Inhibition of JAK3 and PKC via Immunosuppressive Drugs Tofacitinib and Sotrastaurin Inhibits Proliferation of Human B Lymphocytes In Vitro

Transplant Proc. 2016 Nov;48(9):3046-3052. doi: 10.1016/j.transproceed.2016.07.052.

Abstract

Background: Antibody-mediated response in solid organ transplantation is critical for graft dysfunction and loss. The use of immunosuppressive agents partially inhibits the B-lymphocyte response leading to a risk of acute and chronic antibody-mediated rejection. This study evaluated the impact of JAK3 and PKC inhibitors tofacitinib (Tofa) and sotrastaurin (STN), respectively, on B-cell proliferation, apoptosis, and activation in vitro.

Methods: Human B cells isolated from peripheral blood of healthy volunteers were cocultured with CD40 ligand-transfected fibroblasts as feeder cells in the presence of interleukin (IL) 2, IL-10, and IL-21. The cocultures were treated with immunosuppressants Tofa, STN, and rapamycin (as a control), to analyze the proliferation and apoptosis of B cells by means of Cyquant and flow cytometry, respectively. CD27 and IgG staining were applied to evaluate whether treatments modified the activation of B cells.

Results: Tofa and STN were able to inhibit B-cell proliferation to the same extent as rapamycin, without inducing cell apoptosis. After 6 days in coculture with feeder cells, all B cells showed CD27 memory B-cell phenotype. None of the immunosuppressive treatments modified the proportion between class-switched and non-class-switched memory B cells observed in nontreated cultures. The high predominance of CD27+CD24+ phenotype was not modified by any immunosuppressive treatment.

Conclusions: Our results show that Tofa and STN can suppress B-cell antibody responses to an extent similar to rapamycin, in vitro; therefore these compounds may be a useful therapy against antibody-mediated rejection in transplantation.

MeSH terms

  • Apoptosis / drug effects
  • B-Lymphocytes / drug effects*
  • B-Lymphocytes / immunology
  • CD40 Ligand / pharmacology
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Humans
  • Immunosuppressive Agents / pharmacology
  • Interleukin-10 / pharmacology
  • Interleukin-2 / pharmacology
  • Interleukins / pharmacokinetics
  • Janus Kinase 3 / antagonists & inhibitors*
  • Leukocytes, Mononuclear / drug effects
  • Lymphocyte Activation / drug effects
  • Piperidines / pharmacology*
  • Protein Kinase C / antagonists & inhibitors*
  • Protein Kinase Inhibitors / pharmacology*
  • Pyrimidines / pharmacology*
  • Pyrroles / pharmacology*
  • Quinazolines / pharmacology*
  • Sirolimus / pharmacology

Substances

  • IL10 protein, human
  • Immunosuppressive Agents
  • Interleukin-2
  • Interleukins
  • Piperidines
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Pyrroles
  • Quinazolines
  • Interleukin-10
  • CD40 Ligand
  • sotrastaurin
  • tofacitinib
  • JAK3 protein, human
  • Janus Kinase 3
  • Protein Kinase C
  • interleukin-21
  • Sirolimus