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      Profiling the metabolites of astrapterocarpan in rat hepatic 9000 g supernatant

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          Astrapterocarpan (AP) is a bioactive constituent of Astragali Radix and was selected as a model compound for investigating the in vitro metabolism of pterocarpans in this study. Its in vitro metabolism was conducted by incubation with rat hepatic 9000 g supernatant (S9) in the presence of an NADPH-generating system. At first, four compounds were isolated and their structures were elucidated as 6a-hydroxy-AP ( M1), astrametabolin I [ M2, 1a-hydroxy-9, 10-dimethoxy-pterocarp-1(2), 4-diene-3-one], 9-demethyl-AP ( M3, nissolin) and 4-methoxy-astraisoflavan ( M4, 7, 2´-dihydroxy-4, 3´, 4´-trimethoxy-isoflavan) on the basis of NMR data, respectively. Among them, M1, M2 and M4 were new compounds. Next, the metabolite profile of AP in rat hepatic S9 was obtained via HPLC-DAD-ESI-IT-TOF-MS n, and 40 new metabolites were tentatively identified. These newly identified metabolites included 9 monohydroxylated metabolites, 1 demethylated metabolite, 7 demethylated and monohydroxylated metabolites, 4 dihydroxylated metabolites, 1 hydration metabolite, 1 didemethylated metabolite, 2 glucosylated metabolites, 1 monohydroxylated and dehydrogenated metabolite, 2 monohydroxylated and demethylated and dehydrogenated metabolites, 2 dimerized metabolites, 3 dimerized and monohydroxylated metabolites, 2 dimerized and didemethylated metabolites, and 5 dimerized and demethylated metabolites. Finally, the major metabolic reactions of AP in rat hepatic S9 were summarized and found to be hydroxylation, demethylation, dimerization, hydration, and dehydrogenation. More importantly, the biotransformation from AP to M2 and the dimerization of AP by incubation with hepatic S9 were reported for the first time. In conclusion, this is the first report on the metabolism of a pure pterocarpan in animal tissues, and these findings will provide a solid basis for further studies on the metabolism of other pterocarpans.

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          Author and article information

          Chinese Journal of Natural Medicines
          Elsevier BV
          20 November 2019
          : 17
          : 11
          : 842-857
          1 State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 10000, China
          2 School of Pharmaceutical Sciences, Guizhou University, Guiyang 550000, China
          3 Shimadzu China MS Center, Beijing 10000, China
          Author notes
          *Corresponding author: XU Feng, E-mail: xufeng76@ ; CAI Shao-Qing, sqcai@

          These authors have no conflict of interest to declare.

          Copyright © 2019 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.
          Funded by: National Natural Science Foundation of China
          Award ID: 81673595
          Funded by: China Postdoctoral Science Foundation
          Award ID: 20080430293
          Funded by: China Postdoctoral Science Foundation
          Award ID: 200902040
          Funded by: Guizhou Natural Science Foundation
          Award ID: QIANKEHE [2018]1071
          This work was supported by the National Natural Science Foundation of China (No. 81673595) and China Postdoctoral Science Foundation (Nos. 20080430293 and 200902040), and Guizhou Natural Science Foundation (No. QIANKEHE [2018]1071).
          Research article


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