Abstract:
INTRODUCTION:Antimicrobial peptides are proving to be promising lead compounds for therapeutics. The major disadvantage of antimicrobial peptides is their proteolytic instability in the body, with half-lives averaging less than an hour. Peptoids, or N-substituted glycines, have emerged as a promising field of peptidomimetics by retaining the beneficial properties of antimicrobial peptides while improving their stability. METHODS:This study evaluated peptoid derivatives of ultra-short lipophilic antimicrobial peptides, comparing their potency side-by-side with the most prevalent multidrug-resistant bacteria (ESKAPE) and yeast pathogens (Candida albicans and Cryptococcus neoformans). RESULTS:Both peptide and peptoid counterparts were most effective against Gram-positive bacteria with minimum inhibitory concentration (MIC) values as low as 1.6 and 6.3 µg/mL, respectively. In general, peptides retained better antimicrobial activity than their peptoid counterparts; however, certain peptoids proved to be more effective than peptides against Gram-negative bacteria. For example, peptoid MG10 displayed an MIC of 6.3 µg/mL against Pseudomonas aeruginosa compared with the peptide counterpart with an MIC of 100 µg/mL. All tested compounds were more potent against Cryptococcus neoformans compared with Candida albicans. Cytotoxicity analysis indicated that peptoids were generally slightly less toxic than their peptide counterparts. Additionally, trypsin rapidly degraded one of the evaluated peptides, while having no effect on comparable peptoids, demonstrating the proteolytic stability of peptoids. CONCLUSION:These results indicate that direct conversion of lipopeptides to lipopeptoids can result in compounds with comparable antimicrobial activity, favorable mammalian cell toxicity, and excellent proteolytic stability.
journal_name
Int J Antimicrob Agentsjournal_title
International journal of antimicrobial agentsauthors
Green RM,Bicker KLdoi
10.1016/j.ijantimicag.2020.106048subject
Has Abstractpub_date
2020-08-01 00:00:00pages
106048issue
2eissn
0924-8579issn
1872-7913pii
S0924-8579(20)30218-1journal_volume
56pub_type
杂志文章abstract::Chemotherapy is a cornerstone of cancer treatment but it can have serious side effects, such as intestinal mucositis. This work reports the susceptibility/resistance profiles of 34 species of lactic acid bacteria (LAB), bifidobacteria and other intestinal bacteria from different collections to various chemotherapeutic...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2016.07.011
更新日期:2016-11-01 00:00:00
abstract::This study looked for beta-lactamase production in 100 Prevotella isolates. MICs were determined for amoxycillin, ticarcillin, amoxycillin+clavulanate, cephalothin, cefuroxime, cefixime, cefpodoxime and cefotaxime using the reference agar dilution method (standard M11 A4, NCCLS). Beta-lactamase activity was detected i...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/s0924-8579(02)00352-7
更新日期:2003-03-01 00:00:00
abstract::An open, multicentre study was performed in hospital in-patients at a total of 12 German hospitals to investigate the efficacy and tolerability of sulbactam combined with mezlocillin, piperacillin or cefotaxime in severe bacterial infections. A total of 155 patients were recruited into the study, of whom 48 were suffe...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:
更新日期:1996-04-01 00:00:00
abstract::Due to the ever-increasing number of immunocompromised patients, both localised and life-threatening systemic fungal infections are on the increase. Conventional treatment is of limited help, not in the least due to a less optimum benefit-to-risk ratio. Moreover, emerging pathogens with reduced antimicrobial susceptib...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章,评审
doi:10.1016/s0924-8579(00)00323-x
更新日期:2001-02-01 00:00:00
abstract::Recently, a novel coronavirus (2019-nCoV), officially known as severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), emerged in China. Despite drastic containment measures, the spread of this virus is ongoing. SARS-CoV-2 is the aetiological agent of coronavirus disease 2019 (COVID-19) characterised by pulmonar...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2020.105938
更新日期:2020-05-01 00:00:00
abstract::We report seven cases of infective endocarditis caused by USA300 methicillin-resistant Staphylococcus aureus (MRSA) at an urban, tertiary care, academic institution. Five strains were community associated and two were healthcare associated. All patients were injection drug users. Staphylococcus aureus isolates were ch...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2007.02.007
更新日期:2007-07-01 00:00:00
abstract::The role of membrane permeabilisation and disruption in the mechanism of action of some polymyxin analogues against Gram-negative organisms is contentious. The effects of polymyxin B (PMB) and its analogue polymyxin B nonapeptide (PMBN) on Escherichia coli envelopes should correlate, but previous work by other workers...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2007.10.005
