Hyperbranched Cationic Glycogen Derivative-Mediated I κ B α Gene Silencing Regulates the Uveoscleral Outflow Pathway in Rats

Biomed Res Int. 2020 Dec 17:2020:8206849. doi: 10.1155/2020/8206849. eCollection 2020.

Abstract

The role of the IκB/NF-κB signaling pathway in the uveoscleral outflow pathway was investigated with IκBα gene silencing mediated by the 3-(dimethylamino)-1-propylamine-conjugated glycogen (DMAPA-Glyp) derivative. The IκBα-siRNA-loaded DMAPA-Glyp complex was transfected into the ciliary muscles of rats by intracameral injection (labeled as the DMAPA-Glyp+siRNA group). The Lipofectamine™ 2000 (Lipo)/siRNA complex and the naked siRNA were set as the controls. The mRNA and protein expression of IκBα, NF-κBp65, and MMP-2 were analyzed by real-time PCR, western blotting, and in situ gelatin zymography. Nuclear translocation of NF-κBp65 was analyzed by immunofluorescence. Rat intraocular pressure (IOP) was monitored pre- and postinjection. Gene transfection efficiency and toxicity of the DMAPA-Glyp derivative were also evaluated. After RNA interference (RNAi), IκBα mRNA and protein expression were significantly inhibited. NF-κBp65 mRNA and protein expression showed no significant differences. Nevertheless, nuclear translocation of NF-κBp65 occurred in the DMAPA-Glyp+siRNA group. Both mRNA expression and activity of MMP-2 increased, with the largest increase in the DMAPA-Glyp+siRNA group. IOP in the DMAPA-Glyp+siRNA group fell to the lowest level on day 3 after RNAi. The levels of Cy3-siRNA in the ciliary muscle of the DMAPA-Glyp+siRNA group did not significantly decrease over time. At 7 and 14 d after RNAi, no significant pathological damage was detectable in the eyes injected with the DMAPA-Glyp derivative or the DMAPA-Glyp/siRNA complex. Taken together, our results suggest that downregulation of IκBα expression in the ciliary muscle plays a crucial role in reducing the IOP values of rats. IκBα may become a new molecular target for lowering IOP in glaucoma. The DMAPA-Glyp derivative is safe and feasible as an effective siRNA vector in rat eyes.

MeSH terms

  • Animals
  • Anterior Eye Segment* / metabolism
  • Anterior Eye Segment* / physiology
  • Aqueous Humor* / metabolism
  • Aqueous Humor* / physiology
  • Diamines / chemistry
  • Drug Delivery Systems
  • Gene Silencing / physiology*
  • Glycogen / chemistry
  • I-kappa B Proteins* / genetics
  • I-kappa B Proteins* / metabolism
  • Male
  • NF-kappa B / genetics
  • NF-kappa B / metabolism
  • RNA, Small Interfering / genetics
  • Rats
  • Rats, Wistar
  • Signal Transduction / genetics*
  • Transfection

Substances

  • Diamines
  • I-kappa B Proteins
  • NF-kappa B
  • RNA, Small Interfering
  • Glycogen
  • 3-dimethylaminopropylamine