• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.237-237
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• 1996

DA-1131, imipenem(IPM) 및 meropenem(MEPM)은 각종 $\beta$-lactamase를 산생하는 세균에 대하여 우수한 항균력을 나타내었으나 cefpirome(CPR), ceftazidime(CAZ) 및 azthreonam(AZT)의 경우에는 extended broad spectrum cephalosporinase 산생 균주를 포함하여 일부 균주의 내성획득이 확인되었다. DA-ll3l의 $\beta$-lactamase Inducible activity는 DA-1131, IPM 및 MEPM이 거의 동일하였으며, imipenemase 산생균주로 동점된 Serratia marcescens 11001이 산생하는 $\beta$-lactamase이외의 효소에는 대부분 가수분해되지 않는 결과를 나타내었다. S. marcescens 11001이 산생하는 $\beta$-lactamase에 대한 효소역학상수는 DA-1131, IPM 및 MEPM에서 모두 유사하였고, $\beta$-lactamase에 대한 affinity도 큰 차이를 나타내지 않았다.

• Archives of Pharmacal Research
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• v.21 no.5
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• pp.527-530
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• 1998

The antibacterial activity of novel ${\beta}$-lactamase inhibitors, 6-exomethylene penamsulfones (CH1240, CH2140), has been compared in vivo with that of sulbactam and clavulanic acid against b-lactamase producing strains. In vivo microbiological assessment was used as experimental mouse infection model by gram negative strains. Against Pseudomonas aeruginosa F0013, cefoperazone/CH 1240 was slightly less active than sulbactam. ampicillin/CH 2140 was less effective than sulbactam against escheriachia coli 3457. Especially against Citrobacter diversus 2046E, amoxicillin/CH 2140 was the most potent and amoxicillin/CH 1240 was slightly more active than clavulanic acid. consequently the difference in efficacy between the drug combinations appers to be related to the degree of protection afforded the animals by the b-lactamasse inhibitors. CH1240 and CH2140 are promising new agents and should undergo further investigations.

• Korean Journal of Microbiology
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• v.26 no.4
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• pp.355-361
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• 1988

The aims of the present studies were to understand the physiolosical and genetic characters of Streptomyces sp. isolated from soil. It revealed that Streptomyces sp. SMF301 had very fast growth rate and produced extracellular protease and heavily sporulated on rich media. It also showed $\beta$-lactamase activity and pigment production. Nonsporulating mutants were isolated after NTG or acriflavin treatment and their characters were compared with the parent strain. It was found that the mutants obtained by acriflavin treatment and ghier characters were compared with the parent strain. It was found that the mutants obtained by acriflavin treatment lost the pigment formation and $\beta$-lactamase production. Protease actibity of the mutant was lowered and the pH optimum was changed toward neutral. It was found that the changes were resulted from the reduction of alkaline protease biosynthesis in the bald mutant. Therefore it is considered that sporulation, pigment formation, $\beta$-lactamase production, and alkaline protease production in Streptomyces sp. might be controlled with a closely related relationship.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.161-161
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• 1996

10종의 6-exomethylene penamsulfone 유도체의 Type I, Type IV, TEM 효소에 대한 $\beta$-lactamase 저해 효과를 측정하였다. 7종의 합성 화합물은 Type I penicillinase에 대해서는 저해 효과가 없었으나, Type IV cephalosporinase에 대해서는 기존의 sulbactam이나 tazobactam에 비하여 강한 효과를 나타내었고, 특히 CH 1145는 tazobactam보다 약 30배 강한 활성을 보여주었다. CH 2140은 TEM 효소에 대하여 tazobactam과 유사한 저해효과를 보였다.

• Korean Journal of Microbiology
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• v.30 no.1
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• pp.60-64
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• 1992

The secretion vector with promoter and signal sequence region of neutral protease gene (npr) from Bacillus amyloliquefaciens was constructed by the technique of polymerase chain reaction (PCR). A unique restriction iste was introduced into the 3' of the signal coding region by the synthesis of PCR primer. To demonstrate the function of cloned promoter and signal sequence, we used the E. coli .betha.-lactamase structural gene as a foreign gene. The signal sequence of .betha.-lactamase gene was deleted by Bal31 exonuclease and only mature region was introduced into the secretion vector. Bacillus subtilis cells transformed by the recombinant vector synthesized the fusion protein and were also capable of removing the signal peptide from the original fusion protein, as judged by the assay of .betha.-lactamase activity and secretion into the growth medium by western blotting.

• Applied Biological Chemistry
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• v.40 no.1
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• pp.23-29
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• 1997

To develop novel cephem antibiotics, We have synthesized a new compound, named YH-487, by attaching the thiol and aminothiazole residue to $C_3$ and $C_7$ position of 7-ACA, respectively. Several characteristics such as structure, antibiotic spectrum, action mechanism, stability against ${\beta}-lactamase$ and synergistic effect were investigated. Anti-bactericidal activity of YH-487 against gram-positive and gram-negative bacteria were superior to that of the other cephem antibiotics. We have examined the action mechanisms of YH-487 using penicillin binding protein (PBP) assay, and found that the bactericidal activity was obtained by inhibiting PBP-1A, PBP-1B and PBP-3. YH-487 showed synergistic effect with gentamicin, tobramycin, and amikacin against Pseudomonas aeruginosa. In addition, YH-487 was effective against Enterobacter cloacae in combination with amikacin. Based on the above observations, YH-487 was classified as a novel third-generation ${\beta}-lactam$ antibiotics.

