• Title/Summary/Keyword: Antiinflammatory

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Synthesis of galactosylglycerol from Melibiose as M-5 Intermediate (Melibiose로부터 M-5중간체 galactosylglycerol의 합성)

  • 차배천
    • YAKHAK HOEJI
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    • v.45 no.6
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    • pp.575-581
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    • 2001
  • The galactolipid M-5, which showed anti-inflammatory activity is glycoglycerolipid isolated from the Okinawa marine sponge Phyllospongia foliascens. Glycolipids have been synthesized by various methods, especially it were generally known that synthetic method of M-5 analogue and synthetic method of various glycolipids by glycosidation after synthesis of glycerolipid part. The others, it was not suggested that synthetic method via glycosylglycerol obtained by degradation from diglycoside. This study was carried out to investigate the synthesis of galactosylglycerol from melibiose as M-5 intermediate. Synthesis of galactosylglycerol was accomplished by selective protection of hydroxy group of sugar and diol cleavage by Pb(OAc)$_4$. As a result, galactosylglycerol was synthesized by 8 steps pathway and their structures were elucidated by analysis instrument.

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Studies on the Antiinflammatory Compounds from Sorbus Commixta (정공피으로부터 항염증물질의 연구)

  • Yun, Young-Gab;Chai, Kyu-Yun;Lee, Kyung-Kwan;Bhatt, Lok Ranjan;Baek, Seung-Hwa
    • YAKHAK HOEJI
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    • v.53 no.6
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    • pp.351-356
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    • 2009
  • Sakuranetin, prunetin and dihydroquercetin were isolated from the methanol extract of Sorbus commixta by 1D/2D-NMR and LC-MASS spectrometry. Medicating these compounds to RAW264.7 cell that was pre-treated by lipopolysaccharide revealed anti-inflammatory effects that greatly inhibited the production of NO (nitric oxide) and PEG2 (prostaglandin E2), which are well known to cause the expression of iNOS (inducible nitric oxide synthase) and COX-2 (Cyclooxygenase-2). These results suggest that these compounds can be used as stable anti-inflammatory materials.

A Clinical Report of 1 Case of Cold Urticaria treated with Bee-venom Acpuncture Therapy (봉약침요법(蜂藥鍼療法)으로 치료한 한랭 두드러기 환자 1례 보고)

  • Hwang, Gue-Tae;Kang, Jae-Hui;Lee, Hyun
    • Journal of Haehwa Medicine
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    • v.17 no.2
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    • pp.149-153
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    • 2008
  • Objective : Cold Urticaria is a symptom of edema and pruritus that appear when a patient is exposed to the coldness. The effect of Bee-venom Acpuncture Therapy is antiinflammatory, pain-killing, and blood circulation promotion. The aim of this study is to report the effect of Bee-venom Acpuncture Therapy to Cold Urticaria. Methods : The Cold Urticaria patients were treated with Bee-venom Acpuncture Therapy. Result and Conclusion : Edema and Pruritus of Cold Urticaria patient improved after Bee-venom Acpuncture Therapy.

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Benorylate Interaction with Ethoxybenzamide and Lorazepam (Benorylate와 Ethoxybenzamide 밍 Lorazepam 과의 상호작용)

  • 허인회;이명환
    • YAKHAK HOEJI
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    • v.23 no.1
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    • pp.11-16
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    • 1979
  • Benorylate and ethoxybenzamide have been used alone or in combination as an analgesic, antipyretic and antiinflammatory agent. We investigated the significance of the differences of analgesic activities between single and concurrent administration of benorylate and ethoxybenzamide and lorazepam in mice and also antipyretic activity between single and concurrent administration of benorylate and ethoxybenzamide in rats. 1). Concurrent administration of each half dose of benorylate and ethoxybenamide showed much inhibiting effect on the acetic acid-induced writhing syndrome of mice than the above drug alone, and the some increased analgesic response by hot plate method. 2). The synergistic and analgesic effect of combined administration of benorylate and lorazepam was found to be significant. 3). Antipyretic effect of half-dose combined administration of benorylate and ethoxybenzamide on the rat pyrexia induced by yeast(s.c.) and T.T.G. (i.v.) was shown to be similar to the effect of each drug.

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Eudesmin Inhibits Tumor Necrosis Factor-$\alpha$ Production and T cell Proliferation

  • Cho, Jae-Youl;Yoo, Eun-Sook;Baik, Kyoung-Up;Park, Myung-Hwan
    • Archives of Pharmacal Research
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    • v.22 no.4
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    • pp.348-353
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    • 1999
  • Possible antiinflammatory effect of eudesmin were examined by assessing the effects on tumor necrosis factor (TNF)-$\alpha$ production and lymphocyte proliferation as well as cytotoxicity against murine and human macrophages. the compound significantly inhibited TNF-$\alpha$, production by lipopolysaccaride (LPS)-stimulated murine macrophage RAW264.7 without displaying cytotoxicity suggesting that eudesmin may inhibit TNF-$\alpha$ production without any interference of normal cell function. It also significantly attenuated T cell proliferation stimulated by concanavalin A (Con A) in a dose-dependent manner.

