• Nutrition Research and Practice
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• v.8 no.6
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• pp.655-661
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• 2014

BACKGROUND/OBJECTIVES: The purpose of this study was to examine the effects and associated mechanisms of arctiin, a lignan compound found in burdock, on adipogenesis in 3T3-L1 cells. Also, the effects of arctiin supplementation in obese mice fed a high-fat diet on adiposity were examined. MATERIALS/METHODS: 3T3-L1 cells were treated with arctiin (12.5 to $100{\mu}M$) during differentiation for 8 days. The accumulation of lipid droplets was determined by Oil Red O staining and intracellular triglyceride contents. The expressions of genes related to adipogenesis were measured by real-time RT-PCR and Western blot analyses. For in vivo study, C57BL/6J mice were first fed either a control diet (CON) or high-fat diet (HF) to induce obesity, and then fed CON, HF, or HF with 500 mg/kg BW arctiin (HF + AC) for four weeks. RESULTS: Arctiin treatment to 3T3-L1 pre-adipocytes markedly decreased adipogenesis in a dose-dependent manner. The arctiin treatment significantly decreased the protein levels of the key adipogenic regulators $PPAR{\gamma}$ and $C/EBP{\alpha}$, and also significantly inhibited the expression of SREBP-1c, fatty acid synthase, fatty acid-binding protein and lipoprotein lipase. Also, arctiin greatly increased the phosphorylation of AMP-activated protein kinase (AMPK) and its downstream target phosphorylated-acetyl CoA carboxylase. Furthermore, administration of arctiin significantly decreased the body weight in obese mice fed with the high-fat diet. The epididymal, perirenal or total visceral adipose tissue weights of mice were all significantly lower in the HF + AC than in the HF. Arctiin administration also decreased the sizes of lipid droplets in the epididymal adipose tissue. CONCLUSIONS: Arctiin inhibited adipogenesis in 3T3-L1 adipocytes through the inhibition of $PPAR{\gamma}$ and $C/EBP{\alpha}$ and the activation of AMPK signaling pathways. These findings suggest that arctiin has a potential benefit in preventing obesity.

• Archives of Pharmacal Research
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• v.18 no.6
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• pp.462-463
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• 1995

• Journal of Life Science
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• v.22 no.8
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• pp.1092-1098
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• 2012

This study was carried out to discover the skin wrinkle reducing components in the seeds of Arctium lappa. The isolation of a methylene chloride-soluble fraction of 70% ethanol extract from the seeds of Arctium lappa using a procollagen type-1 synthesis and MMP-1 activity resulted in the isolation and identification of four lignin compounds: arctiin, arctigenin, matairesinol, and diarctigenin. All structures were confirmed via NMR and MS spectroscopic data. To determine cell viability and procollagen type-1 synthesis, human dermal fibroblasts were treated with 10-100 ${\mu}M$. As a result, none of the four compounds showed cytotoxicity up to 50 ${\mu}M$. We also investigated their procollagen type-1 synthesis and MMP-1 inhibition activity and found that arctiin had the highest activity in terms of both procollagen synthesis and MMP-1 inhibition among all four compounds. Putting all the data together, we suggest that arctiin be used in cosmetics as an anti-wrinkle material.

• Natural Product Sciences
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• v.28 no.3
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• pp.153-160
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• 2022

Neuroinflammation is known to be associated with brain injury in Alzheimer's disease (AD), and the inhibition of microglial activation, a key player in inflammatory response, is considerd as important target for AD. In this study, the ethanol extract of aerial parts of Forsythia velutina Nakai, a Korean native species, significantly inhibited nitric oxide (NO) production in LPS-stimulated BV2 microglial cells. Thus, the active principles in F. velutina aerial parts were isolated based on activity-guided isolation method. As a result, six compounds were isolated and their structures were elucidated based on NMR data and the comparison with the relevant references as arctigenin (1), matairesinol (2), rengyolone (3), ursolic acid (4), secoisolariciresinol (5), and arctiin (6). Among them, four compounds including arctigenin (1), matairesinol (2), secoisolariciresinol (5), and arctiin (6) significantly inhibited NO production in a dose-dependent manner. In particular, matairesinol (2) and secoisolariciresinol (5) reduced 60% of NO production compared to LPS-treated group. This inhibitory effects of matairesinol (2) and secoisolariciresinol (5) were accompanied with the reduced expression levels of iNOS and COX-2. These results suggest that the extract of F. velutina and its active compounds could be beneficial for neuroinflammatory diseases including AD.

