• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.15 no.2
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• pp.33-52
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• 2002

The effects of Arctii fructus extract on allegenic inflammation were investigated using in vivo and in vitro test models. Firstly, the cytotoxicity of Arctii fructus extract was validated using MTT assay. As a result, Arctii fructus extract showed no cytotoxic potential, while SDS, a positive control, revealed strong cytotoxic effect. In LLNA assay, Arctii fructus extract showed no skin allergenicity. Next, the anti-allergic actions of Arctii fructus extract were evaluated using rodent experimental models. The oral, intraperitoneal and intradermal administration of Arctii fructus extract significantly inhibited the compound 48／80-induced vascular permeability documented by Evans blue extravasation. In addition, Arctii fructus extract showed potent inhibitory effect on passive cutaneous anaphylaxis activated by anti-dinitrophenyl (DNP) IgE when orally administered. In an in vitro study, Arctii fructus extract revealed to possess inhibitory potential on the compound 48／80-induced histamine release from rat peritoneal mast cells. Moreover, Arctii fructus extract inhibited the IL-4 and TNF-${\alpha}$ mRNA induction by PMA and A23187 in human leukemia mast cells, HMC-1. Finally, it revealed that Arctii fructus extract significantly suppressed histamin-provoked antigenic inflammation reactions in human prick test. Taken together, these results suggest that anti-allergic action of Arctii fructus extract may be due to the inhibition of histamine release and cytokine gene expression in the mast cells.

• Journal of Haehwa Medicine
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• v.13 no.2
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• pp.259-265
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• 2004

Objective; This study was designed to investigate the effect of Sa-am acupuncture and Arctii Fructus water extract on Post-herpetic Neuralgia. Method: We have treated them with acupuncture treatment of Sa-am acupuncture and Arctii Fructus water extract and evaluated the effect by Pain Rating Score(P.R.S.) and Visual Analogue Scale(V.A.S.) scale. Result: Before theraphy, the grades of Song's scale were P.R.S. 80 and V.A.S. 100, Kim's sclae's P.R.S. 77 and V.A.S. 100. After theraphy, the grades of song's scale were P.R.S. 5 and V.A.S. 10, Kim's scales's P.R.S. 10 and V.A.S. 10 Conclusion: The treatment of Sa-am-acupuncture and Arctii Fructus water extract on Post-herpetic Neuralgia was effective and will be attempted to the patients with it.

• Journal of Nutrition and Health
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• v.36 no.8
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• pp.819-827
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• 2003

Linoleic acid [LA; 18: 2 (n-6)] is the most abundant polyunsaturated fatty acid in human skin. The exclusion of LA from diet induces epidermal hyperproliferation, which is reversible by the inclusion of LA in diet, and hence, LA is heralded as an essential fatty acid (EFA). Since safflower oil (SO) has been widely recognized as the major dietary source of LA and Arctii Fructus (Arctium lappa L.) is recently reported to contain high level of LA, we compared the antiproliferative effects of SO and Arctii Fructus in this study. Epidermal hyperproliferation was induced in guinea pigs by hydrogenated coconut oil (HCO) diet for 8 wk. During following 2 wk, EFA deficient guinea pigs were fed diets of safflower oil (group HS), water extract of Arctii Fructus (group AW) or organic extract of Arctii Fructus (group AO). Normal control group was fed SO containing diet (group SO) and EFA deficient group was fed HCO containing diet (group HCO) for 10 wk. Epidermal hyperproliferation was reversed in groups AO (55.9% of group HCO) and HS(74.1% of group HCO). However, the thymidine incorporation into epidermal DNA of group HS was greater than of normal control group SO. Epidermal hyperproliferation was not reversed in group AW. The accumulations of LA into phospholipids and ceramides, and of 13-hydroxyoctadecadienoic acid (13-HODE), the potent antiproliferative metabolite of LA in the epidermis of group AO were greater than of group HS. In contrast, the de novo synthesis of ceramides, the major lipids maintaining epidermal barrier, did not differ between all of groups. Together, our data demonstrate that organic extract of Arctii Fructus is more prominent than safflower oil in reversing epidermal hyperproliferation by inducing the higher accumulations of LA and 13-HODE in the epidermis of guinea pigs.

