当前位置: X-MOL 学术Toxicol. In Vitro › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Piceatannol exhibits potential food-drug interactions through the inhibition of human UDP-glucuronosyltransferase (UGT) in Vitro.
Toxicology in Vitro ( IF 3.2 ) Pub Date : 2020-05-22 , DOI: 10.1016/j.tiv.2020.104890
Lili Jiang 1 , Zhen Wang 1 , Xiaoyu Wang 1 , Shujuan Wang 1 , Zhe Wang 1 , Yong Liu 1
Affiliation  

Piceatannol is a natural polyphenol compound found in passion fruit and blueberry with several biological activities. However, it is unclear whether piceatannol affects the activity of human UDP-glucuronosyltransferases (UGTs) enzymes. The present study aims to assess the potential inhibitory effect of piceatannol against UGTs enzymes, as well as to evaluate its potential food-drug interactions risk via UGTs inhibition. We systematically evaluated the inhibitory effects of piceatannol on UGTs using high-performance liquid chromatography by measuring the formation rates for 4-methylumbelliferoneglucuronide and imipramine N-glucuronide. The results indicated that piceatannol displayed broad-spectrum inhibition against human UGTs. Kinetic analysis showed that inhibition of piceatannol on UGT1A6 and UGT1A7 followed noncompetitive inhibition mechanism, while the inhibition on UGT1A8 and UGT1A9 obeyed competitive and mixed inhibition mechanism, respectively. The quantitative prediction of risks showed that the coadministration of piceatannol with drugs primarily cleared by UGT1A6, UGT1A7, UGT1A8, and UGT1A9 may result in potential food-drug interaction. In conclusion, additional caution should be taken when piceatannol and food containing piceatannol are co-administered with drugs metabolized by UGTs.

中文翻译:

通过体外抑制人UDP-葡萄糖醛酸转移酶(UGT),Piceatannol表现出潜在的食品-药物相互作用。

Piceatannol是一种在百香果和蓝莓中发现的天然多酚化合物,具有多种生物活性。但是,目前尚不清楚piceatannol是否会影响人类UDP-葡萄糖醛酸糖基转移酶(UGTs)酶的活性。本研究旨在评估皮卡季诺醇对UGTs酶的潜在抑制作用,并评估其通过UGTs抑制作用的潜在食品与药物相互作用的风险。我们通过测量4-甲基伞形酮葡糖醛酸和丙咪嗪N-葡糖醛酸的形成速率,使用高效液相色谱系统地评估了皮卡替诺醇对UGTs的抑制作用。结果表明,皮卡季诺醇显示出对人UGT的广谱抑制作用。动力学分析表明,皮卡季诺醇对UGT1A6和UGT1A7的抑制作用遵循非竞争性抑制机理,对UGT1A8和UGT1A9的抑制分别遵循竞争和混合抑制机制。风险的定量预测表明,皮卡季诺尔与主要由UGT1A6,UGT1A7,UGT1A8和UGT1A9清除的药物共同给药可能导致潜在的食品与药物相互作用。总之,当将皮卡替诺醇和含有皮卡替诺醇的食物与经UGT代谢的药物合用时,应格外小心。
更新日期:2020-05-22
down
wechat
bug