Potential Metabolic Drug-Drug Interaction of Citrus aurantium L. (Rutaceae) Evaluating by Its Effect on 3 CYP450.

摘要: Aim:Fructus aurantii (FA) is widely used in clinic as an expectorant and digestant herb traditional Chinese medicine proven to have a variety of pharmacological functions. FA close grapefruit either by botanical taxonomy or their same components (flavonoids, etc.) has been cause drug-drug interaction when co-administrated with CYP3A4 substrates. Besides, contains many compounds, such flavonoids, which reported impact the expressions CYP450. However, effect on CYP450, whose change may affect drug safety clinical efficacy attributed interaction, still remains unknown. Methods: The protein, mRNA expression enzyme activity CYP1A2, CYP3A4, CYP2E1 rat were determined Western Blotting, RT-PCR method, cocktail respectively, after orally administration succession for 7 days. investigated HepG2 cells following FA-medicated serum incubation 24 h. Results: In rat, compared control group, significantly induced consistent corresponding CYP activities; protein was upregulated, while showed no significant change. cells, CYP1A2 up-regulated statistically not inhibited. Conclusion: be potential slight inducer unlikely until researches are conducted.