• YAKHAK HOEJI
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• v.55 no.4
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• pp.295-300
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• 2011

We investigated the effects of butanol fraction of Asterias amurensis (BFA) on the anti-allergic activity. BFA inhibited both cyclooxygenase-2 dependent prostaglandin $D_2$ and 5-lipoxygenase dependent leukotriene $C_4$ generation in a concentration-dependent manner with $IC_{50}$ values of 174.6 and 22.2 ${\mu}g$/ml, respectively. In addition, BFA also inhibited the degranulation in a dose dependent manner. Furthermore, oral administration of BFA inhibited IgE-mediated passive cutaneous anaphylaxis in mice. These results suggested that BFA may be useful in regulating mast cell-mediated allergic diseases.

• Journal of Microbiology and Biotechnology
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• v.11 no.1
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• pp.138-142
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• 2001

During the course of searching for anti-allergic substances from unexplored plant sources, an inhibitor of leukotriene $D_4$-induced tracheal contraction was isolated from Euphoribia helioscopia. This isolated polyphenol compound, known as helioscopinin-A, showed a certain inhibitory activity on capillary permeability in passive cutaneous anaphylaxis responses of rats and also on antigen-induced bronchial constriction in an experimental asthma model of guinea pigs. The compound at a high concentration weakly inhibited histamine release from isolated mast cells of rats. It is suggested that this compound is an anti-allergic and anti-asthmatic which exerts its activity through antagonism on leukotrene $D_4$-induced responses. A partial inhibition of allergic mediator relase may also bee involved.

• Natural Product Sciences
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• v.17 no.2
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• pp.90-94
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• 2011

An in vitro bioassay-guide revealed that the methanol (MeOH) extract of the whole plant of Patrinia saniculaefolia (Valerianaceae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin $D_2$ ($PGD_2$) and leukotriene $C_4$ ($LTC_4$) in mouse bone marrow-derived mast cells (BMMCs). Phytochemical study of the MeOH extract of this plant led to the isolation of twelve compounds; ${\beta}$-farnesene (1), squalene (2), nardostachin (3), patridoid I (4), patridoid II (5), patridoid II-A (6), oleanolic acid (7), oleanonic acid (8), 23-hydroxyursolic acid (9), oleanolic acid 3-O-${\alpha}$-L-arabinopyranoside (10), oleanolic acid 3-O-${\beta}$-D-glucopyranoside (11), oleanolic acid 3-O-[${\beta}$-D-xylopyranosyl-(1${\rightarrow}$3)-${\beta}$-D-(6-O-butyl)glucuronopyranoside] (12). Among the compounds, 4 and 5 strongly inhibited both the COX-2-dependent $PGD_2$ generation with $IC_{50}$ values of 8.7 and 13.6 ${\mu}M$, respectively, and the generation of $LTC_4$ in the 5-LOX dependent phase with $IC_{50}$ values of 41.7 and 46.9 ${\mu}M$, respectively, which suggest that the anti-inflammatory activity of P. saniculaefolia might occur in part via the inhibition of both $PGD_2$ and $LTC_4$ generation by 4 and 5.

• Biomolecules & Therapeutics
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• v.17 no.1
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• pp.86-91
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• 2009

In our ongoing search for biological components from the Korea endemic plants, the MeOH extract of Ailanthus altissima leaves (Simaroubaceae) showed cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin $D_2$ ($PGD_2$) and leukotriene $C_4$ ($LTC_4$) in mouse bone marrow-derived mast cells (BMMCs). In further study, eight compounds, squalene (1), ${\beta}$-sitosterol (2), scopoletin (3), quercetin (4), luteolin (5), astragalin (6), scopolin (7), and daucosterol (8) were isolated, the chemical structures were elucidated on the basis of physicochemical and spectroscopic data and by comparison with those of published literatures. Among the compounds, 2, 4, and 5 strongly inhibited both the COX-2-dependent PGD2 generation with $IC_{50}$ values of 2.6, 7.3 and 2.5 ${\mu}M$, respectively and the generation of $LTC_4$ in the 5-LOX dependent phase with $IC_{50}$ values of 2.0, 5.1 and 1.8 ${\mu}M$, respectively, which suggest that the anti-inflammatory activity of A. altissima might occur in part via the inhibition of both $PGD_2$ and $LTC_4$ generation by 2, 4 and 5.

