• The Korean Journal of Physiology and Pharmacology
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• 제2권2호
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• pp.251-260
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• 1998

Cromakalim (BRL 34915), known as an airway smooth muscle relaxant, inhibited the releases of mediators in the antigen-induced mast cell activation. It has been suggested that cromakalim, in part, inhibited mediator releases by inhibiting the initial increase of 1,2-diacylglycerol (DAG) produced by the activation of the other phospholipase system which is different from phosphatidylcholine-phospholipase D pathway. The aim of this study is to further examine the inhibitory mechanism of cromakalim on the mediator release in the mast cell activation. Guinea pig lung mast cells were purified by using enzyme digestion and percoll density gradient. In purified mast cells prelabeled with $[^3H]PIP_2$, phospholipase C (PLC) activity was assessed by the production of $[^3H]$insitol phosphates. Protein kinase C (PKC) activity was assessed by measuring the protein phosphorylated from mast cells prelabeled with $[{\gamma}-32P]ATP$, and Phospholipase $A_2\;(PLA_2)$ activity by measuring the lyso-phosphatidylcholine produced from mast cell prelabeled with 1-palmitoyl-2-arachidonyl $phosphatidyl-[^{14}C]choline$. Histamine was assayed by fluorometric analyzer, and leukotrienes by radioimmunoassay. The PLC activity was increased by activation of the passively sensitized mast cells. This increased PLC activity was decreased by cromakalim pretreatment. The PKC activity increased by the activation of the passively sensitized mast cells was decreased by calphostin C, staurosporine and cromakalim, respectively. The $PLA_2$ activity was increased in the activated mast cells. The pretreatment of cromakalim did not significantly decrease $PLA_2$ activity. These data show that cromakalim inhibits histamine release by continuously inhibiting signal transduction processes which is mediated via PLC pathway during mast cell activation, but that cromakalim does not affect $PLA_2$ activity related to leukotriene release.

• 대한수의학회지
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• 제31권3호
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• pp.343-353
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• 1991

In order to investigate the histopathological, mechanism of Rompun-induced shock, the development of mammary carcinoma, the numerical changes and the morphological findings of the mast cells appeared in the carcinoma were microscopically observed in the rat treated with DMBA and each chemical of compound 48/80 and Rompun. Also mast cell degranulation induced by Rompun was observed with electron microscope. The results observed were summarized as follows: Tumor appeared in 100% of the animals. Tumors grew more rapidly to $10{\times}10mm$ in rats depleted of mast cells ($37.7{\pm}4.2$ days) than was observed in the control group ($42.5{\pm}4.7$ days) (p<0.005). The mean number of tumors per rat was $2.8{\pm}1.3$ in the compound 48/80- treated group in contrast to $3.4{\pm}1.3$ in the control group. No significant difference was apparent in the tumor induction time of Rompun treated group compared with the compound 48/80-treated group, but the tumor measuring at least $10{\times}10mm$ appeared more quickly in the Rompun treated group than in the control group (p<0.005). The numbers of mast cells in the control group were inclined to increase significantly according to the mammary tumor development (p<0.005). In contrast, the mast cells were fewer significantly in the compound 48/80-treated group and Rompun-treated group than in the control group (p<0.005). The numbers of mast cells in the compound 48/80-treated group and Rompun-treated group were inclined to reduce significantly according to the stages of the mammary carcinoma growth in contrast to the control group respectively. The ultrastructural morphologies of mast cells at 30 minutes after Rompun injection were appeared many normal granules in the cytoplasm, but many normal and degranulated granules were scattered along the cell membrane. And at 1 hour after Rompun injection mast cell granules were disappeared nearly or rarely seen. many long cytoplasmic projections were folded back to adhere to their own surface membrane. and mast cells resulted in a reduced size of these cells. Otherwise. compound 48/80 caused extensive degranulation of mast cells by disrupting cell membrane. but mast cell degranulation by Rompun was observed exocytosis of granules through a channel. From the above results. it is concluded that the Rompun may give rise to the dealth of animals as a shock caused by mast cell degranulation.

