• Archives of Pharmacal Research
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• 제27권5호
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• pp.518-523
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• 2004

An allergic reaction ensues after antigen binds to mast cell or basophil high affinity IgE receptor, Fc$\varepsilon$RI, resulting in degranulation of various inflammatory mediators that produce various allergic symptoms. In this study, i) we isolated the active component for the inhibition of mast cell degranulation from the extract of leaves of Castanea crenata and identified it as quercetin; ii) we established the total synthesis procedure of quercetin; iii) using quercetin as positive control, we excavated some lead compounds that possess inhibitory activities for mast cell degranulation by screening the chemical libraries of 1,3-oxazolidine derivatives prepared by solid phase combinatorial chemistry. Some of 1,3-oxazolidine compounds possessing acetyl and 3',4'-dichlorophenyl group displayed strong inhibitory activities on Fc$\varepsilon$RI-mediated mast cell degranulation, suggesting that they can be used as lead compounds for the development of anti-allergic agents.

• Natural Product Sciences
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• 제10권5호
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• pp.211-216
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• 2004

Citrus unshiu (Rutaceae) has long been known as an anti-inflammatory and anti-allergic agent. In the present study, the inhibitory effect of CUWE (Citus unshiu water extract) on the production of $TNF-{\alpha}$ and tryptase was examined. In addition, a possible mechanism for the inhibition of trypsin-stimulated human leukemic mast cell-1 (HMC- 1 ) activation was determined. To do so, $TNF-{\alpha}$ production from the HMC-1 cells that were stimulated by trypsin (100 nM) in the presence or absence of CUWE $(10,\;100,\;and\;100\;{\mu}g/ml)$ was measured by enzyme-linked immunosorbent assay (ELISA) and reverse transcription-PCR. The tryptase production was evaluated by reverse transcription-PCR. Extracellular signal-regulated kinase (ERK) activation was analyzed by Western blot. Trypsin activity was measured by using Bz-DL-Arg-p-nitroanilide (BAPNA) as substrate. Results showed that the CUWE inhibited production of both $TNF-{\alpha}$ and tryptase from the trypsin-stimulated HMC-1 in a dose-dependent manner. The CUWE a1so inhibited the ERK phosphorylation and trysin activity. These results indicate that the CUWE had an inhibitory effect on $TNF-{\alpha}$ and the tryptase productions by blocking the ERK phosphorylation and trypsin activity.

• 한국식품저장유통학회지
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• 제17권5호
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• pp.757-761
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• 2010

자소는 여러 질환을 치료하는 식물로 알려져 있는데, 본 연구는 자소 추출물을 이용하여 항산화 활성 및 항염증 활성을 알아보았다. 자소 추출물을 이용한 DPPH, FRAP 실험 결과, 농도에 따른 항산화 활성을 확인할 수 있었으며, 자소자 추출물의 경우 고온/고압 추출시 활성이 증가하는 것을 알 수 있었다. 마우스 동물모델을 이용한 항아토피활성 결과 귀와 상피의 비후를 감소시키고, 면역세포의 침투현상을 억제하는 것으로 나타났다. 이상의 결과로, 자소는 항산화 및 염증완화 소재로 이용할 수 있음을 확인하였다.

• 동의생리병리학회지
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• 제26권4호
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• pp.469-474
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• 2012

Fagopyrum esculentum(FE) is an important food crop and medicinal plant that is used to improve diabetes, obesity, hypertension, hypercholesterolemia and constipation in Korea, but the underlying mechanisms involved in its anti-allergic activity are not fully understood. We investigated the effects on the release of inflammatory mediator and proximal signal events in $Fc{\varepsilon}RI$-mediated RBL-2H3 cell activation. FE reduced antigen (DNP-HSA)-induced release of histamine, prostaglandin D2 (PGD2) and cysteinyl Leukotriene (cysLT) in IgE-sensitized RBL-2H3 cells. In addition, it inhibited antigen-induced HDC2 and COX-2 and 5-LO mRNA expression in IgE-sensitized RBL-2H3 cells. FE also suppressed antigen-induced $Fc{\varepsilon}RI{\beta}$ and $Fc{\varepsilon}RI{\gamma}$ subunit mRNA expression in these cells. To identify the mechanisms underpinning the inhibition of release of inflammatory mediators such as histamine and PGD2 and cysLT by FE, we examined the proximal signal events of intracellular FceRI signaling molecules. FE suppressed antigen-induced phosphorylation of Lyn, Syk, LAT, $PLC{\gamma}1$, PI3K, Akt and cPLA2. Collectively, the anti-allergic effects of FE in vitro suggest its possible therapeutic application to inflammatory allergic diseases, in which its inhibition of inflammatory mediator and FceRI-dependent signaling events in mast cells may be hugely beneficial.

• Biomolecules & Therapeutics
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• 제27권3호
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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.

• 디지털융복합연구
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• 제17권8호
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• pp.257-264
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• 2019

본 연구는 부채마 70% 에탄올 추출물(DR)이 RBL-2H3 마스트 세포에서 항원에 의한 세포활성의 영향과 BALB/c 쥐에서 dinitrofluorobenzene에 의해 유도된 마스트 세포-매개 알레르기 접촉성피부염에 미치는 영향을 조사했다. DNP-HSA 항원과 Anti-DNP IgE 항체에 의해 활성 된 RBL-2H3 세포에서 에탄올 추출물은 급성 항원반응 표지인 ${\beta}$-hexosaminidase 분비와 히스타민 등을 억제하였고, 후기 항원반응 표지인 IL-4와 $TNF-{\alpha}$ 생성을 억압하였다. DNFB-유도 접촉성 알러지성 피부염 동물 모델에서 에탄올 추출물 처리는 귀 부기를 감소시키고 혈청 히스타민과 IL-4 분비를 억제시켰으며, DR 처리는 피부염 유발 부분에서 마스트 세포 유입을 효과적으로 방지하였다. 이러한 결과로, 에탄올 추출물은 아토피 피부염과 같은 마스트 세포-매개 알러지성 질병의 치료제로 사용할 수 있을 것이다.