• Archives of Pharmacal Research
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• v.29 no.8
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• pp.617-623
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• 2006

In our ongoing search for bioactive compounds originating from the endemic species in Korea, we found that the hexane and EtOAc fractions of the MeOH extract from the root of Dystaenia takeshimana (Nakai) Kitagawa (Umbelliferae) showed cyclooxygenase-2 (COX-2) and 5- lipoxygenase (5-LOX) dual inhibitory activity by assessing their effects on the production of prostaglandin $D_2\;(PGD_2)$ and leukotriene $C_4\;(LTC_4)$ in mouse bone marrow-derived mast cells. By activity-guided fractionation, five coumarins, viz. psoralen (2), xanthotoxin (3), scopoletin (4), umbelliferone (5), and (+)-marmesin (6), together with ${\beta}-sitosterol$ (1), were isolated from the hexane fraction, and two phenethyl alcohol derivatives, viz. 2-methoxy-2-(4'-hydroxyphenyl)ethanol (7) and 2-hydroxy-2-(4'-hydroxyphenyl)ethanol (8), three flavonoids, viz. apigenin (9), luteolin (10), and cynaroside (11), as well as daucosterol (12) were isolated from the EtOAc fraction using silica gel column chromatography. In addition, D-mannitol (13) was isolated from the BuOH fraction by recrystallization. Two of the coumarins, scopoletin (4) and (+)- marmesin (6), the two phenethyl alcohol derivatives (7, 8) and the three flavonoids (9-11) were isolated for the first time from this plant. Among the compounds isolated from this plant, the five coumarins as well as the three flavonoids showed COX-2/5-LOX dual inhibitory activity. These results suggest that the anti-inflammatory activity of D. takeshimana might in part occur via the inhibition of the generation of eicosanoids.

• Korean Journal of Pharmacognosy
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• v.30 no.4
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• pp.377-383
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• 1999

The anti-asthmatic activities of the extract of Lonicera japonica (BuOH fraction) and its mode of action were investigated using several in vitro and in vivo models. Lonicera japonica was extracted with 30% ethanol (v/v) and successively partitioned into BuOH. The BuOH fraction reduced antigen-induced contraction of isolated trachea from sensitized guinea pigs in a concentration-dependent manner. The BuOH fraction also inhibited histamine release from rat peritoneal mast cells induced by antigen or calcium ionophore A23187 ($IC_{50}=0.26$ and 0.32mg/ml, respectively). Eosinophil infiltration into bronchoalveolar lavage fluids induced by aeroallergen challenge in passively sensitized guinea pigs was inhibited by the BuOH fraction at a dose of 800mg/kg (51.7%). In addition, the BuOH fraction inhibited leukotriene $B_4$ prodution in rat basophilic leukemia cells ($IC_{50}=0.42\;mg/ml$) as well as phosphodiesterase 4 (PDE4) isolated from rat brain ($IC_{50}=0.015\;mg/ml$). All results from this study strongly suggest that the BuOH fraction of Lonicera japonica may be useful in the treatment of asthma and its mode of action may be related with inhibition of both 5-lipoxygenase and PDE4 enzyme.

• Journal of Physiology & Pathology in Korean Medicine
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• v.25 no.3
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• pp.438-444
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• 2011

Dojuk-San is known to be effective for treating a urinary diseases and stomatitis. However, its effects on the bone marrow-derived mast cell(BMMC) mediated allergy and inflammation mechanism remain unknown. In this study, the biological effects of Dojuk-San ethanol extract(DJS) were evaluated while focusing on its effects on the allergic mediator in phorbol 12-myristate 13-acetate(PMA) plus calcium ionophore A23187(A23187)-stimulated BMMCs. An investigation was also conducted to determine its effects on the production of several allergic mediators including interleukin-6(IL-6), prostaglandin D2($PGD_2$), leukotrieneC4(LTC4) and ${\beta}$-Hexosaminidase(${\beta}$-Hex). The results revealed that DJS inhibited the PMA plus A23187 induced production of IL-6, PGD2, LTC4 and ${\beta}$-Hex. Taken together, these findings indicate that DJS has the potential using in the treatment of allergy.

