Determination of novel nitrogen-containing metabolite after oral administration of swertiamarin to rats

Determination of novel nitrogen-containing metabolite after oral administration of swertiamarin to rats
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DOI:
10.1080/10286020.2011.631132
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发表时间:
2012-02
影响因子:
1.7
通讯作者:
Zhigang Wang;Xi-jun Wang;Hui Sun;Li Chen;Chao-Mei Ma
Zhigang Wang;Xi-jun Wang;Hui Sun;Li Chen;Chao-Mei Ma
中科院分区:
医学4区
文献类型:
--
作者:
Zhigang Wang;Xi-jun Wang;Hui Sun;Li Chen;Chao-Mei Ma

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在一系列环烯醚萜类化合物代谢的研究中,我们研究了当药苦苷(1)在Wistar大鼠中的代谢命运。液相色谱/离子阱质谱法在大鼠血浆中检测到新的含氮代谢产物龙胆二醇(3)。通过与由当药苦苷(1)合成的真实化合物的保留时间和质谱进行比较,明确鉴定了代谢产物的结构。首次证实了当药苦苷在体内可转化为含氮代谢产物龙胆二醇(3)。了解这种独特的代谢途径可能有助于阐明当药苦苷的临床疗效(1),也有助于研究其他天然环烯醚萜类化合物的体内代谢。
In a series of studies on the metabolism of iridoid compounds, we investigated the metabolic fate of swertiamarin (1) in Wistar rats. Liquid chromatography/ion trap mass spectrometry detected new nitrogen-containing metabolite gentiandiol (3) in rat plasma. The structure of the metabolite was unequivocally identified by comparing the retention time as well as the mass spectrum with those of authentic compound, which was synthesized from swertiamarin (1). The transformation of swertiamarin to nitrogen-containing metabolite gentiandiol (3) in vivo was verified for the first time. Understanding of this unique metabolic pathway may shed light on clinical efficacy of swertiamarin (1) and will also assist in studies for the metabolism of other natural iridoids in vivo.