Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2020 Apr;41(4-5):221-225.
doi: 10.1002/bdd.2230. Epub 2020 May 22.

Deoxyshikonin reversibly inhibits cytochrome P450 2B6

Ju-Hyun Kim  1 , Su Min Choi  2 , Riya Shreatha  2 , Gil-Saeng Jeong  3 , Tae Cheon Jeong  1 , Sangkyu Lee  2
Affiliations

Deoxyshikonin reversibly inhibits cytochrome P450 2B6

Ju-Hyun Kim et al. Biopharm Drug Dispos. 2020 Apr.

Abstract

Deoxyshikonin, a natural shikonin derivative, is the major component of Lithospermum erythrorhizon and exhibits various pharmacological effects such as lymphangiogenetic, antibacterial, wound healing, and anticancer effects. To investigate the herb-drug interaction potential associated with deoxyshikonin, the inhibitory effects of deoxyshikonin on eight major cytochrome P450 (CYP) enzymes were examined using cocktail substrate-incubated human liver microsomes. Deoxyshikonin strongly inhibited CYP2B6-catalyzed bupropion hydroxylation, with a Ki value of 3.5 μM, and the inhibition was confirmed using purified human CYP2B6. The inhibition was reversible because the inhibitory effect of deoxyshikonin was not dependent on the preincubation time. The results indicated that deoxyshikonin-induced drug-drug interaction should be considered when any herb containing deoxyshikonin is used for conventional medications.

Keywords: cytochrome P450 2B6; deoxyshikonin; herb-drug interaction; reversible inhibition.

PubMed Disclaimer

References

REFERENCES

    1. Andujar, I., Rios, J. L., Giner, R. M., & Recio, M. C. (2013). Pharmacological properties of shikonin - a review of literature since 2002. Planta Medica, 79(18), 1685-1697. https://doi.org/10.1055/s-0033-1350934
    1. Asher, G. N., Corbett, A. H., & Hawke, R. L. (2017). Common herbal dietary supplement-drug interactions. American Family Physician, 96(2), 101-107.
    1. Brantley, S. J., Argikar, A. A., Lin, Y. S., Nagar, S., & Paine, M. F. (2014). Herb-drug interactions: challenges and opportunities for improved predictions. Drug Metabolism and Disposition, 42(3), 301-317. https://doi.org/10.1124/dmd.113.055236
    1. Chen, X., Yang, L., Oppenheim, J. J., & Howard, M. Z. (2002). Cellular pharmacology studies of shikonin derivatives. Phytotherapy Research, 16(3), 199-209. https://doi.org/10.1002/ptr.1100
    1. Court, M. H., Duan, S. X., Hesse, L. M., Venkatakrishnan, K., & Greenblatt, D. J. (2001). Cytochrome P-450 2B6 is responsible for interindividual variability of propofol hydroxylation by human liver microsomes. Anesthesiology: The Journal of the American Society of Anesthesiologists, 94(1), 110-119.

MeSH terms

LinkOut - more resources