• 제목/요약/키워드: Active chemical

검색결과 2,296건 처리시간 0.031초

가상 검색 및 시험관 시험을 이용한 총명탕 중 주성분들에 대한 약물작용 및 대사 예측 (In silico Prediction and In vitro Screening of Biological Activities and Pharmacokinetics for the Major Compounds in Chong Myung Tang)

  • 권영이
    • 약학회지
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    • 제51권6호
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    • pp.463-468
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    • 2007
  • Chong Myung Tang is consisted of three medicinal herbs (Acori Graminei Rhizoma, Polygalae Radix and Hoelen cum Radix). It has been used as a medicine for the purpose of learning and memory improvement. In this paper, Chong Myung Tang was screened the biological activities for Alzheimer's disease. The extract (70% ethanol) of Acari Graminei Rhizoma (1 mg/ml) showed that acetylcholinesterase (AChE) and amyloid beta ($A{\beta}$) peptide aggregation inhibitory potency are 43.1% and 76.5%, respectively. The extract of Polygalae Radix showed inhibitory activity against $A{\beta}_{1-42}$ peptide aggregation (51.5%). To predict the drug-likeness, oral absorption ability; blood-brain barrier (BBB) penetraion rate, mutagenecity and carcinogenicity; in silico screening was performed against 16 compounds in the three medicinal herbs. According to the results, all compounds have appropriate chemical structures as medicines. The six compounds in Acori Graminei Rhizoma and the five compounds in Hoelen cum Radix showed excellent oral absorption rate and BBB penetration rate. The four compounds in Polygalae Radix showed excellent oral absorption rate, but their BBB penetration was presented low rate. And, the extract of Hoelen cum Radix didn't show AChE and $A{\beta}_{1-42}$ peptide aggregation inhibitory activities in vitro. Therefore, their activity in brain may be other mechanism. According to all of the results, in silico prediction technology is convenient and effective to determine biological active compounds in medicinal herbs.

Aspergillus niger ATCC 16513과 대두(Glycine max. L) $\alpha$-galactosidase의 kinetic 성질 (Kinetic Properties of $\alpha$-Galactosidase from Aspergillus niger ATCC 16513 and Soybean(Glycine max. L))

  • 금종화;이종수;신철승
    • 자연과학논문집
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    • 제5권1호
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    • pp.53-57
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    • 1992
  • Aspergillus niger ATCC 16513과 대두(Glycine max. L)의 정제 $\alpha$-galactosidase를 사용 하여 몇가지 이들의 kinetic성질을 조사 하였다. Asp. niger $\alpha$-galactosidase의 raffinose와 stachyose에 대한 Km값은 각각 37.0mM과 55.5mM, 대두 $\alpha$-galactosidase는 50.0mM과 55.5mM로서 PNPG보다 이들에 대한 친화성이 적었다. 또한 galactose는 ASP. niger와 대두 $\alpha$-galactosidase 모두의 활성을 저해 하였으나 2-mereaptoethanol과 L-cystene은 대두 $\alpha$-galatosidase의 활성만을 약간 저해 하였다. Asp. niger와 대두 $\alpha$-galactosidase의 활성에 관여하는 아미노산은 diethyl pyrocarbonate에 의한 화학수식에 의하여 histidine임이 확인 되었고 Asp. niger $\alpha$-galactosidase의 1mole당 아미노산 잔기수는 모두 902개, 대두$\alpha$-galactosidase는 286개 이었다.

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Alantolactone의 구조와 생물학적 활성 (Relationship Between Biological Activity and Structure of Alantolactone)

