Pharmacokinetics of protocatechuic acid in mouse and its quantification in human plasma using LC-tandem mass spectrometry.
Pharmacokinetics of protocatechuic acid in mouse and its quantification in human plasma using LC-tandem mass spectrometry.
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DOI：
10.1016/j.jchromb.2012.09.032
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发表时间：
2012-11-01
影响因子：
3
通讯作者：
Liu, Zhongfa
中科院分区：
文献类型：
--
作者：
Chen, Wei;Wang, Dian;Wang, Li-shu;Bei, Di;Wang, Jiang;See, William A.;Mallery, Susan R.;Stoner, Gary D.;Liu, Zhongfa
原儿茶酸（PCA）是花青素的主要微生物代谢产物，具有显著的体内外抗氧化和抗癌活性，但其药代动力学尚不清楚。在本报告中，开发并验证了一种灵敏、快速的LC-MS/MS方法，用于测量小鼠和人血浆中的五氯苯甲醚浓度。该方法在小鼠和人血浆中均显示线性范围为1-1000 ng/mL，定量下限为1 ng/mL。日内和日间变异系数为1.18 ~ 11.8%，准确度为92 ~ 110%。应用该方法表征了小鼠口服50 mg/kg PCA后PCA的药代动力学特征。五氯苯甲醚吸收迅速，半衰期为2.9分钟，5分钟时达到血浆峰浓度（Cmax）73.6 μM，PCA的血药浓度-时间曲线下面积（AUC 0 →8h）为1456 μM·min-1，该方法能够检测低ng/ml的PCA，前列腺癌患者口服60 g黑树莓（BRB）粉末后血浆中PCA的mL量。由于PCA来源于BRB中的花色苷，因此我们的方法为进一步研究花色苷的代谢以及PCA在未来临床前和临床研究中的药理作用提供了有用的分析工具。
Protocatechuic acid (PCA), a major microbial-mediated metabolite of anthocyanins, has significant anti-oxidative and anti-carcinogenic activities in vitro and in vivo; however, its pharmacokinetics remains largely unknown. In this report, a sensitive and rapid LC-MS/MS method was developed and validated for the measurement of PCA concentrations in both mouse and human plasma. This method showed a linearity of 1-1000 ng/mL in both mouse and human plasma with a lower limit of quantification of 1 ng/mL. The within-day and between-day coefficient of variation ranged from 1.18 to 11.8% and accuracy from 92 to 110%. The method was applied to characterize the pharmacokinetics of PCA in mice after oral administration of 50 mg/kg PCA. PCA was absorbed rapidly with a half-life of 2.9 min, reached a peak plasma level (Cmax) of 73.6 μM at 5 min, and remained detectable up to 8 h with the initial elimination half-life of about 3 min and a terminal half-life of 16 min. The area under the plasma concentration-time curve (AUC0→8h) of PCA was 1456 μM.min. The method was capable of detecting low ng/mL quantities of PCA in the plasma of patients with prostate cancer after an oral ingestion of 60 g of black raspberry (BRB) powder. Because PCA is derived from the anthocyanins in BRB, our method provides a useful analytical tool to further investigate the metabolism of anthocyanins, and the pharmacology of PCA in future preclinical and clinical studies.
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