• 제목/요약/키워드: Structure-Activity Relationship

검색결과 543건 처리시간 0.035초

Alkamides from Piper longum and Piper nigrum as Inhibitors of IL-6 action

  • Lee, Seung-Woong;Kim, Myo-Sun;Park, Mi-Hye;Park, Su-Jin;Lee, Woo-Song;Chang, Jong-Sun;Rho, Mun-Chual
    • Bulletin of the Korean Chemical Society
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    • 제31권4호
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    • pp.921-924
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    • 2010
  • Blocking of IL-6 has been postulated to be an effective therapy in the pathogenesis of several inflammatory diseases. The current study was performed to examine the potential effects of alkamides isolated from P. longum and P. nigrum on IL-6 induced Stat3 activation and identify the structure-activity relationship of these alkamides in human hepatoma cells. Among 10 alkamides isolated from P. longum and P. nigrum, compounds 6, 7 and 9 were identified as strong inhibitors of IL-6 action, which inhibit IL-6 induced Stat3-dependent luciferase activities. These inhibitory activities were positively influenced by the presence of piperidine moiety.

친환경적 One Pot 합성, In Vitro에서 Morpholino Pyrimidines의 분광학적 특성과 항균성 및 항진균성 (A Green Chemical Approach towards the 'One-Pot' Synthesis, Spectral Characterization and in Vitro Antibacterial and Antifungal Activities of Morpholino Pyrimidines)

  • Kanagarajan, V.;Thanusu, J.;Gopalakrishnan, M.
    • 대한화학회지
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    • 제53권6호
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    • pp.731-741
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    • 2009
  • $NaHSO_4.SiO_2$ 촉매를 이용한 microwave 및 무수조건하에서 새로운 morpholino pyrimidines의 One-pot합성이다. 합성된 모든 화합물을 이용하여 in vitro에서 임상학적인 단리된 박테리아 품종 즉 Bacillus subtilis, Bacillus cerues, Micrococcus luteus , Salmonella typhii에 대해 항균성을 살펴보았고, 균품종 즉 Aspergillus niger, Candida 6, Candida 51에 대해 항진균성을 살펴보았다. 미생물 결과에 대한 합성된 화합물의 구조적 활동성의 관련성에 대해 토론하였다.

3D QSAR Studies on Cinnamaldehyde Analogues as Farnesyl Protein Transferase Inhibitors

  • Nack-Do, Sung;Cho, Young-Kwon;Kwon, Byoung-Mog;Hyun, Kwan-Hoon;Kim, Chang-Kyung
    • Archives of Pharmacal Research
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    • 제27권10호
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    • pp.1001-1008
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    • 2004
  • Three-dimensional quantitative structure-activity relationship (3D-QSAR) studies on 59 cinnamaldehyde analogues as Farnesyl Protein Transferase (FPTase) inhibitors were investigated using comparative molecular field analysis (CoMFA) with the PLS region-focusing method. Forty-nine training set inhibitors were used for CoMFA with two different grid spacings, $2{\AA}\;and\;1{\AA}$ Ten compounds, which were not used in model generation, were used to validate the CoMFA models. After the PLS analysis, the best predictive CoMFA model showed that the cross-validated value $(r^2_{cv})$ and the non-cross validated conventional value$(r^2_{ncv})$ are 0.557 and 0.950, respectively. From the CoMFA contour maps, the steric and electrostatic properties of cinnamaldehyde analogues can be identified and verified.

