• 생약학회지
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• 제33권1호통권128호
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• pp.49-52
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• 2002

Amentoflavone, naturally occurring biflavonoid, isolated from the leaves of Ginko biloba, selectively inhibited human seceretory phospholipase $A_2$. This compound potently and irreversibly inhibited human group IIA in a dose dependent manner with an $IC_50$ about $3\;{\mu}M$. Amentoflavone inhibited phospholipase $A_2$ by a noncompetitive manner with the apparent Ki value of $1{\times}10^{-5}M$. In addition, the inhibitory activity of amentoflavone is rather specific against group IIA phospholipase $A_2$ than group IB phospholipase $A_2$. Furthermore, this compound strong inhibit histamine release from $A_{23187}$ treated rat peritoneal mast cells. These results indicate naturally occurring biflavonoid represents a novel anti-inflammatory agent.

• 한국식품과학회지
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• 제41권4호
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• pp.405-412
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• 2009

본 연구는 꾸지뽕 나무 열매로부터 75 kDa의 당단백질(꾸지뽕 당단백질)을 추출한 후 꾸지뽕 당단백질의 첨가에 따른 알레르기성 염증 인자인 histamine 유리 억제능력 및 COX-2의 활성 억제 효과를 평가하였다. RBL-2H3세포를 22시간 동안 IgE로 감작시킨 후, HSA를 처리하여 histamine의 유리양을 측정한 결과 꾸지뽕 당단백질을 처리한 농도가 증가함에 따라 histamine의 유리와 COX-2의 활성 억제율은 증가하였다. 또한 꾸지뽕 당단백질의 처리는 HSA에 의해 유도된 세포내 ROS 생성량을 농도에 의존적으로 억제하였다. 한편 꾸지뽕 당단백질을 농도별로 처리하여 세포내 단백질을 추출하여 western blot을 실시한 결과 100 ${\mu}g$/mL 농도의 꾸지뽕 당단백질을 처리한 그룹에서 ERK1/2, AP-1과 COX-2의 활성 수준은 현저히 억제 되었다(p<0.05). 따라서 이러 한 결과에 미루어볼 때, 꾸지뽕 당단백질은 세포내 해독효소의 활성을 증가시킴으로써 ROS 수준을 감소시켰으므로 꾸지뽕 당단백질의 역할이 다른 천연물 유래의 당단백질과 마찬가지로 특이적인 항산화 능력을 지니고 있음을 나타내며 histamine의 유리 억제와 COX-2의 활성이 억제되었을 것으로 생각된다. 이는 꾸지뽕 당단백질이 항 알레르기 효능을 갖는 물질로써 알레르기성 비염, 아토피 등과 같은 알레르기 관련 질환의 예방 및 치료제로 사용될 수 있을 것 사료된다.

• 한국자원식물학회지
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• 제24권1호
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• pp.98-104
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• 2011

수삼 추출물에서 홍삼특이 사포닌 성분의 함량을 증대시키고자 추출온도 및 시간에 따른 사포닌 성분별 함량 변화를 조사하였다. 수삼을 $85^{\circ}C$에서 48시간 추출 시 총 사포닌 함량이 23.5 mg/g(D.W.)로 가장 많았으며, 본 조건에서 추출한 인삼추출물의 항알러지 기능성을 검토하고자 랫트 비만세포에서 compound 48/80로 유도된 히스타민 유리 작용을 억제하는 인삼추출물의 효능을 분석하였다. 인삼추출물의 비만세포에 대한 세포 독성 시험 결과 각 추출물은 수시간 노출시 높은 세포 생존율을 보이고 있었고 비교적 고농도인 0.5 mg/ml 처리군에서도 80% 이상의 세포 생존율을 보였다. 인삼추출물의 히스타민 유리 억제 효과를 조사하기 위해 랫트 비만세포에 대표적인 탈과립 유도제인 compound 48/80을 단독 또는 각 추출물을 동시에 처리한 후 얻어진 상청액의 히스타민의 정량을 실시한 결과 비만세포는 compound 48/80의 처리 조건에서 대조군에 비하여 30% 가량의 히스타민 유리량이 증가하였는데, 인삼추출물 처리 시 히스타민 유리 수준이 정상 수준에 가까이 감소하는 것을 확인하였다. 이는 인삼추출물의 항 알러지 목적으로의 이용 가능성을 제시하고 있다.

