• Title/Summary/Keyword: active compound

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Effect of Seaweed Extracts on the Viability of the Crustose Coralline Lithophyllum yessoense

  • Kang Se-Eun;Park Sun-Mee;Choi Jae-Suk;Ahn Dong-Hyun;Kim Young-Dae;Hong Yong-Ki
    • Fisheries and Aquatic Sciences
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    • v.8 no.4
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    • pp.243-246
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    • 2005
  • The addition of seaweed extracts was found to regulate the viability of cultures of the crustose coralline alga Lithophyllum yessoense. The viability was quantitated using a triphenyltetrazolium chloride assay, and the methanol-soluble extracts from 18 prevalent seaweed species were tested. Extracts from Codium fragile and Enteromorpha linza inhibited viability, and a Hizikia fusiform is extract slightly increased viability. The methanol extract of C. fragile, which had the strongest inhibitory activity, decreased viability to 72 or $52\%$ that of the control following addition of 0.2 or 2 mg/mL of extract to the culture, respectively. The main active compound in the C. fragile was lipid. This information is a preliminary result related to the exploration of seaweed restoration in the algal whitening area.

Characterization of Chloroanilines-degrading Bacteria Isolated from Seaside Sediment (연안 갯벌에서 분리한 Chloroaniline 화합물 분해 미생물의 특징)

  • Kang, Min-Seung;Kim, Young-Mog
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.40 no.5
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    • pp.282-287
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    • 2007
  • Chloroanilines are aromatic amines used as intermediate products in the synthesis of herbicides, azo-dyes, and pharmaceuticals. 3,4-dichloroaniline (DCA) is the degradation product of some herbicides (diuron, propanil, and linuron) and of trichlorocarbanilide, a chemical used as an active agent in the cosmetic industry. The compound, however, is considered a potential pollutant due to its toxicity and recalcitrant property to humans and other species. With the increasing necessity for bioremediation, we sought to isolate bacteria that degraded 3,4-DCA. A bacterium capable of growth on 3,4-DCA as the sole carbon source was isolated from seaside sediment using a dilution method with a culture enriched in 3,4-DCA. The isolated strain, YM-7 was identified to be Pseudomonas sp. The isolated strain was also able to degrade other chloroaniline compounds. The isolated strain showed a high level of catechol 2,3-dioxygenase activity on exposure to 3,4-DCA, suggesting that this enzyme is an important factor in 3,4-DCA degradation. The activity toward 4-methylcatechol was 53.1% that of catechol, while the activity toward 3-methylcatechol, 4-chlorocatechol and 4,5-chlorocatechol was 18.1, 33.1, and 6.9%, respectively.

Scavenging Effect of Extract from Perilla frutescens and Rosmarinic Acid from Free Radical and Lipid Peroxidation

  • Wu, Ting Ting;Hwang, Bo-Ra;Cho, Eun-Ju
    • Preventive Nutrition and Food Science
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    • v.16 no.3
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    • pp.224-229
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    • 2011
  • The radical scavenging activity and inhibition effect from lipid peroxidation induced by peroxyl radical of methanol extract from Perilla frutescens and its active compound, rosmarinic acid (RA), were investigated in vitro. The treatment of extract and RA scavenged 1,1-diphenyl-2-picrylhydrazyl, hydroxyl radical (${\cdot}OH$) and nitric oxide in a concentration-dependent manner. In particular, the extract and RA showed strong radical scavenging activity against ${\cdot}OH$, the most toxic and reactive radical. In addition, Perilla frutescens and RA effectively inhibited lipid oxidation induced by sodium nitroprusside and 2,2'-azobis(2-aminopropane) dihydrochloride, determined by the ferric thiocyanate method. The present results suggest that Perilla frutescens and RA play a protective role against oxidative stress induced by free radical and lipid peroxidation.

