A HPLC-MS/MS method for determination of 6 '''-feruloylspinosin in rat plasma and tissues: Pharmacokinetics and tissue distribution study

作者:Qiao, Longdong; Liu, Yan; Chen, Xiaoyan; Xie, Junbo*; Zhang, Yanqing*; Yang, Ke; Zhou, Hongjian; Duan, Yayun; Zheng, Wei; Xie, Wenlin
来源:Journal of Pharmaceutical and Biomedical Analysis, 2016, 121: 77-83.
DOI:10.1016/j.jpba.2016.01.005

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.