• 제목/요약/키워드: bioactivity

검색결과 516건 처리시간 0.031초

Monoamine Oxidase Inhibitors from the Whole Plant of Cayratia japonica

  • Han, Xiang-Hua;Hong, Seong-Su;Park, Seon-Soon;Huh, Jae-Doo;Lee, Kyong-Soon;Lee, Myung-Koo;Hwang, Bang-Yeon;Ro, Jai-Seup
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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    • pp.256.1-256.1
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    • 2003
  • As a part of our ongoing research to discover novel monamine oxidase (MAO) inhibitors of plant origin, we found that a MeOH extract from the whole plant of Cayratia japonica (Vitaceae) strongly inhibited the MAO activity in mouse brain. The EtOAc-soluble fraction was. therefore, subjected to the bioactivity-guided fractionations to isolate the active compounds. (omitted)

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PPAR-$\gamma$ ligands binding energy and bioactivity

  • Lee, Hye-Sun;Chae, Chong-Hak;Yoo, Sung-Eun;Park, Kyung-Lae
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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    • pp.247.1-247.1
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    • 2003
  • PPAR-$\gamma$(Peroxisome Proliferator-Activated Receptor $\gamma$) 리간드들은 논문 조사를 통해 이루어졌다. PPAR-$\gamma$의 45개 알려진 화합물들을 찾았고, 12 생물활성 화합물을 선택했다. 리간드(rosiglitazone)과 단백질의 결합된 구조는 (1fm6)는 PDB로부터 획득했고, 단백질 coordinate를 가져와 PPAR의 활성 영역 잔기들은 확인했다. (2TYR, 1SER, 1HIS). CoMFA와 Flexi Dock을 통해 단백질과 리간드 사이의 상호작용과 결합에너지에 대한 상호 관계를 밝혔다.

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New Cytotoxic Metabolites from a Marine Sponge Homaxinella sp.

  • Mansoor Tayyab A.;Hong, Jong-Ki;Lee, Chong-O;Sim, Chung-Ja;Im, Kwang-Sik;Jung, Jee H.
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.190.3-190.3
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    • 2003
  • Three new butenolides (1-3), and a new cyclopentenone derivative (4) were isolated from a marine sponge Homaxinella sp. by bioactivity guided fractionation. The gross structures were established on the basis of NMR and MS analyses. The stereochemistry of the butenolides and cyclopentenone derivative was defined on the basis of optical rotation and CD spectroscopy. The compounds were tested against a panel of five human solid tumor cell lines and displayed marginal to significant cytotoxicity.

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Isolation of a Potent Mosquito Repellent from Vitex negundo L.: An Alternative Source of Rotundial

  • Amancharla, Praveen K.;Muthuraj, Patrick S.;Rao, Gottumukkala V.;Singh, Om V.
    • Natural Product Sciences
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    • 제5권2호
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    • pp.104-106
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    • 1999
  • The chloroform fraction of the aqueous extract of the fresh leaves of Vitex negundo by bioactivity guided isolation yielded a pure compound, rotundial (1) which has shown potent mosquito repellent activity. Using spectral data (UV, IR, $^1H\;&\;^{13}C$ NMR and MS) its structure has been elucidated.

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Heat or radiofrequency plasma glow discharge treatment of a titanium alloy stimulates osteoblast gene expression in the MC3T3 osteoprogenitor cell line

  • Rapuano, Bruce E.;Hackshaw, Kyle;Macdonald, Daniel E.
    • Journal of Periodontal and Implant Science
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    • 제42권3호
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    • pp.95-104
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    • 2012
  • Purpose: The purpose of this study was to determine whether increasing the Ti6Al4V surface oxide negative charge through heat ($600^{\circ}C$) or radiofrequency plasma glow discharge (RFGD) pretreatment, with or without a subsequent coating with fibronectin, stimulated osteoblast gene marker expression in the MC3T3 osteoprogenitor cell line. Methods: Quantitative real-time polymerase chain reaction was used to measure changes over time in the mRNA levels for osteoblast gene markers, including alkaline phosphatase, bone sialoprotein, collagen type I (${\alpha}1$), osteocalcin, osteopontin and parathyroid hormone-related peptide (PTH-rP), and the osteoblast precursor genes Runx2 and osterix. Results: Osteoprogenitors began to differentiate earlier on disks that were pretreated with heat or RFGD. The pretreatments increased gene marker expression in the absence of a fibronectin coating. However, pretreatments increased osteoblast gene expression for fibronectin-coated disks more than uncoated disks, suggesting a surface oxide-mediated specific enhancement of fibronectin's bioactivity. Heat pretreatment had greater effects on the mRNA expression of genes for PTH-rP, alkaline phosphatase and osteocalcin while RFGD pretreatment had greater effects on osteopontin and bone sialoprotein gene expression. Conclusions: The results suggest that heat and RFGD pretreatments of the Ti6Al4V surface oxide stimulated osteoblast differentiation through an enhancement of (a) coated fibronectin's bioactivity and (b) the bioactivities of other serum or matrix proteins. The quantitative differences in the effects of the two pretreatments on osteoblast gene marker expression may have arisen from the unique physico-chemical characteristics of each resultant oxide surface. Therefore, engineering the Ti6Al4V surface oxide to become more negatively charged can be used to accelerate osteoblast differentiation through fibronectin-dependent and independent mechanisms.

