Vliv standardizovaného extraktu LI 160 (Hypericum perforatum) na metabolickou aktivitu cytochromu P-450 CYP1A2, CYP2C6, CYP2D2 a CYP3A1/2 v preklinickém experimentu.
| Title in English | Effect of standardized extract LI 160 (Hypericum perforatum) on metabolic activity of CYP-450 CYP1A2, CYP2C6, CYP2D2 and CYP3A1/2 in preclinical experiment. |
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| Authors | |
| Year of publication | 2004 |
| Type | Article in Proceedings |
| Conference | In MediFórum. |
| MU Faculty or unit | |
| Citation | |
| Field | Pharmacology and pharmaceutical chemistry |
| Keywords | St Johns wort; CYP-450 |
| Description | St. Johns wort (Hypericum perforatum) is a popular over-the-counter dietary supplement and a herbal antidepressant that has been implicated in drug interactions with substrates of several cytochrome P450 (CYP) isozymes. The effects of the St. Johns wort extract (100 mg/kg, i.p., once daily for 10 days) on metabolic activity of CYP450 was assessed in the system of isolated perfused rat liver. The substrates used in this study were tolbutamide (CYP2C6), dextromethorphan (CYP2D2) and midazolam (CYP3A2). Validated HPLC method was used to quantify all compounds of interest. St. Johns wort administration affected CYP activity, caused a significant decline in AUC of dextromethorphan [F(4,31)=1511, p<0.001; PLSD, p<0.001] and AUC of midazolam [F(3,25)=221, p<0.001; PLSD, p=0.035] and a significant increase in AUC of tolbutamide [F(3,26)=200, p<0.001; PLSD, p<0.001]. St. Johns wort administration resulted in a significant induction of CYP2D2 and CYP3A2, and in a significant inhibition of CYP2C6 metabolic activities. |
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