Issue 6, 2018

A sensitive and rapid radiolabelling method for the in vivo pharmacokinetic study of lentinan

Abstract

The aim of this study is to establish a rapid and sensitive method for detecting lentinan (LNT) in biosamples and to evaluate the pharmacokinetics of LNT in mice and rats. A diethylenetriaminepentaacetic acid (DTPA) derivative of LNT (DTPA-LNT) was synthesized first to allow labelling with 99m-technetium (99mTc). After purification and identification, 99mTc-DTPA-LNT was intravenously administered to mice (2 mg kg−1) and rats at different doses (0.5, 2 and 8 mg kg−1). The results showed that the 99mTc-labelling method was suitable for the quantification of the LNT concentration in biological samples, with satisfactory linearity (r2 > 0.998), precision (<7%), accuracy (95.01–104.51%) and total recovery (∼90%). The blood concentration–time profiles of 99mTc-DTPA-LNT were consistent with the two-compartment model and showed a rapid distribution phase and a slow elimination, and no significant difference in the blood level of LNT was found among the tested doses (0.5, 2 and 8 mg kg−1). LNT was predominantly incorporated into the liver and spleen, and there was a small amount of aggregation in the bile, kidneys, lungs and stomach. Approximately 40% of the administered radioactivity was detected in urine and faeces within 24 h post-dosing. In addition, SPECT imaging of 99mTc-DTPA-LNT was performed to visually reveal the pharmacokinetic characteristics of LNT. These findings provide a reference for further study and for use of LNT and other β-glucans.

Graphical abstract: A sensitive and rapid radiolabelling method for the in vivo pharmacokinetic study of lentinan

Supplementary files

Article information

Article type
Paper
Submitted
08 Feb 2018
Accepted
07 May 2018
First published
15 May 2018

Food Funct., 2018,9, 3114-3125

A sensitive and rapid radiolabelling method for the in vivo pharmacokinetic study of lentinan

Y. Zhang, Z. Zheng, X. Yang, X. Pan, L. Yin, X. Huang, Q. Li, Y. Shu, Q. Zhang and K. Wang, Food Funct., 2018, 9, 3114 DOI: 10.1039/C8FO00272J

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