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Potential food-drug interaction risk of thymoquinone with warfarin
Chemico-Biological Interactions ( IF 4.7 ) Pub Date : 2022-07-31 , DOI: 10.1016/j.cbi.2022.110070
Zhen Wang 1 , Zhe Wang 1 , Xiaoyu Wang 1 , Xin Lv 1 , Hang Yin 1 , Lili Jiang 1 , Yangliu Xia 1 , Wei Li 2 , Wenli Li 1 , Yong Liu 1
Affiliation  

Thymoquinone, predominant bioactive compound in Nigella sativa L. (N.sativa) oil, may inhibit the activity of cytochrome P450 2C9 (CYP2C9). However, it is not clear whether thymoquinone can affect the pharmacokinetic behavior of warfarin. Thus, we further to investigate the effect of thymoquinone on warfarin 7-hydroxylation activity and to quantitatively evaluate their food-drug interactions (FDIs) potential. Our data demonstrated that thymoquinone could inhibit warfarin 7-hydroxylase activity with IC50 value of 11.35 ± 0.25 μM. The kinetic analysis indicated that thymoquinone exhibited competitive inhibition on warfarin 7-hydroxylation with Ki value of 3.50 ± 0.44 μM. FDIs risk prediction suggested that coadministration of thymoquinone (>18 mg/day) or dietary supplements containing thymoquinone (N.sativa > 1 g/day or N. sativa oil >1 g/day) might influence pharmacokinetic behavior of warfarin. In conclusion, coadministration of thymoquinone or dietary supplements containing thymoquinone in warfarin-treated patients would likely trigger off unexpected potential drug interactions.



中文翻译:

百里香醌与华法林的潜在食物-药物相互作用风险

百里醌是Nigella sativa L. ( N.sativa ) 油中的主要生物活性化合物,可抑制细胞色素 P450 2C9 (CYP2C9) 的活性。然而,尚不清楚百里醌是否会影响华法林的药代动力学行为。因此,我们进一步研究百里醌对华法林 7-羟基化活性的影响,并定量评估它们的食物-药物相互作用 (FDI) 潜力。我们的数据表明,百里醌可以抑制华法林 7-羟化酶活性,IC 50值为 11.35 ± 0.25 μM。动力学分析表明,百里醌对华法林 7-羟基化与K i表现出竞争性抑制作用。值为 3.50 ± 0.44 μM。FDI 风险预测表明,同时服用百里醌(>18 mg/天)或含有百里醌的膳食补充剂(N.sativa > 1 g/天或N. sativa oil >1 g/天)可能会影响华法林的药代动力学行为。总之,在华法林治疗的患者中同时服用百里醌或含有百里醌的膳食补充剂可能会引发意想不到的潜在药物相互作用。

更新日期:2022-07-31
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