Hubei University of Science and Technology, No.88, Xianning avenue, Xianan District, Xianning 437000,China.
Xianning Central Hospital, No.228, Jingui road, Xianan District, Xianning 437000, China.
Int J Biol Macromol. 2022 Aug 31;215:541-549. doi: 10.1016/j.ijbiomac.2022.06.078. Epub 2022 Jun 17.
To study the pharmacokinetics and tissue distribution characteristics of Polygonatum sibiricum (P. sibiricum) polysaccharide administered orally and intravenously in rats, the latest quantitative analysis method was established where P. sibiricum polysaccharide was labeled with fluorescein isothiocyanate (FITC) in plasma and tissues. Quantitative analysis method of P. sibiricum polysaccharide in rat plasma and tissues was established by fluorescence spectrophotometry with FITC as a highly sensitive fluorescent molecular probe. The results showed that P. sibiricum polysaccharide was successfully labeled with FITC, and the degree of substitution was 0.55 %. Pharmacokinetic characteristics showed that oral administration (ig) and intravenous injection (iv) were consistent with the characteristics of two-compartment model. PRP-TYR-FITC administered orally was poorly absorbed in rats with low bioavailability. After a single ig and iv administration in rats for 8 h, P. sibiricum polysaccharide can be distributed in most tissues. The analysis results showed that P. sibiricum polysaccharide was distributed mostly in lung, kidney and liver for both routes of administration. When taking orally, the distribution pattern was: lung > liver > kidney > small intestine > stomach > heart > spleen > brain. When taking intravenously, the distribution pattern was: liver > lung > kidney > small intestine > heart > stomach > spleen > brain. Fluorescence labeling of P. sibiricum polysaccharide by FITC was successfully realized. This method was proved to be suitable for the study of pharmacokinetics and tissue distribution of P. sibiricum polysaccharide in rats. The above research lays foundation for further elucidating the clinical pharmacological mechanism of polysaccharide in P. sibiricum.
为研究西伯利亚菝葜多糖（Polygonatum sibiricum）经口服和静脉注射在大鼠体内的药代动力学和组织分布特征，建立了最新的定量分析方法，将菝葜多糖用荧光素异硫氰酸酯（FITC）标记在血浆和组织中。采用荧光分光光度法，以 FITC 作为高灵敏度荧光分子探针，建立了大鼠血浆和组织中西伯利亚菝葜多糖的定量分析方法。结果表明，成功地将西伯利亚菝葜多糖用 FITC 标记，取代度为 0.55%。药代动力学特征表明，口服（ig）和静脉注射（iv）均符合二室模型特征。PRP-TYR-FITC 经口给药在大鼠体内吸收不良，生物利用度低。大鼠单次 ig 和 iv 给药 8 h 后，西伯利亚菝葜多糖可分布于大多数组织。分析结果表明，两种给药途径均以肺、肾和肝分布为主。口服时，分布模式为：肺>肝>肾>小肠>胃>心>脾>脑。静脉注射时，分布模式为：肝>肺>肾>小肠>心>胃>脾>脑。成功实现了 FITC 对西伯利亚菝葜多糖的荧光标记。该方法适用于研究西伯利亚菝葜多糖在大鼠体内的药代动力学和组织分布。上述研究为进一步阐明菝葜多糖的临床药理机制奠定了基础。
