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Synthesis of 6-[2-(Benzoxazol-2-ylmethylamino )ethoxy]-1-Alkyl­1 H-lndole-2-Carboxylic Acid and Inhibitory Activity on $\beta$-Amyloid Aggregation

  • Lee, Sun-Mi;Jeon, Raok
    • Archives of Pharmacal Research
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    • v.28 no.11
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    • pp.1219-1223
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    • 2005
  • 6-[2-(Benzoxazol-2-ylmethylamino)ethoxy]-1-alkyl-1H-indole-2-carboxylic acids were designed and synthesized as $\beta$-amyloid (A$\beta$) fibril assembly inhibitors. Their inhibitory activity on A$\beta$, aggregation was evaluated by thioflavin T assay although their activities were insignificant.

Inhibitory Constituents against HIV-1 Protease from Agastache rugosa

  • Min, Byung-Sun;Masao-Hattori;Lee, Hyeong-Kyu;Kim, Young-Ho
    • Archives of Pharmacal Research
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    • v.22 no.1
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    • pp.75-77
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    • 1999
  • Two diterpenoid compounds, agastanol (1) and agastaquinone (2), were isolated from the roots of Agastache rugosa (Labiatae). Compound 1 and 2 showed significant inhibitory effects against human immunodeficiency virus type 1 (HIV-1) protease activity with $IC_{50}$ values of 360 and $87{\mu}M$, respectively.

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Antioxidant activity of flavonoid, myricetin and (+)-catechin on B16F10 murine melanoma cell in oxidative stress with hydrogen peroxide

  • Yu, Ji-Sun;Kim, An-Keun
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.211.1-211.1
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    • 2003
  • There are now increasing evidences that free radicals and reactive oxygen species are involved in a variety of pathological events. Flavonoids. a group of polypenolic compounds, are widespread in the human food supply. This study was carried out to investigate the antioxidant activity of these compounds. myriceitn and (+)-catechin on B 16Fl0. murine melanoma cell line in oxidative stress. Oxidative stress was induced by exposure to hydrogen peroxide. (omitted)

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The Soluble Expression of the Human Renin Binding Protein Using Fusion Partners: A Comparison of ubquitin, Thioredoxin, Maltose Binding Protein-and NusA

  • Lee, Chung;Lee, Sun-Gu;Saori Takahashi;Kim, Byung-Gee
    • Biotechnology and Bioprocess Engineering:BBE
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    • v.8 no.2
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    • pp.89-93
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    • 2003
  • human renin binding protein (hRnBp), showing N-acetylglucosamine-2-epimerase activity, was over-expressed in E. coli, but was mainly present as an inclusion body. To improve its solubility and activity, ubiquitin (Ub), thioredoxin (Trx), maltose binding protein (MBP) and NusA, were used as fusion partners. The comparative solubilities of the fusion proteins were, from most to least soluble: NusA, MBP, Trx, Ub. Only the MBP fusion did not significantly reduce the activity of hRnBp, but enhanced the stability. The Origami (DE3), permitting a more oxidative environment for the cytoplasm in E. coli; helped to increase its functional activity.

Anti-Thrombosis Activity of Sinapic Acid Isolated from the Lees of Bokbunja Wine

  • Kim, Mi-Sun;Shin, Woo-Chang;Kang, Dong-Kyoon;Sohn, Ho-Yong
    • Journal of Microbiology and Biotechnology
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    • v.26 no.1
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    • pp.61-65
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    • 2016
  • From the lees of bokbunja wine (LBW) made from Rubus coreanus Miquel, we have identified six compounds (1: trans-4-hydroxycinnamic acid; 2: trans-4-hydroxy-3-methoxycinnamic acid; 3: 3,4-dihydroxycinnamic acid; 4: 4-hydroxy-3-methoxybenzoic acid; 5: 3,5-dimethoxy-4-hydroxybenzoic acid; and 6: 3,5-dimethoxy-4-hydroxycinnamic acid (sinapic acid)) through silica gel chromatography and UHPLC-MS. The compounds 1-6 showed strong anticoagulation and platelet aggregation inhibitory activities without hemolytic effect against human red blood cells. To date, this is the first report of the in vitro anti-thrombosis activity of sinapic acid. Our results suggest that different cinnamic and benzoic acid derivatives are closely linked to the anti-thrombosis activity of LBW, and sinapic acid could be developed as a promising anti-thrombosis agent.

Antioxidative Activity of Various Solvent Extracts of Quercisemen to Linoleic Acid (상수리(상실(橡實))의 각종 용매 추출물이 linoleic acid의 항산화력에 미치는 영향)

  • Sin, Du-Ho;Jo, Jeong-Sun
    • Journal of the Korean Applied Science and Technology
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    • v.8 no.1
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    • pp.79-83
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    • 1991
  • The extracts of Quercisemen(Quereus acutissima Carruthers seed) powder was obtained by the extraction with distilled water, water : acetonet(1:1, v/v), ethanol and ethyl ether, respectively. As a result this experiment, the antioxidative activity of each solvent extracts on linoleic acid were examined as follows: 1. Each fraction extracted by the acetone : water(1:1, v/v), water and ethanol respectively showed high antioxidative activity. 2. A fraction of the tannin extracted from the solvent, acetone, water(1:1, v/v) showed even more antioxidative activity than that of the ${\alpha}$-tocopherol or BHT. 3. Acceleration of peroxide reaction by $Fe^{++}$ and $Cu^{++}$ on the linoleic acid was strongly inhibited by adding the tannin, 4. Organic acid, such as malic acid, citiric acid and tartaric acid with the tannin were showed the synergistic effect fo the antioxidation reaction.

Anti-complement Activity of Phenolic Compounds from the Stem Bark of Magnolia obovata

  • Min, Byung-Sun
    • Natural Product Sciences
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    • v.14 no.3
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    • pp.196-201
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    • 2008
  • Five neolignans (1 - 4, 8), two sesquiterpene-lignans (5 - 6), and two phenylpropanoids (7, 9) were isolated from the stem bark of Magnolia obovata Thunberg (Magnoliaceae) by repeated column chromatography. The structures of isolated compounds were identified as 4-methoxyhonokiol (1), obovatol (2), magnolol (3), honokiol (4), eudeshonokiol B (5), eudesobovatol B (6), coumaric acid (7), magnaldehyde B (8), and ${\rho}-coumaric$ acid (9) on the basis of spectroscopic analysis including 2D-NMR and MS data. Compounds 1 - 9 were evaluated for their anti-complement activities against the classical pathway of the complement system. Of them, compound 8 showed significant anti-complement activity on the classical pathway with $IC_{50}$ value of 102.7 ${\mu}M$, whereas compounds 1 - 7 and 9 were inactive. This result indicated that an aldehyde group in the neolignan is important for the anti-complement activity against the classical pathway.