Highly efficient transfection of rat cortical neurons using carbosilane dendrimers unveils a neuroprotective role for HIF-1alpha in early chemical hypoxia-mediated neurotoxicity

Pharm Res. 2009 May;26(5):1181-91. doi: 10.1007/s11095-009-9839-9. Epub 2009 Feb 4.

Abstract

Purpose: To study the effect of a non-viral vector (carbosilane dendrimer) to efficiently deliver small interfering RNA to postmitotic neurons to study the function of hypoxia-inducible factor-1alpha (HIF1-alpha) during chemical hypoxia-mediated neurotoxicity.

Methods: Chemical hypoxia was induced in primary rat cortical neurons by exposure to CoCl(2). HIF1-alpha levels were determined by Western Blot and toxicity was evaluated by both MTT and LDH assays. Neurons were incubated with dendriplexes containing anti-HIF1-alpha siRNA and both uptake and HIF1-alpha knockdown efficiency were evaluated.

Results: We report that a non-viral vector (carbosilane dendrimer) can deliver specific siRNA to neurons and selectively block HIF1-alpha synthesis with similar efficiency to that achieved by viral vectors. Using this method, we have found that this transcription factor plays a neuroprotective role during the early phase of chemical hypoxia-mediated neurotoxicity.

Conclusion: This work represents a proof-of-concept for the use of carbosilane dendrimers to deliver specific siRNA to postmitotic neurons to block selected protein synthesis. This indicates that this type of vector is a good alternative to viral vectors to achieve very high transfection levels in neurons. This also suggests that carbosilane dendrimers might be very useful for gene therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Hypoxia / drug effects
  • Cell Survival / drug effects
  • Cerebral Cortex / cytology
  • Cobalt
  • Dendrimers / chemistry
  • Dendrimers / toxicity*
  • Gene Knockdown Techniques
  • Genetic Therapy
  • Hypoxia / chemically induced
  • Hypoxia / genetics*
  • Hypoxia / therapy*
  • Hypoxia-Inducible Factor 1, alpha Subunit / genetics*
  • Neurons / drug effects*
  • Neurons / metabolism
  • Neuroprotective Agents / administration & dosage
  • Neuroprotective Agents / pharmacology
  • RNA, Small Interfering / administration & dosage*
  • RNA, Small Interfering / genetics
  • RNA, Small Interfering / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Silanes / chemistry
  • Silanes / toxicity*
  • Transfection

Substances

  • Dendrimers
  • Hypoxia-Inducible Factor 1, alpha Subunit
  • Neuroprotective Agents
  • RNA, Small Interfering
  • Silanes
  • carbosilane
  • Cobalt