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首页> 美国卫生研究院文献>Molecules >A UPLC-ESI-MS/MS Method for Simultaneous Quantitation of Chlorogenic Acid Scutellarin and Scutellarein in Rat Plasma: Application to a Comparative Pharmacokinetic Study in Sham-Operated and MCAO Rats after Oral Administration of Erigeron breviscapus Extract
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A UPLC-ESI-MS/MS Method for Simultaneous Quantitation of Chlorogenic Acid Scutellarin and Scutellarein in Rat Plasma: Application to a Comparative Pharmacokinetic Study in Sham-Operated and MCAO Rats after Oral Administration of Erigeron breviscapus Extract

机译：UPLC-ESI-MS / MS方法同时定量大鼠血浆中绿原酸黄S苷和黄S苷的含量：在灯盏花灯盏花提取物口服给药后对假手术和MCAO大鼠的比较药代动力学研究中的应用

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Erigeron breviscapus, a traditional Chinese medicine, is clinically used for the treatment of occlusive cerebral vascular diseases. We developed a sensitive and reliable ultra-performance liquid chromatography-electrospray-tandem mass spectrometry (UPLC-ESI-MS/MS) method for simultaneous quantitation of chlorogenic acid, scutellarin, and scutellarein, the main active constituents in Erigeron breviscapus, and compared the pharmacokinetics of these active ingredients in sham-operated and middle cerebral artery occlusion (MCAO) rats orally administrated with Erigeron breviscapus extract. Plasma samples were collected at 15 time points after oral administration of the Erigeron breviscapus extract. The levels of chlorogenic acid, scutellarin, and scutellarein in rat plasma at various time points were determined by a UPLC-ESI-MS/MS method, and the drug concentration versus time plots were constructed to estimate pharmacokinetic parameters. The concentration of chlorogenic acid in the plasma reached the maximum plasma drug concentration in about 15 min and was below the limit of detection after 4 h. Scutellarin and scutellarein showed the phenomenon of multiple absorption peaks in sham-operated and MCAO rats, respectively. Compared with the sham-operated rats, the terminal elimination half-life of scutellarein in the MCAO rats was prolonged by more than two times and the area under the curve of each component in the MCAO rats was significantly increased. The results showed chlorogenic acid, scutellarin, and scutellarein in MCAO rats had higher drug exposure than that in sham-operated rats, which provided a reference for the development of innovative drugs, optimal dosing regimens, and clinical rational drug use.
机译：灯盏花是传统的中药，临床上用于治疗闭塞性脑血管疾病。我们开发了一种灵敏可靠的超高效液相色谱-电喷雾串联质谱（UPLC-ESI-MS / MS）方法，用于同时定量灯盏花灯盏花中主要活性成分绿原酸，黄cut素和黄cut素的含量，并对其进行了比较。这些活性成分在灯盏花提取物口服给药的假手术和大脑中动脉闭塞（MCAO）大鼠中的药代动力学。灯盏花提取物口服后15个时间点收集血浆样品。通过UPLC-ESI-MS / MS方法测定大鼠血浆在不同时间点的绿原酸，黄cut苷和黄cut苷水平，并建立药物浓度-时间图以估算药代动力学参数。血浆中绿原酸的浓度在约15分钟内达到最大血浆药物浓度，并在4 h后低于检测极限。黄cut苷和黄cut苷分别在假手术和MCAO大鼠中表现出多个吸收峰的现象。与假手术组相比，MCAO组中黄cut素的终末消除半衰期延长了两倍以上，MCAO组中各成分曲线下的面积显着增加。结果表明，与假手术组相比，MCAO组大鼠的绿原酸，黄rin苷和黄re苷含量更高，这为开发新药，最佳给药方案和临床合理用药提供了参考。

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