更新日期:2008-03-01 00:00:00
abstract::The in vitro activities of cefixime, a new third-generation cephalosporin, and of 18 other antimicrobial agents against 18 strains of Helicobacter pylori were determined. The strains of H. pylori were isolated from gastric biopsy specimens and tested for sensitivity to antibiotics by an agar dilution technique under m...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/0924-8579(93)90020-6
更新日期:1993-01-01 00:00:00
abstract::The in vitro activity of the steroidal amide 3beta-acetoxy-17beta-(L-prolyl)amino-5alpha-androstane against 179 gram-positive clinical isolates was examined. The minimum bactericidal concentration (MBC)/MIC ratios were < or = 2 for 73% of methicillin-resistant Staphyllococcus aureus, 59% of vancomycin-resistant Entero...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/s0924-8579(00)00156-4
更新日期:2000-08-01 00:00:00
abstract::As shown in a previous study, the outcome of multidrug-resistant tuberculosis (MDR-TB) in France is not satisfactory (41% success rate). To improve the management and outcome of patients with MDR-TB, a prospective intervention study was carried out in 1998-1999 by National Reference Centre (NRC) staff. NRC staff conta...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2006.11.023
更新日期:2007-04-01 00:00:00
abstract::Skin and soft tissue infections (SSTIs) are common and range in severity from minor, self-limiting, superficial infections to life-threatening diseases requiring all the resources of modern medicine. The classification of SSTIs can be based on the anatomical site, clinical severity or microbial cause, but some classif...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章,评审
doi:10.1016/S0924-8579(09)70541-2
更新日期:2009-07-01 00:00:00
abstract::Febrile neutropenia (FN) is associated with substantial morbidity and necessitates empirical broad-spectrum antimicrobial treatment. In this prospective cohort study, a risk-guided management strategy for FN using empirical piperacillin/tazobactam (TZP) or a carbapenem was evaluated. The analysis involved 723 FN episo...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2018.04.017
更新日期:2018-09-01 00:00:00
abstract::Polymyxins were recently approved for the clinical treatment of carbapenem-resistant Enterobacteriaceae (CRE) infections in China. The aim of this study was to determine the prevalence and molecular mechanisms of polymyxin-resistant CRE prior to the clinical application of polymyxin and to evaluate the potential for e...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2020.106262
更新日期:2020-12-23 00:00:00
abstract::The fungal pathogen Cryptococcus neoformans poses a major threat to immunocompromised patients and is a leading killer of human immunodeficiency virus (HIV)-infected patients worldwide. Cryptococci are known to manipulate host macrophages and can either remain latent or proliferate intracellularly within the host phag...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2016.04.018
更新日期:2016-07-01 00:00:00
abstract::Aspergillus spp. are responsible for an increasing number of fungal infections in immunocompromised and transplant patients. Local anaesthetics (LAs) are growth inhibitors of bacteria and yeasts. Subinhibitory concentrations of the LAs lidocaine and bupivacaine blocked the germination of Aspergillus fumigatus, Aspergi...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2005.11.011
更新日期:2006-04-01 00:00:00
abstract::Aspergillus flavus is the second most common Aspergillus spp. causing invasive infections in immunocompromised patients. Extensive prophylactic use of voriconazole (VCZ) in immunocompromised patients may enhance the selection of VCZ-resistant clinical isolates of A. flavus, compromising the effectiveness of this antif...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2008.06.018
更新日期:2008-12-01 00:00:00
abstract::Of the 16,024 patients hospitalized from January 1995 to October 1997, 397 (2.4%) acquired nosocomial pneumonia and the aetiological agent was defined in 101 (25%). About 82% developed late onset pneumonia (>7 days of hospitalization). The site of isolation of microorganisms was bronchoalveolar lavage (BAL) (49%), blo...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/s0924-8579(00)00316-2
更新日期:2001-02-01 00:00:00
abstract::Many antimicrobial agents including new quinolones (NQs) influence the cellular defense mechanisms such as polymorphonuclear leukocytes (PMNs), macrophages and lymphocytes. We examined the effects of NQs on superoxide (SO) production of PMNs following stimulation of phorbol myristate acetate (PMA). Ofloxacin (OFLX) an...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/0924-8579(95)00024-0
更新日期:1995-12-01 00:00:00
abstract::A total of 89 patients, (>18 years), with symptoms of chronic prostatitis and inflammatory findings as well as the presence of Chlamydia trachomatis confirmed by DNA/RNA DIGENE hybridization method and/or by isolation, McCoy culture and Lugol stain in expressed prostatic secretion or in voided bladder urine collected ...
