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藏红花及其活性成分的药代动力学特性

Pharmacokinetic Properties of Saffron and its Active Components.

作者信息

Hosseini Azar, Razavi Bibi Marjan, Hosseinzadeh Hossein

机构信息

Pharmacological Research Center of Medicinal Plants, Mashhad University of Medical Sciences, Mashhad, Iran.

Targeted Drug Delivery Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.

出版信息

Eur J Drug Metab Pharmacokinet. 2018 Aug;43(4):383-390. doi: 10.1007/s13318-017-0449-3.

Abstract

Saffron as a medicinal plant has many therapeutic effects. Phytochemical studies have reported that saffron is composed of at least four active ingredients which include crocin, crocetin, picrocrocin and safranal. The carotenoids of saffron are sensitive to oxygen, light, heat and enzymatic oxidization. However, regulation of these factors is required for saffron quality. Some pharmacologic effects of saffron and its active compounds include cardioprotective, neuroprotective, memory enhancer, antidepressant and anxiolytic. Among more than 150 chemicals of saffron, the most biologically active components are two carotenoids including crocin and crocetin. Most of the pharmacokinetic studies are related to these compounds. The pharmacokinetic studies have shown that crocin is not available after oral administration in blood circulation. Crocin is converted to crocetin in intestine but after intravenous injection, the level of crocetin in plasma is low. Crocetin can distribute in different tissues because of weak interaction between crocetin and albumin. Also it can penetrate blood-brain barrier and reach CNS by passive transcellular diffusion; thus it can be effective in neurodegenerative disorders. The large portion of crocin is eliminated via feces.

摘要

藏红花作为一种药用植物具有多种治疗作用。植物化学研究报告称,藏红花至少由四种活性成分组成,包括藏花素、藏红花酸、苦藏花素和藏红花醛。藏红花的类胡萝卜素对氧气、光、热和酶氧化敏感。然而,藏红花的品质需要对这些因素进行调控。藏红花及其活性化合物的一些药理作用包括心脏保护、神经保护、增强记忆力、抗抑郁和抗焦虑。在藏红花的150多种化学成分中,最具生物活性的成分是两种类胡萝卜素,即藏花素和藏红花酸。大多数药代动力学研究都与这些化合物有关。药代动力学研究表明,口服后藏花素在血液循环中无法获得。藏花素在肠道中转化为藏红花酸,但静脉注射后,血浆中藏红花酸的水平较低。由于藏红花酸与白蛋白之间的相互作用较弱,藏红花酸可以分布在不同组织中。它还可以穿透血脑屏障,通过被动跨细胞扩散到达中枢神经系统;因此它对神经退行性疾病有效。大部分藏花素通过粪便排出。

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