• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.22 no.2
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• pp.1-18
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• 2009

Objective : Moutan Cortex (the root bark of Paeonia suffruticosa Andr.) is widely used in oriental medicine as a remedy for inflammation. However, as yet there is no clear explanation of how MC(Moutan Cortex) affects the production of inflammatory cytokine. This study was to determine the effects of Essence extracted MC on the mast cell-mediated inflammatory responses. Method : We observed the effect of MC on compound 48/80-induced histamine release of rat peritoneal mast cells and the effect of administering MC on PCA in rat. We measured the amount of inflammatory cytokine production induced by the phorbol myristate acetate (PMA) plus calcium ionophore(A23187) in the human mast cell line (HMC-1) incubated with various concentrations of MC. The TNF-$\alpha$ protein levels were analysised by Western blot. The TNF-$\alpha$, IL-6 and IL-8 secreted protein levels were measured by the ELISA assay. The TNF-$\alpha$, IL-6 and IL-8 mRNA levels were measured by the RT-PCR analysis. NF-$\kappa$B, phospho-I$\kappa$B and MAPKs were exmined by Western blot analysis. The NF-$\kappa$B promoter activity was examined by luciferase assay. Result : 1. Enzyme immunoassay indicated that MC suppressed histamine secretion of rat peritoneal mast cells. 2. In PCA dependent on IgE, MC had anti-allergic effect of the internal surface of rat skin. 3. Western blot indicated that MC decreased TNF-$\alpha$ protein levels. 4. ELISA indicated that MC decreased TNF-$\alpha$, IL-6 but MC had no significant effect on IL-8 in HMC-1 cells. 5. RT-PCR indicated that MC decreased TNF-$\alpha$, IL-8 but MC had no significant effect on IL-6 in HMC-l cells. 6. Western blot indicated that MC suppressed the induction of MAPKs, NF-$\kappa$B & phospho-I$\kappa$B activity in HMC-1 cells. 7. Luciferase assay indicated that MC suppressed the PMA plus A23187-induced NF-$\kappa$B promoting activityin HMC-1 cells. Conclusion : In this study, we have found that MC is an inhibitor of NF-$\kappa$B, MAPKs & cytokines on the mast cell-mediated inflammatory responses.

• Journal of Pharmaceutical Investigation
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• v.31 no.1
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• pp.57-62
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• 2001

Azelastine, a phthalazinone derivative, is an antiallergic agent which demonstrates histamine $H_1-receptor$ antagonist activity and also inhibits histamine release from mast cells following antigen and non-antigen stimuli. Thus, azelastine may be useful in the management of both asthma and allergic disorders. The purpose of the present study was to evaluate the bioequivalence of two azelastine hydrochloride tablets, $Azeptin^{TM}$ (Bu Kwang Pharmaceutical Co., Ltd.) and $Azela^{TM}$ (Kyung Dong Pharmaceutical Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Eighteen normal male volunteers, $22.44{\pm}2.01$ years in age and $61.99{\pm}6.18\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After two tablets containing 1 mg of azelastine hydrochloride per tablet were orally administered, blood was taken at predetermined time intervals and the concentrations of azelastine in serum were determined using HPLC with fluorescence detector. Pharmacokinetic parameters such as $AUC_t$, $C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters. The results showed that the differences in $AUC_t$, $C_{max}\;and\;T_{max}$ between two tablets were -6.45%, -2.60% and -7.14%, respectively, when calculated against the $Azeptin^{TM}$ tablet. The powers $(1-{\beta})$ for $AUC_t\;and\;C_{max}$ were 96.65% and 88.47%, respectively. Minimum detectable differences $({\Delta})$ at ${\alpha}=0.05$ and $1-{\beta}=0.8$ were less than 20% (e.g., 14.40% and 17.65% for $AUC_t\;and\;C_{max}$, respectively). The 90% confidence intervals were within ${\pm}20%$ (e.g., $-14.87{\sim}1.97$ and $-12.92{\sim}7.72$ for $AUC_t\;and\;C_{max}$, respectively). Two parameters met the criteria of KFDA for bioequivalence, indicating that $Azela^{TM]$ tablet is bioequivalent to $Azeptin^{TM}$ tablet.

