• 제목/요약/키워드: in vivo activity

검색결과 2,537건 처리시간 0.029초

신규 퀴놀론 항균제 DW-116의 in vivo 및 in vivo 항균활성 (Jn vivo and Jn vivo Antibacterial Activity of DW-ll6, a New Quinolone Antibiotic)

  • 황연하;한경오;이진;양희복;정용호;윤성준;이덕근
    • Biomolecules & Therapeutics
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    • 제5권2호
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    • pp.187-193
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    • 1997
  • The in vivo and in vivo antibacterial activity of DW-116, a newly synthesized fluoroquinolone, were compared with those of other quinolones. DW-116 exhibited more potent antibacterial activity than rufloxacin and lower activity than ofloxacin and ciprofloxacin in in vivo assay But, DW-116 particularly showed strong activity against the family of staphylococci including methicillin-sensitive staphylococcus and its activity was more active than that of ciprofloxacin. The time-kill curve studies showed rapid bactericidal activity for DW-116. The post-antibiotic effect of DW-116 was observed between 0.66 and 5 hours. The therapeutic efficacy of DW-116 against respiratory infection with P. aeruginosa was as strong as that of ciprofloxacin and its effect against urinary tract in(traction with E. coli was more effective than rufloxacin. The excellent therapeutic efficacy of DW-116 against these local infections is due to its good pharmacokinetic profiles.

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Effects of Iron, Chelators and Nitrate Concentration on in vivo Fluorescence and Nitrate Reductase of the Red Tide Organism Amphidinium carterae

  • Yang, Sung-Ryull;Song, Hwan-Seok;Pae, Se-Jin;Huh, Sung-Hoi
    • Journal of the korean society of oceanography
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    • 제34권1호
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    • pp.49-57
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    • 1999
  • A red tide organism, Amphidinium carterae was incubated under different iron/chelator and nitrate concentrations to investigate the factors controlling the growth. The chelation capacity played a critical role in regulating the nitrate reductase (NR) activity and in vivo fluorescence of this organism. However, there was a significant difference between the NR activity and in vivo fluorescence in response to trace metals and chelator treatments. In vivo fluorescence was the highest in FeEDTA 10 ${\mu}$M treatments and the lowest in DTPA 10 ${\mu}$M treatments. This indicates that the availability of the trace metal is important in regulating the in vivo fluorescence of this photosynthetic microalgae In contrast, NR activity showed the highest values in trace metal enriched treatments, and trace metal + DTPA treatments showed fairly high NR activities. This suggests that DTPA treatment did not hinder the NR activity as much as it did in vivo fluorescence. In vivo fluorescence and NR activity increased with nitrate concentration of up to 50 ${\mu}$M and remained relatively constant or the rate of increase decreased above that concentration, indicating that initial nitrate concentration of higher than a certain level would not accelerate the growth of A. carterae. Further investigation is needed to elucidate the reason for the difference in timing sequence between the NR and in vivo fluorescence in response to different metal treatments and chelation capacity.

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마늘 성분의 산화방지작용에 대한 연구 제2보 과산소 분해효소의 활성에 미치는 영향 (Studies on antioxidative action of garlic components isolated from garlic Part II: Effects of garlic components on peroxidase and superoxide dismutase activity)

  • 전희정
    • 대한가정학회지
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    • 제24권1호
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    • pp.53-58
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    • 1986
  • In order to study the antioxidative action of the effectient garlic components, peroxidase and superoxide dismutase activity were compared through the in vitro and in vivo experiments. RESULTS : 1. Observing the effects on peroxidase activity of efficient components in vitro, garlic oil, alliin and ethanol fraction showed effective, which was similar to the trend of TBA value, peroxide value and induction time for the first period of lipoperoxide formation in vitro. 2. In vivo experiment with peroxidase activity, the ethanol fraction and garlic oil were effective when intraperitoneally administered as well as orally administered. 3. Considering the superoxide disutase activity in vitro, the garlic oil, alliin and ethanol fraction were effective in efficient components. But non-kaolin fraction inhibited the activity on the contrary. 4. In terms of the efefcts on superoxide dismutase activity in vivo, alliin and garlic oil wee effective in intraperitoneal adminstraton and the ethanol fraction and alliin in oral administration.

