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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 study the inflow components after the administration of aqueous extract of crocus sativus in rats, and to reveal the potential drug substance base and the metabolic process of the main components of infiltration in safflower. Methods HPLC chromatograms before and after the administration of saffron ig, HPLC-DAD-ESI-MSn identification of components of infiltration and changes over time. Results Eleven main chemical components were identified in saffron. Four compounds were found to be absorbed into the bloodstream after ig administration, including one prototype component and three metabolites. The “Chinese Pharmacopoeia” crocus quality evaluation indicators crocin -I and crocin-II, were not found in plasma at all time points, and the detected crocetin compounds metabolites ( Crocetin and crocetin glucuronic acid conjugate). The concentration of bitter crocin absorbed into the blood peaked at 60 min, while crocetin, a metabolite of crocin, appeared “bimodal” at 30 and 120 min. Conclusion The metabolites of bitter crocidin and crocin absorbed into the blood may be the underlying material basis for the efficacy of saffron in vivo. The study provides a reference for selecting the quality evaluation index of crocus sativus and improving the quality control standard of crocus sativus, and also provides a theoretical basis for further systematic study on the pharmacokinetics of crocus sativus.