• 제목/요약/키워드: anti-derivative

검색결과 202건 처리시간 0.019초

Endophytic Diaporthe sp. ED2 Produces a Novel Anti-Candidal Ketone Derivative

  • Yenn, Tong Woei;Ring, Leong Chean;Nee, Tan Wen;Khairuddean, Melati;Zakaria, Latiffah;Ibrahim, Darah
    • Journal of Microbiology and Biotechnology
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    • 제27권6호
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    • pp.1065-1070
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    • 2017
  • This study aimed to examine the anti-candidal efficacy of a novel ketone derivative isolated from Diaporthe sp. ED2, an endophytic fungus residing in medicinal herb Orthosiphon stamieus Benth. The ethyl acetate extract of the fungal culture was separated by open column and reverse phase high-performance liquid chromatography (HPLC). The eluent at retention time 5.64 min in the HPLC system was the only compound that exhibited anti-candidal activity on Kirby-Bauer assay. The structure of the compound was also elucidated by nuclear magnetic resonance and spectroscopy techniques. The purified anti-candidal compound was obtained as a colorless solid and characterized as 3-hydroxy-5-methoxyhex-5-ene-2,4-dione. On broth microdilution assay, the compound also exhibited fungicidal activity on a clinical strain of Candida albicans at a minimal inhibitory concentration of $3.1{\mu}g/ml$. The killing kinetic analysis also revealed that the compound was fungicidal against C. albicans in a concentration- and time-dependent manner. The compound was heat-stable up to $70^{\circ}C$, but its anti-candidal activity was affected at pH 2.

LIPID-SOLUBLE VC DERIVATIVE ASCORBIC ACID TETRA-2-HEXYLDECANOATE (VC-IP) AS AN ANTI-AGING AGENT

  • Obayashi, K.;Ochiai, Y.;Ochiai, Y.;Masaki, H.;Kurata, Y.
    • 대한화장품학회:학술대회논문집
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    • 대한화장품학회 2003년도 IFSCC Conference Proceeding Book I
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    • pp.313-319
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    • 2003
  • It is well known that ascorbic acid (VC) is an important factor for several physiological reactions. In the skin, VC works as an anti-aging agent due to removing of oxidative stress generated by UV irradiation and stimulation of collagen synthesis. Thus, developing more effective VC derivatives is an important issue in creating anti-aging skin care products. Our study succeeded to develop a novel ascorbic acid derivative, ascorbic acid tetra-2-hexyldecanoate (VC-IP), which is a lipid-soluble pro-VC. The purpose of this study was to indicate the effects of VC-IP as pro-VC and anti-aging agent. First, it was examined whether VC-IP is converted to VC in physiological conditions. Since VC was detected from the cell extracts treated with VC-IP, it was indicated that VC-IP is a pro- VC.(omiited)

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Facile Preparation of Water Dispersible Red Fluorescent Organic Nanoparticles for Cell Imaging

  • Luo, Miao
    • Bulletin of the Korean Chemical Society
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    • 제35권6호
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    • pp.1732-1736
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    • 2014
  • Red fluorescent organic nanopaticles (FONs) based on a diarylacrylonitrile derivative conjugated molecule were facilely prepared by surfactant modification. Such red FONs showed excellent water solubility and biocompatibility, making them promising for cell imaging applications.

공대생의 역도함수 그래프 추측 (The Conjecture of Anti-Derivative Graph of Engineering Students)

