Lentinan (LNT), a typical triple helix β-glucan, has been widely used as drug and biomaterial. However, its pharmacokinetics in vivo is rarely reported, which severely limits its further development and application. The aim of this study is to establish a sensitive method for detecting LNT in biosamples and to evaluate the plasma level, tissue distribution and metabolic degradation of LNT in rats. 5-([4,6-Dichlorotriazin-2-yl] amino) fluorescein (DTAF) was labelled to LNT. After purification and identification, FLNT was intravenously administered to rats at dose of 32 mg/kg. LNT was predominantly incorporated into the liver and liver microsomes were used to study the degradation mechanism of LNT in the liver. The results showed that two cytochrome P450 (CYP450) enzymes subtypes (CYP2D6 and CYP2C9), as well as epoxide hydrolase, were involved in the metabolic degradation of LNT. These findings provide a pharmacokinetic reference for further study and application of LNT and other β-glucans.

典型的三重螺旋β-葡聚糖-香菇多糖（LNT）已被广泛用作药物和生物材料。但是，其体内药代动力学很少报道，这严重限制了它的进一步开发和应用。这项研究的目的是建立一种检测生物样品中LNT的灵敏方法，并评估大鼠LNT的血浆水平，组织分布和代谢降解。将5-（[4,6-二氯三嗪-2-基]氨基）荧光素（DTAF）标记为LNT。纯化和鉴定后，将FLNT以32 mg / kg的剂量静脉内给予大鼠。LNT主要掺入肝脏，肝微粒体用于研究LNT在肝脏中的降解机理。结果表明，LNT的代谢降解涉及两种细胞色素P450（CYP450）酶亚型（CYP2D6和CYP2C9）以及环氧化物水解酶。