• 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.

• 한국가금학회:학술대회논문집
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• 한국가금학회 2003년도 제20차 정기총회 및 학술발표회
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• pp.82-83
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• 2003

크릴밀 사료가 육계병아리의 생산성을 감소시키는 경향을 완화하기 위하여 항산화작용이 있은 콩추출물이 함유된 크릴밀을 급여하여 육계병아리의 생산성을 조사하고, 파두유의 피하주입으로 급성기반응을 발생시켜 비장세표와 PBMC 증식도, 그리고 TNF-$\alpha$와 Ovotranferrin의 발현에 미치는 콩 추출물 함유 크릴밀 사료의 영향을 조사하였다. 육계 병아리에서 콩 추출물 함유 크릴밀 사료는 생산성을 증가시켰다. 급성기 반응시 콩 추출물 함유 크릴밀 사료는 비장세포의 증식도를 낮추나 PBMC의 증식조는 높았다. 혈장내 순환 TNF-$\alpha$와 Ovotranferrin의 농도는 콩 추출물 함유 크릴밀 사료 급여로 감소하였다. 본 성적은 콩 추출물 함유 크릴밀 사료가 육계 병아리의 급성기 반응에 관여하고 있다는 것을 나타내었다.

• Biomolecules & Therapeutics
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• 제5권2호
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• pp.117-124
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• 1997

The analgesic effects of DA-5018, a new caosaucin derivative, were evaluated in various experimental pain models. Drugs were administered subcutaneously or topically. When drugs were administered subcutaneously, 1) the $ED_{50}$ of DA-5018, morphine . HCI, capsaicin and acetaminophen were 0.091-2.0, 0.3-4.3, 1.4-26.5 and 45.4-643 mg/kg, respectively in various pain or inflammatory models including acetic acid writhing, formalin, tail flick, Randall-Selitto, hot plate and crouton oil-induced ear edema test, 2) the AD2 values (the dose for doubling of pain threshold of vehicle control) of DA-5018, capsaicin and ketoprpgin were 1.07 $\pm$ 0. 18, 23.47$\pm$4.46 and 2.97$\pm$0.43 mg/kg in Freund's complete adjuvant (FCA)-induced arthritic pain model. And by topical application, 1) neither DA-5018 0.3% cream nor Zostrix-HP (capsaicin 0.075%) were effective in formalin test, 2) although DA-5018 0.3% cream significantly inhibited the croton oil-induced ear edema being better than Zostrix-HP and Kenofen (ketoprofen 3%). 3) In FCA model, DA-5018 0.3% cream reversed the decreased pain threshold of arthritic rat from 136.4 g (day 0) to 289.0 g (day 5) and 250.1 g (day 10), which was similar to Zostrix-HP. These results suggest that DA-5018 administered subcutaneously has a potent and broad analgesic spectrum than nonsteroidal antiinflammatory drugs against acute and chronic pain, and by topical application it exerts comparable analgesic and antiinglammaatory effects to capsaicin cream.

• 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.

• 대한화장품학회지
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• 제24권3호
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• pp.17-23
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• 1998

Inner nutshell of Castanea mollisima BL (chestnut) has been used as an anti-aging and anti-wrinkle agent from the ancient time in east Asia. In order to develop new anti-aging and anti-wrinkle, ethanolic extract of inner nutshell of Castanea mollisima BL (Cor-285) was prepared and various biological activities were evaluated. Cor-285 showed potent antioxidant activity, Especially, Cor-285 possessed potent free radical scavenging activity in vitro (IC50:7.6 g/ml) compared to gallic acid (IC50:12.5 g/ml), Cor-285 showed the preventive effect against UV-induced cytotoxicity of fibroblast at concentration of 25-250 g/ml. When Cor-285 was evaluated for its anti-allergic activity, it effectively inhibited histamine release from mast cells induced by compound 48/80 (86% inhibition at 10 mg/ml). The inhibitory activity was stronger than that of glycyrrhiznate. Cor-285 also showed in vivo inhibition against delayed hypersensitivity as well as croton-oil induced ear edema in mice when topically applied These results strongly suggest that Cor-285 may reduce immunoregulatory 1 inflammatory skin trouble. From the attempts to isolate the constituents, citropten (simple coumarin) and ellagic acid, a well known radical scavenger, were isolated. In a clinical trial of twenty healthy volunteers with aged skin,6 weeks application of Cor-285 (3% cream) decreased wrinkle about 26% and increased moisturizing 20% on the skin. All of these results indicate that Cor-285 may be an effective anti-aging and anti-wrinkle agent.

