Feng Rui, Li Luya, Zhang Xiaowei, Zhang Yuqian, Chen Yuting, Feng Xue, Zhang Lantong, Zhang Guohua
Department of Pharmacy, The Fourth Hospital of Hebei Medical University Shijiazhuang 050011 P. R. China.
Department of Pharmaceutical Analysis, School of Pharmacy, Hebei Medical University Shijiazhuang 050017 P. R. China
RSC Adv. 2020 Aug 28;10(53):32020-32026. doi: 10.1039/d0ra03350b. eCollection 2020 Aug 26.
Eupatorin, a bioactive compound extracted from Java tea (), possesses potent anti-cancer, anti-inflammatory and vasodilation activities. To date, no pharmacokinetics studies on eupatorin have yet been performed. Here, we established and validated a sensitive and selective LC-MS/MS (liquid chromatography-tandem mass spectrometry) approach for determining plasma eupatorin in rats. Chromatographic fractionation was conducted on a Wonda Cract ODS-2 C18 Column (4.6 mm × 150 mm, 5 μm) with a mobile phase containing aqueous 0.1% formic acid and acetonitrile using a flow rate of 0.8 ml min. In multiple reaction monitoring mode, precursor-to-product ion transitions for quantification of eupatorin and the internal standard were set at 343.1 → 328.1 and 252.0 → 155.9, respectively. The intra- and inter-day precision and accuracy were found to be below 6.72% and within ±8.26% in rat plasma, respectively. Meanwhile, all values of the matrix effect, recovery and stability were within the accepted ranges. Furthermore, we carried out the pharmacokinetic analysis using the developed method. The pharmacokinetic study revealed that while the (maximum plasma concentration) of eupatorin and time for reaching the ( ) were 974.886 ± 293.898 μg L and 0.25 h, respectively, the half-life was 0.353 ± 0.026 h. This study will be of great significance to the research on the pharmacology, clinical pharmacy and drug action mechanism of eupatorin.
泽兰素是从毛相思子中提取的一种生物活性化合物，具有强大的抗癌、抗炎和血管舒张活性。迄今为止，尚未对泽兰素进行药代动力学研究。在此，我们建立并验证了一种灵敏且选择性的液相色谱 - 串联质谱法（LC-MS/MS），用于测定大鼠血浆中的泽兰素。色谱分离在Wonda Cract ODS - 2 C18柱（4.6 mm×150 mm，5μm）上进行，流动相为含0.1%甲酸水溶液和乙腈，流速为0.8 ml/min。在多反应监测模式下，用于定量泽兰素和内标的前体离子到产物离子的跃迁分别设定为343.1→328.1和252.0→155.9。发现大鼠血浆中的日内和日间精密度和准确度分别低于6.72%和在±8.26%以内。同时，基质效应、回收率和稳定性的所有值均在可接受范围内。此外，我们使用所建立的方法进行了药代动力学分析。药代动力学研究表明，泽兰素的Cmax（最大血浆浓度）和达峰时间Tmax分别为974.886±293.898μg/L和0.25 h，半衰期为0.353±0.026 h。本研究对泽兰素的药理学、临床药学及药物作用机制研究具有重要意义。
