• 한국식품과학회지
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• 제28권4호
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• pp.730-735
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• 1996

마늘이 상처를 입으면 마늘중에 존재하는 alliin이 alliinase에 의해 allicin으로 분해되며 allicin은 마늘의 주된 항미생물 작용 물질로 알려져 있다. 이 성분에 의한 미생물번식 저해작용을 크게 받는 E. coli는 1%의 마늘즙액이 들어있는 TSB에서 사멸효과가 나타났으며 농도가 높을수록 사멸속도는 더욱 빨랐다. 마늘즙액에 의한 미생물생육 저해효과는 pH에 따라서도 다르게 나타나는데 pH 7.2에 비해 5.2와 6.2에서 저해작용이 강하게 나타났다. 초기 접종균수가 $10^{6}\;CFU/ml 이상일 때는 번식에 대한 저해효과가 나타나지 않았으나 $10^{5}\;CFU/ml 이하일 때는 저해효과가 나타나서 항미생물 작용에 대한 초기 미생물 수도 중요한 변수였다. 유리 SH기를 가진 cysteine이나 glutathione을 첨가하면 마늘즙액의 번식 저해효과로부터 E. coli를 보호하였다. 결과적으로 E. coli에 대한 마늘즙액의 번식 저해효과는 마늘즙액의 농도뿐만 아니라 pH, cystein이나 glutathione같은 SH화합물의 존재여부, 접종균수에 의해서 영향을 받음을 알 수 있었다.

• 생약학회지
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• 제24권2호
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• pp.140-152
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• 1993

This study was attempted to investigate the effect of Ganoderma lucidum extract on digestive system in experimental animals. Ganoderma lucidum water extract (GWE) was found to be promoted the charcol transport rate in the small intestine of mice. GWE exhibited the augmentation of spontaneus movement(motility) and contractile response(tension) in the ileum and colon strips of rabbit, and these action were inhibited by atropine. GWE given intraduodenaly(i.d.) exhibited the significant increase of gastric acid secretion in pylorus-ligated rats. GWE inhibited the formation of some experimental gastric ulcers(pylorus ligation ulcer i.d., indomethacin-induced ulcer p.o., i.d. and aspirin-induced ulcer p.o.) in rats, which are considered to relate to a protective action. GWE and EtOH extract(water soluble phase) were remarkably increase of bile excretion, when administration of i.d., intravenation(i.v.) and per os (p.o.) compared with normal-control group. GWE was observed antibacterial activity aginst several intestinal microoganisms and others bacteria in vitro test.

• 생약학회지
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• 제25권3호
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• pp.278-292
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• 1994

This study was attempted to investigate the effect of Machili Cortex extract(Machilus thunbergii Sieb. et Zucc. ) on digestive system in experimental animals. EtOH and MeOH extracts(E.E. and M.E.) were found to inhibit the charcoal transport rate in the small intestine of mice. E.E. exhibited the inhibition of spontaneous movement(motility) and tension in the ileum and colon strips of rabbit, and these actions were inhibited by action of acetylcholine. E.E. and M.E. given intraduodenaly(i.d.) exhibitied the significant decrease of gastric acid secretion in pylorus-ligated rats. E.E. and M.E. inhibited the formation of some experimental gastric ulcers(pylorus ligation-ulcer i.d., indomethacin-induced ulcer p.o. and aspirin-induced ulcer p.o. ) in rats, which are considered to relate to a protective action. E.E. and M.E. caused remarkable increase of bile excretion, compared with normal-control group, when adminstered through i.d., i.v. and p.o. The antibacterial activity against several intestinal microorganisms and other bacteria in vitro test was observed in the administration of E.E. and M.E.

