In vitro anti-inflammatory effects of arctigenin, a lignan from Arctium lappa L., through inhibition on iNOS pathway

Zhao, Feng; Wang, Lu; Liu, Ke

doi:10.1016/j.jep.2009.01.038

Cited by 184 publications

(137 citation statements)

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“…As a natural product derived from Arctium lappa, arctigenin has been demonstrated to induce various biological activities, such as anti-inflammatory and cortical neuronprotecting effects [24]. A recent study showed that arctigenin served as an anti-tumour agent by blocking the expression of unfolded protein response (UPR) target genes [25].…”

Section: Discussionmentioning

confidence: 99%

Arctigenin, a natural compound, activates AMP-activated protein kinase via inhibition of mitochondria complex I and ameliorates metabolic disorders in ob/ob mice

Huang

Gong

et al. 2011

Diabetologia

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Aims/hypothesis Arctigenin is a natural compound that had never been previously demonstrated to have a glucoselowering effect. Here it was found to activate AMPactivated protein kinase (AMPK), and the mechanism by which this occurred, as well as the effects on glucose and lipid metabolism were investigated. Methods 2-Deoxyglucose uptake and AMPK phosphorylation were examined in L6 myotubes and isolated skeletal muscle. Gluconeogenesis and lipid synthesis were evaluated in rat primary hepatocytes. The acute and chronic effects of arctigenin on metabolic abnormalities were observed in C57BL/6J and ob/ob mice. Changes in mitochondrial membrane potential were measured using the J-aggregate-forming dye, JC-1. Analysis of respiration of L6 myotubes or isolated mitochondria was conducted in a channel oxygen system. Results Arctigenin increased AMPK phosphorylation and stimulated glucose uptake in L6 myotubes and isolated skeletal muscles. In primary hepatocytes, it decreased gluconeogenesis and lipid synthesis. The enhancement of glucose uptake and suppression of hepatic gluconeogenesis and lipid synthesis by arctigenin were prevented by blockade of AMPK activation. The respiration of L6 myotubes or isolated mitochondria was inhibited by arctigenin with a specific effect on respiratory complex I. A single oral dose of arctigenin reduced gluconeogenesis in C57BL/6J mice. Chronic oral administration of arctigenin lowered blood glucose and improved lipid metabolism in ob/ob mice. Conclusions/interpretation This study demonstrates a new role for arctigenin as a potent indirect activator of AMPK via inhibition of respiratory complex I, with beneficial effects on metabolic disorders in ob/ob mice. This highlights the potential value of arctigenin as a possible treatment of type 2 diabetes.

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Section: Discussionmentioning

confidence: 99%

Arctigenin, a natural compound, activates AMP-activated protein kinase via inhibition of mitochondria complex I and ameliorates metabolic disorders in ob/ob mice

Huang

Gong

et al. 2011

Diabetologia

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“…NO levels were determined by measuring the quantity of nitrite in the cell culture supernatant using Griess reagent (Yantai Science & Biotechnology, Co., Ltd.) (18). RAW 264.7 cells were cultured in 96-well plates at a density of 2x10 5 cells/well.…”

Section: Carrageenan-induced Paw Edema In Ratsmentioning

confidence: 99%

Tiliroside, the major component of Agrimonia pilosa Ledeb ethanol extract, inhibits MAPK/JNK/p38-mediated inflammation in lipopolysaccharide-activated RAW 264.7 macrophages