• Journal of the Korean Society of Food Science and Nutrition
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• v.36 no.2
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• pp.155-162
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• 2007

The purpose of this study is to investigate the anti type I allergic effects and mechanisms of the phyto extract mixture (PEM381) which contains Camellia sinensis (leaf), Psidium guajava (leaf), and Rosa hybrida (flower). PEM381 was tested for its inhibitory effects on arachidonic acid cascade related enzymes (5-lipoxygenase and cyclooxygenase), the mast cell mediated allergic reaction and passive cutaneous anaphylaxis. $IC_{50}$ value of PEM381 against 5-lipoxygenase was $14.11{\pm}0.51ppm$ while that of positive control (nordihy-droguaiaretic acid) was $0.54{\pm}0.08ppm$. PEM381 also exhibited considerable selective inhibition of cyclooxygenase-2. PEM381 could inhibit both degranulation and histamine release in a dose dependent manner from rat peritoneal mast cells activated by compound 48/80. In addition, oral administration of PEM381 showed an inhibitory effect on passive cutaneous anaphylaxis reaction activated by anti-dinitrophenyl IgE antibody in mice. These results suggest that PEM381 may be useful for the prevention and treatment of type Ⅰ allergy related diseases.

• Journal of Life Science
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• v.21 no.3
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• pp.393-399
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• 2011

The mast cell is one of the major effector cells in inflammatory reactions and can be found in most tissues throughout the body. Activated mast cells can produce histamine, as well as a wide variety of other inflammatory mediators such as eicosanoids, proteoglycans, proteases, and several pro-inflammatory cytokines, such as tumor necrosis factor (TNF)-${\alpha}$, and interleukins (IL-6), IL-8, IL-4, IL-13. In the present study, we isolated two bacterial strains (J80 and G147) from fermented soybean and Jeotgal, and investigated the inhibitory effects of their extracts which were prepared by several pretreatment methods (sonication for 20 min, heating at $100^{\circ}C$ for 30 min, autoclaving at $121^{\circ}C$ for 15 min) on the mast cell-mediated inflammatory response. The pretreated bacterial extracts had no cytotoxicity against Human Mast Cell (HMC-1). Among various pretreatments, the extracts treated at $100^{\circ}C$ showed highest inhibition of histamine release (J80, 28.46%; G147, 41.14%). The J80 and G147 extracts treated at $100^{\circ}C$ resulted in the inhibition of IL-6 secretion by 38.46% and 56.45%, respectively. The J80 extract treated at $100^{\circ}C$ resulted in the inhibition of TNF-${\alpha}$ secretion by 66.67%, but G147 extract showed the highest inhibition effect by 41.1% when treated with sonication. These results suggest that bacterial extracts treated at $100^{\circ}C$ have a higher level of anti-inflammatory effects than other treatments such as sonication or autoclaving.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.14 no.1
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• pp.117-128
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• 2001