Effect of Microwave Assisted Water Extraction on Insoluble Phenolic Compounds through Bioactivity of Fagopyrum esculentum

  • Kim, Hyun Gi;Kim, Yong Ju;Lian, Thang Tung;Song, Sueng Yeob;Bang, Kuek Soo
    • 한국자원식물학회지
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    • 제32권6호
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    • pp.723-729
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    • 2019
  • Fagopyrum esculentum (Buckwheat) is a globally used alternative crop that contains several useful substances with various effects; however, many of these substances (rutin, quercetin, etc.) are water insoluble. To extract these substances, alcohols is required, which is inconvenient because these solvents cause diverse problems. Many studies are underway to achieve effective extraction of these substances with water. Among of these studies, microwave assisted water extraction (MAE) has been performed extensively. In this study, we performed the extraction in various solvents and/or microwave from Fagopyrum esculentum. The analysis of the content of useful substances and the bioactivity were performed and shown to increase in MAE. Liquid chromatography-mass was performed in order to identify of the useful water-insoluble substances. Catechin, quercetin, and rutin, which are all insoluble in water, were hardly extracted with water even on heating (4.4 ppb, 3.9 ppb and 60.3 ppb, respectively). However, MAE was found to extract much more of these substances than water (1204 ppb, 110.8 ppb and 2946 ppb, respectively). Although less efficient than alcohols, MAE showed much higher efficiency than simple water extraction. These results indicate that water extraction using microwave technology is effective in cases where it is difficult to extract useful substances using water.

공유결합으로 고정화된 urokinase 칼럼의 스케일업과 solid-phase refolding에 의한 반복 사용

  • 서창우;안상점;이은규
    • 한국생물공학회:학술대회논문집
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    • 한국생물공학회 2001년도 추계학술발표대회
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    • pp.85-88
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    • 2001
  • hGH 와 GST 절편으로 구성된 융합 단백질의 고정화 UK 칼럼에 의한 절단 반응 후 용출액의 pH를 3.5 로 낮춤으로써 이물질들을 침전시키고 이를 expanded bed chromatography 칼럼에 통과시킨 결과, 이물질들의 제거와 hGH 단량체의 흡착분리가 동시에 이루어겼다 . 흡착된 단량체는 NaCl 에 의해 용출되었으며 이 단계의 수율은 거의 100% 이었다 , 따라서 칼럼에 의한 절단 반응과 산 침전에 의한 이물질 침잔 반응 EBA 에 의한 이물질 제거 및 단량체 회수 반응을 연속적으로 진행할 수 있는 기초를 제시하였다 . 또한 고정화된 UK 는 guanidine HCl(6M)을 이용하여 unfolding 시키고 이를 세척하여 refolding 시킨 결과 20 회의 반복적인 처리 후에도 초기 활성의 약 80% 수준을 유지하였다. 이는 UK 가 공유결합된 상태에서 solid-phase refolding 이 가능하다는 증거이며, 고정화 효소 칼럼의 수영을 크게 향상시켜 경제성을 확보하는 방안으로 이용될 것으로 기대된다.

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공유결합으로 고정화된 urokinase 칼럼의 스케일업과 solid-phase refolding에 의한 반복 사용 (Scale-up of Covalently Immobilized Urokinase Column and Repeated Use of It by Solid-Phase Refolding)

  • 서창우;최강선;이은규
    • KSBB Journal
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    • 제16권5호
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    • pp.500-504
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    • 2001
  • Sepharose CL-6B 의 기능기를 aldehyderl로 활성화시킨 후 urokinase와 공유결합 시켜 고정화하는 방법을 6mL 규모에서 250 mL 규모로 스케일업한 결과 고정화 수율 및 고정화 된 UK에 의한 절단반응 수율 등에서 스케일업 전후의 결과에 차이가 없었다. 따라서 위의 고정화 방법의 scale-up 효능은 매우 우수한 것으로 나타났다. hGH와 GST 절편으로 구성된 융합 단백질의 고정화 UK 컬럼에 의한 절단 반응 후 용출액의 pH를 3.5로 낮춤으로써 이물질들을 침전시키고 이를 expanded bed chromatography zf칼럼에 통과시킨 결과, 이 물질들의 제거와 hGH 단량체의 흡착분리가 동시에 이루어졌다. 흡착된 단량체는 NaCL에의해 용출되었으며 이 단계의 수율은 거의 100%이었다. 따라서 칼럼에 의한 절단 반응과 t산 침전에 의한 이물질 침전 바능, EBA에 의한 이물질 제거 및 단량체 회수 반응을 연속적으로 진행할 수 있는 기초를 제시하였다. 또한 고정화된 UK는 guanidine HCl(6 M)을 이용하여 unfolding 시키고 이를 세적하여 refolding 시킨 결과 20회의 반복적인 처리 후에도 초기 활성의 약 80% 수준을 유지하였다. 이는 UK 가 공유결합된 상태에서 solid-phase refolding이 가능하다는 증거이며, 고정화 효소 칼럼의 수명을 크게 향상시켜 경제성을 확보하는 방안으로 이용될 것으로 기대된다.

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