• 대한화장품학회지
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• 제22권2호
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• pp.41-51
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• 1996

Phaseolus aureus (mung bean), Leguminosae, has been used as an antidote from the ancient time. Especially, it has been widely used for cleaning face and skin in oriental countries. Although several constituents such as fatty acids, phytoallexin and phaseol derivatives were reported in P. aureus and related species including seedlings, there has been a few report to describe its biological activity. Therefore, in this investigation, the ethanol extract from P. aureus was obtained and its biological activities including the antioxidative and anti-inflammatory activities were studied. The 70% ethanol extract from P. aureus showed dose-dependent antioxidative activity (52.3% inhibition at 4 mg/ml) against lipid peroxidation assay, while the extract did not show the inhibitory activity of superoxide radical formation. The extract also showed the topical anti-inflammatory activity against croton-oil and arachidonic acid induced mouse ear edema test (18-19% inhibition at 7.5 mg/ear) as well as mild inhibitory activity against picryl chloride induced delayed hypersensitivity in mouse. For investigating active principles, vitexin and isovitexin (apigenin C-glycoside) as flavonoids, and adenosine were isolated from the extract using silica gel chromatography. The actual contents of vitexin and isovitexin were found to be 3.7 and 2.4 mg/g extract, respectively. Vitexin and isovitexin showed the antioxidative activity. They showed the topical anti-inflammatory activity, although the activities were not potent compared to the reference compounds. These results suggested that vitexin and isovitexin may be, at least in part, the compounds contributing the antioxidative activity in vitro and the topical anti-inflammatory activity of P. aureus in vivo. All results of present study might be one of the scientific rationale in using mung bean for skin care from the ancient time.

• KSBB Journal
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• 제30권4호
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• pp.182-190
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• 2015

The Zostera marina ethanolic extract (ZMEE) was tested in this study to investigate the anti-inflammatory activity in LPS-induced RAW 264.7 cells and mouse model. Nitric oxide production and inducible nitiric oxide synthase expression in cells treated with ZMEE was reduced significantly in a dose-dependent manner. Similarly, the secretion of pro-inflammatory cytokines such as interleukin (IL)-6, IL-$1{\beta}$, and TNF-${\alpha}$ was inhibited markedly. In addition, the expression of nuclear factor kappa B (NF-${\kappa}B$) and the phosphorylation of JNK, ERK, and p38 MAPKs was suppressed by ZMEE as well. In vivo test, ZMEE attenuated the croton oil-induced mouse ear edema and there were no mortalities in mice administered 5,000 mg/kg body weight of ZMEE during the observation periods. The results in photomicrograph of mice ear tissue showed the reduction of dermal thickness and the number of infiltrated mast cells. These results indicate that ZMEE inhibits the production of LPS-induced pro-inflammatory mediators, suggesting that ZMEE may be a potential material for anti-inflammatory therapies.

• 한국미생물·생명공학회지
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• 제44권3호
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• pp.268-277
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• 2016

본 연구는 COHEE의 항염증 효과를 확인하기 위한 실험으로써 pro-inflammatory cytokine의 분비량 및 iNOS, COX-2, NF-κB와 MAPKs의 발현량을 관찰하였다. 먼저 MTT assay를 통해 COHEE가 세포 생존율에 있어 독성을 나타내지 않음을 확인한 후 동일한 농도로 추후실험을 진행하였다. COHEE에 의해 NO 분비량이 농도 의존적으로 감소하였으며 IL-6, TNF-α 및 IL-1β의 분비량 또한 유의적으로 감소하였다. 특히 100 μg/ml의 농도에서 LPS 단독처리구인 대조구에 비하여 IL-6, TNF-α 및 IL-1β의 분비량을 각각 66%, 43% 및 93% 억제시켰다. 이러한 결과가 전염증성 매개인자의 전사인자인 NF-κB와 MAPKs 경로에 의한 것인지 확인하기 위하여 발현량을 관찰한 결과, COHEE가 LPS 처리에 의해 현저히 증가한 단백질의 발현을 농도 의존적으로 유의성 있게 억제하였다. 또한 COHEE는 croton oil로 부종을 유발한 마우스모델에서 귀부종 억제효과를 나타내었고 250 mg/kg 농도에서 조직의 경피 및 진피 두께의 발달을 prednisolone 10 mg/kg 처리구와 유사한 정도까지 현저히 억제시키고 염증성 세포인 mast cell의 침윤 억제 효과도 확인하였다. 이를 통해 COHEE는 염증 반응의 전사인자인 NF-κB의 발현을 조절함으로써 iNOS와 COX-2의 발현을 억제하고 그에 따라 전염증성 매개인자인 NO, IL-6, TNF-α 및 IL-1β의 분비를 억제하여 항염증 활성을 가지는 것을 확인하였으며, 이 결과를 종합해볼 때, COHEE가 염증 치료제로써의 소재로 이용될 가치가 충분할 것으로 사료된다.

