An in vitro Study of Drug-induced Degranulation of Human HMC-1 Mast Cells and Rat RBL-2H3 Cells

Mast cells and basophils participate in biological responses such as inflammation and allergic reactions and contain potent mediators such as histamine and cytokines. Some drugs, for example opioids, are known to trigger mast cell degranulation with the release of immunogenic mediators that may cause severe side effects. The aim of this study was to investigate if the human mast cell line HMC-1 is a useful model to study codeine-induced degranulation in vitro. The rat basophilic leukemia RBL-2H3 cell line was used as a reference. Timeand concentration-dependent effects of codeine, compound 48/80, and A23187 on the degranulation of HMC-1 cells and RBL-2H3 cells were investigated by measuring extracellular levels of β-hexosaminidase and [H]serotonin. Neither codeine nor compound 48/80 produced any significant basophil or mast cell degranulation, whereas the calcium ionophore A23187 triggered a degranulation of both cell lines. In conclusion, none of the cell lines are useful as relevant, robust and reproducible in vitro models to study drug-induced mast cell degranulation.