사회자본 정도 및 건강행동이 한국인의 주관적 건강에 미치는 영향 분석 (The Influence of Social Capital and Health Behaviors on Self-rated Health in South Korea)

  • 송예리아;남은우
    • 보건교육건강증진학회지
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    • 제26권3호
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    • pp.1-13
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    • 2009
  • Objectives: This study intended to examine the influence of social capital and health behaviors on self-rated health in Korea. Methods: The data of the social statistics survey that the Korea National Statistical Office conducted in 2006 were chosen and 36,266 people from them, who were 30~59 years old were sampled. This paper made logistic regression analysis to examine the effect of social capital and health behaviors on self-rated health. Results: Odds ratios of social capital are family structure(1.321), marriage(1.214), satisfaction with family relationship(2.207), reliability of institutions(1.307), economic support(1.199), citizen's participation(1.531), and religious activity(1.138). Odds ratios of health behaviors are meal(1.431), exercise(1.356), and no drinking(0.648). Conclusion: Based on the results, this paper can suggest that the plan of keeping and building up social capital should be considered in the whole aspects of the society and the project of moderation in drink is required to consider social culture more.

Assessment of the Influence of Physical Impairments on Activities in Persons With Stroke

  • Woo, Young-Keun
    • 한국전문물리치료학회지
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    • 제18권4호
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    • pp.11-18
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    • 2011
  • The aim of this study was to analyze the relationship between physical impairments and daily activities on the basis of the outcome measurements in stroke patients. Seventy-six stroke patients participated in this study. Two physical therapists evaluated 3 clinical common measurements, i.e., the Fugl-Meyer Assessment (FMA), the Berg Balance Scale (BBS), and the Functional Independence Measure (FIM). Multiple regression analysis was used, as the dependent variables were the BBS and FIM; the independent variables were post-stroke duration, FMA of Upper Extremity (FMU), and FMA of Lower Extremity (FML). In the regression equation of the BBS, the coefficient of determination ($R^2$) was .383, and the FML was found to be the most important variable for determining the BBS score. In the regression equation of the FIM, $R^2$ was .531, and the FML was found to be the most important variable for determining the FIM. These results suggest that there is a need to determine the function of activities on the basis of the physical impairments of stroke patients. More variable measurement tools on the levels of body function and structure, as well as activity limitations are required.

지속 감항성 유지 프로그램 운영 경험의 항공기 설계와 인증 단계 적용 (Application of Operational Experience of the Continuous Airworthiness Program at the stage of Aircraft Design and Certification)

  • 구민성
    • 한국항공운항학회지
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    • 제21권3호
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    • pp.9-14
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    • 2013
  • Continuous airworthiness system is comprised of regulations and procedures to assure the safety and reliability through the total stage of development, certification and operation of aircraft. The purpose of this system is not only to provide the guidelines that should be kept by manufacturers and operators, but also to evaluate the maintenance capability in every activity of safety related procedures. During the development process of the mid and large size aircraft, operational experience should be reflected systematically for a safer and more reliable product by using the meaningful data base from operation. The relationship of safety roles between manufacturer and operator is mutually complementary, and the roles of each function have an influence to the next step. Overall structure of the procedure contains the concept of continuous analysis and feedback to achieve highest degree of safety and reliability during the entire life of aircraft. Finally, this paper describes how the feedback is made and used for aircraft design from operational experience under the continuous analysis and surveillance system.

Functional Studies of Cysteine Residues in Human Glutathione S-Transferase P1-1 by Site-Directed Mutagenesis

  • 박희중;이광수;공광훈
    • Bulletin of the Korean Chemical Society
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    • 제22권1호
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    • pp.77-83
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    • 2001
  • To gain further insight into the relationship between structure and function of glutathione S-transferase (GST), the four cysteine mutants, C14S, C47S, C101S and C169S, of human GST P1-1 were expressed in Escherichia coli and purified to electrophoretic homogeneity by affinity chromatography on immobilized glutathione (GSH). The catalytic activities of the four mutant enzymes were characterized with five different substrates as well as by their binding to four different inhibitors. Cys14 seems to participate in the catalytic reaction of GST by stabilizing the conformation of the active-site loop, not in the GSH binding directly. The substitution of Cys47 with serine significantly reduces the affinity of GSH binding, although it does not prevent GSH binding. On the other hand, the substitution of Cys101 with serine appears to change the binding affinity of electrophilic substrate by inducing a conformational change of the $\alpha-helix$ D. Cys169 seems to be important for maintaining the stable conformation of the enzyme. In addition, all four cysteine residues are not needed for the steroid isomerase activity of human glutathione S-transferase P1-1.

