• 약학회지
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• 제43권6호
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• pp.782-788
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• 1999

7-Oxocephalosporanate 1 was treated with phosphonium salts 2~4 by Wittig reaction to afford 7-exomethylene cephalosporanates 5~7. They were oxidized to sulfones 8~10 with mCPBA. Deprotecton of benzhydryl 7-exomethylene cephalosporanate with $AlCl_3$ and NaHCO_3$ gave sodium salts of 7-exomethylene cephalosporanates 11~16. The ${\beta}-lactamase$ inhibitory activity of synthesized compounds 11~16 were compared with sulbactam, tazobactam and clavulanic acid against Type I, II, III, IV and TEM-2 $\beta$-lactamase in vitro. Compound 15 showed more potent activity than sulbactam and clavulanic acid against Type III, IV ${\beta}-lactamase$ enzyme.

• 한국수산과학회지
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• 제47권6호
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• pp.740-744
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• 2014

In this study, the ${\beta}$-lactamase (VPA0477) gene was used as a new target for the PCR-based detection of Vibrio parahaemolyticus. Primers specific for the ${\beta}$-lactamase (VPA0477) gene of V. parahaemolyticus, were designed and incorporated into a PCR-based assay. The assay was able to specifically detect all of the 191 V. parahaemolyticus strains tested, but did not result in amplification of 39 other Vibrio spp. and non-Vibrio spp. strains tested. The detection limit of the assay was 10 CFU of V. parahaemolyticus RIMD2210633 from pure culture broth. The ${\beta}$-lactamase (VPA0477) gene-based assay developed in this study was sensitive and specific, and has great potential for the accurate detection and identification of V. parahaemolyticus in seawater or seafood samples.

• 약학회지
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• 제52권4호
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• pp.306-310
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• 2008

In vitro ${\beta}-lactamase$ inhibitory activity of 6-benzothiazole penicillins (1, 2, 3 and 4) was compared with clavulanic acid, sulbactam and tazobactam. The inhibitory activity of exomethylene compounds (3 and 4) was stronger than those of non-exomethylene compounds (1 and 2). The sulfide 3 showed stronger inhibitory activity than sulbactam, clavulanic acid andsimilar to tazobactam against ${\beta}-lactamase$ Type I enzymes. The inhibitory activity of 4 was stronger than those of sulbactam, clavulanic acid and tazobactam against Type III and IV enzymes. The in vitro antimicrobial activity of ampicillin or cefoperazone combined with 3 or 4 was stronger than those of ampicillin or cefoperazone alone against many ${\beta}-lactamase$ producing strains to show that compounds 3 and 4 have some synergistic effect. The synergistic activity of 3 and 4 was comparable to sulbactam in some ${\beta}-lactamase$ producing strains, but it was inferior to tazobactam.

• 대한화학회지
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• 제49권5호
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• pp.461-469
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• 2005

• 대한의생명과학회지
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• 제22권2호
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• pp.29-36
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• 2016

Among the several agents causing carbapenem resistance of Acinetobacter baumannii, the most common cause is OXA-23 ${\beta}$-lactamase, which is known to hydrolyze carbapenem. To effectively control dissemination of carbapenem-resistant Acinetobacter baumannii (CRAB), development of both rapid and easy-to-use detection methods are required. The aim of this study is to develop a novel immunochromatographic assay (ICA) for rapid detection of OXA-23 ${\beta}$-lactamase. Of the seven monoclonal antibodies (mAbs) screened by ELISA, four mAbs (4G6, 4H6, 6G4, 9A4) exhibited high reactivity. Of these four specific antibodies, the combination of 6G4/4G6 showed the greatest reactivity and this combination of mAbs (6G4/4G6 mAbs) was used to develop the OXA-23 ${\beta}$-lactamase ICA. Of 102 A. baumannii isolates tested, the OXA-23 ${\beta}$-lactamase ICA results were consistent with PCR analysis except one false positive and one false negative isolate. The overall sensitivity and specificity were 98.36% and 97.56%, respectively. In conclusion, to the best of our knowledge, we have developed the first specific antibody set to detect OXA-23 ${\beta}$-lactamase using an ICA kit. This novel ICA can be used as a reliable and easy-to-use immunological assay for detection of OXA-23 ${\beta}$-lactamase producing CRAB in clinical laboratories.

