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首页> 外文期刊>Journal of Pharmaceutical and Biomedical Analysis: An International Journal on All Drug-Related Topics in Pharmaceutical, Biomedical and Clinical Analysis >A HPLC-MS/MS method for determination of 6 '''-feruloylspinosin in rat plasma and tissues: Pharmacokinetics and tissue distribution study
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A HPLC-MS/MS method for determination of 6 '''-feruloylspinosin in rat plasma and tissues: Pharmacokinetics and tissue distribution study

机译：HPLC-MS / MS法测定大鼠血浆和组织中的6'''-阿魏酰基纺丝菌素：药代动力学和组织分布研究

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摘要

A sensitive, reliable and accurate HPLC-MS/MS method was developed and validated for the quantification of 6 '''-feruloylspinosin in rat plasma and tissues with puerarin as the internal standard. The separation was performed on a Proshell 120 EC-C-18 column (4.6 x 150 mm, 2.7 mu m) with a mobile phase consisting of acetonitrile and 0.1% formic acid (20:80, v/v) at 0.3 mL/min. The quantification was performed by MRM with m/z [M-H](-) 783.3 -> 427.2 for 6 '''-feruloylspinosin and m/z [M-H](-) 415.4 -> 295.4 for the internal standard, respectively. The calibration curves covered over a concentration range of 20-2000 ng/mL in plasma and various tissues samples (heart, liver, spleen, lung, kidney, stomach, intestine, muscle, cerebrum and cerebellum) with good linearity (r(2) >= 0.9914). Both the intra- and inter-day precisions were less than 14.70%, and the accuracy (RE%) ranged from -5.80% to 4.93%. The extraction recoveries were within 75.21-92.96%, and the matrix effect ranged from 87.21% to 113.44%. Compared with spinosin, 6 '''-feruloylspinosin was distributed in rats faster whereas more slowly eliminated from the plasma. 6 ''' Feruloylspinosin could be distributed rapidly and widely in various tissues, and transfer across the blood-brain barrier. In addition, both 6 '''-feruloylspinosin and spinosin could enhance the expression of GAB(A alpha 1), GABA(A alpha 5), GABA(B)R(1) mRNA in rat hippocampal neurons significantly, indicating the bioactivity mechanism of 6 '''-feruloylspinosin was involved in the GABA receptors. (C) 2016 Elsevier B.V. All rights reserved.
机译：开发了一种灵敏，可靠，准确的HPLC-MS / MS方法，并以葛根素为内标对用于大鼠血浆和组织中6'''-阿魏酰基纺丝蛋白的定量进行了验证。分离在Proshell 120 EC-C-18色谱柱（4.6 x 150 mm，2.7μm）上进行，流动相由乙腈和0.1％甲酸（20:80，v / v）组成，流速为0.3 mL / min 。通过MRM进行定量，对于6′′-阿魏酰基鞘氨醇，m / z [M-H]（-）783.3→427.2，对于内标，m / z [M-H]（-）415.4→295.4。校准曲线涵盖了血浆和各种组织样品（心脏，肝脏，脾脏，肺，肾，胃，肠，肌肉，大脑和小脑）的浓度范围为20-2000 ng / mL，线性良好（r（2） > = 0.9914）。日内和日间精度均低于14.70％，精度（RE％）介于-5.80％至4.93％之间。提取回收率在75.21-92.96％之间，基质效应在87.21％至113.44％之间。与斯皮诺辛相比，6'''-阿魏酰基斯皮诺辛在大鼠中的分布更快，而从血浆中清除的速度更慢。 6'''阿魏酰基纺丝蛋白可以迅速广泛地分布在各种组织中，并通过血脑屏障转移。此外，6'''-阿魏酰基纺丝蛋白和刺糖蛋白都可以显着增强大鼠海马神经元中GAB（A alpha 1），GABA（A alpha 5），GABA（B）R（1）mRNA的表达，表明其生物活性机制GABA受体参与了6'''-阿魏酰基鞘氨醇的合成。 （C）2016 Elsevier B.V.保留所有权利。

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