• 한국미생물·생명공학회지
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• 제45권2호
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• pp.101-109
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• 2017

본 실험에서는 참치 심장 70% ethanol 추출물을 dichloromethane으로 분획한 후 항염증 효과를 확인하기 위해 RAW 264.7 세포에 LPS로 염증을 유도시켜 염증 매개성 물질인 NO와 pro-inflammatory cytokine의 분비량의 변화를 확인하였다. 그 결과, 참치 심장 dichloromethane 분획물을 처리하였을 때, 농도 의존적으로 NO의 생성량을 감소시키는 것을 확인하였으며, 특히, $100{\mu}g/ml$에서 가장 높은 억제효과를 나타내었다. 따라서 dichloromethane 분획물의 억제 활성이 세포사멸에 의한 감소인지 알아보기 위해서 MTT assay를 하였을 때, 세포 생존율이 dichloromethane 분획물을 PBS 처리군과 비교하였을 때 유의적인 차이가 나타나지 않음을 확인하였고, 이를 통해 dichloromethane 분획물이 NO 및 전염증성 cytokine의 분비를 효과적으로 억제할 수 있는 물질임을 확인할 수 있었다. Dichloromethane 분획물을 처리하였을 때, 염증 관련 단백질 발현 정도를 western blot을 통해 확인한 결과, LPS에 의해 발현이 증가된 $NF-{\kappa}B$, iNOS 및 COX-2는 분획물을 처리함으로써 농도 의존적으로 감소되는 것을 확인할 수 있었다. 또한 dichloromethane 분획물의 처리가 인산화된 MAPKs의 발현을 저해함을 확인하여 참치 심장 dichloromethane 분획물이 $NF-{\kappa}B$와 MAPKs의 발현을 억제시킴으로써 NO 및 pro-inflammatory cytokine의 분비량을 감소시킴을 확인할 수 있었다. 동물 모델에서는, dichloromethane 분획물을 처리하였을 때 croton oil에 의한 귀 부종이 농도 의존적으로 감소함을 확인하였고, 특히, $250mg/kg{\cdot}body\;weight$ 농도로 투여시 시판 항염증제인 predinisolone을 $50mg/kg{\cdot}body\;weight$ 농도로 투여한 그룹과 유사한 효과를 나타내었다. 조직학적 변화를 확인한 결과에서는, 진피와 경피의 두께가 감소하였으며 진피내 mast cell 침윤이 감소되는 것을 확인할 수 있었다. 따라서 참치심장 dichloromethane 분획물이 효과적인 염증 예방 및 부종 완화를 위한 치료제로서 활용 가능성을 확인하였다.

• 한국미생물·생명공학회지
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• 제43권1호
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• pp.45-55
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• 2015

본 연구에서는 참치유의 항염증 효과를 알아보기 위하여 in vitro 및 in vivo type의 실험을 진행하였다. 먼저 참치유(TO)가 세포독성을 가지는지에 대해 알아보기 위해 MTT assay를 진행한 결과, 모든 첨가 농도에서 세포독성을 가지지 않는 것을 확인하였다. 세포독성을 가지지 않은 농도에서의 항염증 효과를 알아보기 위하여 염증성 매개 인자인 NO, IL-6, TNF-α 및 IL-1β에 대한 항염증 효과를 살펴본 결과, TO의 첨가에 따라 각각 45%, 93%, 97%, 83%의 억제효과를 보임을 확인하였다. 또한 그 up-stream의 전사인자인 NF-κB 및 MAPKs와 전염증성 효소인 iNOS, COX-2의 발현을 효과적으로 억제하는 것을 확인하였다. In vivo type 실험의 일환으로 croton oil 유도 마우스 귀 부종에 대한 억제 효과를 살펴본 결과, TO의 처리에 의해 경피 및 진피 두께의 발달과, 염증 부위로의 mast cell 침윤이 억제됨을 확인하였다. TO의 효과적인 이용을 위해 그 안전성에 대한 평가로 급성 경구독성 평가를 진행한 결과, 경구독성을 유발하지 않음을 확인하였다. 본 연구 결과로 TO의 적용이 in vitro 및 in vivo type의 염증 모델에서 우수한 효과를 보임을 확인하여, TO 가 효과적인 염증 예방 및 치료제로의 활용 가능성이 충분함을 입증하였다.