Jin

Song

Wang

et al. 2016

Experimental and Therapeutic Medicine

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Abstract. In the present study, the in vivo anti-inflammatory activity of Agrimonia pilosa Ledeb (AP) ethanol extract was confirmed in experimental animal models, including xylene-induced ear edema in mice and carrageenan-induced paw edema in rats. Tiliroside, the major component of AP extract, was isolated and purified by high-performance liquid chromatography. The anti-inflammatory mechanism of tiliroside was then examined using lipopolysaccharide (LPS)-activated RAW 264.7 macrophage cells. An MTT assay was used to determine cytotoxicity and a Griess assay was used to determine nitric oxide (NO) production. Concentration levels of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) were determined by enzyme-linked immunosorbent assay. Protein expression levels of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), phosphorylated (p)-extracellular signal-regulated kinase (ERK) 1/2, p-c-Jun N-terminal kinases (JNK), p-p38 and inhibitor of κB-α were detected by western blot analysis. AP ethanol extract was revealed to inhibit xylene-induced ear edema in mice and carrageenan-induced paw edema in rats. Tiliroside significantly suppressed the overproduction of NO (P<0.01), but revealed no notable inhibition of the release of TNF-α and IL-6. In addition, tiliroside significantly downregulated the elevated expression levels of iNOS and COX-2 induced by LPS (P<0.01). The phosphorylation of JNK and p38 proteins were also significantly inhibited (P<0.01), however, tiliroside exhibited no obvious inhibition on the phosphorylation of ERK 1/2 and the degradation of IκB-α protein.In conclusion, the anti-inflammatory molecular mechanism of tiliroside may involve the downregulation of iNOS and COX-2 protein expression levels, and the inactivation of mitogen-activated protein kinase (MAPK)/JNK, in addition to the MAPK/p38 signaling pathway. IntroductionAgrimonia pilosa Ledeb (Rosaceae; AP) is a perennial herbaceous flowering plant distributed in the temperate regions of the Northern hemisphere, including Asia. As a traditional medicinal plant, it has been used for the treatment of abdominal pain, sore throat, headaches, bloody discharge, parasitic infections and eczema (1). Pharmacological research has revealed that AP extracts possess diverse pharmacological properties, including antinociceptive (1), antiplatelet (2) and antihemostatic effects (3), in addition to antioxidant (4), antiviral (5), antitumor (6), anti-inflammatory, anti-allergic (7,8), anti-microbial (9) and anti-hyperglycemic (10) activity, amongst others. Tiliroside, a glycosidic flavonoid (Fig. 1), is the major component of AP extracts. Tiliroside has been reported to exhibit the following: Anti-diabetic properties by enhancing glucose consumption by insulin-resistant HepG2 cells (11,12); antihypertensive and vasorelaxant effects in resistance arteries (13); anti-hyperglycemic, anti-hyperlipidemic and antioxidant activities (14)

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“…In addition, arctigenin strongly inhibited the expression of pro-inflammatory cytokines tumor necrosis factor-α (TNF-α) and IL-6, in LPS-stimulated RAW264.7 cells, THP-1 human monocyte-macrophage and differentiated human macrophage U937 (Cho et al, 2002;Zhao et al, 2009). Further study showed that arctigenin-induced inhibition of TNF-α production might be mediated by arctigenin's potent inactivation of mitogen-activated protein (MAP) kinases including ERK1/2, p38 kinase and JNK through the inhibition of MAP kinase kinase (MKK) activity, leading to inactivation of activator protein-1 (AP-1) (Cho et al, 2004;Zhao et al, 2009). …”

Section: Anti-inflammatory Effectsmentioning

confidence: 99%

A review of the pharmacological effects of Arctium lappa (burdock)

et al. 2010

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Abstract. Arctium lappa, commonly known as burdock, is being promoted/recommended as a healthy and nutritive food in Chinese societies. Burdock has been used therapeutically in Europe, North America and Asia for hundreds of years. The roots, seeds and leaves of burdock have been investigated in view of its popular uses in Traditional Chinese Medicine (TCM). In this review, the reported therapeutic effects of the active compounds present in the different botanical parts of burdock are summarized. In the root, the active ingredients have been found to "detoxify" blood in TCM term and promote blood circulation to the skin surface, improving the skin quality/texture and curing skin diseases like eczema. Antioxidants and anti-diabetic compounds have also been found in the root. In the seeds, some active compounds possess anti-inflammatory effects, and potent inhibitory effects on the growth of tumors such as the pancreatic carcinoma. In the leaf extract, the active compounds isolated can inhibit the growth of micro-organisms in the oral cavity. The medicinal uses of burdock in treating chronic diseases like cancers, diabetes and AIDS have been reported. However, it is also essential to be aware of the side-effects of burdock including contact dermatitis and other allergic/inflammatory responses that might be evoked by burdock.

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In vitro anti-inflammatory effects of arctigenin, a lignan from Arctium lappa L., through inhibition on iNOS pathway

Cited by 184 publications

References 20 publications

Arctigenin, a natural compound, activates AMP-activated protein kinase via inhibition of mitochondria complex I and ameliorates metabolic disorders in ob/ob mice

Arctigenin, a natural compound, activates AMP-activated protein kinase via inhibition of mitochondria complex I and ameliorates metabolic disorders in ob/ob mice

Tiliroside, the major component of Agrimonia pilosa Ledeb ethanol extract, inhibits MAPK/JNK/p38-mediated inflammation in lipopolysaccharide-activated RAW 264.7 macrophages

A review of the pharmacological effects of Arctium lappa (burdock)

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