Systemic application of sirolimus prevents neointima formation not via a direct anti-proliferative effect but via its anti-inflammatory properties

Int J Cardiol. 2017 Jul 1:238:79-91. doi: 10.1016/j.ijcard.2017.03.052. Epub 2017 Mar 14.

Abstract

Background: Systemic treatment with sirolimus, as used for immunosuppression in transplant patients, results in markedly low rates of in-stent restenosis. Since the underlying mechanisms remain obscure, we aimed to determine the molecular and cellular effects of systemic sirolimus treatment on vascular remodeling processes.

Methods and results: Systemic sirolimus treatment significantly reduced smooth muscle cell (SMC) proliferation 14days after wire-induced injury and neointima formation 28days after injury in C57BL/6 mice, while simultaneously impairing re-endothelialization. Interestingly, in vitro, sirolimus had no direct effect on the proliferation of SMC or endothelial cells (EC) at serum concentrations observed after systemic application. In contrast, sirolimus reduced the adhesion of leukocytes (CD45+) and bone marrow-derived progenitor cells (CD34+) to activated EC by down-regulating the adhesion molecules ICAM-1 and VCAM-1. In addition, sirolimus treatment also significantly reduced the upregulation of ICAM-1 and VCAM-1 and the recruitment of monocytic cells (MOMA-2+) in neointimal lesions in vivo.

Conclusion: Our findings show that systemic sirolimus treatment effectively prevents SMC and EC proliferation in vivo without directly affecting these cells. Instead, sirolimus prevents neointima formation and re-endothelialization by attenuating the inflammatory response after injury with secondary effects on SMC and EC proliferation. Thus, despite a similar net effect, the mechanisms of systemic sirolimus treatment are largely different from the local effects achieved after application of sirolimus-eluting stents.

Keywords: Inflammation; Neointima formation; Progenitor cells; Re-endothelialization; Sirolimus; Smooth muscle cells.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use*
  • Cell Proliferation / drug effects*
  • Cell Proliferation / physiology
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Humans
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Transgenic
  • Neointima / pathology
  • Neointima / prevention & control*
  • Random Allocation
  • Sirolimus / pharmacology
  • Sirolimus / therapeutic use*
  • Treatment Outcome

Substances

  • Anti-Inflammatory Agents
  • Sirolimus