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Chinese Chemical Letters 2011年第3期22卷 334-337页

作者： Cai Sheng Wu Jin Lan Zhang Yan Ling Qiao Yi Lin Wang Zhi Rong Chen Institute of Materia Medica Chinese Academy of Medical Sciences Peking Union Medical College Beijing 100050 China

In this study,a simple and rapid high-performance liquid chromatography-tandem mass spectrometry（HPLC-MS/MS） method was established and validated to determine the 14β-lactam antibiotics in cosmetic products,including 1（ceftazidime）,2（cefaclor）, 3（cefdinir）,4（ampicillin）,5（cefalexin）,6（ceftezole）,7（cefotaxim）,8（cefradine）,9（cefuroxime）,10（cephazoline）,11 （cefathiamidine）,12（cefoperazone）,13（cafalotin）,14（piperacillin）.

关键词： High-performance liquid chromatography-tandem mass spectrometry(HPLC-MS/MS) Cosmetic β-lactam antibiotics

液相色谱-串联离子阱质谱测定牛奶中的12种β-内酰胺类药物残留的方法研究

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分析测试学报 2007年第Z1期26卷 272-274页

作者：殷晓燕刘艳琴曹红王浩杨红梅刘小力阎龙宝北京市海淀区产品质量监督检验所北京100083

This thesis developed a LC-ESI-TRAP-MS method for twelve β-lactam antibiotics residues in *** massspectrometer was operated in the positive ion mode using multiple reaction *** limit of detection is 1.0 and 2.0 μg/*... 详细信息

关键词： LC-MS β-lactam antibiotics Residue Milk

Synthesis of new penicillin derivatives as drug-like molecules for biological screening

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Chinese Chemical Letters 2015年第1期26卷 113-117页

作者： Chun-Jing Liu Dinah Dutta Lester Mitscher Higuchi Biosciences Center The University of Kansas Department of Medicinal Chemistry The University of Kansas

Chemical modification of penicillin β-lactam ring was *** thiazolidine amides were produced through N4-C7 β-lactam ring opening of penicillin V methyl ester with various aliphatic,aromatic,and heterocyclic primary *** 8-hydroxypenillic acid derivatives with side chains of methyl,propyl,benzyl,and diethylaminoethyl groups were yielded via β-lactam ring rearrangement from6-aminopenicillanic acid（6-APA）.Parallel synthetic methods were used for the alkylation of8-hydroxypenillic acid and β-lactam ring opening of penicillin V methyl *** biological activities of the compounds were evaluated.

关键词： Penicillin Rearrangement β-lactam antibiotics Nucleophilic ring opening

Identification and preliminary characterization of novel B3-type metallo-β-lactamases

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American Journal of Molecular Biology 2013年第4期3卷 198-203页

作者： Manfredi Miraula Conor SBrunton Gerhard Schenk Natasa Mitić Department of Chemistry National University of Ireland—MaynoothMaynoothCo.KildareIreland School of Chemistry and Molecular Biosciences The University of QueenslandBrisbaneAustralia

Antibiotic resistance has emerged as a major global threat to human health. Among the strategies employed by pathogens to acquire resistance the use of metallo-β-lactamases (MBLs), a family of dinuclear metalloenzymes, is among the most potent. MBLs are subdivided into three groups (i.e. B1, B2 and B3) with most of the virulence factors belonging to the B1 group. The recent discovery of AIM-1, a B3-type MBL, however, has illustrated the potential health threat of this group of MBLs. Here, we employed a bioinformatics approach to identify and characterize novel B3-type MBLs from Novosphingobium pentaromativorans and Simiduia agarivorans. These enzymes may not yet pose a direct risk to human health, but their structures and function may provide important insight into the design and synthesis of a still elusive universal MBL inhibitor.

