• 제목/요약/키워드: compound-K

검색결과 8,272건 처리시간 0.041초

Identification of a Novel Small Molecule Inhibitor Against SARS Coronavirus Helicase

  • Cho, Jin-Beom;Lee, Jin-Moo;Ahn, Hee-Chul;Jeong, Yong-Joo
    • Journal of Microbiology and Biotechnology
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    • 제25권12호
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    • pp.2007-2010
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    • 2015
  • A new chemical inhibitor against severe acute respiratory syndrome (SARS) coronavirus helicase, 7-ethyl-8-mercapto-3-methyl-3,7-dihydro-1H-purine-2,6-dione, was identified. We investigated the inhibitory effect of the compound by conducting colorimetry-based ATP hydrolysis assay and fluorescence resonance energy transfer-based double-stranded DNA unwinding assay. The compound suppressed both ATP hydrolysis and double-stranded DNA unwinding activities of helicase with IC50 values of 8.66 ± 0.26 μM and 41.6 ± 2.3 μM, respectively. Moreover, we observed that the compound did not show cytotoxicity up to 80 μM concentration. Our results suggest that the compound might serve as a SARS coronavirus inhibitor.

오갈피나무 잎의 트리테르펜 성분 (Triterpene Components from the Leaves of Acanthopanax sessiliflorus Seem)

  • 류효선;장승엽;육창수;박상용
    • 생약학회지
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    • 제34권4호통권135호
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    • pp.269-273
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    • 2003
  • The leaves of Acanthopanax sessiliflorus Seem. (Araliaceae), which is native plant to Korea, have not been studied yet on triterpene constituents. Three 3,4-seco-lupane triterpenoids (Compound I-III) were isolated from the MeOH extract of this plant using Diaion HP-20P, silica gel and ODS column chromatographes. Based on physicochemical and spectroscopic data, the chemical structures of these compounds were identified as follows ; chiisanogenin (Compound I), chiisanoside (Compound II), $22{\alpha}-hydroxychiisanoside$ (Compound III).

Reverse Engineering of Compound Surfaces Using Boundary Detection Method

  • Cho, Myeong-Woo;Seo, Tae-Il;Kim, Jae-Doc;Kwon, Oh-Yang
    • Journal of Mechanical Science and Technology
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    • 제14권10호
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    • pp.1104-1113
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    • 2000
  • This paper proposes an efficient reverse engineering technique for compound surfaces using a boundary detection method. This approach consists in extracting geometric edge information using a vision system, which can be used in order to drastically reduce geometric errors in the vicinity of compound surface boundaries. Through the image-processing technique and the interpolation process, boundaries are reconstructed by either analytic curves (e. g. circle, ellipse, line) or parametric curves (B-spline curve). In other regions, except boundaries, geometric data are acquired on CMM as points inspected using a touch type probe, and then they are interpolated on several surfaces using a B-spline skinning method. Finally, the boundary edge and the skinned surfaces are combined to reconstruct the final compound surface. Through simulations and experimental works, the effectiveness of the proposed method is confirmed.

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Biophysical study of bioactive-substance conformation and interaction with drugs in solution

  • Yu, Byung-Sul;Lee, Bong-Jin;Sohn, Dong-Hwan
    • Archives of Pharmacal Research
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    • 제8권3호
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    • pp.109-117
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    • 1985
  • The interaction of salicylic acid (S. A.), salicylamide (S,M) with nucleic acid base derivatives such as 9-ethyl adenine (A), 1-cyclohexyl uracil (U), 2', 3'-benzylidine-5' trityl-cytidine (C), gaunosine-2', 3', 5'-isobutylate (G) has been spectroscopically investigated to determine the binding mechanism. NMR and IR spectra were measured in nonpolar solvents. The association constant K of the formation of complex was calculated from the IR spectra. Compounds S. A. and A form a 1:1 or 1:2 cyclic hydrogen-bonded complex depending on the sample concentration. Compounds S. A. and U form a 1:1 or 1:2 hydrogen-bonded complex on the sample concentration. Compounds S. A. and C form a 2:1 hydrogen-bonded complex at low concentration (0.0016M). Compound S. A. binds compound G, but its binding does not completely break the self-association of compound G, Compound S. M. binds compounds A. U. C. G. very weakly.

