• 약학회지
• /
• 제55권1호
• /
• pp.11-15
• /
• 2011

Zabofloxacin is a novel broad spectrum fluoroquinolone with excellent anti-pneumococcal activity. We investigated the in vitro activity of zabofloxacin against clinical isolates of gram-positive bacteria and the in vivo activity against systemic infection in mice. Zabofloxacin was very active against gram-positive bacteria except QRSA (Quinolone-resistant S. aureus) and VRE(Vancomycin-resistant Enterococci). Especially, zabofloxacin was extremely potent against clinical isolates of Streptococci. Zabofloxacin was as active as gemifloxacin against systemic infection in mice. In view of its improved antibacterial activities against gram-positive bacteria and good pharmacokinetic profiles in animals, the clinical usefulness of zabofloxacin should be established by further studies.

• 한국염색가공학회지
• /
• 제35권2호
• /
• pp.67-81
• /
• 2023

This study aims to examine the possibility of using dried Dondropanax morbiferus extract as a functional dye. The leaves and branches of were extracted with distilled water and 30% ethanol, and the dyeability and functionality of silk fabrics were examined according to the color characteristics of the extract and dyeing conditions. As a result of analyzing the ultraviolet and visible light absorption spectrum of the extract, it was possible to confirm the peak of flavonoid belonging to polyphenol, and the peak of riboflavin expressing yellow color was confirmed. Adsorption equilibrium was observed at 4% dyeing concentration and 60 minutes of dyeing time, and as the temperature increased, dyeing amount increased without color change of Y-series. Aluminum mordanting also increased the yellow color. The color fastness of washing and UV irradiation was low, but the color fastness of rubbing was evaluated as relatively good. The silk fabric dyed with the distilled water extract of the leaves showed a 99.9% bacteriostatic reduction against Staphylococcus aureus and Klebsiella pneumoniae, showing excellent antibacterial properties.

• Bulletin of the Korean Chemical Society
• /
• 제33권8호
• /
• pp.2603-2608
• /
• 2012

A novel mononuclear supramolecule of copper(II) has been synthesized with Ippyt ligand (Ippyt=3-(4'-imidazole phenyl)-5-(pyrid-2''-yl)-1,2,4-triazole) (1). Compound 1, namely [$Cu(Ippyt)_2(H_2O)_2$], has been characterized by single-crystal X-ray diffraction, IR spectrum, elemental analysis and thermogravimetric analysis. Structure determination reveals that the elongated-octahedral geometry is formed in the vicinity of the copper (II) atom being coordinated by four nitrogen atoms from two Ippyt ligands occupying the equatorial position and two oxygen atoms from two coordinated water molecules in the axial position, which together form the $N_4O_2$ donor set. Hydrogen bonding interactions between nitrogen and oxygen atoms result in the set up of a supramolecular network architecture. Biological properties including antibacterial activity and superoxide dismutase (SOD) mimetic activity of compound 1 have been investigated by agar diffusion method and the modified Marklund method, respectively. The results indicate that compound 1 exhibits a stronger antibacterial efficiency than the parent ligand and it also has a certain radical-scavenging activity.

• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 1997년도 춘계학술대회
• /
• pp.40-47
• /
• 1997

New quinolones generally have a broad antibacterial spectrum against gram-positive, gram-negative, glucose-nonfermenting and anaerobic bacteria. Some of newly developed quinolones have potent activities against S. aureus including MRSA, S.pneumoniae including PRSP, B. fragilis, chlamydiae, mycoplasmas and mycobacteria as well, and show good activities against various strains resistant to antibacterial agents of other classes. Quinolones display postantibiotic effects in vitro and are bactericidal at concentrations similar to or twice that of the minimum inhibitory concentrations (MICs) for susceptible pathogens. In experimental murine infection models including systemic infections with various pathogens such as S. aureus, S. pyogenes, S. pneumoniae, E. coli and P. aeruginosa, quinolones have shown good oral efficacy as well as parenteral efficacy. Good oral absorption and good tissue penetration of quinolones account for good therapeutic effects in clinical settings. The target of quinolones are two structurally related type II topoisomerases, DNA gyrase and DNA topoisomerase IV. Quinolones are shown to stabilize the ternary quinolone-gyrase-DNA complex and inhibit the religation of the cleaved double-stranded DNA. Bacteria can acquire resistance to quinolones by mutations of these target enzymes. Mutation sites and amino acid changes in DNA gyrase and DNA topoisomerase IV are similar in the organisms examined, suggesting that the mechanism of quinolone resistance in the target enzymes is essentially the same among various organisms. Quinolones act on both the target enzymes to different degrees depending on the organisms or agents tested, and bacteria become highly resistant to quinolones in a step-wise fashion. Incomplete cross-resistance among quinolones in some strains of E. coli and S. aureus suggests the possibility of finding quinolones active against quinolone-resistant strains which are prevailing now. To find such quinolones, the potency toward two target enzymes and the membrane permeability including influx and/or efflux systems should be taken into account.

