Simultaneous determination of the pharmacokinetics of A-type EGCG and ECG dimers in mice plasma and its metabolites by UPLC-QTOF-MS
Simultaneous determination of the pharmacokinetics of A-type EGCG and ECG dimers in mice plasma and its metabolites by UPLC-QTOF-MS
复制标题
UPLC-QTOF-MS同时测定小鼠血浆中A型EGCG和ECG二聚体及其代谢物的药代动力学
DOI：
10.1080/09637486.2019.1635089
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发表时间：
2019-07-01
影响因子：
3.9
通讯作者：
Li, Chun-Mei
中科院分区：
文献类型：
--
作者：
Li, Jin;Zeng, Jian;Li, Chun-Mei
a型表没食子儿茶素-3-没食子酸酯（EGCG）和表儿茶素-3- o -没食子酸酯（ECG）二聚体具有多种生物活性。本研究采用单次静脉给药后研究其在小鼠体内的药代动力学，并采用超高效液相色谱-四极杆飞行时间质谱仪（UPLC-QTOF-MS）研究其在小鼠血浆和尿液中的代谢产物。结果表明，a型EGCG和ECG二聚体的半衰期（t1/2）分别为116.37 min和33.04 min，血浆最大浓度分别为32.81 μg/mL和55.59 μg/mL。发现两种二聚体首先通过醌甲基（QM）裂变形成EGCG和ECG类似物，随后产生II期代谢物。血浆和尿液中的主要代谢物为糖醛酸化和磺化衍生物。此外，还检测了尿中酚酸的小分子质量。
Abstract A-type epigallocatechin-3-gallate (EGCG) and epicatechin-3-O-gallate (ECG) dimers have multiply biological activities. In this study, the pharmacokinetics of them were investigated in mice after a single dose intravenous administration, and the metabolites in mice plasma and urine were investigated by ultra-performance liquid chromatography-Quadrupole-time of flight mass spectrometer (UPLC-QTOF-MS). Our results showed that the half-life (t1/2) of A-type EGCG and ECG dimers were 116.37 min and 33.04 min, respectively, and the maximal concentration in plasma was 32.81 μg/mL and 55.59 μg/mL, respectively. It was found that two dimers were firstly experienced by quinone methide (QM) fission to form the EGCG and ECG analogue, and the phase II metabolites were generated subsequently. The main metabolites in plasma and urine were glucuronidation and sulphation derivatives. In addition, small molecule weight of phenolic acids were detected in urine.