ArticleThe AAPS journal2016
In Vivo Exposure of Kaempferol Is Driven by Phase II Metabolic Enzymes and Efflux Transporters.
Article in The AAPS journal, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 48 citations in OpenAlex.
- Anticancer Potential of Cherry Extracts and Major Flavonols: Focus on Quercetin and Kaempferol Molecular Mechanisms in Breast Cancer.International journal of molecular sciences · 2026Review
- AI-guided identification of natural CTSL inhibitors with therapeutic potential for renal injury.PLoS computational biology · 2026Article
- PEGylated liposomes enhance the pharmacokinetics, biodistribution, anticancer efficacy, and safety of Kaempferol, a phytomolecule enrolled in clinical trials.Scientific reports · 2026Article
- Targeting neuroimmune interactions: the therapeutic potential of kaempferol in immune-related central nervous system disorders.Frontiers in immunology · 2026Review
- Orchestration of kaempferol nuclear translocation by phase ii metabolic enzymes and efflux transporters suppresses colorectal cancer.PloS one · 2026Article
- Immunomodulatory Potential of Kaempferol Isolated fromInternational journal of molecular sciences · 2025Article
- The Prebiotic Effect of Kaempferol in Regulating Bile Acid Metabolism.Food science & nutrition · 2025Article
- An acute herb-drug interaction of Magnoliae Officinalis Cortex with methotrexate via inhibiting multidrug resistance-associated protein 2.Journal of food and drug analysis · 2024Article
- Beneficial role of kaempferol and its derivatives from different plant sources on respiratory diseases in experimental models.Inflammopharmacology · 2023Review
- Natural Blockers of PD-1/PD-L1 Interaction for the Immunotherapy of Triple-Negative Breast Cancer-Brain Metastasis.Cancers · 2022Review
- Therapeutic Importance of Kaempferol in the Treatment of Cancer through the Modulation of Cell Signalling Pathways.Molecules (Basel, Switzerland) · 2022Review
- Systematically Exploring the Chemical Ingredients and Absorbed Constituents ofMolecules (Basel, Switzerland) · 2022Article
- Bioactive Compounds and Metabolites from Grapes and Red Wine in Breast Cancer Chemoprevention and Therapy.Molecules (Basel, Switzerland) · 2020Review
- Dihydromyricetin: A review on identification and quantification methods, biological activities, chemical stability, metabolism and approaches to enhance its bioavailability.Trends in food science & technology · 2019Review
- Kaempferol: A Key Emphasis to Its Anticancer Potential.Molecules (Basel, Switzerland) · 2019Review
- The roles of breast cancer resistance protein (BCRP/ABCG2) and multidrug resistance-associated proteins (MRPs/ABCCs) in the excretion of cycloicaritin-3-O-glucoronide in UGT1A1-overexpressing HeLa cells.Chemico-biological interactions · 2018Article
- Breast Cancer Resistance Protein and Multidrug Resistance Protein 2 Regulate the Disposition of Acacetin Glucuronides.Pharmaceutical research · 2017Article
- Non-digestible stachyose promotes bioavailability of genistein through inhibiting intestinal degradation and first-pass metabolism of genistein in mice.Food & nutrition research · 2017Article
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 2 countries.
Funding
Abstract
Kaempferol is a well-known flavonoid; however, it lacks extensive pharmacokinetic studies. Phase II metabolic enzymes and efflux transporters play an important role in the disposition of flavonoids. This study aimed to investigate the mechanism by which phase II metabolic enzymes and efflux transporters determine the in vivo exposure of kaempferol. Pharmacokinetic analysis in Sprague-Dawley rats revealed that kaempferol was mostly biotransformed to conjugates, namely, kaempferol-3-glucuronide (K-3-G), kaempferol-7-glucuronide (K-7-G), and kaempferol-7-sulfate, in plasma. K-3-G represented the major metabolite. Compared with that in wild-type mice, pharmacokinetics in knockout FVB mice demonstrated that the absence of multidrug resistance protein 2 (MRP2) and breast cancer resistance protein (BCRP) significantly increased the area under the curve (AUC) of the conjugates. The lack of MRP1 resulted in a much lower AUC of the conjugates. Intestinal perfusion in rats revealed that the glucuronide conjugates were mainly excreted in the small intestine, but 7-sulfate was mainly excreted in the colon. In Caco-2 monolayers, K-7-G efflux toward the apical (AP) side was significantly higher than K-3-G efflux. In contrast, K-3-G efflux toward the basolateral (BL) side was significantly higher than K-7-G efflux. The BL-to-AP efflux was significantly reduced in the presence of the MRP2 inhibitor LTC4. The AP-to-BL efflux was significantly decreased in the presence of the BL-side MRPs inhibitor MK571. The BCRP inhibitor Ko143 decreased the glucuronide conjugate efflux. Therefore, kaempferol is mainly exposed as K-3-G in vivo, which is driven by phase II metabolic enzymes and efflux transporters (i.e., BCRP and MRPs).
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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.