• 미생물학회지
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• 제30권3호
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• pp.149-153
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• 1992

Cloning of the gene encoding extracellular .betha.-lactamase from Streptomyces sp. SMF13 in a plasmid pIJ702 and expression of the gene in Streptomyces invidans were carried out. Optimal conditions for the formation of protoplasts of S.lividans and the regeneration of the protoplasts were evaluated. Streptomyces sp. SMF-13 was selected as a donor strain of .betha.-lactamase gene and totla DNA of the strain was partially digested with Sau3A I. DNA fragments ranged from 4kb to 10 kb were ligated to pIJ702 AT Bgl II site and then the ligated DNAs were transformed to the protoplasts of S, livivans. The transformation efficiency was $2 *10^{3}$ .$\mu$g DNA for the ligated DNA mixture. One colony among a thousand colonies regenerated showed extracellular .betha.-lactamase and the size of the inserted DNA fragment was estimated to be 3.94 kb. The .betha.-lactamase activity in the culture broth of the recombinant strain was maximum at 3 days culture to be 1.0 unit/ml.

• 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.

• 생명과학회지
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• 제20권8호
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• pp.1214-1220
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• 2010

대한민국 순천의 병원 입원 환자의 검체로부터 imipenem 내성 세균을 분리하였다. 54개의 분리균을 16S rRNA 유전자와 gyrB 유전자 염기서열 비교를 기초로 하여 계통분류학적으로 동정하였다. 분리균들은 Pseudomonas aeruginosa (30균주; 55.6%), Acinetobacter baumannii (21; 38.9%), Enterobacter hormaechei (2)와 Pseudomonas putida (2)에 속했다. 22개의 균주가 metallo-$\beta$-lactamase (MBL)를 생산하였으며 종별 구성은 다음과 같다; Acinetobacter baumannii 12균주, Pseudomonas aeruginosa 7균주, P. putida 2균주 그리고 Enterobacter hormaechei 1균주. 분리균들의 항생제 감수성은 디스크 확산법과 Vitek 을 이용하여 조사하였다. IMP 와 VIM 형의 metallo-$\beta$-lactamase를 생산하는 균주들은 OXA 와 SHV 형 $\beta$-lactamase를 생산하는 균주들에 비해 ceftazidime, aztreonam, amikacin과 gentamicin에 대한 내성율이 높았다.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1996년도 춘계학술대회
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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.

• 생명과학회지
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• 제19권12호
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• pp.1718-1723
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• 2009

Chromosomal 인 SHV-11 $\beta$-lactamase가 plasmid를 매개로 다른 균주로 전달 되는 현상은 흔하지 않다. 본 연구에서는 플라스미드성 SHV-11 $\beta$-lactamase를 동시에 가지고 있는 ESBL생성 두 균주를 검출하였다. 따라서 이들 균주에 대한 유전적 특성과 임상적 의의에 대해 알아보고자 하였다. Vitek system과 이중디스크확산법을 이용하여 ESBL생성균주를 검출하였고, PCR과 DNA 염기서열분석을 이용하여 SHV-11 $\beta$-lactamase를 가지고 있는 ESBL생성균주를 확인 하였다. 이들 균주를 교차접합실험과 형질전환실험을 이용하여 유전자전이를 확인하고 액체배지 희석법으로 3세대 cephalosphorin 항생제에 대한 최소억제농도를 측정하였다. 이들 균주의 유전형 분석결과는 SHV-11 $\beta$-lactamase 유전자와 CTX-M-15 ESBL 유전자를 동시에 가지고 있었다. 3세대 cephalosphorin 항생제에 대한 최소억제농도는 SHV-11 $\beta$-lactamase와 CTX-M-15 ESBL 유전자를 동시에 가지고 있는 균주에서 $64{\mu}g/ml$ 이상이었고, SHV-11 $\beta$-lactamase 만을 가지고 재조합 한 균주에서 $0.5{\mu}g/ml$ 이하로 나타났다.