Pharmacokinetics of pure silybin diastereoisomers and identification of their metabolites in rat plasma

0455575 - MBÚ 2016 RIV GB eng J - Článek v odborném periodiku
Marhol, Petr - Bednář, P. - Kolářová, P. - Večeřa, R. - Ulrichová, J. - Tesařová, E. - Vavříková, Eva - Kuzma, Marek - Křen, Vladimír
Pharmacokinetics of pure silybin diastereoisomers and identification of their metabolites in rat plasma.
Journal of Functional Foods. Roč. 14, APR 2015 (2015), s. 570-580. ISSN 1756-4646. E-ISSN 2214-9414
Grant CEP: GA ČR(CZ) GAP301/11/0767; GA MŠMT LH13097
Institucionální podpora: RVO:61388971
Klíčová slova: Silybin * Silibinin * Silybin glucuronide
Kód oboru RIV: CE - Biochemie
Impakt faktor: 3.973, rok: 2015

The flavonolignan silybin (isolated from the fruits of the milk thistle, Silybum marianum), is a mixture of two diastereoisomers and has anticancer, chemoprotective, hepatoprotective and dermatoprotective properties. This compound is largely used in various functional foods, nutraceutics and food supplements. The pharmacokinetic profiles of optically pure silybins (silybin A and silybin B) were monitored in rat plasma after the intragastric administration (200 mg.kg(-1) of body weight) of each diastereoisomer. Free (unconjugated) and total (free + conjugated) silybins were monitored for 6 hours by HPLC-PDA.The metabolic profiles of each silybin diastereoisomer were completely different. Our results clearly demonstrate that silybin B (C-max = 14.50 pg.mL(-1), T-max = 2.6 hours, Tin = 2.9 hours; total silybin B) was absorbed faster and in a substantially higher amount than silybin A (C-max = 1.05 mu g.mL(-1), T-max = 3.9 hours, T-1/2 = 2.2 hours; total silybin A). The oral bioavailability of silybin B was estimated to be 0.3%.
Trvalý link: http://hdl.handle.net/11104/0256209