Properties and pozzolanic reaction degree of tuff in cement-based composite

  • Yu, Lehua;Zhou, Shuangxi;Deng, Wenwu
    • Advances in concrete construction
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    • 제3권1호
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    • pp.71-90
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    • 2015
  • In order to investigate the feasibility and advantage of tuff used as pozzolan in cement-based composite, the representative specimens of tuff were collected, and their chemical compositions, proportion of vitreous phase, mineral species, and rock structure were measured by chemical composition analysis, petrographic analysis, and XRD. Pozzolanic activity strength index of tuff was tested by the ratio of the compression strength of the tuff/cement mortar to that of a control cement mortar. Pozzolanic reaction degree, and the contents of CH and bond water in the tuff/cement paste were determined by selective hydrochloric acid dissolution, and DSC-TG, respectively. The tuffs were demonstrated to be qualified supplementary binding material in cement-based composite according to relevant standards. The tuffs possessed abundant $SiO_2+Al_2O_3$ on chemical composition and plentiful content of amorphous phase on rock texture. The pozzolanic reaction degrees of the tuffs in the tuff/cement pastes were gradually increased with prolongation of curing time. The consistency of CH consumption and pozzolanic reaction degree was revealed. Variation of the pozzolanic reaction degree was enhanced with the bond water content and relationship between them appeared to satisfy an approximating linear law. The fitting linear regression equation can be applied to mutual conversion between pozzolanic reaction degree and bond water content.

북경사합원의 공간 변화 분석 - 중국 북경 고대와 근대시기 전통주택의 비교를 중심으로 - (Spatial Variation Analysis of Beijing Siheyuan - Comparison of the Beijing Traditional Housing in ancient and modern China -)

  • 진즈룬;조항만
    • 대한건축학회논문집:계획계
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    • 제35권12호
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    • pp.75-82
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    • 2019
  • After 1840 the first opium war, that changed the social nature and living habitats in China. The purpose of this study is to observe the influence of the war on the plan layout of traditional Chinese residential houses in Beijing Siheyuan. To find out the changes that were made after 1840, and reservation of the past, the space syntax model is used to analyze different social contexts and also compare the ancient and modern residential buildings. The result of the study indicate the following: Before the war, the ancient Siheyuan people's way of life strictly abide by the hierarchy system; External emphasis shows the host's status. However, in modern times, the social status became equal, efficient and harmonious relationship internally, while externally, it arranged the orientation and position of buildings to adapt to the natural environment. However, the boundaries between family members and visitors the emphasis on the courtyard and respect for private life remain unchanged.

고전기에서 후기고전기로의 마야 사회의 변화: 돋을새김의 분석 (A Study of Social Change from Classic to Postclassic)

  • 정혜주
    • 비교문화연구
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    • 제22권
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    • pp.177-201
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    • 2011
  • The Lord of Mayan society was a person who was thought to be able to understand phenomena in the universe. And also the Lord could realize these activities of heaven on Earth through ritual. But the manifested ritual function of lordship was very different depends on Classic and Postclassic period. The Classic Mayan rituals were closely related to personal dignity, specially royal blood tradition meanwhile the Postclassic Mayans focused on public function of ritual. The ritual sacrifices of blood letting from their own body, manifested in Yaxchilan Lintel 24, 25 and 17, were focused on royal family's activity, showing the dignity of royal blood. The same ritual about the birth of family successor was observed at the Structure 5C4 from Postclassic ruin of Chichen Itza. However, this scene in focus, was two representative men and the answer of ancestor, not a special person. Also at the Lintel 1 of Temple of Four Lintels it was observed names of four Lords of Chichen Itza, their relationship, their action of firing to dedicate temple instead of writing long history of great royal family. All above shows that during Postclassic period the lords preferred a public function of their lordship than to dignify some royal persons through ritual.