• BMB Reports
• /
• 제35권3호
• /
• pp.291-296
• /
• 2002

Thanatin, a 21-residue peptide, is an inducible insect peptide with a broad range of activity against bacteria and fungi. It has a C-terminal disulfide loop, like the frog skin secretion antimicrobial peptides of the brevinin family. In this study, we tried to find the effect of a number of amino acids between the disulfide bond. Thanatin showed stronger antibacterial activity to Gram negative bacteria than other mutants, except Th1; whereas, the mutant peptides with deletion had higher activity to Gram positive bacteria than thanatin. An increase in the number of amino acid(s) using the alanine residue decreased the antibacterial activity in all of the bacteria. Th1 with deletion of threonine at position 15 ($Thr^{15}$) showed similar antibacterial activity against Gram-negative bacteria, but had higher activity against the Gram positive bacteria. In order to study the structure-function relationship, we measured liposome disruption by the peptides and CD spectra of the peptides. Th1 also showed the highest liposome leaking activity and α-helical propensity in the sodium dodecyl sulfate solution, compared with other peptides. Liposome disruption activity was closely correlated with the anti-Gram positive bacterial activity. All of the peptides showed no hemolytic activity. Th1 was considered to be useful as an antimicrobial peptide with broad spectrum without toxicity.

• 약학회지
• /
• 제40권1호
• /
• pp.95-101
• /
• 1996

The in vitro antibacterial activities of LB10522, a new catechol-substituted cephalosporin, were compared with those of cefpirome, ceftazidime, ceftriaxone, and cefoperaz one against clinical isolates and laboratory standard anaerobes. LB10522 had broad spectrum antibacterial activities against both gram-positive and gram-negative microorganisms. It was most active against gram-positve bacteria among the reference cephalosporins tested. Against gram-negative strains such as the family Enterobacteriaceae, LB10522 showed an activity comparable to that of cefpirome. But LB10522 was more potent than ceftazidime, ceftriaxone and cefoperazone. In particular, Pseudomonas aeruginosa was highly susceptible to LB10522, which was 32-fold and 64-fold more active than ceftazidime and cefpirome, respectively. Against anaerobic strains, the activity of LB10522 was similar to those of reference compounds. LB10522 exhibited potent therapeutic activities against experimental local infections in mice. The therapeutic effect of LB10522 against urinary tract infection (UTI) caused by P. aeruginosa 1912E in mice was superior to that of cefpirome. Against experimental respiratory tract infection (RTI) caused by K. pneumoniae DT-S in mice, LB10522 was as effective as cefpirome. The in vivo efficacy of LB10522 was correlated well with its in vitro activity.

• 동아시아식생활학회지
• /
• 제15권4호
• /
• pp.457-464
• /
• 2005

The optimal concentration of ethanol to separate a high quantity of propolis was $60\%$ but that for the best flavonoids extraction was $80\%$ We compared the yields of propolis from different countries. In this study we used $60\%$ ethanol concentration as a standard. The yield of propolis was proportional to the contents of flavonoids. Namely, Polish propolis which showed the highest yield with $56\%$ by the extraction with $60\%$ ethanol revealed also the highest flavonoids content with $3.49\%$ among all the samples tested The major constituents of propolis differed from country to country. It has been suggested that the different geographical origin influenced the efficacy and the constituents of propolis. Antibacterial activity of ethanol extracted propolis from different countries was tested against 6 microbial strains of type cultures including Gram-positive (Staphylococcus aureus, Streptococcus uberis, Streptococcus agalactiae) and Gram- negative bacteria (Klebsiella pneumoniae, Proteus vulgaris and E coli) in vitro. Propolis extract showed anti-microbial activity against all the tested bacterial strains. In addition, propolis was sensitive to E coli which was resistant to broad spectrum antibiotics like ampicillin. These results showed that propolis may substituted for commercial antibiotics. The efficiency of anti-microbial activity of the propolis was slightly higher in $80\%$ than $97\%$ ethanol extract.

