ArticleXenobiotica; the fate of foreign compounds in biological systems2018
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.
Article in Xenobiotica; the fate of foreign compounds in biological systems, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers, 1 of them a synthesis that pooled it.
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Who cites it
16 citing papers in PubMed, 1 synthesis or guideline pooled it, 34 citations in OpenAlex.
- Human variability in isoform-specific UDP-glucuronosyltransferases: markers of acute and chronic exposure, polymorphisms and uncertainty factors.Archives of toxicology · 2020Pooled it
- Protective effects of icariin in atherosclerotic cardiovascular disease: mechanistic basis, post-ischemic protection and translational limitations.Pharmaceutical biology · 2026Review
- Article
- UGT1A1 and UGT1A9 Are Responsible for Phase II Metabolism of Tectorigenin and Irigenin In Vitro.Molecules (Basel, Switzerland) · 2022Article
- Antiosteoporosis Effects, Pharmacokinetics, and Drug Delivery Systems of Icaritin: Advances and Prospects.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Article
- Identification of low-frequency variants of UGT1A3 associated with bladder cancer risk by next-generation sequencing.Oncogene · 2021Article
- 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.The Journal of pharmacy and pharmacology · 2020Article
- Potential metabolism determinants and drug-drug interactions of a natural flavanone bavachinin.RSC advances · 2020Article
- Metabolism and disposition of corylifol A fromXenobiotica; the fate of foreign compounds in biological systems · 2020Article
- Article
- Article
- 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 · 2018Article
- 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 · 2018Article
- 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 · 2018Article
- Metabolic profiling of corylin in vivo and in vitro.Journal of pharmaceutical and biomedical analysis · 2018Article
Corrections and comments
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Authors and funding
9 authors at 2 institutions in 2 countries.
Funding
Abstract
1. Icaritin is a natural flavonoid with anti-osteoporosis activity. This study aimed to characterize icaritin glucuronidation by pooled human liver microsomes (HLM) and pooled human intestine microsomes (HIM), and to determine the contribution of individual UDP-glucuronosyltrans-ferase (UGT) enzyme to icaritin glucuronidation. 2. Glucuronidation rates were determined by incubating icaritin with uridine diphosphate glucuronic acid (UDPGA)-supplemented microsomes. Kinetic parameters were derived by appropriate model fitting. Relative activity factors and activity correlation analysis were performed to identify main UGT isoforms. 3. UGT1A3, 1A7, 1A8, 1A9 and 2B7 were mainly responsible for catalyzing the formation of two glucuronides (G1 and G2). Icaritin 3-O-glucuronidation (G1) was significantly correlated with Chenodeoxycholic acid (CDCA) glucuronidation (r = 0.787, p = 0.002), propofol glucuronidation (r = 0.661, p = 0.019) and Zidovudine (AZT) glucuronidation (r = 0.805, p = 0.002). Similarly, icaritin 7-O-glucuronidation (G2) was also correlated with CDCA glucuronidation (r = 0.640, p = 0.025), propofol glucuronidation (r = 0.592, p = 0.043) and AZT glucuronidation (r = 0.661, p = 0.019). In addition, UGT1A3, 1A9 and 2B7 contributed 37.5, 33.8 and 21.3% for G1 in pooled HLM, respectively. Also, UGT1A3, 1A9 and 2B7 contributed 34.3, 20.0 and 8.6% for G2 in pooled HLM, respectively. 4. Icaritin was subjected to significant glucuronidation, wherein UGT1A3, 1A7, 1A8, 1A9 and 2B7 were main contributing enzymes.
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