关键词： Antibiotic Resistance β-lactam antibiotics Metallo-β-lactamases Sequence Homology Novosphingobium Pentaromativorans Simiduia Agarivorans

Metallo-β-lactamases:A Major Threat to Human Health

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American Journal of Molecular Biology 2014年第3期4卷 89-104页

作者： Emer K.Phelan Manfredi Miraula Christopher Selleck David L.Ollis Gerhard Schenk Natasa Mitic Department of Chemistry National University of Ireland-MaynoothMaynoothIreland School of Chemistry and Molecular Biosciences The University of QueenslandBrisbaneAustralia Research School of Chemistry Australian National UniversityCanberraAustralia

Antibiotic resistance is one of the most significant challenges facing global healthcare. Since the 1940s, antibiotics have been used to fight infections, initially with penicillin and subsequently with various derivatives including cephalosporins, carbapenams and monobactams. A common characteristic of these antibiotics is the four-memberedβ-lactam ring. Alarmingly, in recent years an increasing number of bacteria have become resistant to these antibiotics. A major strategy employed by these pathogens is to use Zn(II)-dependent enzymes, the metallo-β-lactamases (MBLs), which hydrolyse theβ-lactam ring. Clinically useful MBL inhibitors are not yet available. Consequently, MBLs remain a major threat to human health. In this review biochemical properties of MBLs are discussed, focusing in particular on the interactions between the enzymes and the functionally essential metal ions. The precise role(s) of these metal ions is still debated and may differ between different MBLs. However, since they are required for catalysis, their binding site may present an alternative target for inhibitor design.

关键词： Antibiotic Resistance β-lactam antibiotics Metallo-β-lactamases Reaction Mechanism Metal Ion Binding

Unusual metallo-β-lactamases may constitute a new subgroup in this family of enzymes

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American Journal of Molecular Biology 2014年第1期4卷 11-15页

作者： Chun-Feng D.Hou Emer K.Phelan Manfredi Miraula David L.Ollis Gerhard Schenk Natasa Mitic Research School of Chemistry Australian National UniversityCanberraAustralia Department of Chemistry National University of Ireland-MaynoothMaynoothIreland School of Chemistry and Molecular Biosciences The University of QueenslandBrisbaneAustralia

Metallo-β-lactamases (MBLs) are a family of Zn2+-dependent enzymes that have contributed strongly to the emergence and spread of antibiotic resistance. Novel members as well as variants of existing members of this family are discovered continuously, compounding their threat to global health care. MBLs are divided into three subgroups, i.e. B1, B2 and B3. The recent discovery of an unusual MBL from Serratia proteamaculans (SPR-1) suggests the presence of an additional subgroup, i.e. B4. A database search reveals that SPR-1 has only one homologue from Cronobacter sakazakii, *** two MBLs have a unique active site and may employ a mechanism distinct from other MBLs, but reminiscent of some organophosphate-degrading hydrolases.

关键词： Antibiotic Resistance β-lactam antibiotics Metallo-β-lactamases Sequence Homology Serratia proteamaculans Cronobacter sakazakii

Rapid Detection of β-lactam Antibiotic Residue in Milk Using Biolayer Interferometry

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Agricultural Biotechnology 2014年第1期3卷 9-11,15页

作者： Xiaojun LIU Hui FU Feng XUE Tao MA Xiangxiang ZENG Hai ZHU Nanjing Weigang Dairy Co. Ltd. Shenzhen Bioeasy Technology Inc. Testing Center of Animals Plants and FoodJiangsu Entry and Exit Inspection and Quarantine Bureau

[ Objective] This study aimed to establish a high-sensitivity method for rapid detection of^-lactam antibiotic residue in milk. [Method] Based on bio- layer interferometry technology, ampicillin-BSA conjugate was fixed on the bottom of APS fiber optic biosensor probe through hydrophobic interaction and bound to 40 mn colloidal gold-labeled/3-1actam antibiotic receptor, to detect β-lactam antibiotics in milk. [ Result] The sensitivity of colloidal gold-labeled BLI method was twice as high as that of immunechromatographic test strip in detection of β-1actam antibiotic residue in milk. Colloidal gold-labeled BLI method exhibited good speci- ficity and had no cross-reaction with 1 000 ng/ml aflatoxin M1, gentamicin, kanamycin, streptomycin, tylosin, chloromycetin and melamine. [Condusion] The colloidal gold-labeled BLI method is not suitable for quantitative detection in actual production due to its small quantitative range in detection of β-lactam antibiot- ics, but it is a simple and rapid qualitative detection method that can be used in rapid detection of β-1actam antibiotic residue in milk.

关键词： Bialayer interferometry β-lactam antibiotics Receptor-colloidal gold conjugate Milk Receptor