Gamiseunggal-tang(G-tang) has long been used for the treatment of acute and chronic allergic diseases(especially, urticaria) in oriental medicine. But, It's mechanism of action is not well investigated. Anal therapy is another way of taking medicine, which is not used in common situation but available for the treatment of colon and anal diseases. It is also used in GI tract diseases, Gynecological diseases, and pediatric diseases and so on. It is especially benefitable for patients who are in such situations as coma, severe vomiting, and swallowing difficulty. In this study, the author investigated the effects of G-tang by anal therapy on acute and chronic allergic reactions in murine model. The results obtained are as follows: 1. G-tang(0.01, 0.1 g/kg) inhibited the compound 48/80-induced ear swelling response in mice. Inhibitory effects of G-tang was significant (P<0.05) at the dose of 0.01 g/kg. 2. G-tang(0.001-0.1 g/kg) inhibited the cutaneous allergic reaction activated by anti-dinitrophenyl(DNP) IgE in rats. Especially, G-tang 0.01, 0.1 g/kg inhibited the cutaneous allergic reaction significantly. 3. G-tang(0.01-1 g/L) dose-dependently inhibited the compound 48/80-induced histamine release from the peritoneal mast cells. 4. G-tang(0.001-0.1 g/L) had a inhibitory effect on anti-DNP IgE-induced tumor necrosis factor-${\alpha}$ production. Above results indicate that anal therapy of G-tang may be beneficial in the treatment of acute and chronic allergic diseases.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1994.04a
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• pp.176-176
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• 1994

Moraceae comprise a large family of sixty genera and neary 1,400 specieses, including important groups such as Artocarpus, Morus, and Ficus. In particular, Morus(mulberry) is a small genus of tree and shrubs found in temperate and subtropical regions of the Northern hemishere and has been widely cultivated in China and Korea, In addition, the root bark of mulberry tree have been used as an antiphlogic, diuretic, and expectorant in white medicine, and the crude drug is known as "Sangbaikpi" in Korea. Recently, some papers have been published reporting the hypotensive effect, antiviral effect, antifungal effect, inhibitory effect of cAMP-phosphodiesterase, and anticancer effect of this extract. Little is known about that Cortex mori could have been an antiallergic effect. The purpose of this study was the development of an antiallergic agent with an antiallergic effect from Cortex mori. For this, several in vivo and in vitro experimental models were used. Results are 1) Cortex mori inhibited the compound 48/80-induced degranu-lation, histamine release and calcium uptake of rat peritoneal mast cells, 2) compound 48/80-induced anaphylactic shock and cutaneous reaction were significantly inhibited by pretreatment of Cortex mori, and 3) Cortex mori inhibited the ovalbumin-induced late astmatic reaction. From the above results it is suggested that Cortex mori has some substances with an antiallergic activity. Our final purpose of this study is to develope the new drug with an antiallergic activity from Cortex mori

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.252-252
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• 1996

We Investigated the peripheral excitatory effect of capsaicin and KR-25018, a newly synthesized capsaicin derivative which was demonstrated to have a potent analgesic activity. KR-25018 and capsaicin were found to be both potent efficacious contractors of isolated guinea pig bronchial smooth muscle. KR-25018 was equipotent with capsaicin and [Sar$\^$9/,Met(O$_2$)$\^$11/]-substance P, 10-fold more potent than histamine and 10-fold less potent than (${\beta}$ -Ala$\^$8/)-neurokinin A(4-10), and their -log(M)EC$\_$50/ values were 6.94${\pm}$0.08, 6.86${\pm}$0.05, 6.96${\pm}$0.07, 5.64${\pm}$0.04, 7.96${\pm}$0.02, respectively. Contractile responses to KR-25018 and capsaicin were potentiated by phosphoramidon (1 ${\mu}$M), an inhibitor of neuropeptide-inactivating endopeptidase, but completely abolished in a calcium-free medium. These responses to KR-25018 and capsaicin were unaffected by the NK-1 antagonist CP96345 (1${\mu}$M), partially inhibited by the NK-2 antagonist SR48968 (1 ${\mu}$M) but almost completely abolished by a combination of the antagonists. A vanilloid receptor antagonist capsazepine competitively antagonized the responses to both KR-25018 and capsaicin (pA$_2$: aganst KR-25018, 5.98${\pm}$0.47; against capsaicin, 5.80${\pm}$0.31), and a capsaicin-sensitive cation channel antagonist ruthenium red caused significant reduction in the maximum responses to KR-25018 and capsaicin (pD'$_2$: against KR-25018, 4.61${\pm}$0.33; against capsaicin 4.96${\pm}$0.21). In conclusion, the present results suggest that KR-25018 and cpasaicin act on the same vanilloid receptor inducing the influx of calcium through ruthenium red-sensitive cation channel and produce contractile responses via the release of tachykinins that act on both NK-1 and NK-2 receptor subtypes.

