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Xenobiotica
the fate of foreign compounds in biological systems
Volume 48, 2018 - Issue 4
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General Xenobiochemistry

Glucuronidation of icaritin by human liver microsomes, human intestine microsomes and expressed UDP-glucuronosyltransferase enzymes: identification of UGT1A3, 1A9 and 2B7 as the main contributing enzymes

Li WangCollege of Pharmacy, Jinan University, Guangzhou, P.R. China, ;Guangdong Provincial Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, P.R. China,
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Xiaodan HongCollege of Pharmacy, Jinan University, Guangzhou, P.R. China, ;Guangdong Provincial Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, P.R. China,
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Zhihong YaoCollege of Pharmacy, Jinan University, Guangzhou, P.R. China, ;Guangdong Provincial Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, P.R. China, Correspondence[email protected] [email protected]
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Yi DaiCollege of Pharmacy, Jinan University, Guangzhou, P.R. China, ;Guangdong Provincial Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, P.R. China,
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Guoping ZhaoIntegrated Chinese and Western Medicine Postdoctoral Research Station, Jinan University, Guangzhou, P.R. China, and
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Zifei QinCollege of Pharmacy, Jinan University, Guangzhou, P.R. China, ;Guangdong Provincial Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, P.R. China, ;Integrated Chinese and Western Medicine Postdoctoral Research Station, Jinan University, Guangzhou, P.R. China, and Correspondence[email protected]
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Baojian WuCollege of Pharmacy, Jinan University, Guangzhou, P.R. China, ;Guangdong Provincial Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, P.R. China, ;Integrated Chinese and Western Medicine Postdoctoral Research Station, Jinan University, Guangzhou, P.R. China, and
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Frank J. GonzalezLaboratory of Metabolism, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, MD, USA
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Xinsheng YaoCollege of Pharmacy, Jinan University, Guangzhou, P.R. China, ;Guangdong Provincial Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, College of Pharmacy, Jinan University, Guangzhou, P.R. China, ;Integrated Chinese and Western Medicine Postdoctoral Research Station, Jinan University, Guangzhou, P.R. China, and
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Pages 357-367 | Received 22 Mar 2017, Accepted 21 Apr 2017, Published online: 15 May 2017

