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Novel amphiphilic dendrimers as antibacterial and antitumoral agents.

Marta K. Sowińska 1Jolanta Solecka 2Aleksandra M. Rajnisz 2Marta Bochynska 3Andrzej W. Lipkowski 3Zofia Lipkowska 1

1. Polish Academy of Science, Institute of Organic Chemistry, Kasprzaka 44/52, Warszawa 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, Pawinskiego 5, Warszawa 02-106, Poland

Abstract

The continuing rise in microbial drug resistance has led to widespread problems in the treatment of bacterial infections. It is therefore necessary, to find new compounds able to overcome this problem. Such a promising new class of antibacterial drugs are dendrimers, which are structurally well-defined artificial macromolecules with branched structure and polyvalent nature. There are innumerable ways of designing dendrimers, as various types of initiator cores and building blocks can be used. Length of the dendritic arms, shape, character of the surface, and display of terminal functional groups can all be customized to fit a specific purpose.

Here, we present the synthesis, antimicrobial activity against Gram(+), Gram(-) bacteria and hemotoxicity of a new type of dendrimers with symmetrical and unsymmetrical interior, containing 3,5-dihydroxybenzoic acid (DHBA) as a branching element. They are designed for effective interactions with biological membranes and therefore, are characterized by relatively wide distribution of long arms, terminated with Lys or Trp amino acids. Additionally their antiproliferative activity against human melanoma cells is given.

Financial support from the National Center for Research and Development, grant NR13-0153-10/2010 and Mazovian PhD Scholarship funded by Mazovia Voivodeship, is acknovledged.

 

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Related papers

Presentation: Poster at VIII Multidyscyplinarna Konferencja Nauki o Leku, by Marta K. Sowińska
See On-line Journal of VIII Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2012-03-15 09:03
Revised:   2012-03-15 09:03