  • 권영명
    • Journal of Plant Biology
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    • 제17권2호
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    • pp.69-83
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    • 1974
  • To elucidate the relationship between chemical structure and biological activity of alantolactone, and also to investigate the relationship between the growth of cells and the respiration of Chlorella pyrenoidosa affected by alantolactone, alantolactone and isoalantolactone were isolated from Inula helenium L., and di-, and tetrahydroalantolactones were prepared by the hydrogenation. At a concentration of 5$\times$10-5M alantolactone, the growth rate of Chlorella was greatly reduced. The viability of cells was also reduced over 50% within 2 hr at a concentration of 2.5$\times$10-4M alantolactone. However, oxygen uptake was increased by 20% over 3 hr. And 14CO2 production from glucose-1-14C, glucose-6-14C and 14C-acetate-U.L. was also increased by alantolactone. Biological activityof alantolactone was significantly reduced by cysteine, reduced glutathione or cystine but not by tryptophan or histidine. It was detected by spectrophotometrically and by TLC that alantolactone was also reacted with thiols except cystine. The solution of alantolactone reached with thiol gave the UV absorption spectrum of $\alpha$-saturated ${\gamma}$-lactone, and most of SH groups were disappeared by the addition reaction. From the reaction mixture of alantolactone and cysteine, a lactone adduct was isolated and purified. Isoalantolactone had shown similar activity as alantolactone, however, it was appeared that di-, and tetrahydroalantolactones were not only inactive biologically but also in vitro. It was concluded that there was no correlationship between increased respiration rate and mortality of Chlorella. During the respiration TCA cycle was activated, however it was uncertain that the activation of EMP or HMP was also appeared. Alantolactone and isoalantolactone were biologically active compounds but others were inactive. The reactivity of $\alpha$-methylene ${\gamma}$-lactone moiety toward SH group was principally responsible for its biological activity in sesquiterpene lactones.

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Anti-Metastatic Activity of Glycoprotein Fractionated from Acanthopanax senticosus, Involvement of NK-cell and Macrophage Activation

  • Ha, Eun-Suk;Hwang, Soo-Hyun;Shin, Kwang-Soon;Yu, Kwang-Won;Lee, Keyong-Ho;Choi, Joo-Sun;Park, Woo-Mun;Yoon, Taek-Joon
    • Archives of Pharmacal Research
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    • 제27권2호
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    • pp.217-224
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    • 2004
  • Previously, we reported that water-extracted Acanthopanax senticasus exhibited anti-meta-static activity by stimulating the immune system. In this study, we fractionated glycoproteins (EN-SP) from the soluble protein layer (GF-AS) of A. senticasus and determined their basic chemical properties. We also investigated the anti-tumor and immunostimulating activities of the fractionated glycoprotein, EN-SP. We found that intravenous (i.v.) administration of GF-AS dramatically inhibited metastasis of colon26-M3.1 carcinoma cells to the lung in a dose-dependent manner. In vitro analysis showed GF-AS to enhance the proliferation of splenocytes. GF-AS also stimulated peritoneal macrophage, which was followed by the production of various cytokines such as IL-1$\beta$, TNF-$\alpha$, IL-12 and IFN-${\gamma}$. Furthermore, the production of these cytokines was partially blocked when peritoneal macrophage was cultured with the polyclonal antibodies against GF-AS. The depletion of NK cells by rabbit anti-asialo GM1 serum partly abolished the inhibitory effect of GF-AS on lung metastasis of colon26-M3.1 cells. Using gel filtration, EN-SP, an active glycoprotein fraction, is isolated from GF-AS. While both GF-AS and EN-SP stimulated the proliferatation of splenocytes of normal mice, EN-SP showed higher anti-metastatic activity and more potently stimulated the proliferation of splenocytes compared to GF-AS. These results suggest the use of EN-SP, the fractionated glycoprotein from A. senticasus, can be used as a therapeutical reagent to prevent or inhibit tumor metastasis.

DeSOx/DeNOx 효율 개선을 위한 펄스 코로나 방전하에서 기체미립자 전환반응의 적용 (Application of Gas to Particle Conversion Reaction to increase the DeSOx/DeNOx Efficiency under Pulsed Corona Discharge)

  • 최유리;김동주;김교선
    • 산업기술연구
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    • 제18권
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    • pp.249-258
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    • 1998
  • In this paper, we investigated the post-combustion removal of nitrogen oxide($NO_x$) and sulfur oxide($SO_x$) which is based on the gas to particle conversion process by the pulsed corona discharge. Under normal pressure, the pulsed corona discharge produces the energetic free electrons which dissociate gas molecules to form the active radicals. These radicals cause the chemical reactions that convert $SO_x$ and $NO_x$ into acid mists and these mists react with $NH_3$ to form solid particles. Those particles can be removed from the gas stream by conventional devices such as electrostatic precipitator or bag filter. The reactor geometry was coaxial with an inner wire discharge electrode and an outer ground electrode wrapped on a glass tube. The simulated flue gas with $SO_x$ and $NO_x$ was used in the experiment. The corona discharge reactor was more efficient in removing $SO_x$ and $NO_x$ by adding $NH_3$ and $H_2O$ in the gas stream. We also measured the removal efficiency of $SO_x$ and $NO_x$ in a cylinder type corona discharge reactor and obtained more than 90 % of removal efficiency in these experimental conditions. The effects of process variables such as the inlet concentrations of $SO_x$, $NH_3$ and $H_2O$, residence time, pulse frequencies and applied voltages were investigated.