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Yang Li, Jinjin Xu, Chunxia Xu, Zifei Qin, Shishi Li, Liufang Hu, Zhihong Yao, Frank J. Gonzalez & Xinsheng Yao. (2020) Metabolism and disposition of corylifol A from Psoralea corylifolia: metabolite mapping, isozyme contribution, species differences and identification of efflux transporters for corylifol A-O-glucuronide in HeLa1A1 cells. Xenobiotica 50:8, pages 997-1008.
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Jie Yang, Kailing Li, Dan He, Jing Gu, Jingyu Xu, Jiaxi Xie, Min Zhang, Yuying Liu, Qunyou Tan & Jingqing Zhang. (2020) Toward a better understanding of metabolic and pharmacokinetic characteristics of low-solubility, low-permeability natural medicines. Drug Metabolism Reviews 52:1, pages 19-43.
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Nguyen Thi Huong & Ninh The Son. (2023) Icaritin: A phytomolecule with enormous pharmacological values. Phytochemistry 213, pages 113772.
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Xiang Chen, Luyao Han, Yulin Zhao, Haoyan Huang, He Pan, Chenmeng Zhang, Huili Chen, Shanliang Sun, Sihui Yao, Xijing Chen & Yongjie Zhang. (2023) Mechanistic Study of Icaritin-Induced Inactivation of Cytochrome P450 2C9. Drug Metabolism and Disposition 51:6, pages 771-781.
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Siva Nageswara Rao Gajula, Sakina Asgar Vora, Amol G. Dikundwar & Rajesh Sonti. 2023. Dosage Forms - Innovation and Future Perspectives. Dosage Forms - Innovation and Future Perspectives.
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Dalong Wang, Jing Liu, Xiaodong Chen, Jing Chen, Tingting Zhao, Jie Du, Changyuan Wang, Qiang Meng, Huijun Sun, Fangjun Wang, Kexin Liu & Jingjing Wu. (2022) Renal transporter OAT1 and PPAR ‐α pathway co‐contribute to icaritin‐induced nephrotoxicity . Phytotherapy Research 37:2, pages 549-562.
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Zhangyang Bi, Wei Zhang & Xiaoyan Yan. (2022) Anti-inflammatory and immunoregulatory effects of icariin and icaritin. Biomedicine & Pharmacotherapy 151, pages 113180.
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Ji Li, Zhangyao Xu & Jifeng Gu. (2022) UGT1A1 and UGT1A9 Are Responsible for Phase II Metabolism of Tectorigenin and Irigenin In Vitro. Molecules 27:13, pages 4104.
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Lifang Gao & Shuang-Qing Zhang. (2022) Antiosteoporosis Effects, Pharmacokinetics, and Drug Delivery Systems of Icaritin: Advances and Prospects. Pharmaceuticals 15:4, pages 397.
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Yawen Yuan, Jun Zhang, Boyu Fang, Xiaoqiang Xiang, Guo Ma, Shunguo Zhang, Bin Zhu & Weimin Cai. (2021) A Novel Method for Predicting the Human Inherent Clearance and Its Application in the Study of the Pharmacokinetics and Drug–Drug Interaction between Azidothymidine and Fluconazole Mediated by UGT Enzyme. Pharmaceutics 13:10, pages 1734.
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Rui Zheng, Mulong Du, Yuqiu Ge, Fang Gao, Junyi Xin, Qiang Lv, Chao Qin, Yao Zhu, Chengyuan Gu, Mengyun Wang, Qiuyuan Zhu, Zheng Guo, Shuai Ben, Haiyan Chu, Dingwei Ye, Zhengdong Zhang & Meilin Wang. (2021) Identification of low-frequency variants of UGT1A3 associated with bladder cancer risk by next-generation sequencing. Oncogene 40:13, pages 2382-2394.
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Han Xing, Jing Yang, Kaidi Ren, Zifei Qin, Peile Wang, Xiaojian Zhang, Zhihong Yao, Frank J Gonzalez & Xinsheng Yao. (2020) Investigation on the metabolic characteristics of isobavachin in Psoralea corylifolia L. (Bu-gu-zhi) and its potential inhibition against human cytochrome P450s and UDP-glucuronosyltransferases . Journal of Pharmacy and Pharmacology 72:12, pages 1865-1878.
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Xinqiang Li, Han Xing, Zifei Qin, Jing Yang, Peile Wang, Xiaojian Zhang, Zhihong Yao & Xinsheng Yao. (2020) Potential metabolism determinants and drug–drug interactions of a natural flavanone bavachinin. RSC Advances 10:58, pages 35141-35152.
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E. E. J. Kasteel, K. Darney, N. I. Kramer, J. L. C. M. Dorne & L. S. Lautz. (2020) Human variability in isoform-specific UDP-glucuronosyltransferases: markers of acute and chronic exposure, polymorphisms and uncertainty factors. Archives of Toxicology 94:8, pages 2637-2661.
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Christian Bailly. (2020) Molecular and cellular basis of the anticancer activity of the prenylated flavonoid icaritin in hepatocellular carcinoma. Chemico-Biological Interactions 325, pages 109124.
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Li Gao, Zifei Qin, Beibei Zhang, Zhao Yin, Xiaojian Zhang & Jing Yang. (2020) An investigation of the metabolic activity, isozyme contribution, species differences and potential drug–drug interactions of PI-103, and the identification of efflux transporters for PI-103- O -glucuronide in HeLa1A9 cells . RSC Advances 10:16, pages 9610-9622.
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Beibei Zhang, Jing Yang, Zifei Qin, Shishi Li, Jinjin Xu, Zhihong Yao, Xiaojian Zhang, Frank J. Gonzalez & Xinsheng Yao. (2019) Mechanism of the efflux transport of demethoxycurcumin-O-glucuronides in HeLa cells stably transfected with UDP-glucuronosyltransferase 1A1. PLOS ONE 14:5, pages e0217695.
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Liangliang He, Jinjin Xu, Qi Wang, Yezi Zhang, Zifei Qin, Yang Yu, Zhengming Qian, Zhihong Yao & Xinsheng Yao. (2018) Glucuronidation of [6]-shogaol, [8]-shogaol and [10]-shogaol by human tissues and expressed UGT enzymes: identification of UGT2B7 as the major contributor. RSC Advances 8:72, pages 41368-41375.
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Shishi Li, Jinjin Xu, Zhihong Yao, Liufang Hu, Zifei Qin, Hao Gao, Kristopher W. Krausz, Frank J. Gonzalez & Xinsheng Yao. (2018) The roles of breast cancer resistance protein (BCRP/ABCG2) and multidrug resistance-associated proteins (MRPs/ABCCs) in the excretion of cycloicaritin-3-O-glucoronide in UGT1A1-overexpressing HeLa cells. Chemico-Biological Interactions 296, pages 45-56.
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Jinjin Xu, Mengsen Li, Zhihong Yao, Yezi Zhang, Shishi Li, Liufang Hu, Zifei Qin, Frank J. Gonzalez & Xinsheng Yao. (2018) In vitrometabolic mapping of neobavaisoflavone in human cytochromes P450 and UDP-glucuronosyltransferase enzymes by ultra high-performance liquid chromatography coupled with quadrupole time-of-flight tandem mass spectrometry. Journal of Pharmaceutical and Biomedical Analysis 158, pages 351-360.
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Zifei Qin, Shishi Li, Zhihong Yao, Xiaodan Hong, Jinjin Xu, Pei Lin, Guoping Zhao, Frank J. Gonzalez & Xinsheng Yao. (2018) Metabolic profiling of corylin in vivo and in vitro. Journal of Pharmaceutical and Biomedical Analysis 155, pages 157-168.
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Zifei Qin, Shishi Li, Zhihong Yao, Xiaodan Hong, Baojian Wu, Kristopher W. Krausz, Frank J. Gonzalez, Hao Gao & Xinsheng Yao. (2018) Chemical inhibition and stable knock-down of efflux transporters leads to reduced glucuronidation of wushanicaritin in UGT1A1-overexpressing HeLa cells: the role of breast cancer resistance protein (BCRP) and multidrug resistance-associated proteins (MRPs) in the excretion of glucuronides. Food & Function 9:3, pages 1410-1423.
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Zhihong Yao, Shishi Li, Zifei Qin, Xiaodan Hong, Yi Dai, Baojian Wu, Wencai Ye, Frank J. Gonzalez & Xinsheng Yao. (2017) Characterization of human UDP-glucuronosyltransferases responsible for glucuronidation and inhibition of norbakuchinic acid, a primary metabolite of hepatotoxicity and nephrotoxicity component bakuchiol in Psoralea corylifolia  L. . RSC Advances 7:83, pages 52661-52671.
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