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

Abstract

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 of A 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.

The Extract of Arctium lappa L. Fruit (Arctii Fructus) Improves Cancer-Induced Cachexia by Inhibiting Weight Loss of Skeletal Muscle and Adipose Tissue

“…Therefore, various pharmacological effects could be expected from plant compounds, including arctiin and arctigenin. It has been reported that arctigenin and arctiin account for approximately 0.5–2% ( w / w ) and 2–10% ( w / w ) of the dry weight of the AF, respectively [ 29 ]. These compounds also possessed an anti-inflammatory effect.…”

Arctigenin promotes bone formation involving PI3K/Akt/PPARγ signaling pathway

“…Due to their chemical structure, phytoestrogens can be classed as isoflavones and lignins. Arctigenin (Ar, Figure 1) is a lignin phytoestrogen extracted from Arctium lappa (Gao, Li, Zhang, & Zeng, 2008) that displays anti-inflammatory (Gao, Yang, & Zuo, 2018), antioxidant (Wu et al, 2014), antifibrosis (Lin et al, 2019), and antitumor effects (Maxwell, Chun, Lee, Kim, & Nam, 2017). In preliminary experiments, we found that arctigenin promotes the differentiation of bone marrow mesenchymal stem cells (BMSCs) of ovariectomized (OVX) rats into osteoblasts, leading to anti-osteoporosis effects.…”

Supercritical Extracts from Arctium lappa as a Potential Inhibitor for the Activation of Complement System

“…Some compounds are more sensitive than others and, depending on the time of exposition to high temperatures or pressures, can be degraded. This may justify the lack of arctigenin in our extracts, a compound identified in fractions of A. lappa with an important anti-inflammatory role [35][36][37]. However, the anti-inflammatory activity observed with E1 and E2 extracts of A. lappa may be due to other components, such as lupeol, amyrin, and phytol [31,34,38], which were also found in extracts from A. lappa leaves obtained by pressurized liquid extraction using aqueous ethanol [20].…”