ArticlePharmaceutical research1998
Decreased expression and activity of P-glycoprotein in rat liver during acute inflammation.
Article in Pharmaceutical research, 1998. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 138 citations in OpenAlex.
- Morphine pharmacokinetics and opioid transporter expression at the blood-retina barrier of male and female mice.Frontiers in pharmacology · 2023Article
- Effects of Pro-Inflammatory Cytokines on Hepatic Metabolism in Primary Human Hepatocytes.International journal of molecular sciences · 2022Article
- Evaluation of phenoconversion phenomenon in obese patients: the effects of bariatric surgery on the CYP450 activity "a protocol for a case-control pharmacokinetic study".Journal of diabetes and metabolic disorders · 2021Article
- Inflammation Induces Changes in the Functional Expression of P-gp, BCRP, and MRP2: An Overview of Different Models and Consequences for Drug Disposition.Pharmaceutics · 2021Review
- Therapeutic Drug Monitoring of Second- and Third-Generation Antipsychotic Drugs-Influence of Smoking Behavior and Inflammation on Pharmacokinetics.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Inhibitory Effect of Berberine on Broiler P-glycoprotein Expression and Function: In Situ and In Vitro Studies.International journal of molecular sciences · 2019Article
- Association between multidrug resistance-1 C3435T gene polymorphism and right ventricular dysfunction in patients with chronic obstructive pulmonary disease: cross-sectional study.Sao Paulo medical journal = Revista paulista de medicina · 2018Article
- Pharmacokinetics, pharmacodynamics and pharmacogenetics associated with nonsteroidal anti-inflammatory drugs and opioids in pediatric cancer patients.Expert opinion on drug metabolism & toxicology · 2017Review
- Article
- Changes of Absorptive and Secretory Transporting System of (1 → 3) β-D-glucan Based on Efflux Transporter in Indomethacin-induced Rat.European journal of drug metabolism and pharmacokinetics · 2015Article
- MDR-1 gene C/T polymorphism in COPD: data from Aegean part of Turkey.International journal of clinical and experimental medicine · 2014Article
- Impact of lipopolysaccharide-induced inflammation on the disposition of the aminocephalosporin cefadroxil.Antimicrobial agents and chemotherapy · 2013Article
- Inflammatory regulation of ATP binding cassette efflux transporter expression and function in microglia.The Journal of pharmacology and experimental therapeutics · 2012Article
- Pro-inflammatory cytokine regulation of P-glycoprotein in the developing blood-brain barrier.PloS one · 2012Article
- Immunological response as a source to variability in drug metabolism and transport.Frontiers in pharmacology · 2012Article
- Frequency of the mdr-1 C>T gene polymorphism in patients with COPD.Clinics (Sao Paulo, Brazil) · 2010Article
- Interleukin-1 beta and tumor necrosis factor-alpha increase ABCG2 expression in MCF-7 breast carcinoma cell line and its mitoxantrone-resistant derivative, MCF-7/MX.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2009Article
- Influence of intermittent hypoxia on myocardial and hepatic P-glycoprotein expression in a rodent model.Pharmacotherapy · 2009Article
- Pharmacology of morphine in obese patients: clinical implications.Clinical pharmacokinetics · 2009Review
- Nuclear receptors: mediators and modifiers of inflammation-induced cholestasis.Frontiers in bioscience (Landmark edition) · 2009Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeDrug disposition is often altered in inflammatory disease. Although the influence of inflammation on hepatic drug metabolism and protein binding has been well studied, its impact on drug transport has largely been overlooked. The multidrug resistance (MDR) gene product, P-glycoprotein (P-gp) is involved in the active secretion of a large variety of drugs. Our goal was to ascertain the influence of acute inflammation (AI) on the expression and functional activity of P-gp.
methodsAI was induced in rats through turpentine or lipopolysaccharide (LPS) administration. Expression of P-gp in liver was detected at the level of protein on Western blots using the monoclonal antibody C-219 and at the level of mRNA using an RNase protection assay. P-gp mediated transport activity was assessed by measuring the verapamil-inhibitable efflux of rhodamine 123 (R123) in freshly isolated hepatocytes.
resultsTurpentine-induced AI significantly decreased the hepatic protein expression of P-gp isoforms by 50-70% and caused a significant 45-65% reduction in the P-gp mediated efflux of R123. Diminished mRNA levels of all three MDR isoforms were seen. LPS-induced AI similarly resulted in significantly reduced levels and activity of P-gp in liver. Although differences in the constitutive levels of P-gp were seen between male and female rats, the influence of AI on P-gp expression and activity was not gender specific.
conclusionsExperimentally-induced inflammation decreases the in vivo expression and activity of P-gp in liver. This is the first evidence that expression of P-gp is modulated in response to experimentally-induced inflammation.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.