Anti-allergic effects of phlorotannins on histamine release via binding inhibition between IgE and Fc epsilonRI

Two bioactive phloroglucinol derivatives, fucodiphloroethol G (1) and phlorofucofuroeckol A (3) were first isolated from Eckolonia cava (EC) and characterized by nuclear magnetic resonance (NMR) spectroscopic methods, along with eckol (2). In this study, anti-allergic activities of phloroglucinol derivatives were assessed on human basophilic leukemia (KU812) and rat basophilic leukemia (RBL-2H3) cell lines using a histamine release assay. Both compounds 1 and 3 exhibited a significant inhibitory activity against histamine release. Meanwhile, the potential inhibitory mechanism was also suggested as the suppression of binding activity between IgE and Fc epsilonRI by the cytometric analysis. These results suggested that compounds 1 and 3 could be the key effectors in the crude methanol extract of EC against allergy disease and used as novel candidates for development in the cosmetic and drug industries potentially.