Effect of silybin and its congeners on human liver microsomal cytochrome P450 activities

Phytotherapy Research

Volumn 16, Issue 7, 2002, Pages 632-638

  Zuber, Roman ^a,b   Modrianský, Martin ^b   Dvořák, Zdeněk ^b   Rohovský, Petr ^b   Ulrichová, Jitka ^b   Šimánek, Vilím ^b   Anzenbacher, Pavel ^b  

^a UNIVERSITY OF PARDUBICE   (Czech Republic)

^b PALACKÝ UNIVERSITY   (Czech Republic)

Author keywords

Cytochrome P450; Flavonolignans; Human; Microsomes; Silybum marianum

Indexed keywords

CYTOCHROME P450; CYTOCHROME P450 2D6; CYTOCHROME P450 2E1; DEHYDROSILYBIN; FLAVONOL; FLAVONOLIGNAN; SILIBININ; SILIDIANIN; SILYCRISTIN; UNCLASSIFIED DRUG;

ARTICLE; BIOTRANSFORMATION; CHEMICAL STRUCTURE; DIET SUPPLEMENTATION; DRUG EFFICACY; DRUG SAFETY; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME KINETICS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HYDROXYLATION; LIVER DISEASE; LIVER MICROSOME;

SILYBUM MARIANUM;

EID: 0036846701     PISSN: 0951418X     EISSN: None     Source Type: Journal    
DOI: 10.1002/ptr.1000     Document Type: Article

References (19)

1. Baer-Dubowska W, Szaefer H, Krajka-Kuzniak V. 1998. Inhibition of murine hepatic cytochrome P450 activities by natural and synthetic phenolic compounds. Xenobiotica 28: 735-743.
2. Beckmann-Knopp S, Rietbrock S, Weyhenmeyer R et al. 2000. Inhibitory effects of silibinin on cytochrome P-450 enzymes in human liver microsomes. Pharmacol Toxicol 86: 250-256.
3. Busby WF Jr, Ackermann JM, Crespi CL. 1999. Effect of methanol, ethanol, dimethylsulfoxide, and acetonitrile on in vitro activities of cDNA-expressed human cytochromes P-450. Drug Metabol Dispos 27: 246-249.
4. Chang TKH, Crespi C, Waxman DJ. 1998. Spectrophotometric analysis of human CYP2E1-catalyzed p-nitrophenol hydroxylation. In Methods in Molecular Biology (107): Cytochrome P450 Protocols, Phillips IR, Shephard EA (ed). Humana Press: Totowa, NJ, 147-152.
5. Chauret N, Gauthier A, Nicoll-Griffith DA. 1998. Effect of common organic solvents on in vitro cytochrome P450-mediated metabolic activities in human liver microsomes. Drug Metabol Dispos 26: 1-4.
6. Crespi CL, Chang TKH, Waxman DJ. 1998. CYP2D6-dependent bufuralol 1′-hydroxylation assayed using a reversed-phase ion-pair HPLC with fluorescence detection. In Methods in Molecular Biology (107): Cytochrome P450 Protocols, Phillips IR, Shephard EA (ed). Humana Press: Totowa, NJ; 141-145.
7. Flora K, Hahn M, Rosen H, Benner K. 1998. Milk thistle (Silybum marianum) for the therapy of liver disease. Am J Gastroenterol 93: 139-143.
8. Guengerich FP, Martin MV, Beaune PH, Kremers P, Wolff T, Waxman DJ. 1986. Characterization of rat and human liver microsomal cytochrome P-450 forms involved in nifedipine oxidation, a prototype for genetic polymorphism in oxidative drug metabolism. J Biol Chem 261: 5051-5060.
9. Lake BG. 1987. Preparation and characterization of microsomal fractions for studies on xenobiotic metabolism. In Biochemical Toxicology: A Practical Approach, Snell K Mullock B (ed). IRL:Oxford; 183-215.
10. Letteron P, Labbe G, Degott C et al. 1990. Mechanism for the protective effects of silymarin against carbon tetrachloride-induced lipid peroxidation and hepatotoxicity in mice. Evidence that silymarin acts both as an inhibitor of metabolic activation and as a chain-breaking antioxidant. Biochem Pharmacol 39: 2027-2034.
11. Lindros KO, Cai Y, Penttilä KE. 1990. Role of ethanol-inducible cytochrome P450 2E1 in carbon tetrachloride-induced damage to centrilobular hepatocytes from ethanol-treated rats. Hepatology 12: 1092-1097.
12. Miguez MP, Anundi I, Sainz-Pardo LA, Lindros KO. 1994. Hepatoprotective mechanism of silymarin: No evidence for involvement of cytochrome P450 2E1. Chem Biol Interact 91: 51-63.
13. Modrianský M, Ulrichová J, Bachleda P et al. 2000. Human hepatocytes - Model for toxicological studies. Functional and biochemical characterization. Gen Physiol Biophys 19: 223-235.
14. Nielsen SE, Breinholt V, Justesen U, Cornett C, Dragsted LO. 1998. In vitro biotransformation of flavonoids by rat liver microsomes. Xenobiotica 28: 389-401.
15. Obermeier MT, White RE, Yang CS. 1995. Effects of bioflavonoids on hepatic P450 activities. Xenobiotica 25: 575-584.
16. Omura T, Sato R. 1964. The carbon monoxide - Binding pigment of liver microsomes. J Biol Chem 239: 2370-2378.
17. Šimánek V, Křen V, Ulrichová J, Vičar J, Cvak L. 2000. Silymarin - What is in the name? Hepatology 32: 442-443.
18. 5. Methods Enzymol 52: 97-101.
19. Weyhenmeyer R, Mascher H, Birkmayer J. 1992. Study on dose-linearity of the pharmacokinetics of silibinin diastereomers using a new stereospecific assay. Int J Clin Pharm Ther Toxicol 30: 134-138.