journal_title:International journal of antimicrobial agents
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1016/s0924-8579(03)00056-6
更新日期:2003-05-01 00:00:00
abstract::Stenotrophomonas maltophilia and Acinetobacter baumannii are recognised as important nosocomial pathogens; however, due to their intrinsic resistance to multiple antibiotics, treatment options are limited. Polyphenols from black tea have been shown to possess antibacterial action. In this study, the antibacterial effe...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2011.07.006
更新日期:2011-11-01 00:00:00
abstract::Changes in the indigenous vaginal microflora with uropathogenic bacteria can predispose women to frequently recurring bacterial cystitis. Lactobacilli used as probiotics have played an important role in preventing the colonization of pathogenic bacteria in the vagina. A prospective clinical pilot study was performed t...
journal_title:International journal of antimicrobial agents
pub_type: 临床试验,杂志文章
doi:10.1016/j.ijantimicag.2006.05.008
更新日期:2006-08-01 00:00:00
abstract::Seventy laboratories in nine European countries (Belgium, France, Germany, Italy, The Netherlands, Portugal, Spain, Switzerland and the UK) each collected 100 consecutive gram-positive bacterial pathogens during 1995. MICs were determined by a co-ordinating laboratory in each country using an agar incorporation method...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章,多中心研究
doi:10.1016/s0924-8579(98)00050-8
更新日期:1998-11-01 00:00:00
abstract::Oritavancin is a lipoglycopeptide antibiotic under investigation for the treatment of serious infections caused by Gram-positive bacteria. Oritavancin has demonstrated rapid dose-dependent bactericidal activity towards vancomycin-susceptible and -resistant enterococci, meticillin-susceptible and -resistant Staphylococ...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章,评审
doi:10.1016/j.ijantimicag.2010.06.048
更新日期:2010-11-01 00:00:00
abstract::Carbapenemase-producing (CP) Pseudomonas aeruginosa is rare compared with mutation-driven carbapenem-resistance, but this situation may be changing. A collection of CP P. aeruginosa isolates was characterized in this study. In 2016, 232 unduplicated carbapenem-resistant P. aeruginosa isolates, of which 71 (30.6%) carr...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2020.106026
更新日期:2020-07-01 00:00:00
abstract::Two hundred and twenty-eight episodes of infective endocarditis in adult patients (mean age 36 years) were reviewed retrospectively. There were 183 episodes (80%) of native valve, 15 (7%) early prosthetic valve and 30 (13%) late prosthetic valve endocarditis. The most common predisposing factor was rheumatic valvular ...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/s0924-8579(01)00344-2
更新日期:2001-07-01 00:00:00
abstract::Pseudomonas aeruginosa (PA) is a major cause of healthcare-associated infections. Antipseudomonal carbapenems are among the antimicrobial agents used to treat PA infections, but several mechanisms of resistance, including the production of a carbapenemase (CP), may compromise their clinical efficacy. The objectives of...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2020.105959
更新日期:2020-06-01 00:00:00
abstract::Nasal colonisation with Staphylococcus aureus is a risk factor for invasive infection in human immunodeficiency virus (HIV)-positive individuals. This study aimed to characterise colonising S. aureus from regions with a high HIV prevalence. Single nasal swabs were taken from a total of 374 HIV-positive and 370 healthy...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2012.05.016
更新日期:2012-09-01 00:00:00
abstract:BACKGROUND:Tuberculosis (TB) causes 25% of all deaths among individuals infected with human immunodeficiency virus (HIV). Rifampicin (RIF) is a potent inducer of drug metabolizing enzymes and drug transporters, and co-administration with dolutegravir (DTG) reduces DTG exposure; this can be overcome by doubling the DTG ...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2019.04.009
更新日期:2019-08-01 00:00:00
abstract::Fifteen carbapenem-non-susceptible Escherichia coli isolates obtained during the period May 2010 to April 2011 in a hospital and a long-term care facility (LTCF) in Larissa (Central Greece) were investigated. Minimum inhibitory concentrations (MICs) to various antimicrobial agents were determined by Etest. Carriage of...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2011.11.003
更新日期:2012-03-01 00:00:00
abstract::Bacteria growing as biofilms are less susceptible to antimicrobial agents than free-living cells. Several infectious processes are now recognised to be related to biofilm formation. Pseudomonas aeruginosa is a known biofilm-producing organism and often resistant to several antibiotics. To assess the relationship betwe...
journal_title:International journal of antimicrobial agents
pub_type: 杂志文章
doi:10.1016/j.ijantimicag.2004.03.012
更新日期:2004-10-01 00:00:00