• YAKHAK HOEJI
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• v.37 no.6
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• pp.625-630
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• 1993

Among the six antihistamine agents tested in this study, homochlorcyclizine showed the highest bradykinin antagonistic activity in the receptor binding assay as well as the isolated rat ileum assay. Schild plot analysis of bradykinin-induced ileal contraction in the presence of three different concentrations of homochlorcyclizine revealed a pA$_{2}$=6.26, and a correlation coefficient of 0.984. Homochlorcyclizine of (100 $\mu{M}$ final concentration) also showed 25% antagonistic activity in the receptor binding assay.

• YAKHAK HOEJI
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• v.37 no.2
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• pp.119-123
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• 1993

A spectrophotomertic method is proposed for the determination of antihistamines. The method is based on solvent extraction of the ion pair formed between antihistamines and colored picric acid into chloroform. The binding state of antihistamines-picric acid complexes were presumed by IR and $^{1}$H-NMR spectra as intermolecular hydrogen bonding. This method was applicable to the determination of antihistamines in the pharamaceutical preparations.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.43 no.2
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• pp.103-114
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• 2017

Gnaphalium affine D. DON (GA) has been used as a vegetable as well as a folk medicine in East Asia. The antioxidant and anti-complementary activity of GA extract (GAE) has also been reported. However, little is known about its anti-inflammatory and anti-allergic effect and mechanism of action. In this study, we evaluated the inhibitory effects of GAE on the production of inflammatory mediators such as NO, $PGE_2$, TLR4, eotaxin-1 and histamine. Our results suggest that GAE inhibits the production of NO and $PGE_2$ by inhibiting transcriptional activation via the involvement of iNOS and COX-2. The LPS-induced expression of Toll-like receptor 4 (TLR4) was also attenuated. In addition, GAE inhibited A23187-induced histamine release from MC/9 mast cells. It also inhibited the production of eotaxin-1 induced by IL-4. Collectively, these results suggest that GAE may have considerable potential as a cosmetic ingredient with anti-inflammatory and anti-allergic properties.

• Journal of the Korean Applied Science and Technology
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• v.38 no.5
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• pp.1292-1301
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• 2021

The purpose of this study was to investigate the anti-pruritic activities such as cell viability and pruritus-related factor using seomaeyakssuk (Artemisia argyi H.; Seomaeyakssuk) extract on MC/9 (mouse mast cell line). Seomaeyakssuk was extracted from hot distilled water. Cell viability was assessed using MTT assay on MC/9 cells. Anti-pruritic activities were measured through changes in the levels of transcription factor (IL4 and IL31) on MC/9 cells. In addition, the expression of linked proteins and histamine was measured. The results confirmed that significant cytotoxicity does not appear in the concentration range of 25, 50, and 100 ㎍/㎖. The levels of IL4 was reduced to 12% (25 ㎍/㎖), 26% (50 ㎍/㎖) and 61% (100 ㎍/㎖). Also, level of IL31 was decreased 33% (50 ㎍/㎖) and 36% (100 ㎍/㎖). In the case of proteins levels decreased significantly IL-4 34%/69% and IL-31 36%/37% at 50 ㎍/㎖ and 100 ㎍/㎖. Histamine decreased by 22, 58% and 61%, respectively, at concentrations of 25, 50, and 100 ㎍/㎖. This results shows possibility of ADD as raw material in anti-pruritic products.

• Journal of the Korean Applied Science and Technology
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• v.29 no.3
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• pp.429-434
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• 2012

A kind of Antihistamines, Azelastine HCl which known as modern H1-blockers, was synthesized by four step process using phthalic anhydride, 4-chlorophenylacetic acid, hydrazine 2HCl. The first step was the reaction of removing carboxyl group and hydroxyl group and the second step was saponification of 3-(4-chlorobenzylidene)phthalide. The third step was the nucleophilic addition reactions of primary amines and the fourth step was addition reaction of N-methyl-1-aza-bicyclo[3,2,0]heptane to 4-(4-chlorobenzyl)-1-(2H)phthalazinone. As a result, product was analyzed by FT-IR and $^1H$-NMR and could be obtained with a yield of 80%.

