• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 2001년도 추계학술대회 및 정기총회
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• pp.82-82
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• 2001

Previously, several prenylated flavonoids having a C-8 lavandulyl moiety were found to inhibit cyclooxygenase-1 (COX-1) as well as 5-lipoxygenase (5-LOX), and sophoraflavanone G was the most potent inhibitor against these eicosanoid generating enzymes among the prenylated flavonoids tested. In this investigation, effects of sophoraflavanone G on COX-2 induction from RAW 264.7 cells and in vivo inflammatory response were studied. Sophoraflavanone G inhibited prostaglandin E$_2$(PGE$_2$) production from lipopolysaccharide (LPS)-treated RAW cells by COX-2 down-regulation without significantly affecting COX-2 activity at 1 50 $\mu$M. Other prenylated flavonoids including kuraridin and sanggenon D also down-regulated COX-2 induction at 10-25 $\mu$M, lirhile kurarinone and echinoisoflavanone did not. In addition, sophoraflavanone G shelved in vivo anti-inflammatory activity against mouse croton oil-induced ear edema and rat carrageenan paw edema via oral (2-250mg/kg) or topical administration (10 - 250 $\mu\textrm{g}$/ear). Although the potencies of inhibition were far less than that of a reference drug, prednisolone, this compound showed higher anti-inflammato교 activity when applied topically, suggesting a potential use for several eicosanoid-related skin inflammation such as atopic dermatitis.

• 한국수산과학회지
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• 제48권6호
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• pp.888-897
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• 2015

The anti-inflammatory effect of alginate oligosaccharides on LPS-induced RAW 264.7 cells was investigated at different time points (0-60 h). The alginate oligosaccharides were produced by an alginate-degrading enzyme from Shewanella oneidensis PKA1008. The alginate oligosaccharides decreased the production of nitric oxide and proinflammatory cytokines [tumor necrosis factor-${\alpha}$, interleukin (IL)-$1{\beta}$, and IL-6] in a dose-dependent manner. The alginate oligosaccharides showed peak anti-inflammatory activity after 36 h of incubation; at that time point, reduced protein expression of NF-${\kappa}B$ p65, iNOS, and COX-2 was detected. Furthermore, the alginate oligosaccharide treatment reduced the formation of ear edema at 36 h compared to samples examined at 0 h when the oligosaccharides were administered at 50 and 250 mg/kg body weight, as well as dermal thickness and mast cell numbers in a histological analysis. These results suggest that alginate oligosaccharides are a promising anti-inflammatory agent.

• Biomolecules & Therapeutics
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• 제20권1호
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• pp.113-117
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• 2012

The fruits of Foeniculum vulgare (Foeniculi Fructus) have been widely used in Chinese medicine as an antiemetic, ameliorating stomach ailments and as an analgesic. In order to establish its potential for antiallergic use, inhibitory actions of the fruit on 5-lipoxgenase (5-LOX) and ${\beta}$-hexosaminidase release were evaluated. The 70% ethanol extract of this plant material (FR) considerably inhibited 5-LOX-catalyzed leukotriene production from A23187-induced rat basophilic leukemia (RBL)-1 cells. The $IC_{50}$ was $3.2{\mu}g/ml$. From this extract, 12 major compounds including sabinene, fenchone, ${\gamma}$-terpinene, ${\alpha}$-pinene, limonene, p-anisylacetone, panisylaldehyde, estragole (4-allylanisole), trans-anethole, scopoletin, bergapten and umbelliferone were isolated. And it was found that several terpene derivatives including ${\gamma}$-terpinene and fenchone as well as phenylpropanoid, trans-anethole, showed considerable inhibitory action of 5-LOX. In particular, the $IC_{50}$ of trans-anethole was $51.6{\mu}M$. In contrast, FR and the isolated compounds did not show considerable inhibitory activity on the degranulation reaction of ${\beta}$-hexosaminidase release from antigen-treated RBL-2H3 cells. Against arachidonic acid-induced ear edema in mice, FR and trans-anethole showed significant inhibition by oral administration at doses of 100-400 mg/kg. In conclusion, FR and several major constituents are 5-LOX inhibitors and they may have potential for treating 5-LOX-related disorders.

• Archives of Pharmacal Research
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• 제28권7호
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• pp.848-853
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• 2005

