Affiliation:
1. School of Pharmaceutical Sciences, Shandong University, Jinan, China
Abstract
Background:
As parasite resistance to the main artemisinin drugs has emerged in Southern Asia, the
traditional herb Artemisia annua L. (AAL) from which artemisinin (QHS) isolated was found to overcome resistance
to QHS. However the component and metabolite profiles of AAL remain unclear.
Objectives:
In this study, component profiling of marker compounds in AAL (amorphane sesquiterpene lactones and flavonoids) was performed, and their subsequent metabolism was investigated in rats.
Methods:
For efficient component classification and structural characterization, an improved liquid chromatography-
tandem high-resolution mass spectrometry (HRMS)-based analytical strategy was applied, i.e., background
subtraction (BS) followed by ring-double-bond (RDB) filter in tandem with repeated BS processing.
Structures of detected components/metabolites were characterized based on integrated information including
their HRMSn patterns, RDB values, the established component/metabolite network, the biosynthesis pathways
of AAL, and/or NMR data.
Results:
A total of 38 amorphane sesquiterpene lactones and 35 flavonoids were found in AAL as prototype
compounds, among which 26 components were previously undescribed. Major compounds were identified by
comparing them with reference standards. Among 73 AAL prototypes administered, 38 were absorbed in the
circulation as the prototype. Moreover, 20 metabolites of amorphane sesquiterpene lactones and 10 metabolites
of flavonoids were detected in rats. The major metabolic pathways included oxidation, methylation, glucuronidation
and sulfation.
Conclusion:
The component and metabolite network were established for marker components in AAL, which
will be valuable to understand the synergistic antimalarial potency of QHS in A. annua L. The analytical strategy
can also be applied to other herbal medicines.
Funder
National Natural Science Foundation of China
Publisher
Bentham Science Publishers Ltd.
Subject
Clinical Biochemistry,Pharmacology
Cited by
1 articles.
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