• 한국응용과학기술학회지
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• 제35권3호
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• pp.975-984
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• 2018

마치현 추출물에 대한 생리활성 소재로서 응용 가능성을 확인하고자 하였다. 마치현 추출물의 측정 결과, 플라보노이드, 폴리페놀 함량과 DPPH radical 소거능을 확인하였으며, 세포실험 결과 HaCaT, RAW 264.7, RBL-2H3 세포에서 유의한 세포독성은 나타나지 않았으며. $H_2O_2$에 의한 유발되는 산화적 스트레스에 대한 HaCaT 세포는 마치현 에탄올 $100{\mu}g/mL$ 농도에서 83% 보호효과가 확인되었다. RAW 264.7 세포에 대한 마치현 추출물의 항염 효과를 확인 결과 저농도에서도 nitric oxide 생성이 억제되었으며, S. aureus, S. epidermidis, P. acnes 균에서도 마치현 추출물의 농도 의존적으로 항균 활성이 확인되었다. 본 연구는 마치현 추출물의 항산화, 항염증 및 항균 효과를 가지는 생리 활성 물질로서 활용 가능성을 확인하였다.

• 한방안이비인후피부과학회지
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• 제24권1호
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• pp.1-15
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• 2011

Objective : To establish the fundament for EBM of Traditional Korean Medicine, the papers on Bangpungtongseong-san (Fangfengtongsheng-san) frequently used in medical institutions of Traditional Korean Medicine were analyzed through researching domestic and international papers. Methods : The papers were classified by the registration of domestic or international journals, the year of publishment, experimental fields and the kinds of studies on biological activities. Results : Among 324 volumes of papers on Bangpungtongseong-san (Fangfengtongsheng-san), 38 volumes were selected according to selective criteria. 18 volumes were published in domestic journals, 20 volumes were in Japanese journal. The papers on instrumental analyses reported the quantification of standard compounds of herbal medicines in Bangpungtongseong-san (Fangfengtongsheng-san) using HPLC method. The papers on biological activities of Bangpungtongseong-san (Fangfengtongsheng-san) showed inhibitory effect to obesity, arteriosclerosis, allergic response, inflammation, pain, hyperlipidemia, hypertension, atopy, diabete mallatus and improvement of gastrointestinal activity and cerebral blood circulation. Among biological activities, papers on anti-obesity effect were reported mostly. Conclusions : Further studies including anti-obesity activity need to be preceeded to establish the fundament for EBM of Bangpungtongseong-san (Fangfengtongsheng-san).

• 동아시아식생활학회지
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• 제17권1호
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• pp.43-50
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• 2007

This study investigated the effects of mycelia of Lentinus edodes mushroom-cultured Glycyrrihiza radix(LMG) on cancer cell lines and sarcoma 180(S-180), as well as on human mast cells. In an anti-cancer tests using Hep3B(hepatic cancer cell), MCF-7(breast cancer), and HeLa(uterine cancer) cells, LMG extract exhibited greater anti-proliferation effects than Glycyrrihiza glabra(GG) extract. LMG extract multiplication restraining effects were 60% that of ethanol at 3 mg/mL extract also displayed tumor suppressive effects in mice injected with S-180 cells. The growth-inhibition rates against tumor cells were 56% for LMG and 37% for GG. When LMG was added to human mast cells, the Intensity of RT-PCR products using primers($FC{\varepsilon}RI\;c-kit$) decreased. significantly compared with that of control. These results suggest that Lentinus edodes Mushroom-Cultured Glycyrrhiza glabra has an anti-proliferation effects against cancer cell lines(Hep3B, MCF-7 and HeLa) and S-180 tumors and will be also beneficial in treating allergic reactions.

• Journal of Nutrition and Health
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• 제51권3호
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• pp.208-214
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• 2018

본 연구는 으뜸도라지추출물의 항알레르기 효과를 조사하기 위해 실시하였다. 으뜸도라지추출물 (50, 100 및 $200{\mu}g/mL$) 처리에 따른 RBL-2H3 비만세포의 세포독성을 조사한 결과 으뜸도라지추출물은 모든 농도에서 세포독성이 관찰되지 않았고, ${\beta}$-hexosaminidase assay를 통해 비만세포의 탈과립 억제능을 평가한 결과 재래종도라지추출물과 비교하여 ${\beta}$-hexosaminidase 억제능이 10배 뛰어남을 확인 하였다. 또한 으뜸도라지추출물은 RBL-2H3 비만세포에서 탈과립 후 유리되는 대표물질인 IL-4, $TNF-{\alpha}$, $PGE_2$ 및 $LTB_4$의 생성 분비를 현저히 감소시켰고, 이러한 효과는 재래종도라지와 비교하여 월등한 것으로 나타났다. 이상의 결과는 으뜸도라지추출물이 알레르기 반응을 효과적으로 억제함을 제시하며 향후 항알레르기 기능성 소재로 개발 가능성이 있음을 나타낸다.