• 한국식품위생안전성학회지
• /
• 제8권1호
• /
• pp.9-15
• /
• 1993

어패류를 포함한 식용 육류중에 잔류하는 항생물질 및 항균성물질을 검출하기 위하여, 분석기기로서 Gas chromatography/ Mass spectrometry(GC/MS)를 사용한 동시분석법을 개발하였다. 여러 항생.항균제중에서 penicillin G, chloramphenicol, thiamphenicol을 중심으로 간단한 전처리과정과 유도체화를 하여 GC/MS 분석을 시행하였다. 전처리 과정을 요약하면 pH 4.0의 0.01 M EDTA-2Na McIlvaine buffer로의 추출, n-hexane으로의 탈지, Bond-Elute $C_{18}$ cartridge에 흡착된 물질의 0.01 M-methnolic oxalic acid로의 용출 그리고 건조 후 유도체화의 순으로 되어 있다. 본 방법에 의한 1 ppm spike시의 회수율은 penicillin G, chloramphenicol, thiamphenicol 각각 63.5%, 76.3%, 84.7%이었고, 검출한계는 각각 시료 g당 0.6, 0.085, $0.084\;\mu\textrm{g}$이었다. 또한 GC/MS 확인과정에서 실제 잔류농도가 1 ppm 이상이면 full scan spectrum으로 확인이 가능하였다. 이와 같은 GC/MS에 의한 잔류물질의 정량 및 확인시험은 앞의 미생물학적 방법의 복원은 물론 식품의 안전성 재고 및 규제독성의 측면에서도 매우 뜻 있는 연구라 하겠다.

• 한국식품영양과학회지
• /
• 제36권2호
• /
• pp.149-154
• /
• 2007

건조 미역 10.4 kg을 acetone으로 추출, 여과한 다음 액-액 분배, 각종 크로마토그라피를 통하여 충치원인균, Streptococcus mutans에 대한 항균물질의 한 성분을 분리, 정제하고(160 mg, 수율 $1.5\times10^{-3}$%) 물질을 동정한 결과는 다음과 같다. 건조 미역 30 g 상당량의 추출액을 기준으로 용매 획분별 항균활성을 조사하였을 때, $CHCl_3$층이 73.2%로 가장 강하였고, hexane층이 62.0%이었으며, BuOH층이나 물층은 거의 없었다. 알루미나 칼럼에서는 산성 획분인 1% $NH_4OH:MeOH(1:1)$용매 획분이 81.0%의 항균활성을 나타내었으며, 실리카 칼럼에서는 $CHCl_3:MeOH(95:5)$용매에서 가장 높은 95.5%의 항균성을 나타내었고, ODS칼럼에서는 85% MeOH에서 96.4%의 항균성을 나타내었다. 최종적으로 ODS칼럼에서 95% MeOH를 이동상으로 하여 3개의 물질 S1(10 mg), S2(90 mg), S3(60 mg)을 분리 정제하였다. TLC에서 각 성분은 동일한 Rf값 0.42를 나타내어 동일한 물질로 추정되었으며, 이들을 메칠 유도체화한 성분들은 Rf값이 0.95로 바뀌어 이들 물질이 carboxyl기를 가지는 지방산으로 추정되었다. GC분석에서 표품 지방산과 비교한 결과, 이들은 $C_{18:4,n-3}$ 지방산과 retention time이 일치하였다. 또한, 메칠 유도체의 mass spectrum 분석 결과, m/z 290에 분자 이온 peak가 관측되어 $C_{18:4,n-3}$ 지방산의 methyl 유도체의 분자량과 일치하여, 이 물질을 3,6,9,12-octadecatetraenoic acid(stearidonic acid, $C_{18:4,n-3}$) 지방산으로 동정하였다.

• Genomics & Informatics
• /
• 제21권1호
• /
• pp.5.1-5.13
• /
• 2023

Neisseria gonorrhoeae is a Gram-negative aerobic diplococcus bacterium that primarily causes sexually transmitted infections through direct human sexual contact. It is a major public health threat due to its impact on reproductive health, the widespread presence of antimicrobial resistance, and the lack of a vaccine. In this study, we used a bioinformatics approach and performed subtractive genomic methods to identify potential drug targets against the core proteome of N. gonorrhoeae (12 strains). In total, 12,300 protein sequences were retrieved, and paralogous proteins were removed using CD-HIT. The remaining sequences were analyzed for non-homology against the human proteome and gut microbiota, and screened for broad-spectrum analysis, druggability, and anti-target analysis. The proteins were also characterized for unique interactions between the host and pathogen through metabolic pathway analysis. Based on the subtractive genomic approach and subcellular localization, we identified one cytoplasmic protein, 2Fe-2S iron-sulfur cluster binding domain-containing protein (NGFG RS03485), as a potential drug target. This protein could be further exploited for drug development to create new medications and therapeutic agents for the treatment of N. gonorrhoeae infections.