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首页> 外文期刊>Phytotherapy research: PTR >Transport Properties of Puerarin and Effect of Extract of Radix Angelicae dahuricae on Puerarin Intestinal Absorption Using In Situ and In Vitro Models
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Transport Properties of Puerarin and Effect of Extract of Radix Angelicae dahuricae on Puerarin Intestinal Absorption Using In Situ and In Vitro Models

机译:葛根素的运输特性和当归提取物对葛根素肠吸收的原位和体外模型

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摘要

The root of Angelica dahurica (Radix Angelicae Dahuricae, RAD), which contains coumarins and volatile oil as its main classes of active components, is often given in conjunction with Pueraria root (Radix Puerariae, RP), which contains the phytoestrogen puerarin. The two herbs are considered to be compatible 'herb-pairs' in traditional Chinese medicine. The present investigation investigates the absorption of puerarin from RP and the effect of the total coumarins and volatile oil from RAD on its absorption. The everted gut sac and singlepass intestinal perfusion methods were used, respectively. The results showed that the absorption of puerarin in the jejunum was significantly increased in the presence of the coumarins and/or volatile oil. The absorption rate constant (K_a) of puerarin increased gradually until the concentration reached 160 μg?mL~(-1), after which its absorption became saturated and the apparent permeability (P_(app)) values significantly decreased. The results showed that the intestinal absorption mechanisms of puerarin involved active transportation processes and that puerarin is likely to be a substrate of P-gp because verapamil significantly affected its P_(app) and K_a. The absorption of puerarin significantly increased (p<0.01) when combined with RAD extracts, as shown by the increase in concentration of puerarin in blood from the hepatic portal vein, supporting the concept of RAD and RP as a compatible herb-pair.
机译:含有香豆素和挥发油作为其主要活性成分的当归(Radix Angelicae Dahuricae,RAD)的根通常与葛根(Purerariae RP)结合使用,后者含有植物雌激素葛根素。两种草药被认为是传统中药兼容的“草药对”。本研究调查了葛根素从RP中的吸收以及RAD中总香豆素和挥发油对其吸收的影响。分别使用外翻肠囊和单次肠道灌注方法。结果表明,在香豆素和/或挥发油的存在下,葛根素在空肠中的吸收显着增加。葛根素的吸收速率常数(K_a)逐渐增加,直至浓度达到160μg?mL〜(-1),此后其吸收达到饱和,表观渗透率(P_(app))值明显降低。结果表明,葛根素的肠道吸收机制涉及主动转运过程,并且葛根素可能是P-gp的底物,因为维拉帕米显着影响其P_(app)和K_a。当与RAD提取物联合使用时,葛根素的吸收显着增加(p <0.01),如肝门静脉血中葛根素的浓度增加所表明的,这支持了RAD和RP作为相容性草药对的概念。

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