The Effects of Citrus Flavonoids on Human Basophil and Neutrophil Function

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Abstract
Fifteen selected citrus flavonoids representing several different chemical classes were studied for their effect on human basophil histamine release stimulated by three secretogogues (antigen; the tumor promoter phorbol ester, tetradecanoyl phorbol acetate (TPA); and the Ca2+ ionophore, A 23187). Each secretogogue stimulates histamine release by a different mechanism. The effect of flavonoids on human neutrophil beta-glucuronidase release stimulated by the chemoattractant peptide, f-methionyl-leucyl-phenylalanine (f-Met-LeuPhe) was also examined. Several citrus flavonoids were very active inhibitors of basophil histamine release and neutrophil beta-glucuronidase release. Compounds active against all three basophil secretogogues tended to have activity against f-MetLeuPhe-induced beta-glucuronidase release from neutrophils. A structure-activity relationship analysis revealed that certain specific chemical structures appeared to be associated with the capacity to inhibit basophil histamine release and neutrophil beta-glucuronidase release. The data suggest indirectly that certain citrus flavonoids might possess in vivo antiallergic and antiinflammatory activity.

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