In vivo efficacy of a phosphodiester TLR-9 aptamer and its beneficial effect in a pulmonary anthrax infection model

Cell Immunol. 2008 Feb;251(2):78-85. doi: 10.1016/j.cellimm.2008.04.001. Epub 2008 May 20.

Abstract

Immunostimulatory oligonucleotide (ISS-ODN) used as adjuvants are commonly modified with phosphorothioate (PS). The PS backbone prevents nuclease degradation, but confers undesired side effects, including systemic cytokine release. Previously, R10-60, a phosphodiester (PO) ISS-ODN, was structurally optimized as an intracellular Toll-like receptor-9 agonist. Here intravenous, intradermal and intranasal administration of PO R10-60 elicit local or adaptive immune responses with minimal systemic effects compared to a prototypic PS ISS-ODN in mice. Furthermore, prophylactic intranasal administration of PO R10-60 significantly delayed death in mice exposed to respiratory anthrax comparable to the PS ISS-ODN. The pattern of cytokine release suggested that early IL-1beta production might contribute to this protective effect, which was replicated with recombinant IL-1beta injections during infection. Hence, the transient effects from a PO TLR-9 agonist may be beneficial for protection in a bacterial bioterrorism attack, by delaying the onset of systemic infection without the induction of a cytokine syndrome.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Anthrax / immunology
  • Anthrax / microbiology
  • Anthrax / therapy*
  • Aptamers, Nucleotide / genetics
  • Aptamers, Nucleotide / pharmacology*
  • Bacillus anthracis / immunology*
  • Cytokines / immunology
  • Disease Models, Animal
  • Enzyme-Linked Immunosorbent Assay
  • Female
  • Immunization
  • Immunoglobulin G / blood
  • Kinetics
  • Lung Diseases / immunology
  • Lung Diseases / microbiology
  • Lung Diseases / therapy*
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Spores, Bacterial / immunology
  • Toll-Like Receptor 9 / genetics*
  • Toll-Like Receptor 9 / immunology

Substances

  • Aptamers, Nucleotide
  • Cytokines
  • Immunoglobulin G
  • Tlr9 protein, mouse
  • Toll-Like Receptor 9