Change search
Link to record
Permanent link

Direct link
Publications (2 of 2) Show all publications
Labrière, C., Kondori, N., Seth Caous, J., Boomgaren, M., Sandholm, K., Ekdahl, K. N. N., . . . Svenson, J. (2018). Development and evaluation of cationic amphiphilic antimicrobial 2,5-diketopiperazines. Journal of Peptide Science, 24(7), Article ID e3090.
Open this publication in new window or tab >>Development and evaluation of cationic amphiphilic antimicrobial 2,5-diketopiperazines
Show others...
2018 (English)In: Journal of Peptide Science, ISSN 1075-2617, E-ISSN 1099-1387, Vol. 24, no 7, article id e3090Article in journal (Refereed) Published
Abstract [en]

Both pathogenic bacteria and fungi are developing resistance to common antimicrobial treatment at an alarming rate. To counteract this development, it is of essence to develop new classes of antimicrobial agents. One such class is antimicrobial peptides, most of which are derived from the innate immune system. In this study, a series of novel 2,5-diketopiperazines were designed, synthesized, and evaluated for their antimicrobial abilities. The compounds were designed to probe the pharmacophore dictated for short linear mimics of antimicrobial cationic peptides, and as such, the compounds contain a range of cationic and hydrophobic functionalities. Several of the prepared compounds displayed high antimicrobial activities toward bacteria and also against human pathogenic fungi. Of particular interest was the high activity toward fungal strains with an inherent increased resistance toward conventional antifungal agents. The most effective compounds displayed inhibition of Candida glabrata and Candida krusei growth at concentrations between 4 and 8 μg/mL, which is comparable to commercial antifungal agents in use. Structure activity relationship studies revealed a similar dependence on cationic charge and the volume of the hydrophobic bulk as for linear cationic antimicrobial peptides. Finally, the hemolytic activity of selected compounds was evaluated, which revealed a potential to produce active compounds with attenuation of unwanted hemolysis. The findings highlight the potential of cyclic cationic amphiphilic peptidomimetics as a class of promising compounds for the treatment of infections caused by microorganisms with an increased resistance to conventional antimicrobial agents. © 2018 European Peptide Society and John Wiley & Sons, Ltd.

Place, publisher, year, edition, pages
John Wiley and Sons Ltd, 2018
2, 5-diketopiperazine, Antifungal agents, Antimicrobial, Candida krusei, MRSA, Structure-activity relationship
National Category
Natural Sciences
urn:nbn:se:ri:diva-34356 (URN)10.1002/psc.3090 (DOI)2-s2.0-85047664224 (Scopus ID)
Available from: 2018-08-07 Created: 2018-08-07 Last updated: 2020-07-28Bibliographically approved
Seth Caous, J., Lövenklev, M., Fäldt, J. & Langton, M. (2013). Adhesion of Streptococcus mitis and Actinomyces oris in co-culture to machined and anodized titanium surfaces as affected by atmosphere and pH (ed.). BMC Oral Health, 13(1), Article ID 4.
Open this publication in new window or tab >>Adhesion of Streptococcus mitis and Actinomyces oris in co-culture to machined and anodized titanium surfaces as affected by atmosphere and pH
2013 (English)In: BMC Oral Health, ISSN 1472-6831, E-ISSN 1472-6831, Vol. 13, no 1, article id 4Article in journal (Refereed) Published
Abstract [en]

Background: With the rising demand for osseointegrated titanium implants for replacing missing teeth, often in patients with a history of periodontitis, implant-related infections have become an issue of growing concern. Novel methods for treating and preventing implant-associated infections are urgently needed. The aim of this study was to investigate if different pH, atmosphere and surface properties could restrict bacterial adhesion to titanium surfaces used in dental implants. Methods: Titanium discs with machined or anodized (TiUnite™) surface were incubated with a co-culture of Streptococcus mitis and Actinomyces oris (early colonizers of oral surfaces) at pH 5.0, 7.0 and 9.0 at aerobic or anaerobic atmosphere. The adhesion was analysed by counting colony forming (CFU) units on agar and by confocal laser scanning microscopy (CLSM).Results: The CFU analysis showed that a pH of 5.0 was found to significantly decrease the adhesion of S. mitis, and an aerobic atmosphere, the adhesion of A. oris. S. mitis was found in significantly less amounts on the anodized surface than the machined surface, while A. oris was found in equal amounts on both surfaces. The CLSM analysis confirmed the results from the CFU count and provided additional information on how the two oral commensal species adhered to the surfaces: mainly in dispersed clusters oriented with the groves of the machined surface and the pores of the anodized surface. Conclusions: Bacterial adhesion by S. mitis and A. oris can be restricted by acidic pH and aerobic atmosphere. The anodized surface reduced the adhesion of S. mitis compared to the machined surface; while A. oris adhered equally well to the pores of the anodized surface and to the grooves of the machined surface. It is difficult to transfer these results directly into a clinical situation. However, it is worth further investigating these findings from an in vitro perspective, as well as clinically, to gain more knowledge of the effects acid pH and aerobic atmosphere have on initial bacterial adhesion.

Food Engineering, Livsmedelsteknik
National Category
Food Science
urn:nbn:se:ri:diva-8407 (URN)10.1186/1472-6831-13-4 (DOI)23298213 (PubMedID)2-s2.0-84873060528 (Scopus ID)
Available from: 2016-09-08 Created: 2016-09-08 Last updated: 2020-12-01Bibliographically approved

Search in DiVA

Show all publications