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Metabolic Profiling of Nuciferine In Vivo and In Vitro
journal contribution
posted on 2020-11-18, 17:25 authored by Hua Gao, Lei Zhang, An Zhu, Xiaoyan Liu, Tianxia Wang, Meiqi Wan, Xiuwei Yang, Yingtao Zhang, Youbo ZhangNuciferine
(NF) is one of the main constituents of Lotus (Nelumbo nucifera) leaves which have been widely used in
both food and drug formulations in China. Although possessing a broad
spectrum of bioactivities, the metabolic characteristics of NF are
inadequately unknown after oral gavage with this NF. The present study
was performed to characterize its metabolism in vivo and in vitro.
After NF oral gavage with mice, a total of 55 metabolites, containing
14 novel phase I metabolites and 18 novel phase II metabolites, were
identified with high-resolution mass spectrometry-based metabolomics.
Recombinant enzyme screenings showed that multiple cytochrome P450s,
two UDP-glucuronosyltransferases (UGT1A4, UGT1A9), and several sulfotransferases
(SULTs) participated in the metabolism of NF. In silico prediction
and molecular docking of NF to the polymorphic enzymes (CYPs) provided
additional support for the above experiments. This research details
metabolic characteristics and provides an important reference basis
for further application of NF.