Synthesis and Cytotoxicity of 4-Carbamoyloxymethyl-1-azaanthraquinones (4-카바모일옥시메틸-1-아자안트라퀴논 유도체들의 합성 및 세포독성)

  • Lee, Hee-Soon;Lee, Seung-Il;Hong, Seoung-Soo;Cho, Jung-Sook;Kim, Young-Ho
    • YAKHAK HOEJI
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    • v.42 no.5
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    • pp.507-512
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    • 1998
  • In the course of developing novel antitumor intercalating agents. We synthesized 4-carbamoyloxymethyl-l-azaanthraquinones 7-12, incorporating the latent alkylating functi onality. These compounds were designed to explore the effect of substituent on the nitrogen of carbamate. The target compounds were prepared by hetero Diels-Alder reaction as a key step followed by functionalization of benzylic methyl to the desired substituents. Growth inhibitory studies of the azaanthraquinones were conducted in vitro against human cancer cell lines (SNU-354; liver and MCF7; breast) and human epidermoid carcinoma cells that are sensitive (KB-3-1) and multidrug-resistant (KB-V-1). The compounds were less potent than doxorubicin against sensitive cell lines. However, the most active compound 12 was not cross-resistant with doxorubicin against KB-V-1.

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Antitcoagulant and antiplatelet activities of scolymoside

  • Yoon, Eun-Kyung;Ku, Sae-Kwang;Lee, Wonhwa;Kwak, Soyoung;Kang, Hyejin;Jung, Byeongjin;Bae, Jong-Sup
    • BMB Reports
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    • v.48 no.10
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    • pp.577-582
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    • 2015
  • Cyclopia subternata is a medicinal plant commonly used in traditional medicine to relieve pain. Here, the anticoagulant effects of scolymoside, an active compound in C. subternata, were examined by monitoring activated partial thromboplastin time (aPTT), prothrombin time (PT), and the activities of thrombin and activated factor X (FXa). The effects of scolymoside on plasminogen activator inhibitor type 1 (PAI-1) and tissue-type plasminogen activator (t-PA) expression were evaluated in tumor necrosis factor (TNF)-α-activated human endothelial cells. Treatment with scolymoside resulted in prolonged aPTT and PT and the inhibition of thrombin and FXa activities and production. In addition, scolymoside inhibited thrombin-catalyzed fibrin polymerization and platelet aggregation. Scolymoside also elicited anticoagulant effects in mice, including a significant reduction in the PAI-1 to t-PA ratio. Collectively, these findings indicate that scolymoside possesses anticoagulant activities and could be developed as a novel anticoagulant.

Numerical Simulation of the Odor Spreading in a Factory (공장에서 퍼지는 냄새에 관한 수치계산적 연구)

  • Vincent, Lijo;Song, Eun-Hwa;Nam, Hyun-Kyu;Shin, Choon-Sik;Kim, Heuy-Dong
    • Proceedings of the KSME Conference
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    • 2008.11b
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    • pp.2540-2543
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    • 2008
  • Liquid crystal displays (LCD's) are continuously coated with some chemicals in the clean room of a factory. Spreading of these chemicals is causing serious problems both in controlling clean room quality as well as to the workers inside the factory. It is required to alleviate or properly control the offensive odor which is mainly composed of propylene glycol mono ethyl acetate, novolak resin and photo active compound. The control strategy employed is to bleed the offensive odor gas out the clean room. A full scale 3D CFD model was created with anisotropic porous media, chemical species transport with no volumetric reaction, and thermal diffusion with propane gas (tracer gas) to simulate the odor spreading. A segregated implicit solver with standard k-$\varepsilon$ model is employed. The detailed CFD analysis made it possible to develop an effective method of ventilating the coater room and optimizing their capacities.

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Inhibitory effects of Cnidium officinale extracts on $\alpha-MSH$ induced melanogenesis

  • Lee, Ghang-Tai;Lee, Jeong-No;Lee, Kwang-Sik;Jeong, Ji-Hean;Jo, Byoung-Kee
    • Proceedings of the SCSK Conference
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    • 2003.09b
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    • pp.44-49
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    • 2003
  • $\alpha$-MSH plays an important role in UV induced melanogenesis in human skin. It is believed to exert its effects by binding to $\alpha$-MSH receptor that in turn activates adenylate cyclase and increase melanocyte proliferation, dendricity and melanogenesis. In this study, we evaluated plant extracts showing the inhibitory activity on $\alpha$-MSH induced melanogenesis. The Cnidium officinale extracts showed high inhibitory activity on $\alpha$-MSH induced melanogenesis. It ($50{\mu}\textrm{g}$/ml) inhibited the melanin synthesis activated by $\alpha$-MSH in B-16 melanoma cells. Also, we isolated active compound from C. officinale extracts by Mass spectrophotometer, HPLC. It was identified as Senkyunolide A. It showed the same inhibitory activity as C. officinale extracts at the lower concentration. Finally, Senkyunolide A from Cnidium officinale extracts could playas $\alpha$-MSH antagonist and be used as a strong ingredient for skin whitening cosmetics.

