Modulation of actin dynamics as potential macrophage subtype-targeting anti-tumour strategy

Sci Rep. 2017 Jan 30:7:41434. doi: 10.1038/srep41434.

Abstract

Tumour-associated macrophages mainly comprise immunosuppressive M2 phenotypes that promote tumour progression besides anti-tumoural M1 subsets. Selective depletion or reprogramming of M2 may represent an innovative anti-cancer strategy. The actin cytoskeleton is central for cellular homeostasis and is targeted for anti-cancer chemotherapy. Here, we show that targeting G-actin nucleation using chondramide A (ChA) predominantly depletes human M2 while promoting the tumour-suppressive M1 phenotype. ChA reduced the viability of M2, with minor effects on M1, but increased tumour necrosis factor (TNF)α release from M1. Interestingly, ChA caused rapid disruption of dynamic F-actin filaments and polymerization of G-actin, followed by reduction of cell size, binucleation and cell division, without cellular collapse. In M1, but not in M2, ChA caused marked activation of SAPK/JNK and NFκB, with slight or no effects on Akt, STAT-1/-3, ERK-1/2, and p38 MAPK, seemingly accounting for the better survival of M1 and TNFα secretion. In a microfluidically-supported human tumour biochip model, circulating ChA-treated M1 markedly reduced tumour cell viability through enhanced release of TNFα. Together, ChA may cause an anti-tumoural microenvironment by depletion of M2 and activation of M1, suggesting induction of G-actin nucleation as potential strategy to target tumour-associated macrophages in addition to neoplastic cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Actins / metabolism*
  • Caspases / metabolism
  • Cell Line, Tumor
  • Cell Movement / drug effects
  • Cell Survival / drug effects
  • Cells, Cultured
  • Cytotoxicity, Immunologic
  • Depsipeptides / pharmacology
  • Dose-Response Relationship, Drug
  • Humans
  • Immunomodulation
  • Macrophage Activation / immunology
  • Macrophages / drug effects
  • Macrophages / immunology*
  • Macrophages / metabolism*
  • Neoplasms / immunology*
  • Neoplasms / metabolism*
  • Neoplasms / pathology
  • Protein Transport
  • Signal Transduction / drug effects
  • Tumor Microenvironment* / immunology
  • Tumor Necrosis Factor-alpha / metabolism

Substances

  • Actins
  • Depsipeptides
  • Tumor Necrosis Factor-alpha
  • chondramide A
  • Caspases