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


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) and rats at different doses (0.5, 2 and 8 mg/kg). The results showed that the 99mTc-labelling method was suitable for 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-compartmental 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). LNT was predominantly incorporated into the liver and spleen, and there was a small amount of aggregation in the bile, kidneys, lung 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 use of LNT and other β-glucans.

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Publication details

The article was received on 08 Feb 2018, accepted on 07 May 2018 and first published on 15 May 2018

Article type: Paper
DOI: 10.1039/C8FO00272J
Citation: Food Funct., 2018, Accepted Manuscript
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    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, Accepted Manuscript , DOI: 10.1039/C8FO00272J

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