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Effects D-tryptophan substitutions on the activity and toxicity of antimicrobial dendrimers

Paulina Zielińska 1Jolanta Solecka 2Aleksandra M. Rajnisz 2Marta Bochyńska 3Andrzej W. Lipkowski 3Zofia Lipkowska 1

1. Polish Academy of Science, Institute of Organic Chemistry, Kasprzaka 44/52, Warsaw 01-224, Poland
2. National Institute of Public Health-National Institute of Hygiene (NIZP-PZH), Chocimska, Warszawa 00-791, Poland
3. Mossakowski Medical Research Centre, Polish Academy of Sciences, Pawińskiego 5, Warsaw 02-106, Poland


The increasing resistance of bacteria to currently available antibiotics necessitates every effort to develop novel antibacterial agents with lower rates of resistance. Amphipathic cationic dendrimers have been proposed as potential new class of antimicrobial agents, which are analogs of natural antimicrobial peptides (AMPs).

According to literature, incorporation of D-isomers alongside L-isomers in previously toxic AMPs reduce their toxicity without reducing their antimicrobial activity. The aim of this study was to examine the influence of introducing D- amino acid residues into dendrimeric molecules on their biological properties.

Therefore, we synthesized a series of dendrimers based on highly tetrabranched amino acid core with lipophilic C-terminus and arms terminated by L- or D-Trp residues. Their potency against Gram(-) and Gram(+) bacteria and their hemolytic activity was studied. The designed compounds were also evaluated for their antiproliferative activity against human melanoma cells.

Financial support from the National Center for Research and Development, grant NR13-0153-10/2010 and in part grant N204 239436 from the Ministry of Sciences and Higher Education,  is acknowledged.


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Related papers

Presentation: Poster at VIII Multidyscyplinarna Konferencja Nauki o Leku, by Paulina Zielińska
See On-line Journal of VIII Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2012-03-15 08:49
Revised:   2012-03-15 08:49