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SCREENING OF SOME SELECTED PLANTS FOR CYP3A INHIBITION AND BIOAVAILABILITY ENHANCEMENT

Journal Name:

  • Advance Research in Pharmaceuticals and Biologicals

Publication Year:

  • 2011

Key Words:

Author Name
Abstract (2. Language): 
Herbals and other natural remedies could affect the disposition of conventional pharmaceuticals through inhibition of human cytochrome P-450 (CYP) enzymes. The inhibitory effect of five selected plants extracts on cytochrome P450 3A were investigated using rat liver microsomes. The methanol soluble fractions of five selected plant samples, prepared from methanolic extracts, demonstrated inhibitory activity of CYP3A enzyme by using in vitro assay, erythromycin n-demethylation (EMD). Among these five plants Daucus carota (Carrot), Embilica officinale (Amla) and Zingiber officinale (Ginger), and ketoconazole (10 mM) (positive control) have shown CYP3A inhibitory activity 669.33 ± 11.135, 868.33 ± 14.107, 484.00 ± 9.292 and 349.67 ± 7.00 nM/mg protein per min, respectively. In another experiment, erythromycin estolate was administered orally (50 mg/kg) to active ginger extract (200 mg/kg) pretreated male rats and its plasma levels were determined at various time points (0.5, 1, 2, 4, 8 and 24 h after oral administration by HPLC. Active ginger extract pretreatment increased AUC0–∞ of erythromycin estolate after oral administration by 6%, suggesting decreased metabolism, which could be due to inhibition of CYP3A by ginger extract. In conclusion, add-on preparations containing ginger may increase the bioavailability of erythromycin, and hence should be cautiously used.
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  • 1
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  • English

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