• Korean Journal of Food Science and Technology
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• v.40 no.6
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• pp.702-706
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• 2008

Punica granatum (PG) evidences a variety of physiological properties, including anti-diabetic, anti-cancer, antiinflammatory, anti-microbial, and anti-oxidative activities. Using the human basophilic KU812F cells, the inhibitory effects of the methanolic extract of PG seed, shell, and juice on calcium ionophore, A23187-induced degranulation were assessed. All of the PG extracts inhibited A23187-induced intracellular $Ca^{2+}$ levels, ${\beta}$-hexosaminidase, and histamine release in a dose-dependent manner. These results showed that all of the PG extracts are potent inhibitors of degranulation in allergic reactions, via the suppression of $Ca^{2+}$ influx.

• Tuberculosis and Respiratory Diseases
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• v.43 no.3
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• pp.308-322
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• 1996

Background : Neutrophils are considered to play critical roles in the development of acute respiratory distress syndrome. Histamine, which is distributed abundantly in lung tissue, increases the rolling of neutrophills via increase of P-selectin expression on the surface of endothelial cells and is known to have some interrelationships with IL-1, IL-8 and TNF-$\alpha$. We studied to investigate the effect of the histamine on the acute lung injury of the rats induced by intratracheal insufflation of TNF-$\alpha$ which has less potency to cause lung injury compared to IL-1 in rats. Methods : We intratracheally instilled saline or TNF(R&D, 500ng), IL-1(R&D, 50ng)or histamine of varius dose(1.1, 11 and $55\;{\mu}g/kg$) with and without TNF separately in Sprague-Dawley rats weighing 270-370 grams. We also intratracheally treated IL-1(50ng) along with histamine($55\;{\mu}g/kg$). In cases, there were synergistic effects induced by histamine on the parameters of TNF-induced acute lung injury, antihistamines(Sigma, mepyramine as a $H_1$ receptor blockade and ranitidine as a $H_2$ receptor blockade, 10 mg/kg in each)were co-administered intravenously to the rats treated TNF along with histamine($1.1\;{\mu}g/kg$) intratraeheally. Then after 5 h we measured lung lavage neutrophil numbers, lavage cytokine-induced neutrophil chemoattractants(CINC), lung myeloperoxidase activity(MPO) and lung leak. We also intratracheally insufflated TNF with/without histamine($11\;{\mu}g/kg$), then after 24 h measured lung leak in rats. Statistical analyses were done by Kruskal-Wallis nonparametric ANOVA test with Dunn's multiple comparison test or by Mann-Whitney U test. Results : We found that rats given TNF, histamine alone(11 and $55\;{\mu}g/kg$), and TNF with histamine(l.1, 11, and $55\;{\mu}g/kg$) intratracheally had increased (p<0.05) lung MPO activity compared with saline-treated control rats. TNF with histamine $11\;{\mu}g/kg$ had increased MPO activity (P=0.0251) compared with TNF-treated rats. TNF and TNF with histamine(1.1, 11, and $55\;{\mu}g/kg$) intratracheally had all increased (p<0.05) lung leak, lavage neutophil numbers and lavage CINC activities compared with saline. TNF with histamine $1.1\;{\mu}g/kg$ had increased (p=0.0367) lavage neutrophil numbers compared with TNF treated rats. But there were no additive effect of histamine with TNF compared with TNF alone in acute lung leak on 5 h and 24 h in rats. Treatment of rats with the $H_1$ and $H_2$ antagonists resulted in inhibitions of lavage neutrophil accumulations and lavage CINC activity elevations elicited by co-treated histamine in TNF-induced acute lung injury intratracheally in rats. We also found that rats given IL-1 along with histamine intratracheally did not have increase in lung leak compared with IL-1 treated rats. Conclusion : Histamine administered intratracheally did not have synergistic effects on TNF-induced acute lung leak inspite of additive effects on increase in MPO activity and lavage neutrophil numbers in rats. These observations suggest that instilling histamine intratracheally would not play synergistic roles in neutrophil-mediated acute lung injury in rats.

