• Biomolecules & Therapeutics
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• v.27 no.3
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• pp.311-317
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• 2019

Mast cells are the most prominent effector cells of Type 1 hypersensitivity immune responses. CYC116 [4-(2-amino-4-methyl-1,3-thiazol-5-yl)-N-[4-(morpholin-4-yl)phenyl] pyrimidin-2-amine] is under development to be used as an anti-cancer drug, but the inhibitory effects of CYC116 on the activation of mast cells and related allergy diseases have not reported as of yet. In this study, we demonstrated, for the first time, that CYC116 inhibited the degranulation of mast cells by antigen stimulation ($IC_{50}$, ${\sim}1.42{\mu}M$). CYC116 also inhibited the secretion of pro-inflammatory cytokines including TNF-${\alpha}$ ($IC_{50}$, ${\sim}1.10{\mu}M$), and IL-6 ($IC_{50}$, ${\sim}1.24{\mu}M$). CYC116 inhibited the mast cell-mediated allergic responses, passive cutaneous anaphylaxis (ED50, ~22.5 mg/kg), and passive systemic anaphylaxis in a dose-dependent manner in laboratory experiments performed on mice. Specifically, CYC116 inhibited the activity of Fyn in mast cells and inhibited the activation of Syk and Syk-dependent signaling proteins including LAT, $PLC{\gamma}$, Akt, and MAP kinases. Our results suggest that CYC116 could be used as an alternative therapeutic medication for mast cell-mediated allergic disorders, such as atopic dermatitis and allergic rhinitis.

• The Korea Journal of Herbology
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• v.28 no.2
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• pp.55-60
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• 2013

Objectives : Atopic dermatitis (AD) is a chronic inflammatory skin disease characterized by eczematous inflammtion of the skin. The chestnut inner shell extracts (CI) has been used as a cosmetic material for a long time in Korea. However, the precise anti-allergy effects of CI have yet to be clearly elucidated. In this study, we attempted to evaluate the effect of CI on mast cell-mediated allergy inflammation. Methods : To find the anti-allergy and inflammatory effect of CI, we investigated the inhibitory effect of CI on the production of inflammatory mediators using by enzyme-linked immunosorbent assay in phorbol 12-myristate 13-acetate (PMA) plus calcium ionophore (A23187) stimulated-human mast cell (HMC-1). Results : In this study, we found that CI did not show cytotoxic effect at up to 10 ug/ml on HMC-1. CI inhibited the production of tumor necrosis factor (TNF)-${\alpha}$, interleukin (IL)-6 and IL-8 in stimulated HMC-1. Maximal rate of TNF-${\alpha}$, IL-6 and IL-8 inhibition by CI (10 ug/ml) were about 47.6%, 44.1% and 22.5% respectively. In addition, we showed that Fr.3 isolated from n-Butyl alcohol layer of CI attenuated the production of TNF-${\alpha}$, IL-6 and IL-8 in HMC-1. Conclusion : Taken together, the findings of this study provide us with a novel insight action of CI as a potential molecule for use in the treatment of allergic inflammation diseases.

• The Korea Journal of Herbology
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• v.29 no.6
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• pp.165-173
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• 2014

Objectives : Platycodon Root is frequently used in traditional medicine to treat inflammatory diseases of the throat. The purpose of this study was to characterize the effect of the EtOH extract of fermented Platycodon grandiflorum on the ameliorative effects on the Antipruritic Effect of atopic dermatitis mouse model induced by compound 48/80 and ovalbumin (OVA)-induced allergic responses in mice. Methods : In the present study, we examined the anti allergic effect of Platycodon grandiflorum (PR) and its fermented production (FPR) in several mouse model. We measured acute ear edema in a mouse model caused by TPA and consecutively histological change of Ear tissue was observed by hematoxylin and eosin (H&E) staining. and also Scratching behaviors by compound 48/80 was investigated. The levels of allergic mediators such as immunoglobulin (Ig) E, and anti-oxidant markers such as SOD and MDA in the sera of OVA induced allergic mice were measured by enzyme-linked immunosorbent assay. Results : FPR inhibited compoud 48/80-induced scratching behavior in mice, as well as acetic acid-induced writhing in mice. The anti-scratching behavioral effect of FPR was more potent than PR. FPR extract significantly decreased the serum levels of IgE and MDA compared with those of OVA control group. Conclusions : These results indicate that Anti allergic effect of Platycodon grandiflorum is enhanced by fermentation with Saccharomyces cerevisae and FPR may be useful for protection from the itching reactions, which are IgE-mediated representative skin allergic diseases.