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Cytotoxicity of Compound K and Ginsenoside $R_{h2}$ against some tumor cells

  • Shin, Ji-Eun;Park, Eun-Kyung;Hong, Yoon-Hee;Kim, Eun-Jin;Lee, Kyung-Tae;Kim, Dong-Hyun
    • 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.160.2-160.2
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    • 2003
  • When ginsenoside $R_{b1}$ and $R_{b2}$ were anaerobically incubated with human fecal microflora, these ginsenosides were metabolized to compound K. When ginsenoside $R_{g3}$ was anaerobically incubated with human fecal microflora, the ginsenoside $R_{g3}$ was metabolized it to ginsenoside $R_{h2}$. Among ginsenosides, compound K and 20(S)-ginsenoside $R_h2$ exhibited the most potent cyotoxicity against tumor cells: 50% cytotoxic concentrations of compound K in the media with and without fetal bovine serum (FBS) were 27.1 - 31.6 mM and0.1 - 0.6 mM, and those of 20(S)-ginsenoside $R_h2$ were 37.5 $\rightarrow$ 50 and 0.7 - 7.1 mM mM, respectively. (omitted)

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플라즈마 산질화처리 조건이 강의 내식성에 미치는 영향 (The Characteristics of Corrosion Resistance during Plasma Oxinitrocarburising for Carbon Steel)

  • 이구현;남기석;이상로;조효석;신평우;박율민
    • 열처리공학회지
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    • 제14권2호
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    • pp.103-109
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    • 2001
  • Plasma nitrocarburising and post oxidation were performed on SM45C steel using a plasma nitriding unit. Nitrocarburising was carried out with various methane gas compositions with 4 torr gas pressure at $570^{\circ}C$ for 3 hours and post oxidation was carried out with 100% oxygen gas atmosphere with 4 torr at different temperatures for various times. It was found that the compound layer produced by plasma nitrocarburising consisted of predominantly ${\varepsilon}-Fe_{2-3}(N,C)$ and a small proportion of ${\gamma}-Fe_4(N,C)$. With increasing methane content in the gas mixture, ${\varepsilon}$ phase compound layer was favoured. In addition, when the methane content was further increased, cementite was observed in the compound layer. The very thin oxide layer on top of the compound layer was obtained by post oxidation. The formation of Oxide phase was initially started from the magnetite($Fe_3O_4$) and with increasing oxidation time, the oxide phase was increased. With increasing oxidation temperature, oxide phase was increased. However the oxide layer was split from the compound layer at high temperature. Corrosion resistance was slightly influenced by oxidation times and temperatures.

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열 산화공정을 이용하여 제작된 고전압 GaN 쇼트키 장벽 다이오드 (High-Voltage GaN Schottky Barrier Diode on Si Substrate Using Thermal Oxidation)

  • 하민우;노정현;최홍구;송홍주;이준호;김영실;한민구;한철구
    • 대한전기학회:학술대회논문집
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    • 대한전기학회 2011년도 제42회 하계학술대회
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    • pp.1418-1419
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    • 2011
  • 차세대 전력 반도체인 고전압 GaN 쇼트키 장벽 다이오드의 역방향 특성을 개선하기 위해서 열 산화공정이 제안되었다. AlGaN/GaN 에피탁시 위에 쇼트키 장벽 다이오드 구조가 제작되었으며, 쇼트키 컨택은 증착 후 $450^{\circ}C$에서 산화되었다. 열 산화공정이 메사 측벽의 AlGaN 및 GaN 표면에 $AlO_x$$GaO_x$를 형성하여 표면으로 흐르는 누설전류를 억제한다. 표면 및 GaN 버퍼를 통한 누설전류는 열 산화 공정 이후 100 ${\mu}m$-너비당 51.3 nA에서 24.9 pA로 1/2000 배 수준으로 감소하였다. 표면 산화물 형성으로 인하여 생성된 Ga-vacancy와 Al-vacancy는 acceptor로 동작하여 surface band bending을 증가시켜 쇼트키 장벽 높이를 증가시킨다. 애노드-캐소드 간격이 5 ${\mu}m$인 제작된 소자는 0.99 eV의 높은 쇼트키 장벽 높이를 획득하여, -100 V에서 0.002 A/$cm^2$의 낮은 누설전류를 확보하였다. 애노드-캐소드 간격이 5에서 10, 20, 50 ${\mu}m$로 증가되면 소자의 항복전압은 348 V에서 396, 606, 941 V로 증가되었다. 열 산화공정은 전력용 GaN 전자소자의 누설전류감소와 항복전압 증가를 위한 후처리 공정으로 적합하다.

