FTY720 Exerts Anti-Glioma Effects by Regulating the Glioma Microenvironment Through Increased CXCR4 Internalization by Glioma-Associated Microglia

Front Immunol. 2020 Mar 4:11:178. doi: 10.3389/fimmu.2020.00178. eCollection 2020.

Abstract

Background: Glioblastoma (GBM) is one of the most malignant and aggressive primary brain tumors. The incurability of glioblastoma is heavily influenced by the glioma microenvironment. FTY720, a potent immunosuppressant, has been reported to exert anti-tumor effects in glioblastoma. However, the impact of FTY720 on the glioma microenvironment remains unclear. Methods: We examined the effects of FTY720 on the distribution and polarization of glioma-associated microglia and macrophages (GAMs) in glioma-bearing rats using immunofluorescence staining. qRT-PCR and Western blotting were used to detect the expressions of CXCR4 and MAPK pathway-related signal molecules on microglia in the coculture system. The levels of inflammatory factors were tested via ELISA. Wound healing assay and Matrigel invasion assay were used to determine the migration and invasion of C6 glioma cells. Results: We discovered that FTY720 could inhibit the growth, migration, and invasion of glioma by targeting GAMs to impede their effect on glioma cells. Simultaneously, FTY720 could block the chemoattraction of GAMs by inhibiting MAPK-mediated secretion of IL-6 through increased internalization of CXCR4. Moreover, microglia and macrophages are polarized from pro-glioma to an anti-tumor phenotype. Conclusion: These results provide novel insights into the inhibitory effects of FTY720 on glioma by targeting GAMs-glioma interaction in the tumor microenvironment.

Keywords: FTY720; chemoattraction; glioma microenvironment; glioma-associated microglia and macrophages; polarization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allografts
  • Animals
  • Antineoplastic Agents / administration & dosage*
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Polarity / drug effects
  • Disease Models, Animal
  • Fingolimod Hydrochloride / administration & dosage*
  • Glioblastoma / drug therapy*
  • Glioblastoma / metabolism*
  • Glioblastoma / pathology
  • Macrophages / drug effects
  • Macrophages / metabolism
  • Male
  • Microglia / drug effects*
  • Microglia / metabolism
  • Mitogen-Activated Protein Kinases / genetics
  • Mitogen-Activated Protein Kinases / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Receptors, CXCR4 / genetics
  • Receptors, CXCR4 / metabolism*
  • Signal Transduction / drug effects
  • Tumor Microenvironment / drug effects*

Substances

  • Antineoplastic Agents
  • Cxcr4 protein, rat
  • Receptors, CXCR4
  • Mitogen-Activated Protein Kinases
  • Fingolimod Hydrochloride