• Archives of Pharmacal Research
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• 제22권1호
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• pp.18-24
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• 1999

Various flavonoid derivatives were previously reported to possess the inhibitory activity on cyclooxygenase/lipoxygenase. And these properties of flavonoids might contribute to their anti-inflammatory activity in vivo. In this study, several polyhydroxylated/methoxylated flavonoid derivatives such as oroxylin A. wogonin, skullcapflavone II, tectorigenin and iristectorigenin A were isolated from the medicinal plants. these compounds were evaluated fro their inhibitory effects on cyclooxygenase/lipoxygenase from the homogenate of human platelets in vitro. It was found that isoflavones including daidzein and tectorigenin possessed the inhibitory activity on cycloooxygenase, although the potency of inhibition was far less than that of indomethacin. In addition, oroxylin A, baicalein and wogonin inhibited 12-lipoxygenase activity without affecting cyclooxygenase, which suggested that 5,6,7- or 5,7,8-trisubstitutions of A-ring of flavone gave favorable results. The IC50 values of oroxylin A and NDGA against 12-lipoxygenase were found to be 100 and 1.5 uM, respectively.

• 한국식품영양과학회지
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• 제22권3호
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• pp.280-285
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• 1993

동물체내에서 천식, 염증, 혈소판 응고 등에 관련된 매개체를 생성시키는 효소인 lipoxygenase작용기 전과 유사한 대두 lipoxygenase (Type IV)를 사용하여 생마늘의 수용액, 에탄올, 클로로포름 추출분획에 의한 lipoxygenase 저해 정도를 측정하였다. 효소를 클로로포름 추출 분획과 10분 preincuba-tion시킨 후의 효소 저해 양상은 비가역적 저해(1$_{50}$값, 55mg/$m\ell$)이었으며, 수용액 추출 분획의 경우는 주로 가역적 저해 양상(1$_{50}$값, 65mg/$m\ell$)을 나타내었다. 한편, diallyldisulfide와 dimethyldisulfide의 1$_{50}$값은 각각 1.3mM, 18mM 이었으며 이들은 가역적, 비가역적 저해 현상을 모두 나타내었다. 합성품 alliin은 비교적 높은 농도(10mM농도에서 22%저해)에서 저해하였으며, alliin의 분해산물은 비가역적 저해 양상을 나타낸 반면에, S-ethylcysteine sulfoxide는 효소를 거의 저해하지 않았다. 따라서 다진 마늘 속에는 가역적 저해제가 주로 함유되어 있고, 소량(25~30%)의 비가역적 저해제가 함유되어 있는 것으로 사료되었다.사료되었다.

• 한국응용과학기술학회지
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• 제9권2호
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• pp.175-179
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• 1992

Methyl linoleate의 자동산화와 인지질에 작용하는 lipoxygenase의 활성에 미치는 탄닌산과 알파토코페롤의 영향을 HPLC로 조사하였다. 반응혼합물은 methyl linoleate 70mM, 라디칼 생성체 AMVN와 탄닌산 및 알파토코페롤 각각 0.7mM를 함유하였다. Hydroperxide 생성량을 측정하여 탄닌산과 알파토코페롤이 상당히 좋은 항상화제임을 알았고, 인지질 1${\mu}M$에 탄닌산과 알파토코페롤을 각각1${\mu}M$ 함유한 혼합물에 효소를 첨가하여 활성 억제효과를 측정하여, 탄닌산과 알파토코페롤이 좋은 효소 활성 억제작용을 하고 있음을 알았다.

• 한국식품과학회지
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• 제5권1호
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• pp.33-35
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• 1973

대두(大豆)를 침지(浸漬)후 $100^{\circ}C$에서 2분간 가열하면 불쾌한 풋 냄새의 발생을 충분히 억제할 수 있다. 건조한 대두(大豆)의 경우는 $100^{\circ}C$에서 3분간 가열하면 같은 효과를 나타낸다. 이와 같은 간단한 열처리(熱處理)는 병아리 사육시험의 결과 발육조해인자(發育阻害因子)를 불활성화(不活性化)시키기에는 불충분하다. 이취(異臭)의 조해(阻害)는 lipoxygenase 활성(活性)의 상실과 일치하며 이것이 그 원인인 것으로 생각된다.

