ArticlePharmaceutical research2010
In vivo inhibition of BCRP/ABCG2 mediated transport of nitrofurantoin by the isoflavones genistein and daidzein: a comparative study in Bcrp1 (-/-) mice.
Article in Pharmaceutical research, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 33 citations in OpenAlex.
- Flavonoids and semi-synthetic derivatives targeting oncogenic inflammation: dose-response relationships, toxicological profiles, and synergistic potential.Inflammopharmacology · 2026Review
- Much More than Nutrients: The Protective Effects of Nutraceuticals on the Blood-Brain Barrier in Diseases.Nutrients · 2025Review
- A close examination of BCRP's role in lactation and methods for predicting drug distribution into milk.CPT: pharmacometrics & systems pharmacology · 2024Review
- Role of the Abcg2 Transporter in Secretion into Milk of the Anthelmintic Clorsulon: Interaction with Ivermectin.Antimicrobial agents and chemotherapy · 2023Article
- Therapeutic Efficacy of Orally Administered Nitrofurantoin against Animal African Trypanosomosis Caused byPathogens (Basel, Switzerland) · 2022Article
- Isoflavones in Soybean as a Daily Nutrient: The Mechanisms of Action and How They Alter the Pharmacokinetics of Drugs.Turkish journal of pharmaceutical sciences · 2021Article
- Lactation during cholestasis: Role of ABC proteins in bile acid traffic across the mammary gland.Scientific reports · 2017Article
- Genetic and Dietary Regulation of Glyburide Efflux by the Human Placental Breast Cancer Resistance Protein Transporter.The Journal of pharmacology and experimental therapeutics · 2016Article
- No effect on pharmacokinetics of tamoxifen and 4-hydroxytamoxifen by multiple doses of red clover capsule in rats.Scientific reports · 2015Article
- Interaction of Isoflavones with the BCRP/ABCG2 Drug Transporter.Current drug metabolism · 2015Review
- Bioavailability and pharmacokinetics of genistein: mechanistic studies on its ADME.Anti-cancer agents in medicinal chemistry · 2012Review
- The anthelmintic triclabendazole and its metabolites inhibit the membrane transporter ABCG2/BCRP.Antimicrobial agents and chemotherapy · 2012Article
- An overview of the evidence and mechanisms of herb-drug interactions.Frontiers in pharmacology · 2012Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThe aim of this study was to determine in vivo inhibition by the isoflavones genistein and daidzein of nitrofurantoin (NTF), a well-known substrate of the ABC transporter BCRP/ABCG2.
methodsMDCKII cells and their human BCRP- and murine Bcrp1-transduced subclones were used to establish inhibition in transepithelial transport assays. Bcrp1(-/-) and wild-type mice were coadministered with nitrofurantoin (20 mg/kg) and a mixture of genistein (100 mg/kg) and daidzein (100 mg/kg).
resultsTransepithelial NFT transport was inhibited by the isoflavones. Plasma concentration of NTF at 30 min was 1.7-fold higher (p ≤ 0.05) in wild-type mice after isoflavone administration. AUC values were not significantly different. BCRP/ABCG2-mediated secretion into milk was inhibited since milk/plasma ratios were lower in wild-type mice with isoflavones (7.1 ± 4.2 vs 4.2 ± 1.6, p ≤ 0.05). NTF bile levels were significantly decreased by isoflavone administration in wild-type animals (8.8 ± 3.4 μg/ml with isoflavones vs 3.7 ± 3.3 μg/ml without isoflavones).
conclusionOur data showed that in vivo interaction of high doses of soy isoflavones with BCRP substrates may affect plasma levels but the main effect occurs in specific target organs, in our case, liver and mammary glands.
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Registered trials
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.