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IQGAP1, a signaling scaffold protein, as a molecular target of a small molecule inhibitor to interfere with T cell receptor-mediated integrin activation

  • Li, Lin-Ying;Nguyen, Thi Minh Nguyet;Woo, Eui Jeon;Park, Jongtae;Hwang, Inkyu
    • 농업과학연구
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    • 제47권2호
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    • pp.361-373
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    • 2020
  • Integrins such as lymphocyte function-associated antigen -1 (LFA-1) have an essential role in T cell immunity. Integrin activation, namely, the transition from the inactive conformation to the active one, takes place when an intracellular signal is generated by specific receptors such as T cell receptors (TCRs) and chemokine receptors in T cells. In an effort to explore the molecular mechanisms underlying the TCR-mediated LFA-1 activation, we had previously established a high-throughput cell-based assay and screened a chemical library deposited in the National Institute of Health in the United States. As a result, several hits had been isolated including HIKS-1 (Benzo[b]thiophene-3-carboxylic acid, 2-[3-[(2-carboxyphenyl) thio]-2,5-dioxo-1-pyrrolinyl]-4,5,6,7-tetrahydro-,3-ethyl ester). In an attempt to reveal the mode of action of HIKS-1, in this study, we did drug affinity responsive target stability (DARTS) assay finding that HIKS-1 interacted with the IQ motif containing GTPase activating protein 1 (IQGAP1), a 189 kDa multidomain scaffold protein critically involved in various signaling mechanisms. Furthermore, the cellular thermal shift assay (CETSA) provided compelling evidence that HIKS-1 also interacted with IQGAP1 in vivo. Taken together, it can be concluded that HIKS-1 interferes with the TCR-mediated LFA-1 activation by interacting with IQGAP1 and thereby disrupting the signaling pathway for LFA-1 activation.

유치열에서 Chlorhexidine Varnish와 Polyurethane Sealant의 Streptococcus mutans억제 효과에 대한 연구 (THE INHIBITORY EFFECT OF CHLORHEXIDINE VARNISH AND POLYURETHANE SEALANT ON STREPTOCOCCUS MUTANS IN THE PRIMARY DENTITION)

  • 이성혁;장기택;김종철
    • 대한소아치과학회지
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    • 제25권1호
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    • pp.116-126
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    • 1998
  • Numerous chemical agents have been developed to reduce the activity of cariogenic bacteria. Of these, chlorhexidine is acknowledged as the most effective. Gel and mouthrinse have been the traditional method of its application in the mouth. It has been reported that chlorhexidine varnish has prolonged inhibitory effect on the number of streptococcus mutans in saliva and plaque. Recently, chlorhexidine varnish and polyurethane sealant have been developed to promote prolonged anticariogenic effect of chlorhexidine. Products containing 10% chlorhexidine varnish and polyurethane sealant have been developed to prevent caries by reducing the number of streptococcus mutans in the oral cavity. The purpose of this study is to investigate the inhibitory effect of chlorhexidine varnish and polyurethane sealant on streptococcus mutans in the primary dentition. Children with primary dentition containing no active carious lesion were divided into two groups. To the experimental group (n=11), chlorhexidine varnish and polyurethane sealant ($Chlorzoin^{(R)}$, Knowell Therapeutic Technologies, Inc. Canada.) was applied once a week for four weeks according to the manufacturer's instruction. Only oral prophylaxis was performed on the control group(n=7). Caries activity was measured after using $Cariescreen^{(R)}$SM (Knowell Therapeutic Technologies, Inc. Canada,) to incubate streptococcus mutans before and 5, 12, 24 weeks after initial varnish application. The following results were observed.; 1. There was statistically significant decrease in the number of streptococcus mutans in the experimental group for 5 weeks(P<0.01), 12 weeks(P<0.05) after the initial application. but, by 24 weeks significant difference had disappeared. 2. As the inhibitory effect of chlorhexidine varnish and polyurethane sealant application is not everlasting, reapplication at 12-24 weeks should be needed.