• Bulletin of the Korean Chemical Society
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• 제35권9호
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• pp.2809-2812
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• 2014

The 43-residue defensin-like peptide coprisin, which is isolated from dung bettle, Copris tripartitus, is a potent antimicrobial peptide. In our previous work, we determined the tertiary structure of coprisin and found that alpha helical region of coprisin from residue 19 to residue 30 is important for its antimicrobial activities. Here, we designed cop12mer and cop9mer analogs of coprisin based on the tertiary structure of coprisin. To investigate the relationship between hydrophobicity and antimicrobial activities and develop the potent peptide antibiotics, we designed cop9mer-1 with substitution of $His^2$ with Trp in cop9mer. The results showed that cop9mer-1 has higher toxicities as well as improved antimicrobial activities compared to cop9mer. In order to reduce the toxicity of cop9mer-1, we designed cop9mer-2 and cop9mer-3 with substitution of $Cys^3$ with Lys or Ser. Substitution of $Cys^3$ with these hydrophilic amino acids results in lower cytotoxicities compared to cop9mer-1. Cop9mer-2 with substitution of $Cys^3$ with Lys in Cop9mer-1 showed high antibacterial activities against drug resistant bacteria without cytotoxicity. Antibiotic action of cop9mer-1 analog appears to involve permeabilization of the bacterial cell membrane while cop9mer-2 and cop9mer-3 may have different mechanism of action. These results imply that that optimum balance in hydrophobicity and hydrophilicity in these 9-meric peptides plays key roles in their antimicrobial activities as well as cytotoxicities.

• 한국응용과학기술학회지
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• 제16권4호
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• pp.293-298
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• 1999

Dual-action agents are unique chemical entities comprised of two different types of antibacterial compounds covalently linked together in a single molecule in such a way that both components are able to exert their bactericidal properties. Crosslinked sulfadiazine-sulfacetamide such as antibiotics synthesized by crosslingking reaction such as glutaraldehyde. These structures of the compounds were confirmed by IR, NMR. 4 strains of Gram(+) and Gram(-) revealed effective susceptibility to synthetic crosslinked sulfadiazine-sulfacetamide.

• Journal of Microbiology and Biotechnology
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• 제29권11호
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• pp.1707-1716
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• 2019

The development of new antimicrobial agents is essential for the effective treatment of diseases such as sepsis. We previously developed a new short peptide, Pap12-6, using the 12 N-terminal residues of papiliocin, which showed potent and effective antimicrobial activity against multidrug-resistant Gram-negative bacteria. Here, we investigated the antimicrobial mechanism of Pap12-6 and a newly designed peptide, Pap12-7, in which the 12^th Trp residue of Pap12-6 was replaced with Val to develop a potent peptide with high bacterial selectivity and a different antibacterial mechanism. Both peptides showed high antimicrobial activity against Gram-negative bacteria, including multidrug-resistant Gram-negative bacteria. In addition, the two peptides showed similar anti-inflammatory activity against lipopolysaccharide-stimulated RAW 264.7 cells, but Pap12-7 showed very low toxicities against sheep red blood cells and mammalian cells compared to that showed by Pap12-6. A calcein dye leakage assay, membrane depolarization, and confocal microscopy observations revealed that the two peptides with one single amino acid change have different mechanisms of antibacterial action: Pap12-6 directly targets the bacterial cell membrane, whereas Pap12-7 appears to penetrate the bacterial cell membrane and exert its activities in the cell. The therapeutic efficacy of Pap12-7 was further examined in a mouse model of sepsis, which increased the survival rate of septic mice. For the first time, we showed that both peptides showed anti-septic activity by reducing the infiltration of neutrophils and the production of inflammatory factors. Overall, these results indicate Pap12-7 as a novel non-toxic peptide with potent antibacterial and anti-septic activities via penetrating the cell membrane.