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Erythropoietin in vivo 시험법의 in vitro 대체 시험법 확립 (Replacement of the in vivo Bioassay for Erythropoietin with the in vitro Bioassay)

  • 백상훈;김진만;권기성;박송용;허재욱
    • KSBB Journal
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    • 제18권4호
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    • pp.255-260
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    • 2003
  • 현재는 재조합 Erythropoietin의 생물학적 활성을 mouse를 이용한 in vivo bioassay로 실시하고 있으나, 이 방법의 여러가서 불편함으로 인하여, 이를 대체하기 위해 Ba/F3 세포주를 이용한 in vitro assay 방법을 확립하였으나, 위에 상술한 바와 같이 in vitro assay는 erythropoietin의 당분포에 의한 차이를 보이지 않게 때문에, 이를 보완하기 위해서는 in vivo bio-activity와 정량적인 상관관계가 있는 당단백질의 isoform 분석법인 Capillary zone electrophoresis (CZE) 와 sialic acid 함량 결과를 동시에 분석해야 했다. 위의 결과 sialic acid 함량은 erythropoietin 원액에서 10 mol/mol,EPO 이상의 sialic acid 함량을 가져야 되며, CZE 결과는 재조합 erythropoietin이 isoform 분포가 isoform 3의 경우 5.594~0.593%, isoform 4의 경우 31.598~11.704%, isoform 5의 경우 37.033~29.301%, isoform 6의 경우 27.837~18.807%, isoform 7의 경우 17.085~7.824%, isoform 8의 경우 7.642~1.964%을 보여줌과 동시에 isoform 4의 면적은 isoform 5의 면적보다 항상 작아야한다. 이상 두 가지 시험결과와 in vitro assay 결과를 combine해서 in vivo assay를 대체할 수 있다는 좋은 실험적 data를 얻었으므로 이상 위의 3가지 분석법을 활용한 combined in vitro bioassay 법의 기초를 확립하였다.

Fluorescent and bioluminescent nanoprobes for in vitro and in vivo detection of matrix metalloproteinase activity

  • Lee, Hawon;Kim, Young-Pil
    • BMB Reports
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    • 제48권6호
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    • pp.313-318
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    • 2015
  • Matrix metalloproteinases (MMPs) are zinc-dependent endopeptidases that degrade the extracellular matrix (ECM) and regulate the extracellular microenvironment. Despite the significant role that MMP activity plays in cell-cell and cell-ECM interactions, migration, and differentiation, analyses of MMPs in vitro and in vivo have relied upon their abundance using conventional immunoassays, rather than their enzymatic activities. To resolve this issue, diverse nanoprobes have emerged and proven useful as effective activity-based detection tools. Here, we review the recent advances in luminescent nanoprobes and their applications in in vitro diagnosis and in vivo imaging of MMP activity. Nanoprobes with the purpose of sensing MMP activity consist of recognition and detection units, which include MMP-specific substrates and luminescent (fluorescent or bioluminescent) nanoparticles, respectively. With further research into improvement of the optical performance, it is anticipated that luminescent nanoprobes will have great potential for the study of the functional roles of proteases in cancer biology and nanomedicine. [BMB Reports 2015; 48(6): 313-318]

Cefatrizine과 clavulanic acid 병합제의 in vitro 및 in vivo 항균력 (Comparative in vitro and in vivo Antibacterial Activities of Cefatrizine/clavulanic Acid Combination and Other $\beta$-lactam Antibiotics)

  • 최성학;김지영;김계원;김원배;심미자
    • Biomolecules & Therapeutics
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    • 제7권1호
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    • pp.44-53
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    • 1999
  • The resistant strains due to the extended-spectrum $\beta$-lactamase (ESBL) were susceptible to cefatrizine combined with clavulanic acid. The purpose of this study was to evaluate the in vitro and in vivo antibacterial activities of cefatrizine/clavulanic acid (CTRZ/CV) combination at a ratio of 2 : 1 in comparison with cefaclor (CCLO), cefuroxime (CRXM), cefuroxime axetil (CRXMA) and amoxicillin/clavulanic acid (AMXCCV). CTRZ/CV showed good activity against laboratory strains of gram-positive and gram-negative bacteria and exhibited excellent antibacterial activity against $\beta$-lactamase-producing strains. The bactericidal activity of CTRZ/CV was superior to that of CCLO and CRXM, and almost equal to that of AMXCCV against the $\beta$-lactamase-producing strains. The in vitro results were substantiated. by in vivo mouse experimental infection studies with $\beta$-lactamase-producing and non-producing strains. In mixed experimental infection due to $\beta$-lactamase-producing and non-producing strains, the therapeutic efficacy of CTRZ/CV was superior to that of CTRZ, CCLO, CRXMA and AMXCCV. In respiratory tract infection in mice due to Klebsiella pneumoniae EB4O, CTRZ/CV was more erective than CCLO, CRXMA and AMXCCV and also more efficacious than CCLO, CRXMA and AMXCCV in urinary tract infection in mice due to Escherichia coli EB13. These results indicate that CTRZ/CV is a useful drug for the treatment of infection caused by $\beta$-1actamase-producing strains including ESBL-producing strains.

