• Biomolecules & Therapeutics
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• 제18권2호
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• pp.159-165
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• 2010

Alpinia katsumadai has been widely used in traditional Chinese and Korean medicine to treat a variety of conditions including emesis and gastric disorders such as gastric pain and distended abdomen. To investigate the antinociceptive potential and mechanism of A. katsumadai, ethanolic extracts of A. katsumadai were assayed on cyclooxygenase-2 and evaluated for analgesic activity based on phenylbenzoquinone (PBQ)-induced writhing and carrageenan-induced hyperalgesia tests. A. katsumadai extracts inhibited the cyclooxygenase-2 enzyme activity in a dose-dependent fashion at an $IC_{50}$ value of 0.044 ${\mu}g$/ml. A. katsumadai extract (30-300 mg/kg, orally (p.o.) administered) significantly inhibited PBQ-induced writhing. This inhibition was judged not to be a false positive because a Rota-rod test revealed no difference in muscular coordination when compared to the controls. With regard to the carrageenan-induced hyperalgesia, A. katsumadai extract (30-300 mg/kg, p.o.) produced a significant, dose-dependent increase in the withdrawal response latencies. Naloxone did not reverse the analgesic effect of A. katsumadai extract in the carrageenan-induced hyperalgesia. Taken together, these results suggest that the antinociceptive activity of A. katsumadai is not related to the opioid receptor. A. katsumadai extract has remarkable, non-opioidreceptor-mediated analgesic effects on PBQ-induced writhing and carrageenan-induced hyperalgesia that occur via cyclooxygenase-2 inhibition.

• 한국식품위생안전성학회지
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• 제8권3호
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• pp.157-161
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• 1993

본 연구는 ethanol의 reactive metabolite인 acetaldehyde의 일차 배양혈관 평활근 세포에 대한 독성 발현 양식을 규명하기 위한 연구의 일환으로, prostaglandin 합성과 세포독성과의 관련성 여부를 확인하기 위하여 수행되었다. Acetaldehyde는, 일차 배양 혈관 평활근 세포에서의 prostaglandin 합성을 현저히 증가 시켰으며, 이때, cyclooxygenase activity 는 큰 변화없거나 오히려 감소시키는 경향을 보였다. Cyclooxygenase inhibitor 인 indometancin은 acetaldehyde에 의한 LDH release를 현저히 차단시켰으며, aspirin 및 salicylic acid는 전혀 영향을 주지 못했다. Phospholipase $A_2\;(PLA_2)$ inhibitor로 알려져 있는 dexamethasone은 유의적인 세포 독성 경감 작용을 보이지 못하였으며, Lipoxygenase inhibitor 들인 NDGA, propyl gallate 등은 현저한 독성 경감 효과를 보였다. 이상의 결과로부터 acetaldehyde에 의한 일차 배양 혈과 평활근 세포에서의 prostaglandin 합성 증가는 Cell death에 대한 직접적인 원인이 아님을 추론할 수 있었으며, $PLA_2/lipoxygenase$ inhibitor들의 강력한 세포독성 경감 작용으로 미루어 볼 때, acetaldehyde 에 의한 세포독성은 lipoxygenase 대사 산물 혹은 $PLA_2$의 직접 작용에 기인할 가능성을 확인할 수 있었다.

• 동의생리병리학회지
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• 제20권2호
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• pp.455-459
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• 2006

The inhibitors of prostaglandin $E_2\;(PGE_2)$ production and cyclooxygenase-2 (COX-2) activity have been considered as potential anti-inflammatory agents. In this study, we evaluated 9 compounds isolated from 5 Korean phytomedicinal plants (Spirea prunifolia, Paeonia suffruticosa, Salvia miltiorrhiza, Scutellaria baicalensis, and Artemisia capillaris) for the inhibition of $PGE_2$production and COX-2 expession in lipopolysaccharide (LPS)-stimulated human macrophages U937 cells. As a result, several compound such as prunioside A, penta-O-galloyl-beta-D-glucose, tanshinone IIA, baicalin, baicalein, wogonin, scopolatin, scoparone and decursinol showed potent inhibition of $PGE_2$production (50-70% inhibition at the test concentration of $10\;{\mu}M$). In addition, these compounds were also considered as potential inhibitors of COX-2 activity (45-73% inhibition at the test concentration of $10\;{\mu}M$). These active compound mediating COX-2 inhibitory activities are warranted for further elucidation of active principles for development of anti-inflammatory agents and these properties may contribute to the anti-atopic dermatitis activity.

• 동의생리병리학회지
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• 제19권5호
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• pp.1419-1426
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• 2005

This study was carried out to investigate the effects of herbal extracts on the skin inflammatory reactions which use the makeup preparations. In experiment 1, among the herbal ingredients of herbal extracts, ethanol extracts and 1,3-BG(Butylene Glycol) extracts of Galla Rhois showed potent radical scavenging activity, more than 91% at all concentrations, tested by DPPH (1,1-diphenyl-2-picryl-hyrazyl) method. In experiment 2, ethanol extracts of Chrysanthemi Flos, Gardenias Flos, Galla Rhois showed potent inhibitory activity of the lipopolysaccharide-induced nitric oxide(NO) production, more than 87% at $10{\mu}g/m{\ell}$, by the macrophage RAW 246.7 cells. And 1,3-BG extracts of Taraxaci Herbs, Corm Fructus, Galla Rhois showed potent inhibitory activity of nitric oxide production, more than 89% at $10{\mu}g/m{\ell}$. In experiment 3, ethanol extracts of Chrysanthemi Flos, Gardeniae Flos, Galla Rhois showed potent inhibitory effects of cyclooxygenase-II activity, more than 78% at $10{\mu}g/m{\ell}$, by using ELISA kit. And 1,3-BG extracts of Galla Rhois, Carthami Flos, Chrysanthemi Flos, Taraxaci Herba, Corm Fructus showed potent inhibitory effects of cyclooxygenase-II(COX-II) activity, more than 80% at $10{\mu}g/m{\ell}$. Therefore, 1 expect that herbal extracts, especially Galla Rhois may be used as a drug for treatment on skin inflammation and a material of the makeup preparations.

