Overview of the anti-inflammatory effects, pharmacokinetic properties and clinical efficacies of arctigenin and arctiin from Arctium lappa L  

作　　者：Qiong GAO Mengbi YANG Zhong ZUO 

机构地区：[1]School of Pharmacy, Faculty of Medicine, The Chinese University of Hong Kong, Hong Kong SAR, China

出　　处：《Acta Pharmacologica Sinica》2018年第5期787-801,共15页中国药理学报（英文版）

摘　　要：Arctigenin （AR） and its glycoside, arctiin, are two major active ingredients of Arctium lappa L （A lappa）, a popular medicinal herb and health supplement frequently used in Asia. In the past several decades, bioactive components from A lappa have attracted the attention of researchers due to their promising therapeutic effects. In the current article, we aimed to provide an overview of the pharmacology of AR and arctiin, focusing on their anti-inflammatory effects, pharmacokinetics properties and clinical efficacies. Compared to acrtiin, AR was reported as the most potent bioactive component ofA lappa in the majority of studies, AR exhibits potent anti-inflammatory activities by inhibiting inducible nitric oxide synthase （iNOS） via modulation of several cytokines. Due to its potent anti-inflammatory effects, AR may serve as a potential therapeutic compound against both acute inflammation and various chronic diseases. However, pharmacokinetic studies demonstrated the extensive glucuronidation and hydrolysis of AR in liver, intestine and plasma, which might hinder its in vivo and clinical efficacy after oral administration. Based on the reviewed pharmacological and pharmacokinetic characteristics of AR, further pharmacokinetic and pharmacodynamic studies of AR via alternative administration routes are suggested to promote its ability to serve as a therapeutic agent as well as an ideal bioactive marker for A lappa.Arctigenin （AR） and its glycoside, arctiin, are two major active ingredients of Arctium lappa L （A lappa）, a popular medicinal herb and health supplement frequently used in Asia. In the past several decades, bioactive components from A lappa have attracted the attention of researchers due to their promising therapeutic effects. In the current article, we aimed to provide an overview of the pharmacology of AR and arctiin, focusing on their anti-inflammatory effects, pharmacokinetics properties and clinical efficacies. Compared to acrtiin, AR was reported as the most potent bioactive component ofA lappa in the majority of studies, AR exhibits potent anti-inflammatory activities by inhibiting inducible nitric oxide synthase （iNOS） via modulation of several cytokines. Due to its potent anti-inflammatory effects, AR may serve as a potential therapeutic compound against both acute inflammation and various chronic diseases. However, pharmacokinetic studies demonstrated the extensive glucuronidation and hydrolysis of AR in liver, intestine and plasma, which might hinder its in vivo and clinical efficacy after oral administration. Based on the reviewed pharmacological and pharmacokinetic characteristics of AR, further pharmacokinetic and pharmacodynamic studies of AR via alternative administration routes are suggested to promote its ability to serve as a therapeutic agent as well as an ideal bioactive marker for A lappa.

关 键 词：ARCTIGENIN ARCTIIN Arctium lappa L Fructus Arctii anti-inflammatory agents PHARMACOKINETICS clinical efficacy 

分 类 号：TP334.7[自动化与计算机技术—计算机系统结构] S858.31[自动化与计算机技术—计算机科学与技术]