Tissue and species differences in the glucuronidation of glabridin with UDP-glucuronosyltransferases

Chemico-biological Interactions
Bin GuoHongzhi Sun

Abstract

Glabridin (GA) has gained wide application in the cosmetics and food industry. This study was performed to investigate its metabolic inactivation and elimination by glucuronidation by use of liver and intestine microsomes from humans (HLM and HIM) and rats (RLM and RIM), and liver microsomes from cynomolgus monkeys and beagle dogs (CyLM and DLM). Both hydroxyl groups at the C2 and C4 positions of the B ring are conjugated to generate two mono-glucuronides (M1 and M2). HIM, RIM and RLM showed the most robust activity in catalyzing M2 formation with intrinsic clearance values (Clint) above 2000 μL/min/mg, with little measurable M1 formation activity. DLM displayed considerable activity both in M1 and M2 formation, with Clint values of 71 and 214 μL/min/mg, respectively, while HLM and CyLM exhibited low activities in catalyzing M1 and M2 formation, with Clint values all below 20 μL/min/mg. It is revealed that UGT1A1, 1A3, 1A9, 2B7, 2B15 and extrahepatic UGT1A8 and 1A10 are involved in GA glucuronidation. Nearly all UGTs preferred M2 formation except for UGT1A1. Notably, UGT1A8 displayed the highest activity with a Clint value more than 5-fold higher than the other isoforms. Chemical inhibition studies, using selective inhibitors o...Continue Reading

References

May 23, 2002·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Ute M KentPaul F Hollenberg
Feb 14, 2003·Drug Metabolism and Disposition : the Biological Fate of Chemicals·M K ShelbyC D Klaassen
Oct 10, 2006·Chemico-biological Interactions·Nobumitsu HaniokaShizuo Narimatsu
Jan 16, 2007·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Jie CaoShu-Feng Zhou
Jul 20, 2007·Journal of the American College of Nutrition·Fumiki AokiTatsumasa Mae
Oct 16, 2007·Journal of Nutritional Science and Vitaminology·Chinatsu ItoKazuki Kanazawa
Nov 5, 2008·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·W LiL Yang
May 12, 2009·Drug Metabolism and Pharmacokinetics·Masuhiro NishimuraShinsaku Naito
Nov 26, 2010·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Hongbo ZhangMoshe Finel
Oct 15, 2011·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Michael H CourtMoshe Finel
May 18, 2012·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Liangliang ZhuLing Yang
Mar 7, 2013·Drug Metabolism Reviews·Satya Prakash TripathiAbhay T Sangamwar
Jul 16, 2013·Fitoterapia·Charlotte SimmlerShao-Nong Chen
Sep 27, 2013·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Limei AiYanyan Zhang

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Citations

Feb 16, 2016·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Hong XinLing Yang
Jul 26, 2018·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Yang-Liu XiaGuang-Bo Ge
Mar 2, 2019·European Journal of Drug Metabolism and Pharmacokinetics·Yangliu Xia, Huilin Pang
Sep 19, 2020·International Journal of Obesity : Journal of the International Association for the Study of Obesity·Leo Sungwong ChoiSang-Ku Yoo
Nov 2, 2019·Chemico-biological Interactions·Ya-Qiao WangHui Tang

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