[关键词]
[摘要]
西红花苷来源于西红花Crocus sativus柱头和栀子Gardenia jasminoides果实,是一类具长共轭独特水溶性类胡萝卜素,具有显著神经保护、心血管保护及抗肿瘤等药理活性。西红花苷口服不能以原型吸收入血,而是在胃肠道水解为西红花酸后吸收进入血液循环,之后转变为葡萄糖醛酸缀合物,而代谢产物西红花酸主要分布到心、肝、脾、肺等血液充盈组织中。由于西红花苷及代谢物西红花酸体内生物利用度较低、稳定性差,可采用新型递药系统应用于西红花苷(酸),提高其稳定性、生物利用度及药理活性。综述近年西红花苷和西红花酸的体内代谢及制剂学相关研究进展,为该类天然产物进一步深入研究与开发利用提供参考。
[Key word]
[Abstract]
Crocin is derived from stigmas of Crocus sativus and fruits of Gardenia jasminoides. It is a type of unique water-soluble carotenoids with long conjugate, possessing remarkable neuroprotection, cardiovascular protection, antitumor, and other pharmacological activities. Data showed that orally administrated crocin couldn't permeate into the bloodstream as the prototype, but it can be absorbed into the blood circulation after being hydrolyzed to crocetin in gastrointestinal tract. Then, crocetin is converted to glucuronic acid conjugate. Moreover, the metabolite crocetin are mainly distributed in heart, liver, spleen, lung, and other blood-rich tissues. In view of the low bioavailability and poor stability of crocin and its metabolite crocetin, researchers have extensively employed novel drug delivery system to study crocin (crocetin) in order to improve its stability, bioavailability, and pharmacological activity. This article reviews in vivo metabolism of crocin (crocetin) in recent years and investigations on drug delivery system, therefore, facilitating further research and development of these natural products.
[中图分类号]
[基金项目]
国家自然科学基金资助项目(21562051);国家自然科学基金资助项目(21162046);国家自然科学基金资助项目(81860617);贵州省教育厅创新群体重大研究项目(黔教合KY字[2017]044);贵州省科技厅科技支撑项目(黔科合支撑[2018]2766);贵州省国内一流学科建设(药学YLXKJS-YS-05);贵州省留学人员科技活动择优资助项目[黔人社资助项目(2018)0013]