NATURAL PRODUCT RESEARCH AND DEVELOPMENT ›› 2019, Vol. 31 ›› Issue (11): 1968-1974. doi: 10.16333/j.10016880.2019.11.017

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Metabolism of camptothecin derivative NCP4 in liver microsomes among different species in vitro

LIU Qiongyan1,ZHANG Meiqin1,2,QING Chen1*,LI Ji1*   

  1. 1School of Pharmaceutical Science & Yunnan Key Laboratory of Pharmacology for Natural Products,Kunming 650500,China;2Yunnan Xinxing College of Professional Technology,Kunming 650501,China
  • Online:2019-11-28 Published:2019-12-16

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Abstract: The metabolic stability and metabolites of NCP4 incubated with human,SD rat and dog liver microsomes in vitro were studied.NCP4 and its metabolites were separated and tested by HPLCUVMS (QTOF).The results showed that Tl/2 (min) of NCP4 obtained from dog and human liver microsomes were comparable;In addition,4 metabolites generated from NCP4 in rat liver microsome were found,and another 3 metabolites generated from NCP4 in human and dog liver microsomes were detected.All results mentioned above indicated that the metabolites of NCP4 in liver microsome from dogs were consistent with that from human．The results can be used to select 1aboratory animals for safety evaluation of NCP4 in preclinical study．

Key words: NCP4, camptothecin derivative, liver microsome, metabolite, metabolic stability

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