Glucuronidation of aurantio-obtusin: identification of human UDP-glucuronosyltransferases and species differences

Bao-Li MiPharmaceutical College, Liaoning University of Traditional Chinese Medicine DalianChina

Qi SunResearch and Development Department, JiLin Aodong Medicine Industry Group Co., Ltd. DunhuaChina

Yan-Qing QuThyroid Surgery, Yantaishan Hospital, Yantai ShandongChina

Xiao-Xu GaoPharmaceutical College, Liaoning University of Traditional Chinese Medicine DalianChina

Zhen-Wen YuPharmaceutical College, Liaoning University of Traditional Chinese Medicine DalianChina

Guang-Bo GeLaboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Academy of Sciences DalianChina

Shan-Shan CaiPharmaceutical College, Liaoning University of Traditional Chinese Medicine DalianChina

Jie ZhangPharmaceutical College, Liaoning University of Traditional Chinese Medicine DalianChina

Yan-Chao ZhengPharmaceutical College, Liaoning University of Traditional Chinese Medicine DalianChina

Zhen-Qiu ZhangPharmaceutical College, Liaoning University of Traditional Chinese Medicine DalianChinaCorrespondence[email protected]

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Abstract

1. The aurantio-obtusin’s glucuronide was detected when aurantio-obtusin was incubated with human liver microsomes (HLMs). Recombinant UGT isoforms screening experiment showed that UGT1A8 was the major isoform contributed to the glucuronidation.

2. The metabolic profiles for aurantio-obtusin in liver microsomes from different species were similar, however, the intrinsic clearance values (V_max/K_m) among the species were: Monkey > Human > Rat > Rabbit > Dog > Pig > Mouse > Guinea pig.

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Glucuronidation of aurantio-obtusin: identification of human UDP-glucuronosyltransferases and species differences

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Glucuronidation of aurantio-obtusin: identification of human UDP-glucuronosyltransferases and species differences

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