Antimicrobial activities of LCB10-0200, a novel siderophore cephalosporin, against the clinical isolates of Pseudomonas aeruginosa and other pathogens

Oh, Sang‐Hun; Park, Hee-Soo; Kim, Hye‐Shin; Yun, Jeong-Yul; Oh, Kyuman; Cho, Young Lag; Kwak, Jin‐Hwan

doi:10.1016/j.ijantimicag.2017.06.001

Cited by 14 publications

(32 citation statements)

References 41 publications

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“…When compared with two‐thirds generation cephalosporins (ceftazidime and ceftriaxone) and ciprofloxacin, LCB10‐0200 exhibited the lowest MIC 90 (MIC at which 90% of bacteria are inhibited) against P. aeruginosa (MIC 90 , 0.5 mg/L). This conjugate also showed potent antibacterial activity against E. coli , Serratia marcescens and Enterobacter aerogenes , and was able to inhibit the growth of A. baumannii . Furthermore, the authors demonstrated that the conjugate ( 20 ) was more effective than ceftazidime in treating systemic, high, respiratory tract, and urinary tract infections caused by drug‐susceptible and drug‐resistant P. aeruginosa strains in in vivo mouse models …”

Section: Trojan Horse Approaches To Overcome Antimicrobial Resistancementioning

confidence: 99%

“…Albomycins, ferrimycins, danomycins, and salmycins are a few representative examples of these naturally occurring sideromycins (for more details, see the recent review by Klahn and Brönstrup). Up till now, β‐lactam antibiotics (notably cephalosporins) appear to be the drugs most selected for conjugation with siderophores or siderophore mimics . Antibiotics from other classes, including ciprofloxacin, spiramycin, vancomycin, norfloxacin, and daptomycin have also been conjugated with siderophores.…”

Section: Trojan Horse Approaches To Overcome Antimicrobial Resistancementioning

confidence: 99%

“…Recently, Oh et al investigated the bacterial activity of LCB10‐0200 ( 20 , Figure ), a synthetic siderophore‐cephalosporin conjugate, composed of N ‐(2‐((4‐aminopyrimidin‐5‐yl)amino)ethyl)‐1,5‐dihydroxy‐4‐oxo‐1,4‐dihydropyridine‐2‐carboxamide, as the siderophore component, and a modified aminothiazolylglycyl‐cephalosporin as the antibiotic component. When compared with two‐thirds generation cephalosporins (ceftazidime and ceftriaxone) and ciprofloxacin, LCB10‐0200 exhibited the lowest MIC 90 (MIC at which 90% of bacteria are inhibited) against P. aeruginosa (MIC 90 , 0.5 mg/L).…”

Section: Trojan Horse Approaches To Overcome Antimicrobial Resistancementioning

confidence: 99%

“…59 siderophores or siderophore mimics. [78][79][80] Antibiotics from other classes, including ciprofloxacin, 81 spiramycin, 82 vancomycin, 83 norfloxacin, 84,85 and daptomycin 86,87 have also been conjugated with siderophores. Synthetic siderophore-ATB conjugates have been reported to enhance the uptake of the drugs, thus boosting and/or expanding the effectiveness of common ATBs.…”

Section: Siderophore-atb Conjugationsmentioning

confidence: 99%

“…Moreover, in both apo and iron-bound forms, the enterobactin-ampicillin conjugate (18) exhibited low cytotoxicity levels against human T84 intestinal cells. 95 Recently, Oh et al 78 investigated the bacterial activity of LCB10-0200 (20, Figure 5 aeruginosa (MIC 90 , 0.5 mg/L). This conjugate also showed potent antibacterial activity against E. coli, Serratia marcescens and Enterobacter aerogenes, and was able to inhibit the growth of A. baumannii.…”

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confidence: 99%

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Drug delivery systems designed to overcome antimicrobial resistance

Pham

Loupias

Dassonville‐Klimpt

et al. 2019

Medicinal Research Reviews

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Antimicrobial resistance has emerged as a huge challenge to the effective treatment of infectious diseases. Aside from a modest number of novel anti‐infective agents, very few new classes of antibiotics have been successfully developed for therapeutic use. Despite the research efforts of numerous scientists, the fight against antimicrobial (ATB) resistance has been a longstanding continued effort, as pathogens rapidly adapt and evolve through various strategies, to escape the action of ATBs. Among other mechanisms of resistance to antibiotics, the sophisticated envelopes surrounding microbes especially form a major barrier for almost all anti‐infective agents. In addition, the mammalian cell membrane presents another obstacle to the ATBs that target intracellular pathogens. To negotiate these biological membranes, scientists have developed drug delivery systems to help drugs traverse the cell wall; these are called “Trojan horse” strategies. Within these delivery systems, ATB molecules can be conjugated with one of many different types of carriers. These carriers could include any of the following: siderophores, antimicrobial peptides, cell‐penetrating peptides, antibodies, or even nanoparticles. In recent years, the Trojan horse‐inspired delivery systems have been increasingly reported as efficient strategies to expand the arsenal of therapeutic solutions and/or reinforce the effectiveness of conventional ATBs against drug‐resistant microbes, while also minimizing the side effects of these drugs. In this paper, we aim to review and report on the recent progress made in these newly prevalent ATB delivery strategies, within the current context of increasing ATB resistance.

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Section: Trojan Horse Approaches To Overcome Antimicrobial Resistancementioning

confidence: 99%