• YAKHAK HOEJI
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• v.39 no.6
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• pp.616-621
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• 1995

The effect of WK101 on compound 48/80-induced anaphylaxis was studied in rat. WK101 was found to exhibit a inhibitory activity on the compound 48/80-induced anaphylaxis. WK101 also inhibited the serum histamine release induced in anaphylaxis by compound 48/80. The effect of WK101 on the histamine release from rat peritoneal mast cells was studied. WK101 ($10^{3}-1mg/ml$) inhibited the histamine release induced by compound 48/80($5{\;}\mu\textrm{g}/ml$) in rat peritoneal mast cells. To clarify the mechanism of these inhibitons, we investigated the effects of WK101 on cAMP and intracellular calcium content of rat peritoneal mast cell. The content of cAMP in mast cells, when WK101 was added, was increased transiently, and was significantly increased more 53 fold at 10 sec than that of basal cells. Moreover, WK101 inhibited intracellular calcium release induced by compoound 48/80. This results suggest that WK101 may be useful for the prevention and treatment of allergy-related disease.

• The Journal of Internal Korean Medicine
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• v.21 no.1
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• pp.156-161
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• 2000

The unripe fruit of Poncirus trifoliata Raf has been used for the treatment of allergic disease. Recently it was reported that the fruit inhibits passive cutaneous anaphylaxis and histamine release at mast cell. Type I immediate hypersensitivity of anaphylactic type is caused by released mediate chemical at mast cell. Histamine is also known as one of potent mediate chemical. Also release of mediate chemical is affected by specific stimulation of IgE combined with mast cell. Activation of mast cell is known to be stimulated by compound 48/80 and inhibited by increase of cAMP. In this experiment, the effect of water extract of Poncirus trifoliata Raf fruit (PT) on a histamine release, cAMP concentration and IgE production was measured. Compound 48/80 was administrated to the mouse peritoneal cell which was pretreated with PT. PT dosedependently inhibited histamine release at peritoneal mast cell and the serum level of histamine induced by compound 48/80. PT also instantly increased cAMP level of peritoneal mast cell right after it was added and the level gradually decreased. Production of IgE induced by antigens at mouse peritoneal cell was inhibited by PT. The IgE synthesis is induced by IL-4 and it is known that lipopolysaccharide(LPS) plus IL-4 cause an increase in IgE secretion by murine B cells. The effects of PT inhibited the production of IgE activated by LPS plus IL-4 at human U266B1 cells. These results indicate that PT has antiallergic activity by Inhibition of IgE production from B cells and histamine release by increase of cAMP.

• Korean Journal of Pharmacognosy
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• v.20 no.1
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• pp.37-42
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• 1989

This study was carried out to investigate the effect of Glycyrrhizae Radix on serum corticosterone and blood histamine content by immobilization stress in mice. Corticosterone secretion and blood histamine level was significantly increased in mice by subjecting the animals to immobilization stress 1 hr. after intraperitoneal injection of Glycyrrhizae Radix extract (150 mg/kg) and glycyrrhizinic and (15 mg/kg). whereas, administration of cortisol $(7.5\;{\mu}g/kg)$ provoked a decrease in corticosterone secretion and histamine levels. These results suggested that glycyrrhizinic acid was effective on cortiosterone release provoked by immobilization stress and this release was mediated in part by histamine.

• Advances in Traditional Medicine
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• v.10 no.3
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• pp.200-207
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• 2010

The fruits of Piper cubeba L. are used traditionally to treat respiratory disorders in Indonesia. In order to determine the compounds responsible for this activity, the fruits were extracted with nhexane followed by ethanol to give n-hexane and ethanol extracts. Based on tracheospasmolytic assay on these two extracts, the n-hexane extract was more active to inhibit trachea contraction than that of ethanol extract. Upon bioassay guided isolation of the n-hexane extract, a tracheospasmolytic active compound was isolated and identified as dihydrocubebin [(3,4),(3',4')-bis-methylenedioxy-9,9'dihydroxylignan] $(\underline{1})$. Compound $\underline{1}$ was tested further for its ability to inhibit histamine released from mast cells, using rat basophilic leukemia (RBL-2H3) cell line and rat peritoneal mast cells RPMCs) as models; and $DNP_{24}$-BSA, thapsigargin, ionomycin, compound 48/80 and PMA were used as inducers for histamine released from mast cell. The test result showed that $\underline{1}$ inhibited histamine release from RBL-2H3 cells induced by $DNP_{24}$-BSA, thapsigargin and ionomycin. In addition, $\underline{1}$ suppressed histamine release from RPMC induced by either thapsigargin or ionomycin. However, $\underline{1}$ did not inhibit histamine release from RPMC induced by either compound 48/80 or combination PMA-sub optimum dose of ionomycin. Therefore, it was concluded that the inhibitory effects of $\underline{1}$ on the histamine released from mast cells may involve mechanisms related to intracellular $Ca^{2+}$ signaling events or downstream processes of intracellular $Ca^{2+}$ signaling in mast cells.