• Journal of Microbiology and Biotechnology
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• v.27 no.3
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• pp.542-551
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• 2017

Small phytochemicals have been successfully adopted as antibacterial chemotherapies and are being increasingly viewed as potential antibiofilm agents. Some of these molecules are known to repress biofilm and toxin production by certain bacterial and yeast pathogens, but information is lacking with regard to the genes allied with biofilm formation. The present study was performed to investigate the inhibitory effect of burdock root extract (BRE) and of chlorogenic acid (CGA; a component of BRE) on clinical isolates of Klebsiella pneumoniae. BRE and CGA exhibited significant antibiofilm activity against K. pneumoniae without inflicting any harm to its planktonic counterparts. In vitro assays supported the ${\beta}$-lactamase inhibitory effect of CGA and BRE while in silico docking showed that CGA bound strongly with the active sites of sulfhydryl-variable-1 ${\beta}$-lactamase. Furthermore, the mRNA transcript levels of two biofilm-associated genes (type 3 fimbriae mrkD and trehalose-6-phosphate hydrolase treC) were significantly downregulated in CGA- and BRE-treated samples. In addition, CGA inhibited biofilm formation by Escherichia coli and Candida albicans without affecting their planktonic cell growth. These findings show that BRE and its component CGA have potential use in antibiofilm strategies against persistent K. pneumoniae infections.

• YAKHAK HOEJI
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• v.41 no.1
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• pp.126-131
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• 1997

To overcome the problems of the resistance to clavulanic acid, many researchers are developing novel inhibitors that are not sensitive to new mutant ${\beta}$-lactamases. In order to evaluate newly synthesized compound CH2150 (Sodium (3S.5R)-6(Z)-[1-{1-(2-{2-benzoxazoly}thioethyl)-l.2,3-txiazol-4-yl}methylene] penicillanate-1,1-dioxide) as a ${\beta}$-lactamase inhibitor, we examined inhibitory activity of CH2150 against ${\beta}$-lactamases of clinical isolates resistant to ampicillin/sulbactam(12 strains of Escherichia coli and 13 strains of Staphylococcus aureus), and compared with that of sulbactam. Nitrocefin was used as substrate for ${\beta}$-lactamases, and the increase of absorbance was measured spectrophotometerically at 482 nm. ${\beta}$-Lactarnase inhibition of CH2150 against ${\beta}$-lactamases was 73 ~ 96% in E. coli and 76 ~ 79% in S. aureus. Comparatively, that of sulbactam was 96 ~ 100% and 96 ~ 100%, respectively. The inhibitory activity of CH2150 was slightly lower than that of sulbactam. The MIC values of ampicillin combined with CH2150 (2:1) for the clinical isolates were 4~512 ${\mu}$g/ml for E. coli and 1.0 ~ 64 ${\mu}$g/ml for S. aureus, whereas 0.5~16 ${\mu}$g/ml for E. coli and 0.25~8 ${\mu}$g/ml for S. aureus when combined with sulbactam (2:1).

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.314.1-314.1
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• 2002

Bacterial ${\beta}$-lactamases provide resistance to ${\beta}$-lactams by hydrolyzing the ${\beta}$-lactam bond, On the basis of their catalytic mechanisms. ${\beta}$-lactamases are divided into two major groups. Class A. C and D which belong to the first group require serine in the active site and class B which is the second group require Zn(II) for their activity. Among class B enzymes, Bacteroides fragilis ${\beta}$-lactamase (CcrA enzyme) require two Zn(II) ions per monomer for maximal enzymatic activities. (omitted)

• Journal of Microbiology and Biotechnology
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• v.2 no.1
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• pp.35-40
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• 1992

The influence of the nature of plasmids on fermentation parameters such as cell growth, cell viability, plasmid stability, and product formation has been investigated using E. coli M5248 and its recombinant derivatives M5248 [pBR322], M5248[pAS1], and M5248[pNKM21]. At a low temperature ($30^\circ{C}$), the cell growth, cell viability, and protein synthesis of the recombinants were nearly identical to those of the host cell. However, at high temperature ($42^\circ{C}$), in which transcription from the P_L$ promoter is derepressed, the recombinant cells showed decreased stability along with lower growth rates and cell viability. The ratio of total protein to cell mass was in the order of E. coli M5248>M5248[pBR322]>M5248[pAS1]>M5248[pNKM21]. It was found that transcription from the $P_L$ promoter adversely affect the plasmid maintenance and host cell metabolism even in the absence of the cloned-gene expression. Furthermore, profiles of ${\beta}$ activity were shown to vary with recombinant strains. E coli M5248[pBR322] showed highest ${\beta}-lactamase$ activity at $30^\circ{C}$, while at $42^\circ{C}\;{\beta}-lactamase$ activity was significantly reduced irrespective of the strains. The effect of the plasmid properties on plasmid-encoded gene expression has been further examined based on the relationship between $\{beta}-lactamase$ activity and plasmid-harboring cell numbers.