• Journal of Life Science
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• v.25 no.7
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• pp.810-818
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• 2015

We analyzed whether lactic acid bacteria could control the expression of IL-4 and IL-13 in activated mast cells and whether these bacteria could inhibit the activity of transcription factors such as GATA-1, GATA-2, NF-AT1, NF-AT2, and NF-κB p65. We previously described a technique for identification of lactic acid bacteria with anti-atopy functionality by confirming increased expression of CD4+/CD25+/foxp3+ in T cells. We also confirmed that a double-culture method increased the antibacterial activity of these lactic acid bacteria against Staphylococcus aureus (S. aureus). In the present study, we characterized the effect of lactic acid bacteria cultured by this double-culture method on inhibition of allergic inflammatory reactions of RBL-2H3 mast cells, a cellular model of atopic dermatitis. The strongest anti-allergic effects of the lactic acid bacteria were seen in the following order: Lactococcus lactis broth cultured with medium containing Lactobacillus plantarum culture supernatant > Lc. lactis > Lc. lactis broth cultured with medium containing Lb. plantarum culture supernatant > Lb. plantarum. Thus, Lc. lactis cultured in medium containing Lb. plantarum culture supernatant had the strongest inhibitory effect on the differentiation of mast cells during allergic reactions, which may be mediated through the selective regulation of expression of relevant genes.

• Journal of Veterinary Clinics
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• v.31 no.2
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• pp.95-101
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• 2014

Five dogs were used to determine whether 0.1% tacrolimus ointment application for one day would inhibit IgE-mediated late-phase reactions (LPRs). It was consisted of three periods: one period without therapeutic administration (control) and two periods of treatment with either the tacrolimus ointment or vehicle. Induction of IgE-mediated LPRs was induced by intradermal injections of 0.05 ml (0.14 mg/ml) of solution of goat anti-canine IgE polyclonal antibodies. Each section for mast cells (MCs) and eosinophils (EPs) was stained with acidified toluidine blue, and Luna's stain, respectively. Assessment of anti-inflammatory effect of tacrolimus ointment composed of cell counts of MC and EP from lesions of induced LPR. In normal canine biopsies, the number of dermal MCs and EPs were $12.3{\pm}1.4cells/mm^2$ and $3.1{\pm}1.3cells/mm^2$, respectively. MC counts dramatically decreased at time dependent manner after anti-IgE administration. However, the number of MCs on 6 hours after challenge was significantly less decreased in the groups treated with the tacrolimus, as compared with control and vehicle group. The number of EPs on 24 hours after challenge was significantly lower in the group treated with the tacrolimus than in the control and vehicle groups. In conclusion, this study revealed that 0.1% tacrolimus ointment in dogs may exert a potent anti-inflammatory effect on inhibition of MC degranulation and also secondary prevention of EP infiltration during LPR.

• The Journal of the Convergence on Culture Technology
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• v.8 no.6
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• pp.849-854
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• 2022

In this study, the anti-inflammatory effect of supercritical carbon dioxide selective extracts, which extract decursin and decursinol angelate, the vital active ingredients of Angelica gigas Nakai, in high yield, was measured compared to that of ethanol extracts. To measure the anti-inflammatory effect, the production of nitric oxide(NO), an inflammatory mediator, and interleukin(IL)-6 and IL-8, inflammatory cytokines, was measured. NO production was measured by Griess assay on Raw 264.7 cells induced inflammatory response by lipopolysaccharide(LPS), and IL-6 and IL-8 production was measured by enzyme-linked immunoadsorbent assay(ELISA) on human keratinocyte cell line(HaCaT) cells induced inflammatory response by tumor necrosis factor(TNF)-α. The amount of NO production was suppressed outstandingly by the supercritical carbon dioxide extracts compared to the ethanol extracts. The amount of IL-6 and IL-8 production was increased by the ethanol extracts, whereas statistically significantly inhibited by supercritical carbon dioxide extracts at the concentration of 6.25 ㎍/mL(P<0.01). Through these results, we confirmed that the supercritical carbon dioxide selective extracts of Angelica gigas Nakai could be used as an anti-inflammatory cosmeceutical material to alleviate atopic dermatitis.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.49 no.3
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• pp.277-283
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• 2023

Fraxinus rhynchophylla Hance (F. rhynchophylla) is a traditional medicinal plant that has been widely used in East Asia and has been used for chronic bronchitis, bacterial dysentery and improved eyesight. F. rhynchophylla contains various type of coumarins such as esculin, esculetin, fraxin and fraxetin. Esculetin possesses versatile activities including antioxidant, anti-inflammatory, antimicrobial, anticancer properties and improvement of atopic dermatitis. However, there is no research on the process of increasing active components in F. rhynchophylla. The objectives of the present study were to apply biotransformation technology to F. rhynchophylla for increasing the content of esculetin, and enhancing anti-inflammatory and antioxidant activities. F. rhynchophylla extract (FRE) treated with viscozyme L (FRE-VL) showed 3.1 times higher content of esculetin than FRE, and exhibited effects such as increased anti-inflammatory activity and DPPH radical scavenging activity. Based on the these results, it is concluded that biotransformed FRE-VL could be potentially applicable as a new active ingredient in the cosmetic field.

