西红花水提液在大鼠血中的移行成分分析

Analysis on transitional components in blood after oral administration of saffron extracts in rats

目的研究西红花水提液ig给予大鼠后的入血成分,初步揭示西红花体内潜在药效物质基础及主要入血成分的体内代谢过程。方法对照西红花ig给药前后的HPLC图谱,采用HPLC-DAD-ESI-MSn鉴定吸收入血成分及随时间变化规律。结果西红花中11个主要化学成分被鉴定,大鼠ig给药后发现4个吸收入血成分,包括1个原型成分和3个代谢产物,其中苦藏花素以原型入血。《中国药典》西红花质量评价指标西红花苷-I和西红花苷-II,在所有时间点的血浆中均未发现,而检测到的是西红花苷类化合物的代谢产物(西红花酸和西红花酸单葡萄糖醛酸结合物)。苦藏花素吸收入血后60 min达峰值,而西红花苷的代谢产物西红花酸在30、120 min出现"双峰"现象。结论吸收入血的苦藏花素和西红花苷的代谢产物可能是西红花体内发挥药效的潜在物质基础。该研究为更合理地选择西红花质量评价指标、完善西红花质量控制标准提供参考,也为进一步系统研究西红花体内药动学行为提供了理论基础。

Objective To analyze the transitional components in blood after oral administration of saffron extracts in rats, in order to initially reveal in vivo potential effective substance and metabolic process of the main components absorbed into blood. Methods The constituents of saffron and metabolites in rat plasma sample after oral administration of saffron were investigated using HPLC-DAD-ESI-MSn. Results Eleven chemical constituents in saffron were identified, and four compounds, including one prototype and three metabolites, were detected in rat plasma sample. Among them, picrocrocin was absorbed in prototype, whereas crocins were absorbed in metabolites （crocetin and crocetin-monoglucuronide）. Crocin-I and crocin-II, used as quality evaluation of saffron in Chinese Pharmacopoeia, were not discovered at all time points. Picrocrocin achieved a Cmax value at 1 h after administration, while metabolites, crocetin, achieved two Cmax values respectively at 0.5 h and 2 h. Conclusion Picrocrocin and metabolic products absorbed into blood may be the effective components of saffron. The work may provide a reference for reasonably choosing the quality control index and improving the quality control standards, and may also lay a foundation for further researching the pharmacokinetics of saffron.