis
- Alteration of Propranolol Pharmacokinetics and Pharmacodynamics by Quinidine in Man
- CHARACTERIZATION OF HIGH MOLECULAR WEIGHT FORMS OF PEPTIDE DRUGS IN VIVO
- IN VIVO CONVERSION OF PEPTIDE DRUGS INTO HIGH MOLECULAR WEIGHT FORMS
- IN VIVO FORMATION OF HIGH MOLECULAR WEIGHT COMPONENTS FROM PEPTIDE DRUGS
- Relationship between Pharmacokinetic Parameters and Occurrence of Adverse Events in Clinical Trials Performed in Europe and United States for an Angiotensin II Receptor Antagonist, Telmisartan
- Pharmacokinetic Comparison of an Angiotensin II Receptor Antagonist, Telmisartan, in Japanese and Western Hypertensive Patients Using Population Pharmacokinetic Method
- Phorbol Myristate Acetate Stimulates Degradation of a Structural Analogue of Platelet-Activating Factor to a Neutral Lipid in Human Leukemic K562 Cells : Relevance to the Release of Lipids(Biochemistry/Molecular Biology)
- Direct Modulation of Secretin Binding Sites by Gastrin in the Rat Stomach
- Regulation of Epidermal Growth Factor Receptors in Rat Gastric Mucosa : Effect of Gastric Ulceration
- Regulation of Epidermal Growth Factor Receptors in Rat Gastric Mucosa : Effect of Fasting and Sialoadenectomy
- Prediction of the efficacy and safety of pioglitazone in patients with type 2 diabetes mellitus
- Serum cystatin C as a new marker for determining the optimal dosage of renally excreted drugs
- CHANGES IN EGF RECEPTORS ON PLASMA MEMBRANES FROM RAT GASTRIC MUCOSA AND INTERACTION WITH DRUGS