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Effects of Yukmijihwangwon on Hypoxia of Neuronal Cells (저산소상태에서 육미지황원의 뇌신경세포 보호효과에 대한 연구)

  • Kang, Bong-Joo;Hong, Seong-Gil;Cho, Dong-Wuk
    • Korean Journal of Oriental Medicine
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    • v.7 no.1
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    • pp.115-124
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    • 2001
  • Yukmijihwangwon (YM) has been known to reinforce the vital essence and have antioxidant activities. This study was designed to examine the inhibitory effects of YM against in vitro hypoxia/reperfusion-induced inflammatory response. We have characterized the production of prostaglandin $E_2$ and arachidonic acid during hypoxia/reperfusion in the human neuroblastoma SK-N-MC and human monocytic macrophage U937 cells and the ingibitory effect of YM on these inflammation-related substance formation has been found out in this study. To investigate inhibition of COX expression by YM during hypoxia in vitro. This result suggested that YM used in this experiment reinforced antiinflammatory potentials and protected cells against hypoxia/reperfusion induced inflammatory response.

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Structure and Antiinflammatory Activity Relationships of Wogonin Derivatives

  • Jang, Jin-Hee;Kim, Hyun-Pyo;Park, Hae-Il
    • Archives of Pharmacal Research
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    • v.28 no.8
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    • pp.877-884
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    • 2005
  • A number of wogonin derivatives have been synthesized as congeners of wogonin and evaluated for their inhibitory activities of $PGE_2$ production. Wogonin derivatives modified at the B ring of wogonin were obtained from 2,4-Dihydroxy-3,6-dimethoxyacetophenone (1) via several steps. Most wogonin derivatives exhibited much reduced inhibitory activities against COX-2 catalyzed $PGE_2$ production compared to that of wogonin. Alkylation of 5,7-phenol groups and substitution at the B ring of wogonin generally caused reduction of inhibitory activity.

Formulation of Sustained-Release Tablets of Flurbiprofen (서방출성 플루르비프로펜 정제의 제제설계)

  • 이상철;박은석;지상철
    • YAKHAK HOEJI
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    • v.39 no.2
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    • pp.185-192
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    • 1995
  • Flurbiprofen, one of potent nonsteroidal antiinflammatory drugs, has several systemic side effects due to dose dumping effect following oral administration of its conventional solid dosage forms. To reduce these side effects and to sustain therapeutic concentration of the drug, matrix tablets of flurbiprofen were prepared and evaluated for sustained release from the tablets. The matrix tablets of flurbiprofen were prepared with Eudragit, Pluronic, (anhydrous) lactose and colloidal silicon dioxide employing two different preparation methods, wet granulation and direct compression. The dissolution rates of the tablets were evaluated using KP 2 method. Formulation factors that affected dissolution rates of flurbiprofen were the type and content of Eudragit, the type and content of Pluronic, and the tablet preparation method. Several formulations of the matrix tablets showed dissolution patterns close to the simulated profile using pharmacokinetic parameters of flurbiprofen.

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The crystal structure of pirprofen$(C_{3},\; H_{14},\; ClNO_2$), a non-steroidal antiinflammmatory agent

  • Kim, Yang-Bae;Park, Il-Yeong
    • Archives of Pharmacal Research
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    • v.19 no.1
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    • pp.71-73
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    • 1996
  • The molecular structure of pirprofen, 3-chloro-4-(2,5-dihydro-1H-pyrrol-1-yl)-.alpha.-methyl-benzeneacetic acid, was determined by single crystal X-ray diffraction analysis. The compound was recrystallized from a mixture of chloroform and toluene in triclinic, space group P over $\bar1,\; with\; a=4.577(1),\; b=11.213(2),\; C=12.485(2){\AA},\alpa.=107.39(1),\;\beta=97.79(1),\;\gamma=92.03(2),\; and Z=2$ The calculated density is $1.384 g/cm^3$. The structure was solved by the direct method and refined by full matrix least-squares procedure to the final R value of 0.034 for 1681 independent reflections. The non-aromatic dihydropyrrol group is found to be coplanar to the central aromatic ring. The molecules are dimerized through the intermolecular hydrogen bonds at the carboxyl group in the crystal.

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Biopharmaceutical Studies on the Alkanol Esters of Naproxen (II) -Pharmaceutical Characteristics of 3 Kinds of the Alkanol Esters of Naproxen- (나프록센의 Alkanol 에스테르류에 관한 생물약제학적 연구 II -3종의 Alkanol 에스테르의 약제학적 특성-)

  • 백우현;김종갑
    • YAKHAK HOEJI
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    • v.30 no.3
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    • pp.128-138
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    • 1986
  • Three newly synthesized alkanol esters of d-2-(6-methoxy-2-naphthyl) propionic acid, NAPROXEN were examined for physicochemical properties and biopharmaceutical characteristics. These esters were very stable in solid state, but more than 90% of these esters were hydrolysed to the parent, naproxen in rabbit's liver hornogenates. They showed higher dissolution rate in the artificial gastric and intestinal juice, and significantly greater partition coefficient in n-octanol, when compared with naproxen. The absorption rate constants of these esters were increased, while the elimination rate constants were decreased, comparing with naproxen. The ulcerogenic doses on gastric and intestinal mucosa were increased remarkably, and the antiinflammatory dose against carrageenininduced edema on rat hind paw was decreased markedly in these esters, and thus the safety indexes of these esters were higher than that of naproxen.

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