• 한국식품조리과학회지
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• 제9권3호
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• pp.215-221
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• 1993

Bioactivity of the extract from various processed garlic was evaluated based on the inhibition of lipoxygenase(LPO), and the effect of some stabilizers on the bioactivity was investigated. Water, ethanol or chloroform extract of 30 min boiled garlic showed 75%, 76% or 70% inhibition, respectively, compared to extracts of fresh garlic. In pickled garlic, LPO inhibition decreased gradually during storage. Chloroform extract of 40 day-stored pickled garlic inhibited LPO by 77%, and even on 60th day storage it still retained inhibitory effect of 73%, compared to that of fresh garlic. Meanwhile, the powdered (freeze-dried) garlic showed more bioactivity(80%) than the other processed garlics, and moreover, the jrreversible/unstable components seem to be stabilized by freeze-drying. The optimum pH for stabilization of bioactive components in garlic macerate was pH 3 for 48 hr incubation and pH 11 for 6 hr incubation. In addition, the effect of NaCl was not so great, although but maximal stabilization was observed at 150 mM. Stabilizing effect of $\alpha$-tocopherol was markedly great, and at 6mM it showed 308% stabilizing effect after 48hr incubation. More stabilizing effect was observed at lower concentrations of ascorbic acid($\leq$0.6mM) than higher concentrations. The stabilizing effect of soybean oil was found to be remarkable only during initial period(6 hr) of incubation.

• Preventive Nutrition and Food Science
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• 제7권4호
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• pp.447-450
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• 2002

Previously, a methanol extract from seeds of Paeonia lactiflora was shown to have a potent inhibitory activities against tyrosinase and soybean lipoxygenase (SLO). Seven stilbenes, trans-resveratrol-4-Ο-$\beta$-D-glucoside, trans resveratrol, trans-$\varepsilon$-viniferin, cis-$\varepsilon$-viniferin, gnetin H, suffruticosol A and B were isolated from the seeds as active principles for inhibition of the enzymatic activity. Among them, the resveratrol trimer, gnetin H exhibited the most potent inhibitory activities against tyrosinase and SLO, respectively. Additionally, the resveratrol dimers, trans-$\varepsilon$-viniferin and cis-$\varepsilon$-viniferin exhibited significant inhibitory activity against the two oxidative enzymes. Meanwhile, three other stilbene derivatives, such as trans-resveratrol, suffruticosol A and suffruticosol B had also weak inhibition activity. The least inhibitory activity was observed in transresveratrol-4-Ο-$\beta$-D-glucoside. These results suggest that resveratrol dimers and trimer in the seeds of Paeonia lactiflora are potentially useful therapeutic agents against pathological disorders such as hyperpigmentation and inflammation.

• The Korean Journal of Physiology and Pharmacology
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• 제2권2호
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• pp.241-249
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• 1998

Platelet-activating factor(PAF) enhanced interleukin-1(IL-1) activity by the interaction with a specific receptor in rat alveolar macrophages. In this study, we investigated the role of endogenous arachidonate metabolites and intracellular calcium mobilization in the PAF-induced IL-1 activity. Alveolar macrophages were preincubated with 5-lipoxygenase and cyclooxygenase inhibitors 30 min before the addition of PAF and lipopolysaccharide(LPS). After 24h culture, IL-1 activity was measured in the supernate of sample using the thymocyte proliferation assay. Inhibition of 5-lipoxygenase by nordihydroguaiaretic acid and AA-861 completely blocked the PAF-induced enhancement of IL-1 activity with $IC_{50}\;of\;2\;{\mu}M\;and\;5\;{\mu}M$, respectively. In contrast, the inhibition of cyclooxygenase pathway by indomethacin and ibuprofen resulted in the potentiation in PAF-induced IL-1 activity with maximal effect at $1\;{\mu}M\;and\;5\;{\mu}M$, respectively. In addition, leukotriene $B_4$ and prostaglandin $E_2$ production were observed in PAF-stimulated alveolar macrophage culture. As could be expected, 5-lipoxygenase and cyclooxygenase inhibitors abolished PAF- stimulated leukotriene $B_4$ and prostaglandin $E_2$ production, respectively. The effects of PAF on intracellular calcium mobilization in alveolar macrophages were evaluated using the calcium-sensitive dye fura-2 at the single cell level. PAF at any dose between $10^{-16}\;and\;10^{-8}$ M did not increase intracellular calcium. Furthermore, there was no effective change of intracellular calcium level when PAF was added to alveolar macrophages in the presence of LPS or LPS+LTB4, and 4, 24 and 48h after treatment of these stimulants. Together, the results indicate that IL-1 activity induced by PAF is differently regulated through subsequent induction of endogenous 5-lipoxygenase and cyclooxygenase pathways, but not dependent on calcium signalling pathway.

