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  • Silymarin, a standard extract from Silybum marianum L. seeds, contains at least 7 flavonolignans and flavonoid taxifolin. It has been used to date, as a hepatoprotectant and chemoprotectant. Flavonolignan silybin, the main component of silymarin, is composed of two diastereomers A and B in an approximately 1:1 ratio. Silybin can inhibit the activities of cytochrome P450 enzymes (CYP) (Beckmann-Knopp S. et al., 2000). In our study, the most prominent inhibition effect was found with CYP3A4 and CYP2C9 (IC50 <= 50 μM). In the second part of our study, the metabolism of silybin in vitro was analyzed in detail. The results indicated that silybin is subjected to O-demethylation by CYP2C8, enzymes of Phase I in xenobiotic metabolism. The contribution of UDP-glucuronosyltransferases (main phase II enzymes) to the metabolism of silybin and its A and B diastereomers was also investigated. Four main metabolites of silybin, namely silybin A-7-O-β-D-glucuronide, B-7-O-β-D-glucuronide, A-20-O
  • Silymarin, a standard extract from Silybum marianum L. seeds, contains at least 7 flavonolignans and flavonoid taxifolin. It has been used to date, as a hepatoprotectant and chemoprotectant. Flavonolignan silybin, the main component of silymarin, is composed of two diastereomers A and B in an approximately 1:1 ratio. Silybin can inhibit the activities of cytochrome P450 enzymes (CYP) (Beckmann-Knopp S. et al., 2000). In our study, the most prominent inhibition effect was found with CYP3A4 and CYP2C9 (IC50 <= 50 μM). In the second part of our study, the metabolism of silybin in vitro was analyzed in detail. The results indicated that silybin is subjected to O-demethylation by CYP2C8, enzymes of Phase I in xenobiotic metabolism. The contribution of UDP-glucuronosyltransferases (main phase II enzymes) to the metabolism of silybin and its A and B diastereomers was also investigated. Four main metabolites of silybin, namely silybin A-7-O-β-D-glucuronide, B-7-O-β-D-glucuronide, A-20-O (en)
Title
  • The molecular mechanism of selected pathological processes in the cell - Metabolism of silybin- a review
  • The molecular mechanism of selected pathological processes in the cell - Metabolism of silybin- a review (en)
skos:prefLabel
  • The molecular mechanism of selected pathological processes in the cell - Metabolism of silybin- a review
  • The molecular mechanism of selected pathological processes in the cell - Metabolism of silybin- a review (en)
skos:notation
  • RIV/70883521:28110/10:63510150!RIV11-MSM-28110___
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  • 272389
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  • RIV/70883521:28110/10:63510150
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  • silybin; metabolism; cytochromes P450; UDP glucuronosyltransferases (en)
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  • [BE85562E618C]
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  • Vyškov
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  • Olomouc
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  • Biomedical Papers of the Faculty of Medicine of Palacký University in Olomouc
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  • Křen, Vladimír
  • Lemr, Karel
  • Papoušková, Barbora
  • Anzenbacher, Pavel
  • Anzenbacherová, Eva
  • Jančová, Petra
  • Tunková, Alena
  • Šiller, Michal
  • Lužná, Pavla
  • Šimánek, Vilém
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issn
  • 1213-8118
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  • Univerzita Palackého v Olomouci
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  • 28110
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