Study on the pharmacokinetics of mulberry fruit polysaccharides through fluorescence labeling

Int J Biol Macromol. 2021 Sep 1:186:462-471. doi: 10.1016/j.ijbiomac.2021.07.075. Epub 2021 Jul 13.

Abstract

A sensitive and efficient fluorescence labeling method was developed and validated for the microanalysis and detection of polysaccharides. Fluorescein isothiocyanate (FITC) was successfully labeled on mulberry fruit polysaccharides (MFP) through a reductive amination reaction with the assistant of tyramine. The fluorescent labeled polysaccharides (FMFP) was identified by fluorescence, UV-visible, flourier transform infrared (FT-IR) and 1H NMR spectrum. Results demonstrated that the labeling efficiency of FMFP was 0.32%, and the FMFP was stable in simulated digestion fluid without cytotoxicity. The pharmacokinetics and biodistribution after administration were analyzed in rats, which indicated that the FMFP obtained could be absorbed in a short time (tmax 0.50 h) but eliminated slowly (t1/2 8.77 ± 1.38 h). At 24 h after administration, the polysaccharide could be tested mainly in intestine, stomach, liver and kidney. The FITC labeling method lays a foundation for investigating the absorption and metabolism of MFP, and provides references for the microanalysis research of bioactive polysaccharides.

Keywords: Digestive stability; Fluorescence labeling; Fructus mori; Pharmacokinetics; Polysaccharide.

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Digestion
  • Fluorescein-5-isothiocyanate / chemistry
  • Fluorescein-5-isothiocyanate / pharmacokinetics*
  • Fluorescent Dyes / chemistry
  • Fluorescent Dyes / pharmacokinetics*
  • Fruit
  • Male
  • Microchemistry
  • Morus* / chemistry
  • Polysaccharides / chemistry
  • Polysaccharides / isolation & purification
  • Polysaccharides / pharmacokinetics*
  • Proton Magnetic Resonance Spectroscopy
  • Rats
  • Rats, Sprague-Dawley
  • Spectrometry, Fluorescence
  • Spectroscopy, Fourier Transform Infrared
  • Tissue Distribution

Substances

  • Fluorescent Dyes
  • Polysaccharides
  • Fluorescein-5-isothiocyanate