• 한국동물학회지
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• 제16권1호
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• pp.13-23
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• 1973

저자들은 성숙한 雄性白鼠(Albino Wistar)에 INH 40mg/kg, pyridoxine 20mg/kg를 경구적으로 투여하여 mast cell과 enterochromaffin cell 의 변동을 관찰하여 다음과 같은 결과를 얻었다. 1. INH투여로 白鼠 약 舌 mast cell 의 심한 파괴와 細胞質顆粒의 逸出作用으로 세포수는 격감하였으나, pyridoxine 투여군에서는 대조군에 비해 상당한 수적증가를 보였다. 2. INH 투여로 白鼠 심이지장 enterochromaffin cell의 세포수와 細胞質顆粒양에 현저한 감소를 나타냈으나 pyridoxine 투여군에서는 대조군에 비해 enterochromaffin cell의 상당한 수적증가를 보였다. 3. 이상의 성적에 있어서 INH의 다량 투여는 mast cell과 enterochromaffin cell의 생성에 심한 장해를 주며 pyridoxine 의 적당한 투여는 mast cell과 enterochromaffin cell의 생성을 조장 하고 顆粒양을 증가시키는 것으로 보아 이들 세포의 分泌産物인 5-Hydroxytryptamine 대사에 pyridoxine이 관여하는 것으로 사료된다.

• Advances in Traditional Medicine
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• 제1권1호
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• pp.82-88
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• 2000

We investigated the effect of aqueous extract of Cichorium intybus (CIAE) on mast cell-mediated immediate type allergic reactions. CIAE dose-dependently inhibited systemic anaphylactic reaction induced by compound 48/80 in mice. Especially, CIAE inhibited compound 48/80-induced anaphylactic reaction 100% with the dose of 1000 mg/kg. CIAE 1000 mg/kg also significantly inhibited local anaphylactic reaction activated by anti-dinitrophenyl (DNP) IgE. When mice were pretreated with CIAE at a concentration ranging from 0.1 to 1000 mg/kg, the plasma histamine levels were reduced in a dose-dependent manner. CIAE (1 to 1000 g/ml) dose-dependently inhibited histamine release from the rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-DNP IgE. These results indicate that CIAE inhibits mast cell-mediated immediate-type allergic reactions.

• 약학회지
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• 제49권5호
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• pp.386-391
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• 2005

The discovery of drugs for the treatment of mast cell-mediated allergic disease is a very important subject in human health. The Amomum xanthiodes (Zingiberaceae) has been used for centuries as a traditional medicine in Korea and is known to have an anti-inflammatory effect. However, its specific mechanism of action is still unknown. In this report, we investigated the effect of hot water extract from Amomum xanthiodes (EAX) on the mast cell-mediated allergic reaction and studied its possible mechanisms of action. EAX inhibited compound 48/80-induced systemic anaphylaxis and serum his­tamine release in mice. EAX decreased the passive cutaneous anaphylaxis reaction activated by anti-dinitrophenyl (DNP) IgE antibody. EAX dose-dependently reduced histamine release from rat peritoneal mast cells activated by compound 48/80 or anti-DNP IgE. EAX increased cAMP and decreased compound 48/80-induced intracellular $Ca^{2+}$ levels. Our findings provide evidence that EAX inhibits mast cell-derived allergic reactions, and also demonstrate the involvement of cAMP and intracellular $Ca^{2+}$ in these effects.

• 대한치과의사협회지
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• 제12권1호
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• pp.21-28
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• 1974

The author has observed the distribution of the tissue mast cells in 67 various tumors and precancerous lesions which occurred in the oral cavity. The specimcns ware obtained from the department of oral pathology, college of dentistry, Seoul National University, from Jan. 1970 to June, 1973. The results are as follows: 1) The number of the tissue mast cell was decrease predominantly in malignant tumors, especially in squamous cell carcinomas and in sarcomas. 2) The number of the tissue mast cell distirbution in adenocarcinomas one of malignant group was sligtly increased in with healthy oral mucosa. 3) The number of tissue mast cells in ameloblastomas one of benign group of the tumor of epithelial originwas more decreased than that in healthy oral mucosa. 4) The number of tissue mast cells in fibromas was more than that in healthy oral mucosa. 5) The number of the tissue mast cells in mixed tumors was increased one and a half times as many as that in healthy oral mucosa. 6) The number of the tissue mast cells in mixed tumors was increased one and a half times as many as that in healthy oral mucosa. 7) The tissue mast cell distribution can be observed more densly in the stroma of tumors than in the parenchyme of tumors.