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탄소나노 튜브위에 성장된 Pd 및 Pt 나노 입자의 제조 및 특성 (Synthesis and Property of Carbon Nanotube-Supported Pd and Pt Nanoparticles)

  • 김형균;이임렬
    • 한국재료학회지
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    • 제19권4호
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    • pp.192-197
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    • 2009
  • Carbon nanotubes (CNT) were used as a catalyst support where catalytically active Pd and Pt metal particles decorated the outside of the external CNT walls. In this study, Pd and Pt nanoparticles supported on $HNO_3$-treated CNT were prepared by microwave-assisted heating of the polyol process using $PdCl_2$ and $H_2PtCl_6{\codt}6H_2O$ precursors, respectively, and were then characterized by SEM, TEM, and Raman. Raman spectroscopy showed that the acid treated CNT had a higher intensity ratio of $I_D/I_G$ compared to that of non-treated CNT, indicating the formation of defects or functional groups on CNT after chemical oxidation. Microwave irradiation for total two minutes resulted in the formation of Pd and Pt nanoparticles on the acid treated CNT. The sizes of Pd and Pt nanoparticles were found to be less than 10 nm and 3 nm, respectively. Furthermore, the $SnO_2$ films doped with CNT decorated by Pd and Pt nanoparticles were prepared, and then the $NO_2$ gas response of these sensor films was evaluated under $1{\sim}5\;ppm$ $NO_2$ concentration at $200^{\circ}C$. It was found that the sensing property of the $SnO_2$ film sensor on $NO_2$ gas was greatly improved by the addition of CNT-supported Pd and Pt nanoparticles.

금 처리를 통한 PEDOT 마이크로튜브 전극의 과산화수소 검출 특성 향상 (Enhanced Sensitivity of PEDOT Microtubule Electrode to Hydrogen Peroxide by Treatment with Gold)

  • 박종서;손용근
    • 폴리머
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    • 제38권6호
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    • pp.809-814
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    • 2014
  • 전류 감응형 바이오센서에 응용하기 위해 전도성 고분자 마이크로튜브 어레이를 제작하였다. Poly(3,4-ethylenedioxythiophene)/poly(4-styrenesulfonic acid)(PEDOT/PSS) composite을 전도성 접착제로 하여 템플릿을 전극에 고정한 후 EDOT을 전기화학적으로 중합하였다. 마이크로튜브 어레이는 자체의 넓은 표면적으로 인해 감도 높은 바이오센서로 응용될 수 있으나, 주요 표적물질 중의 하나인 과산화수소에 대한 전기화학적 반응이 느렸다. 과산화수소 산화에 대한 감도를 향상시키기 위해 어레이 전극에 금을 도포하였다. 증착법과 전기화학적 석출법 두 가지 방법을 시도하여 금을 처리하였는데, 이렇게 처리한 전극은 모두 과산화수소에 대한 반응이 크게 향상되었다. 따라서 전도성 고분자 마이크로튜브 어레이에 금을 도포함으로써 과산화수소를 표적물질로 하는 감도 높은 바이오센서 제작이 가능할 것으로 기대된다.

Radiation Technology in the Preparation of Polyethylene Oxide Hydrophilic Gels and Immobilization of Proteases for Use in Medical Practice

  • E.I.Vereschagin;Han, Do-Hung;A.W.Troitsky;O.V.Grishin;S.E.Petrov;E.P.Gulyaeva;L.A.Bogdanova;M.V.Korobeinikov;V.L.Auslender
    • Archives of Pharmacal Research
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    • 제24권3호
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    • pp.229-233
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    • 2001
  • This Paper deals with the development of a technology for making a hydrophilic gel of Polyethylene oxide reception in which radiating ability is employed to cause cross-linking of Polymers in a water solution. The gel of polyethylene oxide was shown to be nontoxic contain 5-50% of polymer and be useful in composite medicinal forms along with biologically active substances including Bac. subtilis proteases. Proteases immobilized in the gel possess high thermal stability and proteolytic activity and are readily applied in medicine. The effect of immobilized proteolytic and glucolytic enzymes of Bac. subtillis (Immozimase) on the warm ischemia-reperfusion (I/R) which can cause hepatic and jejunum injury was also studied. These enzymes were immobilized on water-soluble polymer polyethylene glycol by means of an electron beam. The number of degraanulated mast cells as well as serum ALT after I/R in the group with Immozimase was decreased to almost half as compared with the control group. Pretreatment with Immozimase resulted in significant reduction of hepatic and gut neutrophil accumulation as compared with control animals. It was concluded that Immozimase has a protective effect for hepatic and gut ischemia/reperfusion, and this effect seems to be associated with prevention of leukocyte accumulation .

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