• Tuberculosis and Respiratory Diseases
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• v.46 no.5
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• pp.697-708
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• 1999

Background : Leukotriene (LT) $C_4$, $D_4$, and $E_4$, the main components of slow-reacting substance of anaphylaxis (SRS-A), have been suggested to play an important role in bronchial asthma such as antigen-induced bronchoconstriction, airway hyperreactivity, and pulmonary eosinophil accumulation. The purpose of this study was to evaluate the effects of treatment with the cysteinyl-LTs (cys-LTs) antagonist, pranlukast on allergen-induced guinea pig asthma model. Methods : Guinea pigs of treatment and placebo groups were sensitized by subcutaneous injection of ovalbumin(OVA) and challenged by inhalation of aerosolized OVA (1% weight/volume OVA). Normal control group did not sensitize with OVA. Oral ingestion of pranlukast and normal saline to the treatment and placebo groups was performed. In the treatment and placebo groups, airway resistance was measured before and after oral ingestion. Serum $LTC_4$ and eosinophilic infiltration of the bronchiolar and peribronchiolar tissues were measured after ingestion in the treatment and placebo groups. Results : Allergen-induced airway constriction developed in 20 (8 in treatment group, 12 in placebo group) among 35 guinea pigs. Airway resistance was significantly decreased at 3 and 6 minutes after OVA challenge in the pranlukast treatment group. In the placebo group, there was no difference of airway resistance between before and after saline ingestion. Serum $LTC_4$ levels showed 348.4 pg/ml in the treatment group, 373.9 pg/ml in the placebo group, and 364.4 pg/ml in the control group. There were no statistically significant difference between treatment and placebo group (p=0.232), and treatment and control group (p=0.501). Eosinophilic infiltrations in the peribronchiolar region per one-microscopic field ($\times$400 high power fields) demonstrated 7.06 in the treatment group, 19.2 in the placebo group, and 4.50 in the control group. There was significant decrement of eosinophilic infiltration in the treatment group which was compared with placebo group (p=0.001). Conclusion : These results demonstrate that pranlukast, a cys-LTs receptor antagonist, can attenuate allergen induced early-phase bronchoconstriction and eosinophilic infiltration in the bronchiolar tissues.

• Biomolecules & Therapeutics
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• v.22 no.3
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• pp.193-199
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• 2014

The aim of this study was to determine whether britanin, isolated from the flowers of Inula japonica (Inulae Flos), modulates the generation of allergic inflammatory mediators in activated mast cells. To understand the biological activity of britanin, the authors investigated its effects on the generation of prostaglandin $D_2$ ($PGD_2$), leukotriene $C_4$ ($LTC_4$), and degranulation in IgE/Ag-induced bone marrow-derived mast cells (BMMCs). Britanin dose dependently inhibited degranulation and the generations of $PGD_2$ and $LTC_4$ in BMMCs. Biochemical analyses of IgE/Ag-mediated signaling pathways demonstrated that britanin suppressed the phosphorylation of Syk kinase and multiple downstream signaling processes, including phospholipase $C{\gamma}1$ ($PLC{\gamma}1$)-mediated calcium influx, the activation of mitogen-activated protein kinases (MAPKs; extracellular signal-regulated kinase 1/2, c-Jun $NH_2$-terminal kinase and p38), and the nuclear factor-${\kappa}B$ ($NF-{\kappa}B$) pathway. Taken together, the findings of this study suggest britanin suppresses degranulation and eicosanoid generation by inhibiting the Syk-dependent pathway and britanin might be useful for the treatment of allergic inflammatory diseases.

• Archives of Pharmacal Research
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• v.29 no.4
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• pp.282-286
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• 2006

Ochnaflavone is a medicinal herbal product isolated from Lonicera japonica that inhibits cyclooxygenase-2 (COX-2) dependent phases of prostaglandin $D_2(PGD_2)$ generation in bone marrow-derived mast cells (BMMC) in a concentration-dependent manner with $IC_{50}$ values of $0.6{\mu}M$. Western blotting probed with specific anti-COX-2 antibodies showed that the decrease in quantity of the $PGD_2$ product was accompanied by a decrease in the COX-2 protein level. In addition, this compound consistently inhibited the production of leukotriene $C_4 (LTC_4)$ in a dose dependent manner, with an $IC_{50}$ value of $6.56 {\mu}M$. These results demonstrate that ochnaflavone has a dual cyclooxygenase-2/5-lipoxygenase inhibitory activity. Furthermore, this compound strongly inhibited degranulation reaction in a dose dependent manner, with an $IC_{50}$ value of $3.01{\mu}M$. Therefore, this compound might provide a basis for novel anti-inflammatory drugs.