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

  • J Pharm Biomed Anal. 2016 Mar 20;121:77-83. doi: 10.1016/j.jpba.2016.01.005.
Longdong Qiao  1 ,  Yan Liu  2 ,  Xiaoyan Chen  3 ,  Junbo Xie  4 ,  Yanqing Zhang  5 ,  Ke Yang  6 ,  Hongjian Zhou  6 ,  Yayun Duan  6 ,  Wei Zheng  6 ,  Wenlin Xie  6
Affiliations
  • 1. College of Biotechnology and Food Science, Tianjin University of Commerce, Tianjin 300134, China; Tianjin Key Laboratory of Food Biotechnology, Tianjin 300134, China.
  • 2. Department of pharmacy, Weifang People's Hospital, Weifang 261041, China.
  • 3. School of Medicine and Pharmacy, Ocean University of China, Qingdao 266100, China.
  • 4. College of Biotechnology and Food Science, Tianjin University of Commerce, Tianjin 300134, China; Tianjin Key Laboratory of Food Biotechnology, Tianjin 300134, China. Electronic address: [email protected].
  • 5. College of Biotechnology and Food Science, Tianjin University of Commerce, Tianjin 300134, China; Tianjin Key Laboratory of Food Biotechnology, Tianjin 300134, China. Electronic address: [email protected].
  • 6. College of Biotechnology and Food Science, Tianjin University of Commerce, Tianjin 300134, China.
PMID: 26780157 DOI: 10.1016/j.jpba.2016.01.005
Abstract

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-C18 column (4.6×150 mm, 2.7 μm) 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 GABAAα1, GABAAα5, GABABR1 mRNA in rat hippocampal neurons significantly, indicating the bioactivity mechanism of 6'''-feruloylspinosin was involved in the GABA receptors.

Keywords
6′′′-Feruloylspinosin; HPLC-MS/MS; Pharmacokinetics; Spinosin; Tissue distribution.
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