  • 김수민;김선희
    • 대한수학교육학회지:학교수학
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    • 제19권1호
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    • pp.171-187
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    • 2017
  • 공대생들에게 미적분은 산업현장에서 발생하는 현상에 대한 수학적 안목을 형성해 주는 수학적 모델이자 지식이며 기능이다. 하지만 공대생들의 미적분학 학습은 기계적인 계산과 수학적 결과만을 적용시켜 문제를 해결하려는 경향을 보인다. 이에 본 연구는 실제적인 상황에서 수학적 개념과 원리를 적용하여 문제를 해결할 수 있는 문제를 제시하고 공대생들에게 이 문제를 풀게 하였다. 산의 경사도 그래프로부터 원래 산의 모양을 알아내는 문제에서 학생들은 주어진 그래프를 도함수의 그래프로 인식하고 역도함수의 그래프를 추측하였다. 그래프 해석에서 오류를 보이기도 하였는데 이는 미적분의 내용을 이해하지 못해서라기보다는 문제를 제대로 파악하지 않고 해결하려는 학습 방식에 기인한 것이었다. 경사도 문제 해결을 통해 공대생들은 수학이 자신이 공부하는 전공의 기초이자 실세계에 활용 가능한 유용성을 갖고 있으며 사고력을 향상시켜준다고 하는 인식의 변화를 경험하였다.

Biological Activity of Multifunctional Oligopeptide Derivatives

  • Kim, Bo Mi
    • 통합자연과학논문집
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    • 제9권2호
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    • pp.86-93
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    • 2016
  • The peptide sequences, GHK(Gly-His-Lys) and KTTKS(Lys-Thr-Thr-Lys-Ser), using a collagen stimulator recently were manipulated at N-terminal as a multifunctional peptide derivative with PEG(polyethyleneglycol) linker connected to gallic acid which presents anti-inflammatory activity. The multifunctional peptide derivatives were obtained in a normal peptide preparation method through SPPS(solid phase peptide synthesis) using Fmoc chemistry and a carboxyl group insertion reaction of PEG-3,4,5-triacetoxy benzoate by using potassium tert-butoxide and ethyl bromoacetate, which was separated by Sephadex DEAE. It gave a good compromise to a cosmetic application for cell cytotoxicity, anti-wrinkle, and anti-inflammation.

Leukotriene D4 Antagonistic Activity of a Stilbene Derivative Isolated from the Bark of Pinus Koraiensis

  • Song, Hong Keun;Jung, Jihyun;Park, Kwan Ha;Lim, Yoongho
    • Journal of Applied Biological Chemistry
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    • 제44권4호
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    • pp.199-201
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    • 2001
  • A phenolic substance was isolated from the bark of Pinus koraiensis. It was identified to be pinostilbenoside. Its anti-$LTD_4$ activity was evaluated using isolated guinea pig trachea, and its half maximal bronchodilating activity ($EC_{50}$) was $593{\pm}56{\mu}g{\cdot}ml^{-1}$. Because it is not known that stilbene derivatives possess anti-asthmatic activity through $LTD_4$ antagonism, here we report the result.

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EXISTENCE RESULTS FOR ANTI-PERIODIC BOUNDARY VALUE PROBLEMS OF NONLINEAR SECOND-ORDER IMPULSIVE qk-DIFFERENCE EQUATIONS

  • Ntouyas, Sotiris K.;Tariboon, Jessada;Thiramanus, Phollakrit
    • 대한수학회보
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    • 제53권2호
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    • pp.335-350
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    • 2016
  • Based on the notion of $q_k$-derivative introduced by the authors in [17], we prove in this paper existence and uniqueness results for nonlinear second-order impulsive $q_k$-difference equations with anti-periodic boundary conditions. Two results are obtained by applying Banach's contraction mapping principle and Krasnoselskii's fixed point theorem. Some examples are presented to illustrate the results.

JS-III-49, a hydroquinone derivative, exerts anti-inflammatory activity by targeting Akt and p38