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Phenolic and Furan Type Compounds Isolated from Gastrodia elata and their Anti-Platelet Effects

  • Pyo Mi Kyung;Jin Jing Ling;Koo Yean Kyoung;Yun-Choi Hye Sook
    • Archives of Pharmacal Research
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    • 제27권4호
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    • pp.381-385
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    • 2004
  • Nine phenolic ($1\~9$) and two furan type (10, 11) compounds, were isolated from the methanolic extract of the tuber of Gastrodia elata Blume (Orchidaceae) in the course of continuing search for platelet anit-aggregating plant components. Compound 1 was identified as 4,4'-dihy-droxybenzyl sulfone, a novel compound for the best of our knowledge. Compound 10, 5-hydroxymethyl-2-furancarboxaldehyde, was isolated for the first time from this plant. Compound 1 ($IC_{50};\;83{\mu}M$) was about four times more inhibitory to U46619 induced aggregation than ASA ($IC_{50};\340{\mu}M$). Compound 9, 4,4'-dihydroxy-dibenzylether, ($IC_{50};\;5{\mu}M$, $3{\mu}M\;and\;33{\mu}M$, respectively) was $10\~}80$ fold more potent than ASA ($IC_{50};\;420\;{\mu}M,\;53\;{\mu}M\;and\;340\;{\mu}M$ respectively) to collagen, epinephrine and U46619 induced aggregation, although it is less active than ASA to AA induced aggregation.

Ab Initio and Experimental Studies on Dibenzothiazyl-Disulfide

  • Jian, Fang-Fang;Zhang, Ke-Jie;Zhao, Pu-Su;Zheng, Jian
    • Bulletin of the Korean Chemical Society
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    • 제27권7호
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    • pp.1048-1052
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    • 2006
  • Ab initio calculations of the structure, atomic charges and natural bond orbital (NBO) have been performed at HF/6-311G** and B3LYP/6-311G** levels for the title compound of dibenzothiazyl-disulfide. The calculated results show that the two nitrogen atoms have the biggest negative charges and they are the potential sites to react with the metallic ions, which make the title compound become a di-dentate ligand. Vibrational frequencies of the title compound have been obtained and compared with the experimental value and the comparison indicates that B3LYP/6-311G** level is better than HF/6-311G** level to predict the vibrational frequencies for the system studied here. For the title compound, electronic absorption spectra calculated by time?ependent density functional theory (TD-DFT) are more accurate than Hartree-Focksingle-excitation CI (CI-Singles) method. NBO analyses show that the electronic transitions are mainly derived from the contribution of bands $\pi\rightarrow\pi^{*}$. Thermodynamic calculated results show that the formation of the title compound from 2-mercaptobenzothiazole is a spontaneous process at room temperature with the change of free Gibbs being negative value.

Antimicrobial Activity of Chemical Substances Derived from S-Alk(en)yl-L-Cysteine Sulfoxide (Alliin) in Garlic, Allium sativum L.

  • Choi, Mi-Kyung;Chae, Kyung-Yeon;Lee, Joo-Young;Kyung, Kyu-Hang
    • Food Science and Biotechnology
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    • 제16권1호
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    • pp.1-7
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    • 2007
  • Garlic (Allium sativum L.) contains a specific sulfur compound, the S-allyl derivative of L-cysteine sulfoxide, and has long been known for its antimicrobial activity against various microorganisms, including bacteria, fungi, and protozoa. The principal antimicrobial compound of garlic is S-allyl-L-propenethiosulfinate (allicin) which is generated by an enzyme, alliinase (L-cysteine sulfoxide lyase), from S-allyl-L-cysteine sulfoxide (alliin). This compound exists exclusively in Allium as a major non-protein sulfur-containing amino acid. S-Allyl-L-propenethiosulfinate belongs to the chemical group of thiosulfinates and is a highly potent antimicrobial. The potency of garlic extract is reduced during storage since thiosulfinates are unstable and are degraded to other compounds some of which do not have antimicrobial activity. Diallyl polysulfides and ajoene are sulfur compounds derived from allicin that do possess antimicrobial activity. It was recently found that garlic becomes antimicrobial on heating at cooking temperatures, and that the compound responsible for this is allyl alcohol, which is generated from alliin by thermal degradation.