Metabolic profile and tissue distribution of Humantenirine, an oxindole alkaloid from Gelsemium, after oral administration in rats
Metabolic profile and tissue distribution of Humantenirine, an oxindole alkaloid from Gelsemium, after oral administration in rats
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DOI：
10.1016/j.jchromb.2021.122901
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发表时间：
2021-08-22
影响因子：
3
通讯作者：
Liu, Zhao-Ying
中科院分区：
文献类型：
--
作者：
Qi, Xue-Jia;Zuo, Meng-Ting;Liu, Zhao-Ying
Humantenirine is an active oxindole alkaloid extracted from Gelsemium elegans Benth (G. elegans). In the present study, the metabolites of humantenirine in liver microsomes were first identified by HPLC/QqTOF-MS. Then, the metabolic profile and tissue distribution after oral administration in rats were further investigated. A total of seven metabolites were identified in vitro, and five metabolites in vitro were found in vivo. Moreover, a II-phase metabolite was identified first in vivo. The results indicated that humantenirine could be metabolized widely. The parent drug and its metabolites were distributed widely in various tissues and highly in the liver and pancreas. However, the parent drug and its metabolites had low peak intensities in plasma. The elimination of humantenirine occurred rapidly as well, the most unconverted forms of which were found in the kidney. Metabolic pathways, including demethylation, dehydrogenation, oxidation and glucuronidation, were proposed. The present findings may provide a basis for the study of pharmacokinetic characteristics and will contribute to the evaluation of the pharmacology and toxicity of G. elegans.
