DNA complexing lipopolythiourea

Bioconjug Chem. 2004 Nov-Dec;15(6):1342-8. doi: 10.1021/bc049920n.

Abstract

We present a neutral lipopolythiourea (DTTU) as a potential DNA-binding agent. Light scattering experiments showed that mixing a lipopolythiourea with dipalmitoylphosphatidylcholine (DPPC/DTTU) led to small particles with sizes ranging from 100 to 150 nm at optimum conditions. Setting a fixed DNA amount, an increasing amount of DTTU/DPPC or DPPC lipids was added. Particle size increased only with DTTU/DPPC, indicating that interaction occurred between the DTTU/DPPC particles and DNA. In the same way, only DTTU/DPPC limited the ethidium bromide accessibility to plasmid DNA. These data suggest that DTTU/DPPC liposomes associate to DNA, which was confirmed by agarose gel experiments. To prove the active part of the DTTU lipid itself in DNA compaction, pegoylated-lipid was used. Cholesterol-PEG(2000) alone was not able to condense DNA. In contrast, DTTU/PEG-cholesterol was able to retain plasmid DNA on an agarose gel. In vivo injection of DTTU/DPPC/complexes was studied. Circulation time increase for noncationic particles as compared to cationic. More obvious was the lack of nonspecific accumulation in the lung, where a gain of 3 to 40 fold was measured.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1,2-Dipalmitoylphosphatidylcholine / chemistry
  • 1,2-Dipalmitoylphosphatidylcholine / metabolism
  • Animals
  • Biological Availability
  • Carcinoma, Lewis Lung / drug therapy
  • Carcinoma, Lewis Lung / metabolism
  • DNA / administration & dosage
  • DNA / chemistry
  • DNA / metabolism*
  • Female
  • Liposomes
  • Mice
  • Mice, Inbred C57BL
  • Neoplasm Transplantation
  • Thiourea / administration & dosage
  • Thiourea / chemical synthesis*
  • Thiourea / metabolism*

Substances

  • Liposomes
  • 1,2-Dipalmitoylphosphatidylcholine
  • DNA
  • Thiourea