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T4 티미딜산 생성효소 유전자의 Splicing 활성에 있어 Internal Guide Sequence 구조의 기능적 역할 (Functional Role of the Internal Guide Sequence in Splicing Activity of T4 Thymidylate Synthase Gene in vivo)

  • Shin, Sook;Park, In-Kook
    • 미생물학회지
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    • 제31권3호
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    • pp.208-213
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    • 1993
  • The structural and functional roles of IGS element of T4 td intron in thymidylate synthase activity in vivo were investigated Site-directed mutagenesis was employed to crete mutations of IGS element of T4 td intron, When a U-G pari was changed to a U-C pari in the 5' splice site of P1 stem of td intron, the activity of thymidylate synthase was completely abolished whereas the wild type retained the normal activity of enzyme. When U at 12 position within IGS element was changed to C, the activity of thymidylate synthase was approximately 32% of that of the wild type. Comparison of enzyme activities suggests that IGS element within P1 structure is an essential requirement for splicing of td gene in vivo.

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Epi-xanthatin의 Side Chain 변환을 통한 새로운 반합성 유도체들의 합성 및 세포독성 (Synthesis of New Semisynthetic Analogs of Epi-xanthatin by Modification of the Side Chain and Their Cytotoxic Activity)

  • 백두종;안종웅;이정옥
    • 약학회지
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    • 제49권1호
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    • pp.68-73
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    • 2005
  • Epi-xanthatin analogs containing hydrophilic substituents such as carboxylic acid, alcohol, morpholine, amino acid, and glucose derivatives were synthesized and their in vitro cytotoxicity and in vivo antitumor activity were evaluated. The target compounds were generally cytotoxic against tumor cell lines of human origin with $ED_{50}$ values of $0.1{\sim}30{\mu}g/ml$, except the highly hydrophilic analog 6 containing aspartic acid. Contrary to the potent cytotoxicity weakly hydrophilic analogs 2 and 8 were not active in vivo, or even toxic to the test animals. As a result, hydrophilic analog of epi-xanthatin did not show in vitro cytotoxicity and hydrophobic analogs did not show in vivo antitumor activity, thus it is presumed that amphiphilic analogs or those with medium hydrophilicity would exhibit the antitumor potency in vivo.

외래 유전자가 이식된 넙치(Paralichthys olivaceus) 생산 I. 근육내 유전자 직접 주입법을 통한 in vivo 유전자 이식 (Production of Transgenic Olive Flounder (Paralichthys olivaceus) I. In vivo Gene Transfer in Olive Flounder by Direct Intramuscular Injection)

  • 남윤권;주수동;정창화;방인철;허성범;김동수
    • 한국양식학회지
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    • 제10권4호
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    • pp.409-415
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    • 1997
  • The carp $\beta$-actin regulatory sequences and RSV/LTR promoter were tested whether they are functinal to express linked structure gene (chloramphenicol acetyltransferas, CAT) in olive flounder (Paralichthys olivaceus) by determining the patterns of gene expression following intramuscular in vivo direct injection. The injection experiments with various concentrations of both pRSVCAT and pFV4CAT clearly revealed the effectiveness of DNA dosage on expression of CAT. The increase of CAT activity was linear in both plasmids, and maximal CAT activity was obtained with 100 ug of pFV4CAT injection. The amounts of CAT expression with pFV4CAT-injected fist were higher than those with pRSVCAT-injected fish. CAT activity was readily detectable as early as one day after injection, slightly increased at day 2, and declined over time. Most amount of DNA intramuscularly injected into olive flounder muscles persisted extrachromosomally without showing any integrated or replicated form in vivo.

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구기자 가공품의 생리기능성 및 항고혈압 활성 검증 (Physiological Functionality of Gugija Products and an In Vivo Examination on Anti-hypertension Effects)

  • 이지수;박영춘;백승우;이석수;안용근;이종수
    • 한국식품영양학회지
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    • 제21권2호
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    • pp.115-120
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    • 2008
  • To develop a new Gugija(Lycium chinensis Mill) product having increased value, the physiological functionality of various commercial Gugija products were investigated. In addition, an in vivo study was performed using spontaneous hypertensive rats(SHR) to examine the anti-hypertension effects of products. The results showed that antioxidant activity was highest in the methanol extract of Gugija leaf pickle(97.7%), and anti-hypertensive angiotensin I -converting enzyme(ACE) inhibitory activity was 80.4% in Gugija doenjang(soybean paste) water extract. Anti-cholesterolemia HMG-CoA reductase inhibitory activity was highest in the methanol extract of Gugija rice cake(66.1 %). However, SOD-like activity was below 30% in most products; and fibrinolytic activity was not detected or was very weak. Ultimately, we selected Gugija tea and Gugija wine as superior anti-hypertensive Gugija products, and subsequent in vivo testing was performed using SHR, comparing the tea and wine to Gugija fruit. Among them, the Gugija fruit demonstrated the best anti-hypertension effects in SHR.