• 대한화장품학회:학술대회논문집
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• 대한화장품학회 2003년도 IFSCC Conference Proceeding Book I
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• pp.601-610
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• 2003

Biotin is a water-soluble vitamin used as a skin conditioning agent and promotes the formation of intercellular lipid layers through increased lipid synthesis, which improves the skin's natural barrier function. The anti-inflammatory effects of biotin have been investigated using in vitro assay models, such as MTT assay, measurements of concentrations of nitric oxide(NO), prostaglandin E2(PGE$_2$), and inhibition rate of 5-lipoxygenase(5-LOX). In comparison with biotin, other plant extracts were tested at the same time which were kudzu vine extract, sage extract, paeonia extract, and dipotassium glycyrrhetinate. Nitric oxide is a signal molecule with functions such as neurotransmission, local vascular relaxation, and anti-inflammation in many physiological and pathological processes. NO can cause apoptosis and necrosis of target cells such as keratinocytes and is generated from L-arginine by nitric oxide synthase (NOS). Prostanoids, including prostaglandins and thromboxanes, are generated by the phospholipase $A_2$/cyclooxygenase(COX) pathway, and leukotrienes are generated by the 5-lipoxygenase pathway from arachidonic acid. Prostaglandin E2 recently have been shown to be beneficial in the resolution of tissue injury and inflammation, also has been implicated as an immunosuppressive agent and plasma levels of PGE$_2$ are elevated in patients sustaining thermal injury. Lipoxygenase metabolites from arachidonic acid have been implicated in inflammation, anti-inflammatory activity of the raw materials was evaluated in vitro by the offered inhibition of lipoxygenase.

• 한국환경농학회지
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• 제3권2호
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• pp.37-42
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• 1984

화학물질(化學物質)에 의(依)한 서양고추냉이와 사과의 peroxidase 및 정제된 대두(大豆) lipoxygenase 역가저해(力價沮害)를 조사(調査)하였다. 서양고추냉이와 사과의 peroxidase 역가(力價)에 저해효과(沮害效果)를 주는 농약중(農藥中) maneb가 zineb의 효과(效果)보다 컸으며 10,20,30ppm의 처리농도(處理濃度)에서 maneb는 12.5,23.0,34.5%, zineb는 9.5, 17.5,27.5%의 역가저해(力價沮害)를 보였다. Maneb와 zineb의 혼합체(混合體)인 mancozeb 를 500 ppm의 농도(濃度)로 사과나무에 철포(撤布)했을때 사과의 peroxidase 역가변화(力價變化)는 무처리구(無處理區)와 별 차이(差異)가 없었다. 대두(大豆)의 lipoxygenase 역가(力價)에 미치는 영향(影響)은 zineb의 경우 가장 저해도(沮害度)가 컸으며 phosphamidon과 carbofuran 이 또한 저해효과(沮害效果)가 있었다. 그러나 maneb는 저해효과(沮害效果)가 없었다. 10, 20, 30 ppm의 처리농도하(處理濃度下)에서의 lipoxygenase 역가저해도(力價沮害度)는 zineb가 14.0, 27.0, 40.0%, carbofuran이 6.5, 12.5, 20.0% 그리고 phosphamidon이 4.5, 9.0, 13.0%였다. 또한 이들 세농약(農藥)은 $100{\sim}200\;ppm$에서 100% lipoxygenase 역가저해(力價沮害)를 보였다.

• Archives of Pharmacal Research
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• 제28권7호
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• pp.761-764
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• 2005

Indigin, alkylated xanthene (1) and indigoferic acid (2) have been isolated from the chloroform soluble fraction of Indigofera oblongifolia, along with $\beta$-sitosterol (3) and 3-hydroxybenzoic acid (4), which are reported for the first time from this species. Their structures were determined through spectroscopic techniques. Both the new compounds 1 and 2 showed significant activity against enzyme lipoxygenase, while 2 further showed moderate inhibition against BChE.