  • Yi, Young-Su;Kim, Mi-Yeon;Cho, Jae Youl
    • The Korean Journal of Physiology and Pharmacology
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    • 제21권3호
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    • pp.345-352
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    • 2017
  • Since previous studies have reported that hydroquinone (HQ) exerted immunosuppressive and anti-inflammatory activity, various HQ derivatives have been synthesized and their biological activities investigated. In this study, we explored the anti-inflammatory activity of JS-III-49, a novel HQ derivative, in macrophage-mediated inflammatory responses. JS-III-49 suppressed the production of the inflammatory mediators nitric oxide (NO) and prostaglandin $E_2$ ($PGE_2$) and down-regulated the mRNA expression of the inflammatory enzymes cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) as well as the expression of the pro-inflammatory cytokines interleukin-6 (IL-6) and IL-$1{\beta}$ without cytotoxicity in LPS-stimulated RAW264.7 cells. JS-III-49 inhibited nuclear translocation of the $NF-{\kappa}B$ transcription factors p65 and p50 by directly targeting Akt, an upstream kinase of the $NF-{\kappa}B$ pathway, in LPS-stimulated RAW264.7 cells. However, JS-III-49 did not directly inhibit the kinase activities of Src and Syk, which are upstream kinases of Akt, in LPS-stimulated RAW264.7 cells. Moreover, JS-III-49 suppressed the nuclear translocation of c-Fos, one of the components of AP-1, by specifically targeting p38, an upstream mitogen-activated protein kinase (MAPK) in the AP-1 pathway in LPS-stimulated RAW264.7 cells. These results suggest that JS-III-49 plays an anti-inflammatory role in LPS-stimulated macrophages by targeting Akt and p38 in the $NF-{\kappa}B$ and AP-1 pathways, respectively.

Development of Novel Pyrone Derivative Retaining Retinoidal Anti-aging Activity with Low Skin Irritation

  • Rho, H.S;Kim, D.H;Kim, S.N;Kim, S.J;Chang, I.S;Kang, H.H;Lee, O.S
    • 대한화장품학회:학술대회논문집
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    • 대한화장품학회 2003년도 IFSCC Conference Proceeding Book II
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    • pp.184-191
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    • 2003
  • New pyranone derivative, 2-((3E)-4(2H, 3H, -benzo[3, 4-d] 1, 3-dioxolan-5-yl)-2-oxo-but-3-enyloxy)-5-hydroxy-4H-pyran-4-one (Seletinoid $G^{TM}$), was designed as a novel retinoid on the assumption that the pyranone ring may mimic the carboxylic acid moiety in retinoid structure. The enolic hydroxy of pyranone at five position was easily deprotonated to form an enolate. The role of enolate was similar to that of carboxylic acid. To evaluate the value of Seletinoid G as an anti-aging ingredient, various tests were performed for example inhibitory effect for MMP-l expression, anti-oxidative activity, procollagen synthesis in hairless mouse and primary skin irritation. The result of this study suggested that our new synthetic retinoid could be used as a safe material for anti-aging cosmetics.

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Ginsenoside Rg3 및 그 유도체 Ginsenoside Rg3-2H의 NO 생성 및 lymphocyte 분열 억제 효과 (Inhibitory Effect of Ginsenoside Rg3 and its derivative Ginsenoside Rg3-2H on NO production and lymphocyte proliferation)

  • 조재열
    • Journal of Ginseng Research
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    • 제32권3호
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    • pp.264-269
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    • 2008
  • Ginsenosides are major components in Panax ginseng and known to have numerous pharmacological activities such as anti-cancer, anti-diabetes, anti-viral and anti-atherosclerosis effects. In this study, the regulatory activities of G-Rg3 and its derivative 25-hydroxy Rg3 (G-Rg3-2H) on the production of nitric oxide (NO) in macrophages and the proliferation of lymphocytes prepared from spleen and bone marrow under treatment of lipopolysaccharide (LPS) or concanavalin (Con) A were examined. G-Rg3 and G-Rg3-2H dose-dependently inhibited NO production from LPS-activated RAW264.7 cells and in agreement, these compounds protected RAW264.7 cells from LPS-mediated cytotoxicity. In contrast, G-Rg3-2H dose-dependently inhibited lymphocyte proliferation induced by both LPS and Con A, while there was no inhibition by G-Rg3. Therefore, our data suggest that these compounds may be applied for NO-mediated or lymphocyte-mediated immunological diseases.