• Journal of Life Science
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• v.19 no.12
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• pp.1808-1814
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• 2009

In our previous study, a new herbal preparation (HemoHIM) was developed as a functional food for the radioprotection and immunomodulatory agents. In order elucidate the mechanism involved, we examined the effect of HemoHIM on the compound 48/80-induced histamine release, and on the phorbol 12-myristate 13-acetate (PMA)/calcium ionophore (A23187)-induced inflammatory cytokine secretion in HMC-1. The cell culture supernatants were harvested, and the cytokines (IL-4, IL-6, IL-8, TNF-$\alpha$, GM-CSF) in the supernatants were measured by enzyme-linked immunosorbent assay. The total RNA of the cells was extracted, and the cytokines or c-kit/tryptase/Fc$\varepsilon$RI's messenger RNA expressions were examined using reverse transcriptase polymerase chain reaction. Under low concentrations, HemoHIM inhibited histamine release in HMC-1 stimulated compound 48/80. Furthermore HemoHIM inhibited PMA/A23187-induced inflammatory cytokines' secreation or mRNA expression in a dose-dependent manner. But IL-8 secretion was not inhibited by low concentrayion of HemoHIM, respectively. The mRNA expression of c-kit and Fc$\varepsilon$RI were also inhibited in a dose-dependent manner. Tryptase mRNA expression was only inhibited by low concentration of HemoHIM. These results indicated that HemoHIM might be an useful agent for protection against allergy as well as immune modulation, especially since it is a relatively nontoxic natural product.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.232-232
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• 1994

인삼이 면역계 질환의 일종인 과민성 반응에 대한 치료약으로서의 가능성을 연구하기 위해서 in viva와 in vitra실험을 수행하였다. in vitra실험으로서는 hyaluronidase의 활성을 지표로 삼았으며, in viva실험에서는 mouse이각, rat등피부, 복강 비만세포, 그리고 guinea pig의 ileum에서 면역반응에 대한 아답타겐의 작용을 관찰하였다. in uitra 실험에서는 hyaluronidase와 histamine 분비를 항알레르기 작용의 지표로 사용하였다. hyaluronidase의 경우 그 활성은 Cacl2로 활성화 시키기 전이나 후에 모두 아답타겐(100, 50, 및 10 mg/ml)에 의해서 현저하게 억제되었다. 한편 rat 복강 비만 세포에서의 histamine유리 시험에서는 아답타겐(0.5, 1, 5mg/ml)이 histamine유리가 증가되었다. Guinea pig의 ileum 평활근에서는 아답타겐이 평활근 자극 작용없이 항히스타민 효과률 나타내었다. in uiua 실험의 첫 단계로 우리는 혈관 투과성에 미치는 아답타겐의 효과를 mouse 이각과 rat 등피부에서 관찰하였다. Mouse이각에서의 실험에서는 hoistamine, serotonin, 그리고 LTC4로 challenge하여 관찰한 결과 histamine과 serotonin의 경우, 혈관투과성 항진은 아답타겐(50-400mg/m1)에 의해서 유의성있게 억제되었으나, rat 등 피부에서는 mouse에서와는 달리 48-hr PCA가 증가 되었고, histamine에 의한 혈관투과성 항진은 아답타겐에 의해 영향을 받지 않았다. 반면에 compound 48/80과 serotonin에 의한 혈관투과성 항진은 mouse 의 경우에서처럼 아답타겐에 의해 억제되었다.

• YAKHAK HOEJI
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• v.14 no.1_2
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• pp.28-35
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• 1970

The absorption of Aminopyrine from the small intestine of a rat in combination with antihistamic agent, Diphenhydramine, Pheniramine, Tripelennamine and Diphenhydramine respectively, was examined. Through the rat small intestine canal, a definite quantity of a sample solution comprising 0.5 mM of Aminopyrine and 0.1 mM of each antihistamic agent in phosphate buffer solution (pH=7.4) was perfused through the rat small intestine at rate 5 ml per minute. The samples of the circulating solution were taken out after 5 minutes of the perfusion to give initial concentration and every 30 minutes for 3 hours. The amount of residual Aminopyrine in the solution was determined photometrically at 720 m.mu. by using 0.4% potassium ferricyanate solution and 1% ferric nitrate in 0.1N nitric solution. The mixed compounds of Aminopyrine with antihistamic agent, such as Aminopyrine with Diphehydramine, Aminopyrine with Pheniramine, Aminopyrine with Tripelennamine and Aminopyrine with Chloropheniramine showed more increased absorption than Aminopyrine alone. the absorption rate constants and apparent permeability coefficients of the mixed compounds were shown in detail.