Suppression of Intracellular Calcium Levels and Inhibition of Degranulation in RBL-2H3 Mast Cells by the Sesquiterpene Lactone Parthenolide

Abstract

Pretreatment with parthenolide for 60 min inhibited the antigen-induced degranulation of RBL-2H3 mast cells; the IC₅₀ value being 4.5 ± 0.4 µM. The inhibition was not due to suppression of the phosphatidylinositol 3-kinase pathway because the antigen-induced phosphorylation of Akt was not inhibited by parthenolide. The antigen-induced increase in intracellular calcium levels was prevented by parthenolide, suggesting that parthenolide inhibited the antigen-induced degranulation by suppressing an increase in intracellular calcium levels. In support of this, parthenolide was found to prevent ionomycin-induced degranulation by inhibiting an increase in intracellular calcium levels. Therefore, parthenolide inhibits the degranulation of mast cells by preventing an increase in intracellular calcium levels.

Key words

Tanacetum parthenium (L.) Sch. Bip. - Asteraceae - parthenolide - RBL‐2H3 mast cells - degranulation - β‐hexosaminidase - intracellular calcium

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