Metabolic profiling of luteolin‐7‐O‐glucoside in rat urine, plasma, bile and feces after oral administration using ultra‐high‐performance liquid chromatography/quadrupole time‐of‐flight mass spectrometry
Metabolic profiling of luteolin‐7‐O‐glucoside in rat urine, plasma, bile and feces after oral administration using ultra‐high‐performance liquid chromatography/quadrupole time‐of‐flight mass spectrometry
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DOI：
10.1002/rcm.7456
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发表时间：
2016-02
影响因子：
2
通讯作者：
Hongxia Liu;X. Huo;Li-qin Ding;Xinchi Feng;Miaomiao Jiang;G. Pan;Lixia Chen;Feng Qiu
中科院分区：
文献类型：
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作者：
Hongxia Liu;X. Huo;Li-qin Ding;Xinchi Feng;Miaomiao Jiang;G. Pan;Lixia Chen;Feng Qiu
木犀草素-7-O-葡萄糖苷（L7 G）是中国灯笼的主要生物活性成分，具有抗炎、抗氧化等多种生物学功能。然而，对木樨草素-7-O-葡萄糖苷的研究主要集中在这种天然产物的提取、分离和生物活性上，而木樨草素-7-O-葡萄糖苷在体内的代谢尚未完全了解。为了探索木樨草素-7-O-葡萄糖苷的代谢特征，我们研究了其在大鼠口服给药后的血浆、胆汁、尿液和粪便样品中的代谢产物。开发了具有工作流解释策略的UPLC/QTOFMS方法，用于分析和鉴别大鼠尿液、血浆、结果在大鼠口服毛地黄黄酮-7-O-葡萄糖苷后的生物样品中共鉴定出44种毛地黄黄酮-7-O-葡萄糖苷相关代谢产物，其中尿中代谢产物35种，血浆中代谢产物17种，胆汁中代谢产物17种，粪便中代谢产物5种。结论毛地黄黄酮-7-O-葡萄糖苷在体内首先水解为毛地黄黄酮，然后进一步吸收、代谢和排泄。结果表明，Ⅰ相代谢产物为水解和还原代谢产物，Ⅱ相代谢产物为硫酸化、葡萄糖醛酸化和甲基化代谢产物。本研究为全面了解木犀草素-7-O-葡萄糖苷的代谢谱提供了科学可靠的支持，为阐明木犀草素-7-O-葡萄糖苷在体内的有效物质基础提供了依据。版权所有© 2016约翰威利父子有限公司.
RationaleLuteolin‐7‐O‐glucoside (L7G), the main bioactive ingredient of Chinese Lantern, has various biological functions, including anti‐inflammatory and anti‐oxidative activities. However, research on luteolin‐7‐O‐glucoside has focused on the extraction, separation and biological activities of this natural product, whereas the metabolism of luteolin‐7‐O‐glucosidein vivois not fully understood. In order to explore the metabolic profile of luteolin‐7‐O‐glucoside, we investigated its metabolites in plasma, bile, urine and feces samples following oral administration to rats.MethodsIn this study, an ultra‐high‐performance liquid chromatography/quadrupole time‐of‐flight mass spectrometry (UPLC/QTOFMS) method with a workflow‐interpretation strategy was developed to profile and identify the major metabolites of luteolin‐7‐O‐glucoside in rat urine, plasma, bile and feces after oral administration.ResultsA total of 44 luteolin‐7‐O‐glucoside‐related metabolites were identified in rat biological samples after oral administration of luteolin‐7‐O‐glucoside, including 35 metabolites in urine, 17 metabolites in plasma, 17 metabolites in bile and 5 metabolites in feces. Additionally, three major metabolites (M22,M40andM44) were isolated as standards from urine and feces.ConclusionsThe study indicated that luteolin‐7‐O‐glucoside was hydrolyzed to luteolin firstly, and then for further absorption, metabolism and excretionin vivo. The results showed that phase I metabolites are hydrolysis and reduction metabolites, and phase II metabolites include sulfation, glucuronidation and methylation metabolites. This research provides scientific and reliable support for full understanding of the metabolic profiling of luteolin‐7‐O‐glucoside and the results provide evidence that should help to elucidate the effective substance basis of luteolin‐7‐O‐glucosidein vivo. Copyright © 2016 John Wiley & Sons, Ltd.