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Mechanism Studies of Substituted Triazol-1-yl-pyrimidine Derivatives Inhibition on Mycobacterium tuberculosis Acetohydroxyacid Synthase

  • Chien, Pham Ngoc;Jung, In-Pil;Reddy, Katta Venugopal;Yoon, Moon-Young
    • Bulletin of the Korean Chemical Society
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    • v.33 no.12
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    • pp.4074-4078
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    • 2012
  • The first step in the common pathway for the biosynthesis of branched chain amino acids is catalyzed by acetohydroxyacid synthase (AHAS). The AHAS is found in plants, fungi and bacteria. With an aim to identify new anti-tuberculosis drugs that inhibit branched chain amino acid biosynthesis, we screened a chemical library against Mycobacterium tuberculosis AHAS. The screening identified four compounds, AVS 2087, AVS 2093, AVS 2236, and AVS 2387 with $IC_{50}$ values of 0.28, 0.21, 3.88, and $0.25{\mu}M$, respectively. Moreover, these four compounds also showed strong inhibition against reconstituted AHAS with $IC_{50}$ values of 0.37, 0.26, 1.0, and $1.18{\mu}M$, respectively. The basic scaffold of the AVS group consists of 1-pyrimidin-2-yl-1H-[1,2,4]-triazole-3-sulfonamide. The most active compound, AVS 2387, showed the lowest total interaction energy -8.75 Kcal/mol and illustrates its binding mode by hydrogen bonding with $H_{\varepsilon}$ of Gln517 with the distance of $2.24{\AA}$.

Virtual Screening of Penicillin-derived Inhibitors for the Metallo-β-lactamase from Bacillus cereus

  • Lee, Jong-Sun;White, Ethan;Kim, Sang-Gon;Kim, Sung-Kun
    • Bulletin of the Korean Chemical Society
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    • v.31 no.12
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    • pp.3644-3652
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    • 2010
  • The metallo-$\beta$-lactamases ($M{\beta}Ls$) are clinically significant enzymes which readily hydrolyze most $\beta$-lactam antibiotics. Discovering potential inhibitors for the $M{\beta}Ls$ is an expensive, time consuming endeavor. Virtual screening can sieve out inhibitor candidates with incompatible features prior to synthesis, decreasing these costs. Using Autodock 4.0, the binding locations and energies of four previously-studied potential inhibitors and four additional compounds obtained from the National Cancer Institute (NCI) database were computationally calculated. Based on the docking models of these eight compounds, we then designed several hypothetical inhibitor structures, compounds A through F, and performed their respective docking experiments. The docking results for compound F showed that it binds to the zinc containing active sites with a lowest predicted binding energy of -6.70 kcal/mol, suggesting F is the most likely potential $M{\beta}L$ inhibitor.

Proliferative and Differentiative Effects of Trachelogenin Isolated from Germinated Safflower (Carthamus tinctorius) Seeds on Calvarial Bone Cells

  • Kim, Eun-Ok;Kim, Kyoung-Soon;Lee, Won-Jung;Choi, Sang-Won
    • Food Science and Biotechnology
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    • v.18 no.3
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    • pp.689-693
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    • 2009
  • Germination is well-known to enhance the digestibility, functionality, and palatability of plant seeds. To examine the functionality of germinated-safflower seed (GSS), proliferative and differentiative effects of GSS extract on the mouse calvarial bone cells were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolinbromide (MTT) assay and alkaline phosphatase activity, respectively. Water extract of GSS increased dose-dependently proliferative and differentiative effects on calvarial bone cell, and its effects were stronger than those of ungerminated-safflower seeds (UGSS) extract. One major component was isolated from GSS extract by a series of purification procedure of solvent fractionation, Diaion HP-20, and Sephadex LH-20 column chromatographies. Its chemical structure was identified as trachelogenin (TC) by nuclear magnetic resonance (NMR) and mass spectrometry (MS) spectral analysis. Trachelogenin showed significant proliferative (125.7%) and differentiative (132.1%) effects on calvarial bone cells at $10^{-8}M$, and its effects were significantly higher than those of $17{\beta}-estradiol\;(E_2)$. TC was found to be a major active compound responsible for high proliferative and differentative effects of the water extract of GSS. Therefore, these results suggest that TC in GSS may be useful as potential therapeutic agent for the prevention and treatment of bone loss.