• The Journal of Pediatrics of Korean Medicine
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• v.18 no.2
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• pp.107-117
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• 2004

Objective : Atopic dermatitis has a close relationship with degranulation of mast cell and separation of Histamine. As there's no experiment with herb, using Arctii Fructus, we investigated experimental influence of Arctii Fructus on degranulation of mast cell and separation of histamine in SD rat. Methods : The SD rats are classified into three groups. One group is normal one treated by normal saline before medical treatment. The other is control group prescribed to Compound 48/80 before normal saline treatment. And the third is experimental group prescribed to compound 48/80 after medical treatment of Arctii Fructus. Then, I investigated the experimental results by measuring the degree of degranulation and separation of histamine. The results of investigation on SD rat group showing the degree of inhibitory effect of degranulation of a mast cell are as follow, the normal group treated by normal saline reflecting the degree of degranulation is $6.10{\pm}0.20\;%$, the control group treated by only compound 48/80 is $87.56{\pm}11.00\;%$, the experimental group which treated by compound 48/80 and Arctii Fructus's medical treatment is $16.26{\pm}4.67\;%$. Results : The normal group treated by only normal saline reflecting the degree of degranulation is $6.10{\pm}0.20\;%$, the control group treated by only compound 48/80 is 87.56=11.00 %, the experimental group treated by compound 48/80 and Arctii Fructus's medical treatment is $16.26{\pm}4.67\;%$. This result indicates that the degree of degranulation of mast cell is obviously inhibited (p<0.0l) in the experimental group in comparison with control one. The analysis of data obtained from plasma, which collected from the experimented SDrats' hearts before their death, and the measurement of quantity of histamine secretion show the following results. The quantity of normal group and control one is $25.34{\pm}4.58$ nM, $348.59{\pm}30.77$ nM respectively, and experimental one prescribed to compound 48/80 after medical treatment of Arctii Fructus is $263.56{\pm}21.34$ nM. This result indicates that separation of histamine isobviously inhibited in the experimental group in comparison with control one (p<0.05). Conclusions : Arctii Fructus does obviously inhibit the degree of degranulation of mast cell (p<0.0l) and separation of histamine in the plasma (p<0.05).

• Korean Journal of Acupuncture
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• v.25 no.1
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• pp.197-211
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• 2008

Objectives : We studied on anti-allergic effects of Arctii Fructus Herbal Acupuncture(AFHA) and Arctii Fructus Herbal Acupuncture Solution(AF). Methods : In vivo, Animals were herbal-acupunctured AFHA at both ST36 three times for 5 days. Then, we investigated compound 48/80-induced active systemic anaphylaxis(ASA) using ICR mice and anti-DNP IgE-induced passive cutaneous anaphylaxis(PCA) using Sprague Dawley rat. In vitro, we measured cell viability, b-hexosaminidase, IL-4 and TNF-a release from RBL-2H3 cells after treatment of AF of various concentrations. Results : In vivo, AFHA pretreatments at both ST36 inhibited compound 48/80-induced ASA. PCA was inhibited by AFHA pretreatments at both ST36. In vitro, AF treatments were not affect on cell viability and inhibited b-hexosaminidase, IL-4 and TNF-a release. Conclusions : These results suggest that AFHA and AF may be beneficial in the inhibition of allergic inflammatory response.

• 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.