• Journal of Evidence-Based Herbal Medicine
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• 제1권1호
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• pp.13-18
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• 2008

Polygoni cuspidati Rhizoma (PCRH) has been used in treatment of menoxenia, skin burn, gallstone, hepatitis, hyperlipidaemia, favus athlete's foot, supperative dermatitis and inflammation. However, its effect in experimental models remains unknown. In this present study, the effect of PCRH for stability on mast cell was analyzed. Two g/kg PCRH inhibited the compound 48/80-induced anaphylaxis by 75%. In addition, PCRH inhibited the tumor necrosis factor-$\alpha$ and interleukin-8 secretion as compared with the phorbol 12-myristate 13-acetate plus calcium ionophore A23187 stimulated human mast cell line, HMC-1 cells. These results suggested PCRH may inhibit mast cell-mediated anaphylactic reaction.

• 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.

• 한국임상수의학회지
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• 제22권3호
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• pp.264-267
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• 2005

구토와 식용부진을 3일전부터 나타내고, 2년전부터 좌측 후지 상부에 종괴를 갖고 있는 12년령, 8.0kg, 난소 제거 잡종 암캐 1두가 충남대학교 부속동물병원에 내원하였다. 환자는 fine-needle aspiration (FNA) 세포진단학 검사에 의하여 mast cell tumor로 진단하였다. Mast cell tumor 진단을 위한 WHO clinical staging system에 의하여 stage IIIa로 분류하였다. 환자는 adjuvant corticosteroid 요법에 의하여 투약되었으며, 축주의 요구에 의하여 완전 외과 절제는 실시하지 아니 하였다. 초기에 adjuvant corticosteroid 단독 요법에 의하여 종괴의 크기가 점차 감소하였으며, 환자의 전신상태는 호전되었다. 그러나 그 후에는 더 이상 glucocorticoid에 반응을 하지 아니 하였으며, 종괴의 크기가 증가하였고, 2개월 후에 간헐적 구토와 심한 호흡곤란 때문에 안락사 하였다. 비장 종괴, 십이지장 궤양, 간 종괴와 후지 상부 근육부위에 침윤된 mast cell tumor가 부검 시에 발견되었다. Mast cell tumor는 grade I 또는 II에서 그리고 .조직학적으로 well-differentiated된 상태에서 외과적 완전절제, 방사선요법, adjuvant corticosteroid 요법, 화학요법을 병용 하여야 양호한 예후를 나타낼 것으로 기대된다.

• The Korean Journal of Physiology and Pharmacology
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• 제2권1호
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• pp.119-131
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• 1998

It has been reported that the glycoprotein extracted from Aloe has strong anti-inflammatory response. However, there has been no research report yet about the effect of Aloe on allergic hypersensitivity reactivity. By using guinea pig lung mast cells, this study aimed to examine the effects of Aloe glycoprotein (NY945) on the mediator releases caused by mast cell activation, and also aimed to assess the effects of NY945 on the mechanism of mediator releases in the mast cell activation. We partially purified mast cell from guinea pig lung tissues by using the enzyme digestion, the rough and the discontinuous density percoll gradient method. Mast cells were sensitized with IgG1 (anti-OA) and challenged with ovalbumin. Histamine was assayed by fluorometric analyzer, leukotrienes by radioimmunoassay. The phospholipase D activity was assessed by the production of labeled phosphatidylalcohol. The amount of mass 1, 2-diacylglycerol (DAG) was measured by the $[^3H]DAG$ produced when prelabeled with $[^3H]myristic$ acid. The phospholipid methylation was assessed by measuring the incorporation of the $[^3H]methyl$ moiety into phospholipids of cellular membranes. Pretreatment of NY945 (10 ${\mu}g$) significantly decreased histamine and leukotrienes releases during mast cell activation. The decrease of histamine release was stronger than that of leukotriene during mast cell activation. The phospholipase D activity increased by the mast cell activation was decreased by the dose-dependent manner in the pretreatment of NY945. The amount of DAG produced by PLC activity was decreased by NY945 pretreatment. The amount of mass 1, 2-diacylglycerol produced by activation of mast cells was decreased in the pretreatment of NY945. NY945 pretreatment strongly inhibited the incorporation of the $[^3H]methyl$ moiety into phospholipids. The data suggest that NY945 purified from Aloe inhibits in part an increase of 1, 2-diacylglycerol which is produced by activating mast cells with antigen-antibody reactions, which is mediated via phosphatidylcholine-phospholipase D and phosphatidylinositol-phospholipase C systems, and then followed by the inhibition of histamine release. Furthermore, NY945 reduces the production of phosphatidylcholine by inhibiting the methyltransferase I and II, which decreases the conversion of phosphatidylcholine into arachidonic acid and inhibits the production of leukotrienes.