• Herbal Formula Science
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• v.25 no.2
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• pp.167-177
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• 2017

Objectives : This study aimed to evaluate inhibitory effects of GHJ on allergic inflammatory response in human mast cells (HMC-1). Methods : To investigate the inhibitory effect of GHJ (62.5, 125, 250, 500, $1000{\mu}g/mL$), HMC-1 cells were stimulated with phorbol 12-myristate 13-acetate plus calcium ionophore A23187 (PMACI). Enzyme-linked immunosorbent assays (ELISAs), RT-PCR and Western blot analysis were investigated using GHJ extract. Results : GHJ inhibited levels of $TNF-{\alpha}$ and IL-6 of $1000{\mu}g/mL$ concentration in ELISA and mRNA expression. GHJ had inhibitory effects in level of MAPKs, $p-I{\kappa}B-{\alpha}$ and p-NF-kB also. GHJ attenuated Compound 48/80-stimulated histamine release. In addition, GHJ inhibited PCA reaction in vivo. Conclusion : This study indicated that GHJ extract can inhibit allergic responses in HMC-1 cell.

• Korean Journal of Pharmacognosy
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• v.40 no.3
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• pp.218-223
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• 2009

The roots of Rumecis Radix have been used for the treatment of heat phlegm, jaundice, constipation, scabies and uterine hemorrhage. The aim of this study was to confirm whether Rumecis Radix water extract (RJWE) has a preventive effect on the development of atopic dermatitis (AD) in 2,4-dinitrochlorobenzene (DNCB)-applied BALB/c mice. Oral administration (12.5 mg/kg, 25 mg/kg) and topical application (0.5 mg/mouse, 1.0 mg/mouse) of RJWE decreased the development of AD-like skin lesions, ear swelling, spleen weight and total serum IgE. RJWE significantly also inhibited the infiltration of mast cells in the dorsal skin. Furthermore, the release of histamine from rat peritoneal mast cells (RPMCs) was suppressed significantly. These results suggest that the inhibitory effect of RJWE on AD might be associated with mast cells.

• YAKHAK HOEJI
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• v.36 no.1
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• pp.17-25
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• 1992

The general and some other pharmacological actions of growth hormone without N-terminal methionine(rhGH) were investigated in animals. The hormone had no influences on the central nervous system and on body temperature at a high oral dose of 40 IU/kg in animals. It had neither analgesic nor antiepileptic actions at the high doses. In the isolated ileum and trachea of guinea-pig and isolated stomach fundus and uterus of rat, it showed neither contractive nor relaxing effects at a concentration of $1{\times}10^{-3}\;IU/ml$ in bath, and no inhibitory action at a dose of $1{\times}10^{-3}\;IU/ml$ against the contractions produced by histamine ($5{\times}10^{-5}\;g/ml$), serotonin($1{\times}10^{-5}\;g/ml$), acetylcholine($1{\times}10^{-5}\;g/ml$) and oxytocin($5{\times}10^{-3}\;IU/ml$). Furthermore, the intravenous injection of 20 IU/kg rhGH had no influences on the normal blood pressure and respiration in rabbits. These negative results in pharmacological profile are thought that the hormone may not elicit serious side effects. On the other hand, the rhGH exhibited a weak inhibitory action of glucose tolerance in normal rats, significantly lowered the blood glucose contents in adrenalectomized rats 20 min after i.v. administration of 80 IU/kg, and showed a significant inhibitory effect on in vitro glycerol release in epinephrine-stimulated epididymal fat pad segments of rats.