Synurus deltoides was previously found to possess significant anti-inflammatory activity especially against chronic inflammation, and strong analgesic activity in vivo. In this study, new anti-inflammatory formulation containing S. deltoides extract as a major ingredient was prepared and in vivo activity was evaluated. The plausible action mechanism was also investigated. The new formulation (SAG) contains 1 part of S. deltoides extract, 0.9 part of Angelica gigas extract and 0.9 part of glucosamine sulfate (w/w). SAG inhibited dose-dependently edematic response of arachidonic acid (AA)- and 12-O-tetradecanoyl 13-acetate (TPA)-induced ear edema in mice, which is an animal model of acute inflammation. SAG showed 44.1 % inhibition of AA-induced ear edema at an oral dose of 50 mg/kg. In an animal model of chronic inflammation, SAG clearly reduced the edematic response of 7 -day model of multiple treatment of TPA (38.1 % inhibition at 200 mg/kg/day). Furthermore, SAG (50-800 mg/kg/day) as well as S. deltoides extract (285 mg/kg/day) significantly inhibited prostaglandin $E_2$ production from the skin lesion of the animals of 7-day model. These results were well correlated with in vitro finding that SAG as well as S. deltoides extract reduced cyclooxygenase (COX)-1- and COX-2-induced prostanoid production, measured in mouse bone marrow-derived mast cells. Therefore, these results suggest that SAG possesses anti-inflammatory activity in vivo against acute as well as chronic inflammatory animal models at least in part by inhibition of prostaglandin production through COX-1/COX-2 inhibition. And COX inhibition of SAG is possibly contributed by S. deltoides extract among the ingredients. Although the anti-inflammatory potencies of SAG were less than those of currently used anti-inflammatory drugs, this formulation may have beneficial effect on inflammatory disorders as a neutraceutical.

• 한방안이비인후피부과학회지
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• 제23권1호
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• pp.8-22
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• 2010

Objectives : The purpose of this study is to investigate the effects of Gyejijakyakjimo-Tang on the Allergic Contact Dermatitis caused by 2,4-dinitro-chlorobezene(DNCB). Methods : Twenty eight mice were divided into four groups ; normal, control, experimental group A and B. Control and experimental groups were induced allergic contact dermatitis by DNCB. Experimental group A was orally administered the Gyejijakyakjimo-Tang and experimental group B was orally administered the prednisolone. In this study, ear thickness measurement, auricle microphotograph observation, MPO(Myeloperoxidase) activity measurement, Reverse transcription-polymerase chain reaction(RT-PCR) analysis of the mRNA level of TNF-$\alpha$, IL-$1{\beta}$ were performed on these four groups. In addition, the effect of Gyejijakyakjimo-Tang on cell viability and the effect of Gyejijakyakjimo-Tang on the compound 48/80-induced histamine release from HMC and RPMC were measured. Results: 1. Both experimental group A and B had decreased ear thickness compared with control group In contact hypersensitivity assay. 2. In experimental group A, inflammatory edema was similarly observed comparing to control group. Nevertheless, inflammatory edema was obviously reduced in experimental group B. In both experimental group A and B, pathological lesion of dermatitis were alleviated. In addition, the numbers of infiltrated inflammatory cells were decreased compared with control group. 3. Compared to the normal group, there was a noticeable increase in MPO activity in control group. However, in experimental group A and B, it showed remarkable inhibition of the increase in MPO activity comparing with control group. 4. The level of expression of TNF-$\alpha$, IL-$1{\beta}$ in experimental group A and B were meaningfully lower than those in control group. 5. In MTT assay, the concentrations of Gyejijakyakjimo-Tang that were used on the test had no cytotoxicity. 6. Gyejijakyakjimo-Tang dose-dependently inhibited the compound 48/80-induced histamine release from both HMC and RPMC. Conclusions : According to above experiments, Gyejijakyakjimo-Tang was effective on allergic contact dermatitis.

• 한국식품영양과학회지
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• 제46권5호
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• pp.537-544
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• 2017

본 연구에서는 참까막살 에탄올 추출물(PAEE)의 항염증 활성을 확인하기 위하여 LPS로 자극된 RAW 264.7 세포에서의 pro-inflammatory cytokine 및 NO의 분비 생성량과 western blot으로 단백질 발현량을 측정하였다. 또한, croton oil로 유도된 귀 부종 모델을 이용하여 알아보았다. RAW 264.7 세포에서 PAEE를 $0.1{\sim}100{\mu}g/mL$ 농도로 처리 시 세포독성을 나타내지 않음을 확인하였다. 그 결과 PAEE는 pro-inflammatory cytokine(IL-6, $TNF-{\alpha}$, $IL-1{\beta}$) 및 NO의 분비량을 농도 의존적으로 억제시켰으며, iNOS와 COX-2의 발현량도 감소시킴을 확인하였다. 이러한 항염증 활성결과는 $NF-{\kappa}B$와 MAPKs 전사인자의 활성 억제에 의한 것으로 확인되었다. 또한, croton oil로 유도된 귀 부종 모델에서 PAEE를 50 mg/kg body weight 처리 시 귀 부종이 prednisolone(10 mg/kg body weight)과 유사한 정도로 억제됨을 확인하였다. 귀 조직 관찰에서도 PAEE는 croton oil에 의해 증가한 진피와 경피의 두께를 감소시켰으며, 진피로 침윤된 mast cell의 수도 감소시켰다. 이 결과를 종합해 보면 참까막살 에탄올 추출물은 $NF-{\kappa}B$와 MAPKs의 활성화 억제를 통해 염증 매개 물질의 생성을 억제시켜 항염증 활성을 나타내는 것으로 확인되었다.

