文献类型： 外文期刊

作者： Chen, Jinqian ¹ ; Zhang, Hao ² ; Hu, Xia ³ ; Xu, Mengyuan ² ; Su, Yanjun ⁴ ; Zhang, Chunze ⁵ ; Yue, Yuan ² ; Zhang, Xiaomin ² ; Wang, Xinyu ² ; Cui, Wei ⁶ ; Zhao, Zhenyu ¹ ; Li, Xichuan ² ;

作者机构： 1.Tianjin Med Univ, Chu Hsien Mem Hosp 1, Dept Pharm, NHC Key Lab Hormones & Dev, Tianjin 300134, Peoples R China

2.Tianjin Normal Univ, Coll Life Sci, Tianjin Key Lab Anim & Plant Resistance, Tianjin 300387, Peoples R China

3.Tianjin Acad Agr Sci, Inst Plant Protect, Dept Agr Insect, Tianjin 300384, Peoples R China

4.Tianjin Med Univ, Canc Inst & Hosp, Tianjin Lung Canc Ctr, Natl Clin Res Ctr Canc, Tianjin 300060, Peoples R China

5.Tianjin Union Med Ctr, Dept Colorectal Surg, Tianjin 300121, Peoples R China

6.Nankai Univ, Sch Math Sci, LPMC, Tianjin 300070, Peoples R China

7.Tianjin Med Univ, Chu Hsien Mem Hosp 1, 6,Huanrui Bei Rd, Tianjin 300134, Peoples R China

8.Tianjin Normal Univ, 393,Binshuixi Rd, Tianjin 300387, Peoples R China

关键词： Phloretin; Apple polyphenols; Food -drug interactions; UGTs; Enzymes inhibition; IVIVE

期刊名称：TOXICOLOGY IN VITRO （ 影响因子：3.2； 五年影响因子：3.3 ）

ISSN： 0887-2333

年卷期： 2022 年 84 卷

页码：

收录情况： SCI

摘要： Phloretin is a well-known apple polyphenol possessing a wide variety of biological effects and has been widely used in many fields. However, it's unclear whether phloretin has an effect on the activity of human UGT enzymes. Our study indicated that phloretin inhibited human UGTs on a broad spectrum. Further kinetic analysis revealed that phloretin inhibited UGT1A1, 1A6, 1A9, 2B7, and 2B15 in a noncompetitive manner, with calculated Ki of 8.34 mu M, 16.69 mu M, 10.58 mu M, 17.74 mu M and 2.46 mu\M, respectively, whereas phloretin inhibited UGT1A7 in an un-competitive manner, with calculated Ki of 5.70 mu M. According to the quantitative risk prediction, co-administration of phloretin with drugs primarily metabolized by UGT1A7 and/or UGT2B15 may result in potential food-drug interactions. To sum up, when phloretin or phloretin-rich food is administered with medications metabolized by UGT1A7 and/or UGT2B15, concern should be exercised.