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白藜芦醇对人肝微粒体中9种细胞色素P450和6种尿苷二磷酸葡萄糖醛酸转移酶同工型立体选择性食物-药物相互作用潜力的综合研究。

Comprehensive Investigation of Stereoselective Food Drug Interaction Potential of Resveratrol on Nine P450 and Six UGT Isoforms in Human Liver Microsomes.

作者信息

Ji Seung-Bae, Park So-Young, Bae Subin, Seo Hyung-Ju, Kim Sin-Eun, Lee Gyung-Min, Wu Zhexue, Liu Kwang-Hyeon

机构信息

BK21 FOUR KNU Community-Based Intelligent Novel Drug Discovery Education Unit, Daegu 41566, Korea.

Research Institute of Pharmaceutical Sciences, College of Pharmacy, Daegu 41566, Korea.

出版信息

Pharmaceutics. 2021 Sep 7;13(9):1419. doi: 10.3390/pharmaceutics13091419.

DOI:10.3390/pharmaceutics13091419
PMID:34575495
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8470274/
Abstract

The stereoselectivity of the food drug inhibition potential of resveratrol on cytochrome P450s and uridine 5'-diphosphoglucuronosyl transferases was investigated in human liver microsomes. Resveratrol enantiomers showed stereoselective inhibition of CYP2C9, CYP3A, and UGT1A1. The inhibitions of CYP1A2, CYP2B6, and CYP2C19 by resveratrol were stereo-nonselective. The estimated values determined for CYP1A2 were 13.8 and 9.2 μM for - and -resveratrol, respectively. -resveratrol noncompetitively inhibited CYP3A and UGT1A1 activities with values of 23.8 and 27.4 μM, respectively. -resveratrol inhibited CYP1A2, CYP2C19, CYP2E1, and CYP3A in a time-dependent manner with shift values >2.0, while -resveratrol time-dependently inhibited CYP2C19 and CYP2E1. The time-dependent inhibition of -resveratrol against CYP3A4, CYP2E1, CYP2C19, and CYP1A2 was elucidated using glutathione as a trapping reagent. This information helped the prediction of food drug interaction potentials between resveratrol and co-administered drugs which are mainly metabolized by UGT1A1, CYP1A2, CYP2C19, CYP2E1, and CYP3A.

摘要

在人肝微粒体中研究了白藜芦醇对细胞色素P450酶和尿苷5'-二磷酸葡萄糖醛酸基转移酶的食物药物抑制潜力的立体选择性。白藜芦醇对映体对CYP2C9、CYP3A和UGT1A1表现出立体选择性抑制。白藜芦醇对CYP1A2、CYP2B6和CYP2C19的抑制无立体选择性。对CYP1A2测定的估计值，反式白藜芦醇和顺式白藜芦醇分别为13.8和9.2μM。反式白藜芦醇非竞争性抑制CYP3A和UGT1A1活性，IC50值分别为23.8和27.4μM。顺式白藜芦醇以时间依赖性方式抑制CYP1A2、CYP2C19、CYP2E1和CYP3A，IC50位移值>2.0，而反式白藜芦醇以时间依赖性方式抑制CYP2C19和CYP2E1。使用谷胱甘肽作为捕获试剂阐明了反式白藜芦醇对CYP3A4、CYP2E1、CYP2C19和CYP1A2的时间依赖性抑制。该信息有助于预测白藜芦醇与主要由UGT1A1、CYP1A2、CYP2C19、CYP2E1和CYP3A代谢的联合用药之间的食物药物相互作用潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/aafbaf87c9c0/pharmaceutics-13-01419-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/13de4b289b57/pharmaceutics-13-01419-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/0c03b4068d63/pharmaceutics-13-01419-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/93d9c2b1beb2/pharmaceutics-13-01419-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/684ac6be58df/pharmaceutics-13-01419-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/aafbaf87c9c0/pharmaceutics-13-01419-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/13de4b289b57/pharmaceutics-13-01419-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/0c03b4068d63/pharmaceutics-13-01419-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/93d9c2b1beb2/pharmaceutics-13-01419-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/684ac6be58df/pharmaceutics-13-01419-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9198/8470274/aafbaf87c9c0/pharmaceutics-13-01419-g005.jpg

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