Characterization of the In Vivo and In Vitro Metabolites of Linarin in Rat Biosamples and Intestinal Flora Using Ultra-High Performance Liquid Chromatography Coupled with Quadrupole Time-of-Flight Tandem Mass Spectrometry.
Characterization of the In Vivo and In Vitro Metabolites of Linarin in Rat Biosamples and Intestinal Flora Using Ultra-High Performance Liquid Chromatography Coupled with Quadrupole Time-of-Flight Tandem Mass Spectrometry.
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使用超高效液相色谱结合四极杆飞行时间串联质谱法表征大鼠生物样品和肠道菌群中 Linarin 的体内和体外代谢物。
DOI：
10.3390/molecules23092140
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发表时间：
2018-08-25
期刊：
影响因子：
--
通讯作者：
Qiu F
中科院分区：
文献类型：
--
作者：
Feng X;Li Y;Guang C;Qiao M;Wang T;Chai L;Qiu F
Linarin是一种黄酮类苷，由于其具有镇痛、解热、抗炎和保肝等多种药理活性，被认为是一种很有前途的天然产物。本研究采用超高效液相色谱/四极杆飞行时间质谱（UPLC/Q-TOF-MS/MS）对大鼠肠道菌群和生物样品中linarin的代谢产物进行了表征。linarin与大鼠肠道菌群孵育后，检测3种环裂解代谢物（4-羟基苯甲酸、4-羟基苯甲醛和间苯三酚）。在口服linarin后的大鼠生物样品中共鉴定出17种代谢物，其中包括一种环裂解代谢物（间苯三酚）。这些结果表明，亚麻素在肠道菌群中能够进行环裂变代谢，水解、去甲基化、糖醛酸化、硫酸化、糖基化、甲基化和环裂解是其主要代谢途径。本研究为进一步了解linarin的代谢机制提供了科学依据，有助于进一步开发linarin作为候选药物。
Linarin, a flavone glycoside, is considered to be a promising natural product due to its diverse pharmacological activities, including analgesic, antipyretic, anti-inflammatory and hepatoprotective activities. In this research, the metabolites of linarin in rat intestinal flora and biosamples were characterized using ultra-high-performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS/MS). Three ring cleavage metabolites (4-hydroxybenzoic acid, 4-hydroxy benzaldehyde and phloroglucinol) were detected after linarin was incubated with rat intestinal flora. A total of 17 metabolites, including one ring cleavage metabolite (phloroglucinol), were identified in rat biosamples after oral administration of linarin. These results indicate that linarin was able to undergo ring fission metabolism in intestinal flora and that hydrolysis, demethylation, glucuronidation, sulfation, glycosylation, methylation and ring cleavage were the major metabolic pathways. This study provides scientific support for the understanding of the metabolism of linarin and contributes to the further development of linarin as a drug candidate.
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DOI：
10.1024/0300-9831.73.2.79
发表时间：
2003-03-01
影响因子：
2.3
作者：
Blaut, M;Schoefer, L;Braune, A
通讯作者：
Braune, A
一种快速、灵敏的 LC-MS/MS 方法，用于测定小体积大鼠血浆和组织样品中的里那林及其在药代动力学和组织分布研究中的应用。
影响因子：
1.8
作者：
Feng, Xinchi;Liu, Youping;Di, Xin
通讯作者：
Di, Xin
影响因子：
2.7
作者：
MartinezVazquez, M;Apan, TOR;Bye, R
通讯作者：
Bye, R
影响因子：
3.4
作者：
Oinonen, Paivi P.;Jokela, Jouni K.;Vuorela, Pia M.
通讯作者：
Vuorela, Pia M.
影响因子：
5
作者：
Kim, Seok-Joo;Cho, Hong-Ik;Lee, Sun-Mee
通讯作者：
Lee, Sun-Mee