• Korean Journal of Medicinal Crop Science
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• v.26 no.1
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• pp.42-54
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• 2018

Background: Allergic diseases like such as atopic dermatitis, asthma, and rhinitis have recently increased both domestically and globally. The present study was undertaken to select candidates with anti-allergic activity from plant resources. Methods and Results: Fifty-six plant extracts at $20{\mu}g/m{\ell}$ were screened against ${\beta}$-hexosaminidase production and interleukin (IL)-4 release in degranulated rat basophilic leukemia (RBL)-2H3 cells. The anti-allergy activity of three plant extracts selected from the preliminary screening experiment, Polygonatum sibiricum F. Delaroche (root), Pyrus pytifolia var. culta (Makino) Nakai (leaf), and Rehmannia glutinosa (Gaertn.) Libosch. ex Steud (root) were measured at concentrations of $2-250{\mu}g/m{\ell}$ in three cell lines as RBL-2H3, HaCaT and Jurkcat T cells. The assay showed the root extract of R. glutinosa to have an inhibitory activity of 4.2% - 28.6% on ${\beta}$-hexosaminidase production from IgE-sensitized RBL-2H3 cells. Each extract of P. sibiricum and R. glutinosa reduced IL-4 release in IgE-sensitized RBL-2H3 cells, respectively. The leaf extract of P. pyrifolia var. culta showed a significantly potent suppressive effect of 10.2% - 74.7% on the mRNA expression of tumor necrosis factor (TNF)-${\alpha}$ in HaCaT cells sensitized with TNF-a and INF-g, and showed inhibitory effect of -8.6% - 90.9% on the mRNA expression of IL-2 in Jurkat T cells sensitized with PMA and A23187. Conclusions: The results showed that the root of R. glutinosa and leaf of P. pyrifolia var. culta could be useful candidates as antiallergy materials.

• Journal of the Korean Society of Food Science and Nutrition
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• v.38 no.8
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• pp.977-982
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• 2009

This study was carried out to investigate physiological activities in the extract of Eriobotrya japonica in order to elevate its utilization as a functional material. The maximum total polyphenol and total flavonoid contents were 28.91$\pm$2.1 mg/g and 10.54$\pm$4.6 mg/g, respectively. The nitrite scavenging abilities at pH 1.2 were in the range of $49.52\pm1.04\sim72.52\pm$0.84% whereas they were $35.28\pm0.78\sim51.20\pm$1.10% at pH 4.2 and $27.90\pm0.36\sim32.26\pm$1.20% at pH 6.0. At the concentrations of 100, 200 and 300 $\mu g$/mL of the hot-water extract, the degranulation of RBL-2H3 cells were inhibited 14.58$\pm$0.97%, 43.69$\pm$0.96% and 95.58$\pm$0.75%, respectively. The anti-inflammation activity was the highest as 44.35$\pm$0.63% at a concentration of 400 $\mu g$/mL.

• Journal of the Korean Society of Food Science and Nutrition
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• v.44 no.1
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• pp.1-6
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• 2015

Atopic dermatitis (AD) is a form of allergic skin inflammatory characterized by late eczematous skin lesions. The incidence of AD is increasing, and it causes problems with administrative costs. Therefore, development of an AD treatment with no side effects is needed. The purpose of this study was to evaluate tuna heart ethanol extract (THEE), a functional extract from by-product of tuna. AD was induced by spreading 2,4-dinitrochlorobenzene (DNCB) on the backside of BALB/c mice. The effect of THEE was tested by measuring skin clinical severity score, secretion of cytokines and IgE, and proliferation. Secretion of $TNF-{\alpha}$, IL-4, IL-5, IL-13, and IgE significantly decreased in a THEE-independent manner. In contrast, levels of IL-10 and $IFN-{\gamma}$ significantly increased in mice sera and splenocytes. In addition, THEE alleviated AD symptoms compared to the DNCB only group. In conclusion, these results demonstrate that THEE has an inhibitory effect on AD and may be a useful substance for the development of cosmeceuticals.