ArticlePloS one2016
Screening of Drug Metabolizing Enzymes for the Ginsenoside Compound K In Vitro: An Efficient Anti-Cancer Substance Originating from Panax Ginseng.
Article in PloS one, 2016. 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, 28 citations in OpenAlex.
- The application ofAnnals of translational medicine · 2025Review
- Article
- Review
- Metabolism and drug interactions of Korean ginseng based on the pharmacokinetic properties of ginsenosides: Current status and future perspectives.Journal of ginseng research · 2024Review
- Emerging nanoformulation strategies for phytocompounds and applications from drug delivery to phototherapy to imaging.Bioactive materials · 2022Review
- Anticancer properties and pharmaceutical applications of ginsenoside compound K: A review.Chemical biology & drug design · 2022Review
- Status of the application of exogenous enzyme technology for the development of natural plant resources.Bioprocess and biosystems engineering · 2021Review
- Article
- Effect of herbs for treating coronary heart disease on the CYP450 enzyme system and transporters.American journal of translational research · 2020Review
- Effects of compound K, an enteric microbiome metabolite of ginseng, in the treatment of inflammation associated colon cancer.Oncology letters · 2018Article
- Review
- Single- and Multiple-Dose Trials to Determine the Pharmacokinetics, Safety, Tolerability, and Sex Effect of Oral Ginsenoside Compound K in Healthy Chinese Volunteers.Frontiers in pharmacology · 2017Article
- Improved oral bioavailability of 20(R)-25-methoxyl-dammarane-3β, 12β, 20-triol using nanoemulsion based on phospholipid complex: design, characterization, and in vivo pharmacokinetics in rats.Drug design, development and therapy · 2016Article
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Authors and funding
11 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Ginsenoside compound K (CK), a rare ginsenoside originating from Panax Ginseng, has been found to possess unique pharmacological activities specifically as anti-cancers. However, the role of cytochrome P450s (CYPs) in the metabolism of CK is unclear. In this study, we screened the CYPs for the metabolism of CK in vitro using human liver microsomes (HLMs) or human recombinant CYPs. The results showed that CK inhibited the enzyme activities of CYP2C9 and CYP3A4 in the HLMs. The Km and Vmax values of CK were 84.20±21.92 μM and 0.28±0.04 nmol/mg protein/min, respectively, for the HLMs; 34.63±10.48 μM and 0.45±0.05 nmol/nmol P450/min, respectively, for CYP2C9; and 27.03±5.04 μM and 0.68±0.04 nmol/nmol P450/min, respectively, for CYP3A4. The IC50 values were 16.00 μM and 9.83 μM, and Ki values were 14.92 μM and 11.42μM for CYP2C9 and CYP3A4, respectively. Other human CYP isoforms, including CYP1A2, CYP2A6, CYP2D6, CYP2E1, and CYP2C19, showed minimal or no effect on CK metabolism. The results suggested that CK was a substrate and also inhibitors for both CYP2C9 and CYP3A4. Patients using CK in combination with therapeutic drugs that are substrates of CYP2C9 and CYP3A4 for different reasons should be careful, although the inhibiting potency of CK is much poorer than that of enzyme-specific inhibitors.
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