Next Article in Journal
Manipulating Enzymes Properties with DNA Nanostructures
Previous Article in Journal
Antibacterial and Antifungal Activity of Three Monosaccharide Monomyristate Derivatives
Previous Article in Special Issue
Formulation Strategies for Enhancing the Bioavailability of Silymarin: The State of the Art
Open AccessReview

Metabolism, Transport and Drug–Drug Interactions of Silymarin

School of Pharmacy, Macau University of Science and Technology, Taipa, Macao 999078, China
Author to whom correspondence should be addressed.
Molecules 2019, 24(20), 3693;
Received: 27 September 2019 / Revised: 11 October 2019 / Accepted: 14 October 2019 / Published: 14 October 2019
(This article belongs to the Special Issue Silymarin and Derivatives: From Biosynthesis to Health Benefits)
Silymarin, the extract of milk thistle, and its major active flavonolignan silybin, are common products widely used in the phytotherapy of liver diseases. They also have promising effects in protecting the pancreas, kidney, myocardium, and the central nervous system. However, inconsistent results are noted in the different clinical studies due to the low bioavailability of silymarin. Extensive studies were conducted to explore the metabolism and transport of silymarin/silybin as well as the impact of its consumption on the pharmacokinetics of other clinical drugs. Here, we aimed to summarize and highlight the current knowledge of the metabolism and transport of silymarin. It was concluded that the major efflux transporters of silybin are multidrug resistance-associated protein (MRP2) and breast cancer resistance protein (BCRP) based on results from the transporter-overexpressing cell lines and MRP2-deficient (TR) rats. Nevertheless, compounds that inhibit the efflux transporters MRP2 and BCRP can enhance the absorption and activity of silybin. Although silymarin does inhibit certain drug-metabolizing enzymes and drug transporters, such effects are unlikely to manifest in clinical settings. Overall, silymarin is a safe and well-tolerated phytomedicine. View Full-Text
Keywords: silybin/silymarin; metabolism; efflux transporters; drug–drug interaction (DDI) silybin/silymarin; metabolism; efflux transporters; drug–drug interaction (DDI)
Show Figures

Figure 1

MDPI and ACS Style

Xie, Y.; Zhang, D.; Zhang, J.; Yuan, J. Metabolism, Transport and Drug–Drug Interactions of Silymarin. Molecules 2019, 24, 3693.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

Back to TopTop