Effects of sotrastaurin, mycophenolic acid and everolimus on human B-lymphocyte function and activation

Transpl Int. 2012 Oct;25(10):1106-16. doi: 10.1111/j.1432-2277.2012.01537.x. Epub 2012 Jul 21.

Abstract

Humoral rejection processes may lead to allograft injury and subsequent dysfunction. Today, only one B-cell-specific agent is in clinical use and the effects of standard and new immunosuppressant substances on B-cell activation and function are not fully clarified. The impact of sotrastaurin, mycophenolic acid and everolimus on human B-lymphocyte function was assessed by analysing proliferation, apoptosis, CD80/CD86 expression and immunoglobulin and IL-10 production in primary stimulated B cells. In addition, B-cell co-cultures with pre-activated T cells were performed to evaluate the effect of the different immunosuppressive agents on T-cell-dependent immunoglobulin production. Sotrastaurin did not inhibit B-cell proliferation, CD80/CD86 expression, and IgG production and had only minor effects on IgM levels at the highest concentration administered. In contrast, mycophenolic acid and everolimus had strong effects on all B-cell functions in a dose-dependent manner. All immunosuppressive agents caused decreased immunoglobulin levels in T-cell-dependent B-cell cultures. The data provided here suggest that mycophenolic acid and everolimus, but not sotrastaurin, are potent inhibitors of human B-lymphocyte function and activation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Apoptosis
  • B-Lymphocytes / drug effects
  • B-Lymphocytes / immunology*
  • B7-1 Antigen / biosynthesis
  • B7-2 Antigen / biosynthesis
  • Cell Membrane / metabolism
  • Cell Proliferation
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / pharmacology
  • Everolimus
  • Graft Rejection
  • Humans
  • Immunity, Humoral
  • Immunoglobulin G / metabolism
  • Immunoglobulin M / metabolism
  • Immunoglobulins / metabolism
  • Immunosuppressive Agents / pharmacology
  • Immunosuppressive Agents / therapeutic use
  • Interleukin-10 / metabolism
  • Leukocytes, Mononuclear / cytology
  • Mycophenolic Acid / therapeutic use*
  • Pyrroles / therapeutic use*
  • Quinazolines / therapeutic use*
  • Sirolimus / analogs & derivatives*
  • Sirolimus / therapeutic use
  • Transplantation, Homologous

Substances

  • B7-1 Antigen
  • B7-2 Antigen
  • Enzyme Inhibitors
  • Immunoglobulin G
  • Immunoglobulin M
  • Immunoglobulins
  • Immunosuppressive Agents
  • Pyrroles
  • Quinazolines
  • Interleukin-10
  • sotrastaurin
  • Everolimus
  • Mycophenolic Acid
  • Sirolimus