• 한방안이비인후피부과학회지
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• 제30권3호
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• pp.46-61
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• 2017

Objectives : Allergic contact dermatitis(ACD) is a type IV delayed hypersensitivity reaction that results from cumulative exposures and subsequent sensitization to an environmental chemical. Lonicerae Caulis(LC) can clear away heat and relieve toxin, disperse wind and heat, dredge the channel. The present study was designed to investigate the effects of LC on allergic contact dermatitis(ACD) induced by 2,4-dinitrochlorobenzene(DNCB) in mice. Methods : In this experiment, the effects of LC on changes in body weights, ear and dorsum skin thicknesses, ear weights, clinical aspects on the dorsum skin, histopathological changes, spleen/body ratio, cytokines were investigated. In addition, the effects on proliferations of splenocytes were also investigated in vitro and vivo study. Results : LC spread(SPR) group and LC spread and administered(SPR+ADM) group showed diminished ear thicknesses. In SPR+ADM group, ear weights were lowered significantly compared to contact dermatitis control(CTL) group. LC treatment diminished erythema, desquamation and keratosis which were induced by repeated painting of DNCB. In histopathological observation, spongiosis and edema were diminished in SPR and SPR+ADM group. In cytokines, SPR+ADM group were increased in IL-10, and SPR and SPR+ADM group were decreased in TNF-${\alpha}$ compared with control group. Conclusions : These data suggest that LC can decrease symptoms of ACD, then LC is useful to treat patient with ACD.

• 한방안이비인후피부과학회지
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• 제30권1호
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• pp.87-105
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• 2017

Objectives : Atopic Dermatitis (AD) is chronic skin disease characterized by allergic hypersensitivity reactions. Saeng-ryo-Samul-tang (SRSM) can treat skin disease by cooling down blood heat, cealering away congenital fever and detoxicating. This study was conducted to investigate the effects of SRSM on AD induced by 2,4-dinitrochlorobenzene (DNCB) in mice Methods : In this study, the effects of SRSM on changes in body weights, thicknesses of dorsum skin, thicknesses and weights of ear, changes of symptoms on the dorsum skin, histopathological degree of ear and dorsum skin, IL-10 and $TNF-{\alpha}$ in serum were observed. And the effects on the proliferation rates of splenocytes were also investigated in vivo and in vitro study. Results : In SRSM topical application (Topical) group, SRSM oral application (Oral) group and SRSM Combination (Combi) group thickness of dorsum skin decreased significantly. But in TPC, ORL and CBN group, weight of ear didn't show any changes, but thickness of ear decreased significantly. And TPC, ORL and CBN group showed meaningful effectiveness symptoms like desquamation and erythema on AD's clinical espect. In histopathological observation, spongiosis, edema and inflammatory cell infiltration of epidermal were remarkably diminished in TPC, ORL and CBN group. And SRSM diminished the proliferation rates of splenocytes in vivo and vitro study. Conclusions : The present study suggests that SRSM can significantly reduced symptoms of AD, therefore SRSM is effective to treatment of AD.

• 한국수산과학회지
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• 제42권5호
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• pp.468-475
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• 2009

This study was conducted to examine the bleaching of an anti-inflammatory agent containing Undaria pinnatifida extract (AIAU). Brown-colored AIAU was irradiated with $^{60}CO$ gamma rays at doses ranging from 10-200 kGy. Discoloring of the anti-inflammatory agent was achieved by gamma irradiation, with significantly removal by 50 kGy irradiation. The main active compound of the agent consisted of 4% U. pinnatifida extract, which inhibited inflammatory symptoms in mouse ear edema by 93%. There was no change in effects against edema, erythema, blood flow and radical scavenging activity by irradiation.

• Archives of Pharmacal Research
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• 제21권4호
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• pp.406-410
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• 1998

Biflavonoid is one of unique classes of naturally-occurring bioflavonoids. Certain biflavonoids including amentoflavone were previously reported to have inhibitory effect on the group 11 phospholipase $A_2$ activity. Amentoflavone was also found to inhibit cyclooxygenase from guinea-pig epidermis without affecting lipoxygenase. In this study, anti-inflammatory and analgesic activities of amentoflavone were evaluated. When amentoflavone was administered intraperitoneally, it showed a potent anti-inflammatory activity as determined by amelioration of croton-oil induced mouse ear edema. It also showed a potent anti-inflammatory activity in the rat carrageenan paw edema model ($ED_{50}$=42 mg/kg) compared to the activity of prednisolone (35 mg/kg) and indomethacin (10 mg/kg). However, amentoflavone did not show a significant inhibitory activity against rat adjuvant-induced arthritis, a chronic inflammatory model. In addition, amentoflavone was found to possess a potent analgesic activity in the acetic acid writhing test ($ED_{50}$=9.6 mg/kg) compared to the activity of indomethacin (3.8 mg/kg). These results suggest that amentoflavone may be a potential lead for a new type of anti-inflammatory agents having dual inhibitory activity of group 11 phospholipase $A_2$ and cyclooxygenase.