• 한국수산과학회지
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• 제55권6호
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• pp.875-885
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• 2022

This study was performed to confirm the optimal extraction method for antimicrobial peptides from the Hard-shelled mussel. Extractions were performed with two processes including 1% HAc/boiling and 1% HAc/non-boiling methods and used extracts for the comparison of the antimicrobial activity, protease stability, action mechanism, AU-PAGE (acid-urea PAGE), and HPLC chromatograms. 1% HAc/boiling extract showed potent antibacterial activities both against Gram-positive and negative bacterium but 1% HAc/non-boiling extract showed antibacterial activity only against Gram-positive bacteria. Treatment of 1% HAc/boiling extract with proteases retained almost antibacterial activity against B. subtilis, but abolished significant antibacterial activity against E. coli D31. Only 1% HAc/boiling extract showed two discrete clearing antibacterial zones including slow migrating and rapid migrating zones. Both extracts showed strong DNA-binding ability but did not show bacterial membrane permeabilizing ability. In comparison of the chromatogram obtained from C₁₈ or cation-exchange HPLC, the eluted peaks from 1% HAc/boiling extract showed high hydrophobic property or absorbance compared to 1% HAc/non-boiling extract, respectively. The concentration of the purified antimicrobial peptide was also higher in 1% HAc/boiling extract than in 1% HAc/non-boiling extract. Our results suggest that the effective extraction condition for antimicrobial peptides from marine invertebrate is boiling process in a weak acetic acid solution (1%).

• Journal of Microbiology and Biotechnology
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• 제31권9호
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• pp.1288-1294
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• 2021

There are a growing number of reports of hospital-acquired infections caused by pathogenic bacteria, especially methicillin-resistant Staphylococcus aureus (MRSA). Many plant products are now being used as a natural means of exploring antimicrobial agents against different types of human pathogenic bacteria. In this research, we sought to isolate and identify an active molecule from Sedum takesimense that has possible antibacterial activity against various clinical isolates of MRSA. NMR analysis revealed that the structure of the HPLC-purified compound was 1,2,4,6-tetra-O-galloyl-glucose. The minimum inhibitory concentration (MIC) of different extract fractions against numerous pathogenic bacteria was determined, and the actively purified compound has potent antibacterial activity against multidrug-resistant pathogenic bacteria, i.e., MRSA and its clinical isolates. In addition, the combination of the active compound and β-lactam antibiotics (e.g., oxacillin) demonstrated synergistic action against MRSA, with a fractional inhibitory concentration (FIC) index of 0.281. The current research revealed an alternative approach to combating pathogenesis caused by multi-drug resistant bacteria using plant materials. Furthermore, using a combination approach in which the active plant-derived compound is combined with antibiotics has proved to be a successful way of destroying pathogens synergistically.

• 약학회지
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• 제39권4호
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• pp.351-359
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• 1995

The in vitro and in vivo antibacterial activities of DWQ-217 (1-cyclopropyl-6-fluoro-8-chloro-7-(3-amino-4-methylthiomethylpyrrolidinyl )-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid) were compared with those of ciprofloxacin (CPFX) and vancomycin(VCM). DWQ-217 was superior to those of CPFX and VCM against gram positive bacteria. DWQ-217 showed excellent activity against MRSA (MIC of methicillin; $\geq$12.5 $\mu\textrm{g}$/ml), MIC$_{90}$=0.013. DWQ-217 possessed strong bactericidal action against gram positive and gram negative strains by MIC/MBC test and killing curve. DWQ-217 and CPFX were administered orally and subcutaneously to mice infected systematically with S. aureus and S. pyogenes, DWQ-217 was $\geq$5-16 fold(p.o.) and $\geq$3-5 fold(s.c.) more active than CPFX.

• Applied Microscopy
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• 제22권1호
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• pp.70-78
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• 1992

Antibacterial effects of the water-soluble extract of Ulmus pumila L. on Staphylococcus aureus and Escherichia coli were studied by cylinder plate dilution method. The cells of S. aureus and E. coli treated with the extract were comparatively examined by scanning and transmission electron microscopies for their morphological features. The normal cells of S. aureus and E. coli showed thypical coccus and rod shapes, respectively, but the cells of S. aureus treated with the extract showed rough surface structures with many granular protrusions and were destroyed to form ghost cells by liberating their cytoplasmic components. E. coli cells treated with the extract were destoryed without enlarging in size and producing granules on their surfaces.