• Food Science and Biotechnology
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• v.15 no.3
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• pp.363-368
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• 2006

Twenty-four different natural food materials extracted with 80% methanol were used to investigate the inhibition of cell-mediated immediate type allergic reactions induced by compound 48/80 in rat peritoneal mast cells (RPMCs). Nine 80% methanol extracts screened at a concentration of $10\;{\mu}g/mL$ inhibited histamine release from RPMCs induced by compound 48/80. Of these, two materials (Ulmus parvifolia and Liriope platyphylla Wang et Tang) were extracted and fractionated into four different solvent types (chloroform, ethylacetate, butanol, and water), and the fractions with major anti-allergic effects were assessed. The chloroform fraction of U. parvifolia (UP) at $5\;{\mu}g/mL$ and the ethylacetate fraction of L. platyphylla Wang et Tang (LPWT) at $1\;{\mu}g/mL$ showed the greatest inhibition of histamine release induced by compound 48/80. The chloroform fraction of UP and the ethylacetate fraction of LPWT in combination showed a greater inhibition of histamine release than either fraction alone. The cAMP levels in RPMCs treated with UP and LPWT were significantly greater than in cells treated with compound 48/80 alone. Our studies suggest that extracts from UP and LPWT may alleviate immediate type hypersensitivity reactions through the increase of cAMP levels in the mast cells.

• Preventive Nutrition and Food Science
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• v.11 no.2
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• pp.89-93
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• 2006

Methanol extracts (80%, $10{\mu}g/mL$) of Actinidia chinensis (AC) and Zizyphus jujube(ZJ) inhibited histamine release from rat peritoneal mast cells (RPMCs) induced by compound 48/80. Evaluation of AC and ZJ solvent fractions (chloroform, ethylacetate, butanol and water) revealed that the butanol fraction of AC at $5{\mu}g/mL$ and water fraction of ZJ at $1{\mu}g/mL$ exhibited the highest anti-allergic effects. Combination of the butanol fraction of AC and water fraction of ZJ when combined showed higher inhibition of histamine release than either alone. The levels of cAMP in RPMCs treated with AC and ZJ were significantly increased compared to the compound 48/80 treated control. Our findings suggest that the extracts from AC and ZJ may alleviate immediate hypersensitivity reactions through the increase of cAMP in the mast cells.

• Biomolecules & Therapeutics
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• v.16 no.4
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• pp.416-424
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• 2008

A series of N,N'-substituted iminodiacetamide derivatives was synthesized and evaluated their inhibitory effects on the histamine-induced smooth muscle contraction in guinea-pig ileum and on the histamine release from IgE-sensitized RBL-2H3 cells (rat basophilic leukemia cell line). Compounds A3, A4 and A5 which have 1-(4-chlorobenzhydryl) piperazine moiety, showed both moderate antihistamine activity and histamine release inhibitory activity.

• The Korean Journal of Physiology and Pharmacology
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• v.10 no.2
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• pp.101-108
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• 2006

The aim of the present study was to elucidate whether gallic acid could modulate the inflammatory allergic reaction and to study its mechanism of action Gallic acid inhibited compound 48/80- or immunoglobulin E (IgE)-induced histamine release from mast cells. The inhibitory effect of gallic acid on the histamine release was mediated by modulation of cAMP and intracellular calcium. Gallic acid decreased the phorbol 12-myristate 13-acetate plus calcium ionophore A23187-stimulated pro-inflammatory cytokine gene expression and production such as TNF- ${\alpha}$ and IL-6 in human mast cells, and the inhibitory effect of gallic acid was on dependent nuclear factor- ${\kappa}$B and p38 mitogen-activated protein kinase. Our findings provide evidence that gallic acid inhibits mast cell-derived inflammatory allergic reaction by blocking histamine release and pro-inflammatory cytokine expression.

• Journal of Microbiology and Biotechnology
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• v.12 no.3
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• pp.483-489
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• 2002

The role of $G{\alpha}12\;and\;G{\alpha}13$ in modulating the IgE receptor-mediated histamine secretion in the streptolysin-o-permeabilized human cultured mast cell was investigated. The expression of $G{\alpha}12\;and\;G{\alpha}13$ proteins were regulated during human cultured mast cell differentiation, and a significant correlation was observed between the levels of expression of $G{\alpha}12\;and\;G{\alpha}13$ proteins and IgE receptor-mediated histamine secretion capability in human cultured mast cells. Antibodies against $G{\alpha}12\;and\;G{\alpha}13$ effectively inhibited the IgE receptor-induced histamine release, and the concentration of anti-$G{\alpha}12$ antibody used to inhibit histamine secretion was shown to also inhibit the IgE receptor-mediated elevation of intracellular $Ca^2+$. Therefore, the results suggest that $G{\alpha}12\;and\;G{\alpha}13$ play roles in modulating IgE receptor-activated $Ca^2+$ influx, thereby regulating histamine release in cultured human mast cells. This is the first report to show that $G{\alpha}12\;and\;G{\alpha}13$ are involved in the regulation of $Ca^2+$ mediated exocytosis in human cultured mast cells.

• Microbiology and Biotechnology Letters
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• v.33 no.4
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• pp.260-266
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• 2005

IgE-dependent histamine releasing factor (HRF), previously known as P23/P21 or translationally controlled tumor protein (TCTP), induces the degranulation of histamine in mast cell and basophil. Yeast two hybrid results showed that HRF interacts with the alpha subunit of Na, K-ATPase, suggesting that HRF is a regulator for governing the activity of Na, K-ATPase. In this study, we examined the interaction of HRF and Wa,K-ATPase after treatments of various PKC isotype inhibitors. Membrane fractionation, pull-down assay and immunoprecipitation results showed that PKC $\alpha,\;PKC\;\beta,\;\delta$ subunits are involved in the phosphorylation of HRF. However, these results did not correlate with the results of histamine release assay since histamine release assay results suggested that some PKC isotype inhibitors induced the histamine release in RBL-2H3 cell.