• Title/Summary/Keyword: in vivo activity

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

  • Hwang, Yun-Ha;Han, Kyung-Oh;Lee, Jin;Yang, Hee-Bog;Chung, Yong-Ho;Yoon, Sung-June;Lee, Dug-Keun
    • Biomolecules & Therapeutics
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    • v.5 no.2
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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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    • v.34 no.1
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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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Studies on antioxidative action of garlic components isolated from garlic Part II: Effects of garlic components on peroxidase and superoxide dismutase activity (마늘 성분의 산화방지작용에 대한 연구 제2보 과산소 분해효소의 활성에 미치는 영향)

  • 전희정
    • Journal of the Korean Home Economics Association
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    • v.24 no.1
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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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Replacement of the in vivo Bioassay for Erythropoietin with the in vitro Bioassay (Erythropoietin in vivo 시험법의 in vitro 대체 시험법 확립)

  • 백상훈;김진만;권기성;박송용;허재욱
    • KSBB Journal
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    • v.18 no.4
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    • pp.255-260
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    • 2003
  • In vivo bioassays for biological medicines have been considered final resort to unequivocally assess the biological activities for them because there are some cases in which the biological activities obtained from in vivo bioassay and in vitro bioassay quite differ each other. The in vivo biological activity of EPO depends on its sialic acid contents which confer microheterogeneity-isoforms to this protein. We have devise a method which consists of a in vitro bioassay using BaF3 cell line and a capillary zone electrophoresis (CZE) for the measurement of the EPO isoform distribution. The biological activity of EPO obtained using in vitro bioassay with BaF3 cell line showed good correlation (C.V.(%) 7.34, 5.85, 8,16, 8.08, 8.8) to EPO content measured either spectrophotometric assay (A280 0.1 % =0.743) or radio immunoassay. The assay validation results of in vitro bioassay with 3 lot of in house EPO showed good results to EPO content measured either in vivo assay or radio immunoassay. and also showed good results the robustness of our method in terms of precision, accuracy, repeatability. The isoform distribution for EPO-BRP (1 : 1 mixture of epoetin-${\alpha}$ and epoetin-${\beta}$, European Pharmacopoeia) by CZE method resulted in isoform 2 through isoform 8. The major peaks in electrophoregram were composed of isoform 3 through 7. Our recombinant EPO (epoetin-${\alpha}$) having equivalent in vivo biological activity showed the isoform distribution of isoform 3 through 9. The major peaks consisted of isoform 4 through 8. The peak area of isoform 4 was always smaller than that of isoform 5. The preparations of recombinant epoetin-${\alpha}$ with lower in vivo biological activity than EPO-BRP showed the isoform 2 through 8 in their electrophoregrams whose major peaks consisted of the isoform 3 through 7. The peak area of isoform 4 was larger than that of isoform 5.

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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    • v.48 no.6
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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]

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

  • 최성학;김지영;김계원;김원배;심미자
    • Biomolecules & Therapeutics
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    • v.7 no.1
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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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Functional Role of the Internal Guide Sequence in Splicing Activity of T4 Thymidylate Synthase Gene in vivo (T4 티미딜산 생성효소 유전자의 Splicing 활성에 있어 Internal Guide Sequence 구조의 기능적 역할)

  • Shin, Sook;Park, In-Kook
    • Korean Journal of Microbiology
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    • v.31 no.3
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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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Synthesis of New Semisynthetic Analogs of Epi-xanthatin by Modification of the Side Chain and Their Cytotoxic Activity (Epi-xanthatin의 Side Chain 변환을 통한 새로운 반합성 유도체들의 합성 및 세포독성)

  • Baek Du-Jong;Ahn Jong-Woong;Lee Chongock
    • YAKHAK HOEJI
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    • v.49 no.1
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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.

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

  • 남윤권;주수동;정창화;방인철;허성범;김동수
    • Journal of Aquaculture
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    • v.10 no.4
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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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Comparison of In Vitro, Ex Vivo, and In Vivo Antibacterial Activity Test Methods for Hand Hygiene Products (손 위생 제품에 대한 in vitro, ex vivo, in vivo 항균 시험법 비교)

  • Daeun Lee;Hyeonju Yeo;Haeyoon Jeong
    • Journal of Food Hygiene and Safety
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    • v.39 no.1
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    • pp.35-43
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    • 2024
  • Numerous methods have been applied to assess the antibacterial effectiveness of hand hygiene products. However, the different results obtained through various evaluation methods have complicated our understanding of the real efficacy of the products. Few studies have compared test methods for assessing the efficacy of hand hygiene products. In particular, reports on ex vivo pig skin testing are limited. This study aimed to compare and characterize the methodologies applied for evaluating hand hygiene products, involving in vitro, ex vivo, and in vivo approaches, applicable to both leave-on sanitizers and wash-off products. Our further aim was to enhance the reliability of ex vivo test protocols by identifying influential factors. We performed an in vitro method (EN1276) and an in vivo test (EN1499 and ASTM2755) with at least 20 participants, against Serratia marcescens or Escherichia coli and Staphylococcus aureus. For the ex vivo experiment, we used pig skin squares prepared in the same way as those used in the in vivo test method and determined the optimal treated sample volumes for sanitizers and the amount of water required to wash off the product. The hand sanitizers showed at least a 5-log reduction in bacterial load in the in vitro test, while they showed little antibacterial activity in the in vivo and ex vivo tests, particularly those with a low alcohol content. For the hand wash products, the in vitro test was limited because of bubble formation or the high viscosity of the products and it showed low antibacterial activity of less than a 1-log reduction against E. coli. In contrast, significantly higher log reductions were observed in ex vivo and in vivo tests, consistently demonstrating these results across the two methods. Our findings revealed that the ex vivo and in vivo tests reflect the two different antibacterial mechanisms of leave-on and wash-off products. Our proposed optimized ex vivo test was more rapid and more precise than the in vitro test to evaluate antibacterial results.