• 동의생리병리학회지
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• 제21권3호
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• pp.617-625
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• 2007

Samul-Tang (SMT) has been used for nourishing of the blood, hematopoiesis as a herbal medicine history. The purpose of this study is to find out anti-allergic inflammatory reaction of SMT. To clarify the mechanism, the effect of SMT on vascular permeability of rat cutaneous tissue and histamine and cytokines (IL-6, IL-8, TNF-${\alpha}$) release from mast cells were observed. The results are the pretreatment with SMT significantly decreased the compound 48/80-induced degranulation and histamine release from RPMC, SMT also inhibited the anti-DNP lgE-induced increment of vascular permeability of rat cutaneous tissue. SMT significantly reduced the PMA plus A23187-induced increment of expression of IL-6, IL-8, and TNF-${\alpha}$ in HMC-1 Cell. The Present study provide evidence that SMT inhibits mast cell-derived inflammatory allergic reactions by blocking histamine release and pro-inflammatory cytokine expression, and suggest the mechanisms of action. Furthermore, in vivo and in vitro anti-allergic effect of SMT suggests a possible therapeutic application of this agent in inflammatory allergic diseases.

• 대한임상검사과학회지
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• 제47권4호
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• pp.306-312
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• 2015

알러지 반응이 일어나면 histamine이 방출되기 때문에 histamine을 정량 측정함으로써 유발된 알러지의 정도를 확인 할 수 있다. 일반적으로는 항원-항체반응으로 microplate reader를 이용하여 흡광도를 측정하여 정량 한다. 본 연구에서는 histamine 방출량을 측정함에 있어서 일반적인 항원-항체반응과 분석 화학적인 방법으로 HPLC-MS를 이용한 방법을 비교하였다. 세포주는 RBL-2H3를 사용하였고, C48/80으로 자극시켜 알러지를 유발하였다. 유발된 알러지는 ${\beta}$-hexosaminidase의 측정으로 탈 과립을 확인하였으며 실험의 정당성을 위하여 세포독성 능을 확인하였다. Histamine 정량에서 항원-항체반응에 의한 측정의 정량한계는 10.257 ppm이었고, HPLC-MS에 의한 정량한계는 0.020 ppm으로 현저한 차이를 보였다. 알러지 활성 및 항 알러지 실험에 있어서 histamine의 측정은 HPLC-MS를 이용한 분석이 더 정밀하고 정확한 실험인 것을 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.

• 대한본초학회지
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• 제28권5호
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• pp.39-44
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• 2013

Objectives : Allergy is an immune dysfunction caused by degranulation from mast cells in the early phase of allergic disease. The purpose of this study was to investigate the anti-allergic effect of fermented Angelicae gigantis Radix in human mast cell line, HMC-1. Method : The Angelicae gigantis Radix was fermented by Lactobacillus acidophilus. The cell toxicity of fermented Angelicae gigantis Radix(FAGR) was determined by MTT assay. The release of ${\beta}$-hexosaminidase from HMC-1 stimulated by phorbol-12-myristate 13-acetate (PMA) plus A23187 was determined by ${\beta}$-hexosaminidase assay. Also, the concentrations of cytokines (interleukin-$1{\beta}$, -6, -8 and tumor necrosis factor-alpha) were measured by enzyme-linked immunosorbent assay. The gene expression of COX-2 from HMC-1 stimulated by phorbol-12-myristate 13-acetate (PMA) plus A23187 was determined by reverse transcription polymerase chain reaction. The release of histamine on substance P-stimulated HMC-1 was measured by histamine assay. Result : The FAGR suppressed the release of ${\beta}$-hexosaminidase, a marker of degranulation, from HMC-1 stimulated by PMA plus A23187. The FAGR inhibited the production of interleukin-$1{\beta}$, -6, -8 and tumor necrosis factor-alpha. The FAGR inhibited the expression of COX-2 mRNA. The FAGR suppressed the release of histamine on substance P-stimulated HMC-1. Conclusion : These results provide that FAGR may be beneficial in the treatment of allergic inflammatory disease.

