Biotransformation of Silybin and its Congeners

0423434 - MBÚ 2014 RIV AE eng J - Journal Article
Křen, Vladimír - Marhol, Petr - Purchartová, Kateřina - Gabrielová, E. - Modrianský, M.
Biotransformation of Silybin and its Congeners.
Current Drug Metabolism. Roč. 14, č. 10 (2013), s. 1009-1021. ISSN 1389-2002. E-ISSN 1875-5453
R&D Projects: GA ČR(CZ) GAP301/11/0662; GA MŠMT(CZ) LD11051
Institutional support: RVO:61388971
Keywords : Biotransformation * cytochrome P450 * diastereoisomers
Subject RIV: CE - Biochemistry
Impact factor: 3.487, year: 2013
http://www.ncbi.nlm.nih.gov/pubmed/24261705

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
Permanent Link: http://hdl.handle.net/11104/0229532