Biotransformation of Silybin and its Congeners
Vladimír Kren, Petr Marhol, Katerina Purchartová, Eva Gabrielová and Martin Modriansky
Affiliation: Institute of Medical Chemistry and Biochemistry, Faculty of Medicine and Dentistry, Palacky University, Hnevotínská 3, CZ-775 15 Olomouc, Czech Republic.
Silybin and its congeners belong to a group of flavonolignans with strong biological activities. These compounds are
potentially applicable in human medicine, e. g. due to their cytoprotective activity. As a part of herbal preparations available on the open
market, they face the risk of potential negative drug-drug interactions. This review aims to evaluate current knowledge on the metabolism
of these compounds by biotransformation enzymes, interactions with other drugs, their pharmacokinetics, and bioavailability. While
silybin and its derivatives interact with cytochrome P450s, only metabolism of silybin by cytochrome P450 2C8 poses a risk of adverse
effects. The main biotransformation route of silybin and derivatives was identified as conjugation, which is stereospecific in case of
silybin. Studies of the metabolism, pharmacokinetics, potentional drug – drug interactions and increasing bioavailability of these flavonolignans
play an important facet of possible therapeutical use of these compounds. The goal of our review is to aid future developments in
the area of silybin research.
Keywords: Biotransformation, cytochrome P450, diastereoisomers, glucuronidation, silibinin, silybin, silymarin, sulfonation.
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