• Journal of Physiology & Pathology in Korean Medicine
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• v.34 no.1
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• pp.1-6
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• 2020

Arctii Lappa Fructus has the numerous health benefits, including antioxidant, anti-inflammatory, and anti-carcinogenic properties. Skin lipids are one of several factors that maintain epidermal barrier function. This study was to explore the lipogenic effect by ethanol extract of Arctii Lappa Fructus (EAF) in sebocytes. First, it was confirmed that EAF exhibited high antioxidant activity and collagenase activity inhibition. We found that cholesterol and triglyceride levels of cells by EAF were increased significantly in a dose-dependent manner. Moreover, EAF increased the expression of transcription factor sterol regulatory element-binding protein-1 (SREBP-1) in the cells. These results suggest that EAF induces lipogenesis in cells through the activation of SREBP-1.

• Korean Journal of Pharmacognosy
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• v.28 no.4
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• pp.275-279
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• 1997

Fruits of Arctium lappa L. (Compositae), which has been used as the antiinflammatory, detoxifying and diuretic agents in the folk remedies, was examined on the in vitro oxidation of human low density lipoprotein (LDL). Several lines of evidence indicate that oxidized LDL (Ox-LDL) may promote atherogenesis. Hence. The role of antioxidants in the prevention of LDL oxidation needs to be determined. The activity of fractions of Arctii Fructus treated with oxidized LDL which was incubated with $16\;{\mu}M$ of $Cu^{2+}$ for metal catalyzed oxidation was investigated. The BuOH fraction (4\;ppm) inhibited the oxidative modification of LDL as evidenced by a decrease in the lipid peroxide content (thiobarbituric acid reacting substances activity), the negative charge of LDL (electrophoretic mobility) and increase of the vitamine E content.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2018.04a
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• pp.9-9
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• 2018

Arctii Fructus (AF), which contains arctigenin (ARC) as a major constituent, is traditionally used as an anti-inflammatory medicine to treat inflammatory sore throat. Although several studies have proven its anti-inflammatory effects, there have been no reports on its use in inflammation related disorders such as obesity, cancer metastasis, and allergic responses. This study investigated the anti-obesity effect and anti-metastasis effect of AF and ARC. AF and ARC inhibited weight gain by reducing the mass of white adipose tissue in high fat diet (HFD)-induced obese mice. Serum cholesterol levels were also improved by AF and ARC. In in vitro experiments, AF and ARC decreased differentiation of white adipocytes. Furthermore, AF induced differentiation of brown adipocytes, which are able to consume surplus energy through non-shivering thermogenesis. Also, AF and ARC inhibited colon cancer and lung metastasis of colon cancer. They suppressed not only colorectal cancer cell progression by inhibiting cell growth, but also prohibited lung metastasis by regulating epithelial-mesenchymal transition (EMT), migration, and the invasion. These effects were confirmed in an experimental metastasis mouse model. In addition, AF and ARC inhibited mast cell mediated allergic responses. Collectively, our study suggests that AF and ARC might show inhibitory effects on inflammation related diseases, including obesity, cancer, cancer metastasis, and allergic responses.

• Journal of the Korean Applied Science and Technology
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• v.32 no.3
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• pp.505-511
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• 2015

In this study, Arctigenin was obtained by using supercritical fluid extraction and bio-conversion process from Arctii Fructus. Arctigenin is efficacious in anti-inflammatory and anti-influenza. For this reason, Arctigenin is studied in various field. It was identified as 4-[(3,4-Dimethoxyphenyl)methyl)]dihydro-3-[(4-hydroxy-3-methoxyphenyl)methyl]-2(3H)-furanone (arctigenin) by FT-IR, $^1H$-NMR and the purity of it was 95.1 % by HPLC analysis. Arctigenin inhibited tyrosinase (up to $85.06{\pm}0.9%$ at $260{\mu}g/m{\ell}$ concentration) and melanin synthesis in a dose dependent manner (up to $51.1{\pm}3.7%$ at the concentration of $3.0{\mu}g/m{\ell}$). The results were better than arbutin. Therefore, it is expected that manufactured Arctigenin is useful for whitening cosmetics.