Han Fei, Li Yan-ting, Mao Xin-juan, Zhang Xiao-shu, Guan Jiao, Song Ai-hua, Yin Ran
School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, China.
Anal Bioanal Chem. 2016 Mar;408(7):1975-81. doi: 10.1007/s00216-015-9080-9. Epub 2015 Nov 12.
A high-performance liquid chromatography coupled to Fourier transform ion cyclotron resonance mass spectrometry (HPLC-FT-ICR MS) method was developed to study the in vivo metabolism of salidroside for the first time. Plasma, urine, bile, and feces samples were collected from male rats after a single intragastric gavage of salidroside at a dose of 50 mg/kg. Besides the parent drug, a total of seven metabolites (three phase I and four phase II metabolites) were detected and tentatively identified by comparing their mass spectrometry profiles with those of salidroside. Results indicated that metabolic pathways of salidroside in male rats included hydroxylation, dehydrogenation, glucuronidation, and sulfate conjugation. Among them, glucuronidation and sulfate conjugation were the major metabolic reactions. And most important, the detection of the sulfation metabolite of p-tyrosol provides a clue for whether the deglycosylation of salidroside occurs in vivo after intragastric gavage. In summary, results obtained in this study may contribute to the better understanding of the safety and mechanism of action of salidroside.
首次开发了一种高效液相色谱-傅里叶变换离子回旋共振质谱联用(HPLC-FT-ICR MS)方法来研究红景天苷的体内代谢。在以50 mg/kg的剂量对雄性大鼠进行单次灌胃给予红景天苷后,收集其血浆、尿液、胆汁和粪便样本。除了母体药物外,通过将它们的质谱图与红景天苷的质谱图进行比较,共检测并初步鉴定出7种代谢物(3种I相代谢物和4种II相代谢物)。结果表明,红景天苷在雄性大鼠体内的代谢途径包括羟基化、脱氢、葡萄糖醛酸化和硫酸化结合。其中,葡萄糖醛酸化和硫酸化结合是主要的代谢反应。最重要的是,对酪醇硫酸化代谢物的检测为灌胃后红景天苷在体内是否发生去糖基化提供了线索。总之,本研究获得的结果可能有助于更好地理解红景天苷的安全性和作用机制。