• 한국식품영양과학회지
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• 제37권8호
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• pp.979-984
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• 2008

본 연구에서는 머위 엽병의 에탄올 추출물을 용매 극성에 따라 hexane, chloroform, ethyl acetate 및 n-butanol로 분배한 분획물에 대해 전자공여능, 지질과산화 억제능 및 lipoxygenase 저해효과 효과를 살펴봄으로써 항산화능을 측정하였다. 분획물 중 ethyl acetate 분획물의 경우 $100\;{\mu}g/mL$ 농도에서 전자공여능, 지질과산화 억제능 및 lipoxygenase 저해능에서 각각 65.41%, 37.04%, 50.67%로 가장 우수한 항산화능을 나타내었다. 이를 근거로 하여 ethyl acetate 분획물로부터 머위 엽병의 항산화 활성 성분을 규명하기 위하여 open column chromatography를 이용하여 화합물 PJ-4를 분리, 정제하였으며, 1H- 및 13C-NMR 분석을 통해 kaempferol로 동정하였다. 단리된 kaempferol의 항산화 활성을 확인하기 위하여 앞에서 언급한 세 가지 항산화 측정법을 통해 실험한 결과, 농도 의존적으로 활성이 증가하는 양상을 보였다. 특히 $100\;{\mu}g/mL$의 농도에서 전자공여능, TBARS에 의한 지질과산화 억제 및 lipoxygenase 저해실험에서 각각 65.76%, 43.47%, 58.60%로 높은 항산화 활성을 나타내었다. 이와 같은 결과를 통해 kaempferol은 머위 엽병의 항산화 활성에 있어서 기여하는 물질일 것으로 보이며, 이로써 머위엽병을 이용한 천연항산화제 개발 및 활용에 긍정적인 가능성을 제시할 것으로 사료된다.

• Molecules and Cells
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• 제27권4호
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• pp.417-422
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• 2009

Lipoxygenase (LO) metabolites are generated in inflamed tissues. However, it is unclear whether the inhibition of the LO activity regulates the expression of c-Fos protein, a pain marker in the spinal cord. Here we used a carrageenan-induced inflammation model to examine the role of LO in the development of c-Fos expression. Intradermally injected carrageenan caused elevated number of cells exhibiting Fos-like immunoreactivity (Fos-LI) in the spinal dorsal horn, and decreased the thermal and mechanical threshold in Hargreaves and von Frey tests. Pretreatment with an inhibitor of phospholipase A2, that generates the LO substrate, prior to the carrageenan injection significantly reduced the number of Fos-(+) cells. A general LO inhibitor NDGA, a 5-LO inhibitor AA-861 and a 12-LO inhibitor baicalein also exhibited the similar effects. Moreover, the LO inhibitors suppressed carrageenan-induced thermal and mechanical hyperalgesic behaviors, which inidcates that the changes in Fos expression correlates with those in the nociceptive behaviors in the inflamed rats. LO products are endogenous TRPV1 activators and pretreatment with BCTC, a TRPV1 antagonist inhibited the thermal but not the mechanical hypersensitivity. Overall, our results from the Fos-LI and behavior tests suggest that LO products released from inflamed tissues contribute to nociception during carrageenan-induced inflammation, indicating that the LO pathway is a possible target for modulating inflammatory pain.

• Biomolecules & Therapeutics
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• 제18권2호
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• pp.197-204
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• 2010

To establish the anti-inflammatory activity of the total flavonoid fraction of the root barks of Broussonetia papyrifera (EBP) and a new formula, the ethanol extract of the root barks of B. papyrifera was fractionated with ethylacetate, yielding the hydrophobic prenylated flavonoid-enriched fraction. EBP and the ethanol extract of the whole Lonicera japonica (ELJ) plant were then mixed at a ratio of 1:1 (w/w) to give a new preparation (BL) in the hope of obtaining an optimal formula with a higher anti-inflammatory activity. Evaluation of the effects of these preparations on A23187-treated rat basophilic leukemia (RBL-1) cells revealed that EBP potently inhibited 5-lipoxygenase (5-LOX), while ELJ showed weak inhibition. Additionally, the mixture (BL) clearly showed stronger inhibitory effects against 5-LOX than either preparation alone. These preparations also inhibited cyclooxygenase-2-catalyzed $PGE_2$ and inducible nitric oxide (NO) synthase-catalyzed NO production by lipopolysaccharide-treated RAW 264.7 cells. When tested against arachidonic acid-induced mouse ear edema, EBP showed strong inhibitory activity at doses of 5-200 mg/kg when administered orally, but BL had obviously stronger inhibitory effects. When tested against ${\lambda}$-carrageenan-induced paw edema in mice, BL showed a potent and synergistic anti-inflammatory effect. In addition, in the acetic acid-induced writhing test, BL was found to have strong analgesic activity at 50-400 mg/kg. Taken together, these results indicate that each of these preparations exert anti-inflammatory activity in vitro and in vivo. In particular, BL showed stronger anti-inflammatory activity than EBP, and these anti-inflammatory effects were partially related to the inhibition of eicosanoid and NO production. BL may be useful for the treatment of human inflammatory disorders.

