ArticleDrug metabolism and disposition: the biological fate of chemicals2012
Inhibition of P-glycoprotein leads to improved oral bioavailability of compound K, an anticancer metabolite of red ginseng extract produced by gut microflora.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 68 citations in OpenAlex.
- Comparative pharmacokinetics of total ginsenosides between young and aging mice.Frontiers in pharmacology · 2026Article
- Metabolism and drug interactions of Korean ginseng based on the pharmacokinetic properties of ginsenosides: Current status and future perspectives.Journal of ginseng research · 2024Review
- The preventive role of the red gingeng ginsenoside Rg3 in the treatment of lung tumorigenesis induced by benzo(a)pyrene.Scientific reports · 2023Article
- Concomitant Administration of Red Ginseng Extract with Lactic Acid Bacteria Increases the Plasma Concentration of Deglycosylated Ginsenosides in Healthy Human Subjects.Biomolecules · 2022Article
- Ginsenoside Compound K Promotes Proliferation, Migration and Differentiation of Schwann Cells via the Activation of MEK/ERK1/2 and PI3K/AKT Pathways.Neurochemical research · 2021Article
- Polymorphic Characterization, Pharmacokinetics, and Anti-Inflammatory Activity of Ginsenoside Compound K Polymorphs.Molecules (Basel, Switzerland) · 2021Article
- Oral administration of hydrolyzed red ginseng extract improves learning and memory capability of scopolamine-treated C57BL/6J mice via upregulation of Nrf2-mediated antioxidant mechanism.Journal of ginseng research · 2021Article
- The Intestinal Efflux Transporter Inhibition Activity of Xanthones from Mangosteen Pericarp: An In Silico, In Vitro and Ex Vivo Approach.Molecules (Basel, Switzerland) · 2020Article
- Caco-2 Cell Permeability of Flavonoids and Saponins fromACS omega · 2020Article
- Pharmacokinetics and Intestinal Metabolism of Compound K in Rats and Mice.Pharmaceutics · 2020Article
- Impact ofJournal of ginseng research · 2019Article
- Synergistic Effects of Plant Derivatives and Conventional Chemotherapeutic Agents: An Update on the Cancer Perspective.Medicina (Kaunas, Lithuania) · 2019Review
- In Vitro and In Situ Characterization of the Intestinal Absorption of Capilliposide B and Capilliposide C fromMolecules (Basel, Switzerland) · 2019Article
- Influence of Nutritional Status on the Absorption of Polyphyllin I, an Anticancer Candidate from Paris polyphylla in Rats.European journal of drug metabolism and pharmacokinetics · 2018Article
- Pharmacokinetic and Metabolism Studies of 12-Riboside-Pseudoginsengenin DQ by UPLC-MS/MS and UPLC-QTOF-MSMolecules (Basel, Switzerland) · 2018Article
- New generation of drug delivery systems based on ginsenoside Rh2-, Lysine- and Arginine-treated highly porous graphene for improving anticancer activity.Scientific reports · 2018Article
- A preliminary review of studies on adaptogens: comparison of their bioactivity in TCM with that of ginseng-like herbs used worldwide.Chinese medicine · 2018Review
- Differences in the intestinal microbiota between uninfected piglets and piglets infected with porcine epidemic diarrhea virus.PloS one · 2018Article
- Preparation of ginsenoside compound-K mixed micelles with improved retention and antitumor efficacy.International journal of nanomedicine · 2018Article
- An Insight into Ginsenoside Metabolite Compound K as a Potential Tool for Skin Disorder.Evidence-based complementary and alternative medicine : eCAM · 2018Review
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
Abstract
Ginsenosides are hydrolyzed extensively by gut microflora after oral administration, and their metabolites are pharmacologically active against lung cancer cells. In this study, we measured the metabolism of various ginsenosides by gut microflora and determined the mechanisms responsible for the observed pharmacokinetic behaviors of its active metabolite, Compound K (C-K). The results showed that biotransformation into C-K is the major metabolic pathway of ginsenosides after the oral administration of the red ginseng extract containing both protopanaxadiol and protopanaxatriol ginsenosides. Pharmacokinetic studies in normal mice showed that C-K exhibited low oral bioavailability. To define the mechanisms responsible for this low bioavailability, two P-glycoprotein (P-gp) inhibitors, verapamil and cyclosporine A, were used, and their presence substantially decreased C-K's efflux ratio in Caco-2 cells (from 26.6 to <3) and significantly increased intracellular concentrations (by as much as 40-fold). Similar results were obtained when transcellular transport of C-K was determined using multidrug resistance 1 (MDR1)-overexpressing Madin-Darby canine kidney II cells. In MDR1a/b(-/-) FVB mice, its plasma C(max) and AUC(0-24h) were increased substantially by 4.0- and 11.7-fold, respectively. These increases appear to be due to slower elimination and faster absorption of C-K in MDR1a/b(-/-) mice. In conclusion, C-K is the major active metabolite of ginsenosides after microflora hydrolysis of primary ginsenosides in the red ginseng extract, and inhibition/deficiency of P-gp can lead to large enhancement of its absorption and bioavailability.
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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.