Tigecycline - how powerful is it in the fight against antibiotic-resistant bacteria?

被引:25
作者
Seputiene, Vaida [1 ]
Povilonis, Justas [1 ]
Armalyte, Julija [1 ,2 ]
Suziedelis, Kestutis [1 ,2 ]
Pavilonis, Alvydas [3 ]
Suziedeliene, Edita [1 ]
机构
[1] Vilnius Univ, Dept Biochem & Biophys, Fac Nat Sci, LT-03101 Vilnius, Lithuania
[2] Vilnius Univ, Inst Oncol, LT-03101 Vilnius, Lithuania
[3] Kaunas Univ Med, Dept Microbiol, Kaunas, Lithuania
来源
MEDICINA-LITHUANIA | 2010年 / 46卷 / 04期
关键词
tigecycline; mechanism of action; in vitro and in vivo activity; resistance; SKIN-STRUCTURE INFECTIONS; IN-VITRO ACTIVITIES; VIVO ANTIBACTERIAL ACTIVITIES; MULTIDRUG EFFLUX PUMP; DECREASED SUSCEPTIBILITY; ACINETOBACTER-BAUMANNII; SURVEILLANCE; TETRACYCLINE; EFFICACY; SAFETY;
D O I
10.3390/medicina46040033
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
Tigecycline is a semisynthetic analogue of earlier tetracyclines and represents the first member of a novel class of antimicrobials - glycylcyclines - recently approved for clinical use. It is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. The exact molecular basis of tigecycline action is not clear at present, although similarly to the tetracyclines, it has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site. Importantly, tigecycline overcomes the action of ribosomal protection proteins and is not a substrate for tetracycline efflux pumps of most bacteria well-known and prevalent cellular mechanisms of microbial tetracycline resistance. The present review-summarizes current knowledge on the molecular mechanism of the tigecycline action, antibacterial activity against various bacteria, clinical application, development of resistance to glycylcyclines.
引用
收藏
页码:240 / 248
页数:9
相关论文
共 52 条
[1]   Molecular dynamics simulations of the 30S ribosomal subunit reveal a preferred tetracycline binding site [J].
Aleksandrov, Alexey ;
Simonson, Thomas .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2008, 130 (04) :1114-+
[2]   Binding of Tetracyclines to Elongation Factor Tu, the Tet Repressor, and the Ribosome: A Molecular Dynamics Simulation Study [J].
Aleksandrov, Alexey ;
Simonson, Thomas .
BIOCHEMISTRY, 2008, 47 (51) :13594-13603
[3]   The efficacy and safety of tigecycline for the treatment of complicated intra-abdominal infections: Analysis of pooled clinical trial data [J].
Babinchak, T ;
Ellis-Grosse, E ;
Dartois, N ;
Rose, GM ;
Loh, E .
CLINICAL INFECTIOUS DISEASES, 2005, 41 :S354-S367
[4]   Comparison of tetracycline and tigecycline binding to ribosomes mapped by dimethylsulphate and drug-directed Fe2+ cleavage of 16S rRNA [J].
Bauer, G ;
Berens, C ;
Projan, SJ ;
Hillen, W .
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 2004, 53 (04) :592-599
[5]   Safety and efficacy of intravenous tigecycline in treatment of community-acquired pneumonia: results from a double-blind randomized phase 3 comparison study with levofloxacin [J].
Bergallo, Carlos ;
Jasovich, Abet ;
Teglia, Osvaldo ;
Eugenia Oliva, Maria ;
Lentnek, Arnold ;
de Wouters, Luisa ;
Zlocowski, Juan Carlos ;
Dukart, Gary ;
Cooper, Angel ;
Mallick, Rajiv .
DIAGNOSTIC MICROBIOLOGY AND INFECTIOUS DISEASE, 2009, 63 (01) :52-61
[6]   Evaluation of the in vitro activity of tigecycline against multiresistant Gram-positive cocci containing tetracycline resistance determinants [J].
Borbone, Sonia ;
Lupo, Agnese ;
Mezzatesta, Maria Lina ;
Campanile, Floriana ;
Santagati, Maria ;
Stefani, Stefania .
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS, 2008, 31 (03) :209-215
[7]   Comparative in vitro activity of tigecycline and other antimicrobials against Gram-negative and Gram-positive organisms collected from the Asia-Pacific Rim as part of the Tigecycline Evaluation and Surveillance Trial (TEST) [J].
Bouchillon, Sam K. ;
Iredell, Jonathan R. ;
Barkham, Timothy ;
Lee, Kyungwon ;
Dowzicky, Michael J. .
INTERNATIONAL JOURNAL OF ANTIMICROBIAL AGENTS, 2009, 33 (02) :130-136
[8]   In vitro activity of tigecycline against isolates from patients enrolled in phase 3 clinical trials of treatment for complicated skin and skin-structure infections and complicated intra-abdominal infections [J].
Bradford, PA ;
Weaver-Sands, DT ;
Petersen, PJ .
CLINICAL INFECTIOUS DISEASES, 2005, 41 :S315-S332
[9]   Safety and efficacy of tigecycline in treatment of skin and skin structure infections: Results of a double-blind phase 3 comparison study with vancomycin-aztreonam [J].
Breedt, J ;
Teras, J ;
Gardovskis, J ;
Maritz, FJ ;
Vaasna, T ;
Ross, DP ;
Gioud-Paquet, M ;
Dartois, N ;
Ellis-Grosse, EJ ;
Loh, E .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2005, 49 (11) :4658-4666
[10]   The structural basis for the action of the antibiotics tetracycline, pactamycin, and hygromycin B on the 30S ribosomal subunit [J].
Brodersen, DE ;
Clemons, WM ;
Carter, AP ;
Morgan-Warren, RJ ;
Wimberly, BT ;
Ramakrishnan, V .
CELL, 2000, 103 (07) :1143-1154