• 한국식품과학회지
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• 제29권2호
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• pp.355-361
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• 1997

털없는 쥐표피를 적출하여 ultraviolet B로서 조사한 후 녹차의 열수 추출물이 표피의 효소의 활성에 대한 항산화 효과를 조사하였다. 녹차의 열수추출물을 5, 25, 50 및 $100\;{\mu}g$으로 쥐표피에 첨가한 후 ultraviolet B을 $1.0\;joule/cm^{2}$로 조사한 후 효소활성을 조사한 결과 catalase와 glutathione reductase는 녹차의 열수 추출물의 첨가용량이 증가할수록 영향을 미치는 것으로 나타났으나 glutathione peroxidase와 superoxide dismutase는 영향을 받지 않았다. 한편 lipoxygenase의 활성을 알아보기 위하여 arachidonic acid에 $50\;{\mu}g$ 녹차의 열수 추출물을 첨가하여 대사를 검토한 결과 대사산물 12 또는 15-hydroxyeicosa- tetraenoic acid보다 5-HETE 및 8-HETE가 억제되었다. 녹차의 열수 추출물을 5, 25, 50 및 $100\;{\mu}g$ 첨가하였을 때 5-HETE는 각각 32, 52, 62 및 80% 억 제되었고 8-HETE는 각각 36, 47, 70 및 84%로 억제됨을 알 수 있었다.

• Biomolecules & Therapeutics
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• 제20권5호
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• pp.477-481
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• 2012

The rhizomes of Acorus gramineus have frequently been used in traditional medicine mainly for sedation as well as enhancing brain function. In this study, the anti-allergic activity of A. gramineus was investigated. The 70% ethanol extract of the rhizomes of A. gramineus was found to inhibit the allergic response against 5-lipoxygenase (5-LOX)-catalyzed leukotriene (LT) production from rat basophilic leukemia (RBL)-1 cells and ${\beta}$-hexosaminidase release from RBL-2H3 cells with $IC_{50}$'s of 48.9 and > $200{\mu}g/ml$, respectively. Among the 9 major constituents isolated, ${\beta}$-asarone, (2R,3R,4S,5S)-2,4-dimethyl-1,3-bis (2',4',5'-trimethoxyphenyl)tetrahydrofuran (AF) and 2,3-dihydro-4,5,7-trimethoxy-1-ethyl-2-methyl-3-(2,4,5-trimethoxyphenyl)indene (AI) strongly inhibited 5-LOX-catalyzed LT production in A23187-treated RBL-1 cells, AI being the most potent ($IC_{50}=6.7{\mu}M$). Against ${\beta}$-hexosaminidase release by antigen-stimulated RBL-2H3 cells, only AI exhibited strong inhibition ($IC_{50}=7.3{\mu}M$) while ${\beta}$-asarone and AF showed 26.0% and 39.9% inhibition at $50{\mu}M$, respectively. In addition, the ethanol extract of A. gramineus showed significant inhibitory action against the hapten-induced delayed hypersensitivity reaction in mice by oral administration at 200 mg/kg. Therefore, it is suggested that A. gramineus possesses anti-allergic activity and the constituents including ${\beta}$-asarone and AI certainly contribute to the anti-allergic activity of the rhizomes of A. gramineus.

• 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.

• Natural Product Sciences
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• 제6권4호
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• pp.170-178
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• 2000

Flavonoids are natural polyphenolic compounds widely distributed in plant kingdom. Although many flavonoids were found to show anti-inflammatory activity in vitro and in vivo, the potency of anti-inflammatory activity was not enough for a clinical trial. Thus, a search for finding potential flavonoid molecules is continuing. In this review, in vivo anti-inflammatory activity of various flavonoid derivatives is summarized mainly based on the results obtained in authors' laboratories. Among them, several biflavonoids such as amentoflavone and ginkgetin were found to possess anti-inflammatory activity on animal models of acute/chronic inflammation comparable to nonsteroidal and steroidal anti-inflammatory drugs currently used. In respect of their action mechanisms, the effects on arachidonic acid metabolism and nitric oxide production were described. Some flavonoids directly inhibit cyclooxygenase and/or lipoxygenase. Biflavones such as ochnaflavone and ginkgetin are inhibitors of phospholipase $A_2$. In recent studies, certain flavonoids were also found to suppress cyclooxygenase-2 and inducible nitric oxide synthase expression induced by inflammatory stimuli. Therefore, it is suggested that anti-inflammatory activity of the certain flavonoids (mainly flavones, flavonols and biflavonoids) may be mediated by direct inhibition of arachidonic acid metabolizing enzymes as well as suppression of the enzyme expression involved in inflammatory responses.

• Biomolecules & Therapeutics
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• 제18권3호
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• pp.321-328
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• 2010

Twenty six compounds (1-26) were isolated from the root barks of Ulmus davidiana var. japonica. The anti-inflammatory activity of the isolated compounds were evaluated agai nst the generation of inflammatory chemical mediators in bone marrow-derived mast cells. Among them, compounds 10, 11, 13, 15 and 19 inhibited not only cyclooxygenase-2 dependent prostaglandin $D_2$ generation but also 5-lipoxygenase dependent leukotrien $C_4$ generation in a concentration-dependent manner. In addition, compounds 11, 12, 13, 15 and 19 also inhibited $\beta$-hexosaminidase release, a marker of mast cell degranulation reaction, from bone marrow-derived mast cell. These results suggest that the anti-inflammatory activity of U. davidiana might in part occur by both the inhibition of eicosanoid generations and the degranulation reaction of mast cells.

• 한국수산과학회지
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• 제27권2호
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• pp.155-165
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• 1994

To evaluate the antioxidant effect of flavonoids and a-tocopherol on purified fish oil(up to $40\%$ of n-3 polyunsaturated fatty acids), lipid peroxidation, and fatty acids content during storage and upon heating were determined. The potential of these compounds for inhibiting and delaying both oxidation and lipoxygenase processes was also evaluated. The oxidation of fish oil was effectively inhibited by flavonoids and a-tocopherol. The antioxidizing effect of these compounds increased in proportion to their concentration. The addition of a-tocopherol and catechin-a-tocopherol mixture were prolonged induction period of lipid oxidation by 3.5 to 4 times. All other flavonoids also shown more than twice the prolonging effect. Lipoxygenase activity was decreased by catechin and a-tocopherol effectively.

• 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.