• Journal of Microbiology and Biotechnology
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• v.15 no.2
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• pp.269-273
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• 2005

Five dibenzylbutyrolactones were isolated from a methanol extract of Arctii fructus (Arctium lappa L.) by bioassay-guided isolation, using the interleukin-l $\beta$ converting enzyme (caspase-l, ICE) production inhibitory assay in vitro. These compounds were spectroscopically identified as lappaol E (1), lappaol A (2), matairesinol (3), arctigenin (4), and arctiin (5). Among the compounds tested, arctigenin (4) showed the strongest inhibitory activity for ICE production in IL-$\beta$-induced proliferation of D 1 OS cells. Western blot analysis demonstrated that the arctigenin suppressed the expression of ICE protein in a dose-dependent manner. To estimate the biotransformation of Arctii fructus in vivo by human intestinal bacteria, we carried out an anaerobic incubation of the Arctii fructus extract with a human fecal suspension. From the HPLC analysis of metabolites, Arctiin (IC$_{50}$=74.2$\mu$g/ml), a major component of Arctii fructus, was transformed to aglycone, arctigenin (IC$_{50}$=12.5$\mu$g/ml), by human intestinal bacteria. The ICE production inhibitory activity of Arctii fructus would be much stronger in vivo than in vitro due to the biotransformation by human intestinal bacteria.

• Natural Product Sciences
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• v.11 no.2
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• pp.85-88
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• 2005

The methanolic extract from the seeds of Arctium lappa was found to inhibit the LPS-induced nitric oxide (NO) production in murine macrophage RAW264.7 cells. Bioassay-guided fractionation of a methylene chloride soluble fraction led to the isolation of three lignan compounds, arctiin (1), arctigenin (2), and lappaol B (3). Their structures were elucidated by UV, IR, MS, and NMR data, as well as by comparison with those of the literatures. Arctigenin (2) and lappaol B (3) had an iNOS inhibitory activity with $IC_{50}$ values of 12.5 and $25.9\;{\mu}M$, respectively.

• Journal of the Korean Society of Food Science and Nutrition
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• v.46 no.8
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• pp.986-996
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• 2017

In this study, we optimized fermentation conditions for burdock vinegar by response surface methodology. We confirmed the fermentation characteristics and major components of burdock vinegar. Alcohol fermentation of burdock extract added with 15% apple concentrates for vinegar production was performed. Consequently, 6.4% alcohol was produced after 5 days of fermentation. Central composite design was applied to investigate the effects of two independent variables, fermentation time (5~17 days; X1) and fermentation temperature ($26{\sim}34^{\circ}C$; X2), on fermentation of burdock vinegar. Fermentation conditions were optimized using characteristics of fermentation broth as a dependent variable. Acetic acid contents of dependent variables were 3.85~4.73% during acetic acid fermentation. The correlation coefficient ($R^2$) of the derived equation from the response surface regression for acetic acid contents was 0.9850 with significance level of 1%. Arctiin contents of all fermentation samples were 0.37~0.50 mg/100 mL, with an $R^2$ value of 0.8380 and significance level of 5%. We elicited a regression equation for each variable and superimposed the optimum area of fermentation conditions for characteristics and effective constituent contents of the fermentation broth. The predicted values for the optimum fermentation conditions for burdock vinegar were at $31^{\circ}C$ and 16 days.

• Natural Product Sciences
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• v.17 no.2
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• pp.147-159
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• 2011

A high-performance liquid chromatography-electrospray ionization-tandem mass spectrometric method was developed to determine simultaneously eight marker constituents of Forsythiae fructus, and subsequently applied it to classify its two botanical origins. The marker compounds of Forsythia suspensa were phillyrin, pinoresinol, phillygenin, lariciresinol and forsythiaside; those of F.viridissima were arctiin, arctigenin and matairesinol. Separation of the eight analytes was achieved on a phenyl-hexyl column (150${\times}$2.0 mm i.d., 3 ${\mu}M$) using gradient elution with the mobile phase: (A) 10% acetonitrile in 0.5% acetic acid, (B) 40% aqueous acetonitrile. A few fragment ions specific to the types of lignans, among the product ions generated by collisonally induced dissociation (CID) of molecular ion clusters, such as [M-H]$^-$ or [M+OAc]$^-$ were used not only for fingerprinting analysis but for the quantification of each epimer by using multiple-reaction monitoring mode. It was shown good linearity ($r^2{\geq}$ 0.9998) over the wide range of all analytes; intra- and inter-day precisions (RSD, %) were within 9.14% and the accuracy ranged from 84.3 to 115.1%. The analytical results of 40 drug samples, combined with multivariate statistical analyses - principal component analysis (PCA) and hierarchical cluster analysis (HCA) - clearly demonstrated the classification of the test samples according to their botanical origins. This method would provide a practical strategy for assessing the authenticity or quality of the herbal drug.