The cannabinoid CB₂ receptor agonist AM1241 enhances neurogenesis in GFAP/Gp120 transgenic mice displaying deficits in neurogenesis

Br J Pharmacol. 2014 Jan;171(2):468-79. doi: 10.1111/bph.12478.

Abstract

Background and purpose: HIV-1 glycoprotein Gp120 induces apoptosis in rodent and human neurons in vitro and in vivo. HIV-1/Gp120 is involved in the pathogenesis of HIV-associated dementia (HAD) and inhibits proliferation of adult neural progenitor cells (NPCs) in glial fibrillary acidic protein (GFAP)/Gp120 transgenic (Tg) mice. As cannabinoids exert neuroprotective effects in several model systems, we examined the protective effects of the CB₂ receptor agonist AM1241 on Gp120-mediated insults on neurogenesis.

Experimental approach: We assessed the effects of AM1241 on survival and apoptosis in cultures of human and murine NPCs with immunohistochemical and TUNEL techniques. Neurogenesis in the hippocampus of GFAP/Gp120 transgenic mice in vivo was also assessed by immunohistochemistry.

Key results: AM1241 inhibited in vitro Gp120-mediated neurotoxicity and apoptosis of primary human and murine NPCs and increased their survival. AM1241 also promoted differentiation of NPCs to neuronal cells. While GFAP/Gp120 Tg mice exhibited impaired neurogenesis, as indicated by reduction in BrdU⁺ cells and doublecortin⁺ (DCX⁺) cells, and a decrease in cells with proliferating cell nuclear antigen (PCNA), administration of AM1241 to GFAP/Gp120 Tg mice resulted in enhanced in vivo neurogenesis in the hippocampus as indicated by increase in neuroblasts, neuronal cells, BrdU⁺ cells and PCNA⁺ cells. Astrogliosis and gliogenesis were decreased in GFAP/Gp120 Tg mice treated with AM1241, compared with those treated with vehicle.

Conclusions and implications: The CB₂ receptor agonist rescued impaired neurogenesis caused by HIV-1/Gp120 insult. Thus, CB₂ receptor agonists may act as neuroprotective agents, restoring impaired neurogenesis in patients with HAD.

Keywords: CB2 agonist; GFAP/Gp120 transgenic mice; HIV-1 Gp120 protein; neural progenitor cells; neurogenesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Cannabinoids / pharmacology
  • Cell Differentiation / drug effects
  • Cell Survival / drug effects
  • Doublecortin Protein
  • Glial Fibrillary Acidic Protein / genetics*
  • HIV Envelope Protein gp120 / genetics*
  • Hippocampus / cytology
  • Hippocampus / drug effects
  • Humans
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Mice, Transgenic
  • Neural Stem Cells / drug effects
  • Neurogenesis / drug effects*
  • Neurogenesis / genetics
  • Neurogenesis / physiology
  • Primary Cell Culture
  • Real-Time Polymerase Chain Reaction
  • Receptor, Cannabinoid, CB2 / agonists*
  • Receptor, Cannabinoid, CB2 / biosynthesis

Substances

  • AM 1241
  • Cannabinoids
  • Dcx protein, mouse
  • Doublecortin Protein
  • Glial Fibrillary Acidic Protein
  • HIV Envelope Protein gp120
  • Receptor, Cannabinoid, CB2