• Journal of Applied Biological Chemistry
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• 제66권
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• pp.114-121
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• 2023

선택적 cyclooxygenase (COX)-2 억제제는 기존의 비스테로이드성 소염제의 위장 부작용을 줄일 수 있는 새로운 대체제이다. 하지만, 최근 혈전을 일으켜 심혈관 질환의 위험을 증가시킨다는 보고가 있다. 따라서 본 연구에서는 유효성분인 ursolic acid를 각각 40, 50%로 극대화한 로즈마리 추출물(RE)의 항염증 효과와 이에 따른 심혈관 부작용의 안전성을 확인하였다. RE의 COX 효소 활성 저해 평가 결과 40, 50% RE는 100 ㎍/mL에서 양성 대조군인 celecoxib 및 rofecoxib와 비슷한 COX-2 저해 활성을 보였고, COX-1 저해 활성은 미미하였다. 이후 Lipopoly-saccharide (LPS)를 조건에 따라 처리한 RAW 264.7 세포에 40, 50% RE 1 ㎍/mL를 처리하여 COX-2, COX-1 유전자 발현, 세포 배양액의 prostaglandin E₂ (PGE₂), thromboxane B₂ (TXB₂) 농도를 확인하였다. 실험 결과 COX-2 유전자 발현은 40% RE가 LPS를 24시간 후처리한 조건에서 감소하였고, 40, 50% RE는 COX-1 유전자 발현 및 PGE₂, TXB₂ 농도에는 유의한 영향을 주지 않는 것으로 확인되었다. 따라서 RE는 혈전 생성에 관여하는 prostaglandins의 균형에 영향을 주지 않아 심혈관 혈전 생성의 위험성이 적을 것으로 사료된다.

• Journal of Microbiology and Biotechnology
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• 제17권9호
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• pp.1546-1549
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• 2007

Chitosan oligosaccharide (COS, 3 kDa

• Archives of Pharmacal Research
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• 제27권4호
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• pp.442-448
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• 2004

Wogonin (5,7-dihydroxy-8-methoxyflavone) is a down-regulator of cyclooxygenase-2 and inducible nitric oxide synthase expression, contributing to anti-inflammatory activity in vivo. For further characterization of modulatory activity on ploinflammatory gene expression in vivo, the effect of wogonin was examined in this experiment using animal models of skin inflammation. By topical application, wogonin inhibited an edematic response as well as ploinflammatory gene expression against contact dermatitis In mice. Wogonin inhibited ear edema ($19.4-22.6\%$) at doses of $50-200\;{\mu}g$/ear and down-regulated interleukin-$1{\beta}$ induction ($23.1\%$) at $200{\mu}g$/ear in phenol-induced simple irritation. Wogonin ($2{\times}50-2{\times}200{\mu}g$/ear) also inhibited edematic response ($51.2-43.9\%$) and down-regulated ploinflammatory gene expression of cyclooxygenase-2, interleukin-$1{\beta}$, interferon-$\gamma$, intercellular adhesion molecule-1 and inducible nitric oxide synthase with some different sensitivity against picryl chloride-induced delayed hypersensitivity reaction. All these results clearly demonstrate that wogonin is a down-regulator of ploinflammatory gene expression in animal models of skin inflammation. Therefore, wogonin may have potential for a new anti-inflammatory agent against skin inflammation.

• Archives of Pharmacal Research
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• 제25권3호
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• pp.329-335
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• 2002

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 19 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 at 1-50 uM. Other prenylated flavonoids including kuraridin and sanggenon D also down-regulated COX-2 induction at 10-25 uM, while kurarinone and echinoisoflavanone did not. In addition, sophoraflavanone G showed in vivo anti-inflammatory activity against mouse croton oil-induced ear edema and rat carrageenan paw edema via oral (2-250 mg/kg) or topical administration (10-250 ug/ear). Although the potencies of inhibition were far less than that of a reference drug, prednisolone, this compound showed higher anti-inflammatory activity when applied topically, suggesting a potential use for several eicosanoidrelated skin inflammation such as atopic dermatitis.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2001년도 International Symposium on Dietary and Medicinal Antimutgens and Anticarcinogens
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• pp.133-134
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• 2001

Abnormal regulation of the inducible form of cyclooxygenase (COX-2) has been often observed in various types of cancerous and transformed cells. Recently, targeted inhibition of COX-2 is recognized as one of the promising strategies for the prevention or treatment of cancer as well as inflammation, As part of a program to evaluate the cancer chemopreventive potential of anti-inflammatory phytochemicals, we initially determined the COX-2 inhibitory activity of some naturally occurring diarylheptanoids structurally related to curcumin.(omitted)

• Biomolecules & Therapeutics
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• 제14권1호
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• pp.11-18
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• 2006

Certain flavonoids possess anti-inflammatory activity. Besides their antioxidative property, the cellular action mechanisms of flavonoids include an inhibition of arachidonate metabolizing enzymes such as cyclooxygenases and lipoxygenases, and a down-regulation of proinflammatory gene expression such as cyclooxygenase-2, inducible nitric oxide synthase and tumor necrosis factor-$\alpha$. In this review, the recent findings of anti-inflammatory flavonoid research since 2004 were summarized. And the cellular mechanisms on signal transduction pathways were also discussed.