• Journal of Ginseng Research
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• 제20권1호
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• pp.1-6
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• 1996

Effects of Panax ginseng on allergic reactions were studied uslng various in vivo and in vitro experimental models such as 48-hr passive cutaneous anaphylaxis, mediators-induced skin reactions, histamine release from rat peritoneal mast cells, hexosaminidase release from RBL-2H3 cells, and lipoxygenase assay . In all of anti-allergic experiments we conducted, ginseng components (50% ethanol extract or ginseng total saponin or ginsenosides) extracted from Korean red ginseng, did not show significant anti-allergic actions. In 48-hr passive cutaneous anaphylaxis and mediators-induced skin reactions, 50% ethanol extract did not suppress hypersensitivity reactions. Total saponin, 50% ethanol extract, and 8 major ginsenosides did not show inhibitory effects on lipoxygeanse activity. Ginseng total saponin did not inhibit histamine release from rat peritoneal mast cells. All of the ginseng components mentioned above were also tested on RBL-2H3 cells, but none of them inhibited hexosaminidase release from this cell line. These results suggest that Panax ginseng does not have effects on allergic reactions at the level of 50% ethanol extract or total saponin used. All of 8 major saponin components tested ($Rb_1$, $Rb_2$, Rc, Rd, Re, Rf, $Rg_1$, $Rg_2$), did not inhibit lipoxygenase activity and degranulation events.

• Natural Product Sciences
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• 제17권3호
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• pp.239-244
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• 2011

Immediate-type hypersensitivity is involved in many allergic diseases such as asthma, allergic rhinitis and anaphylaxis. The discovery of drugs for the treatment of allergic disease is an important subject in human health. Stimulation of mast cells releases inflammatory mediators, such as histamine and pro-inflammatory cytokines with immune regulatory properties. We investigated the effect of the aqueous extract of Schizonepeta tenuifolia (AEST) (Labiatae) on the immediate-type allergic reaction. AEST inhibited compound 48/80-induced systemic allergic reaction. AEST attenuated immunoglobulin E (IgE)-mediated skin allergic reaction and histamine release from human mast cell line (HMC-1) cells. In addition, AEST decreased the gene expression and secretion of pro-inflammatory cytokines in phorbol 12-myristate 13-acetate (PMA) plus calcium ionophore A23187 (A23187)-stimulated HMC-1 cells. Our results indicate that AEST inhibits the mast cell-derived allergic reactions and involvement of histamine and pro-inflammatory cytokines in these effects.

• The Korean Journal of Physiology and Pharmacology
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• 제17권2호
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• pp.149-156
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• 2013

Interstitial cells of Cajal (ICCs) are the pacemaker cells in the gastrointestinal tract, and histamine is known to regulate neuronal activity, control vascular tone, alter endothelial permeability, and modulate gastric acid secretion. However, the action mechanisms of histamine in mouse small intestinal ICCs have not been previously investigated, and thus, in the present study, we investigated the effects of histamine on mouse small intestinal ICCs, and sought to identify the receptors involved. Enzymatic digestions were used to dissociate ICCs from small intestines, and the whole-cell patch-clamp configuration was used to record potentials (in current clamp mode) from cultured ICCs. Histamine was found to depolarize resting membrane potentials concentration dependently, and whereas 2-PEA (a selective H1 receptor agonist) induced membrane depolarizations, Dimaprit (a selective H2-agonist), R-alpha-methylhistamine (R-alpha-MeHa; a selective H3-agonist), and 4-methylhistamine (4-MH; a selective H4-agonist) did not. Pretreatment with $Ca^{2+}$-free solution or thapsigargin (a $Ca^{2+}$-ATPase inhibitor in endoplasmic reticulum) abolished the generation of pacemaker potentials and suppressed histamine-induced membrane depolarization. Furthermore, treatments with U-73122 (a phospholipase C inhibitor) or 5-fluoro-2-indolyl des-chlorohalopemide (FIPI; a phospholipase D inhibitor) blocked histamine-induced membrane depolarizations in ICCs. On the other hand, KT5720 (a protein kinase A inhibitor) did not block histamine-induced membrane depolarization. These results suggest that histamine modulates pacemaker potentials through H1 receptor-mediated pathways via external $Ca^{2+}$ influx and $Ca^{2+}$ release from internal stores in a PLC and PLD dependent manner.