• Title/Summary/Keyword: anti-derivative

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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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    • v.27 no.6
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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.
    • Proceedings of the SCSK Conference
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    • 2003.09a
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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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    • v.35 no.6
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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.

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

  • Kim, Su Min;Kim, Sun Hee
    • School Mathematics
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    • v.19 no.1
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    • pp.171-187
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    • 2017
  • To engineering students, calculus is essential knowledges and skills as a mathematical model and give a perspective to observe phenomenon in the future industrial field. However, engineering students' calculus study tends to solve problems by only applying the mechanical calculation and mathematical results. This study aimed to make engineering students realize the importance of calculus and untypical problems, by suggesting problems that could apply the mathematical concepts and principles and even solve the actual conditions of the problems. Students conjectured the anti-derivative graphs by interpreting the given derivate problems. They showed errors in this process and the errors are contributed by their mathematics leaning styles. As a result, the task would be helpful to engineering students.

Biological Activity of Multifunctional Oligopeptide Derivatives

  • Kim, Bo Mi
    • Journal of Integrative Natural Science
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    • v.9 no.2
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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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    • v.44 no.4
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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
    • Bulletin of the Korean Mathematical Society
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    • v.53 no.2
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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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    • v.21 no.3
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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
    • Proceedings of the SCSK Conference
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    • 2003.09b
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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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Inhibitory Effect of Ginsenoside Rg3 and its derivative Ginsenoside Rg3-2H on NO production and lymphocyte proliferation (Ginsenoside Rg3 및 그 유도체 Ginsenoside Rg3-2H의 NO 생성 및 lymphocyte 분열 억제 효과)

  • Cho, Jae-Youl
    • Journal of Ginseng Research
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    • v.32 no.3
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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.