Anti-inflammatory activity of 2,4,6-trihydroxy-alpha-p-methoxyphenylacetophenone (compound D-58)

Background: Active oxygen radicals as well as a variety of cytosolic protei n tyrosine kinases play a role in the regulation of prostaglandin E-2 (PGE( 2)), a key inflammatory mediator, released by skin cells in response to irr adiation with ultraviolet B light (UVB), Identification of chemical compoun ds that can interrupt such events may provide a basis for the development o f potent anti-inflammatory agents. Objective: To investigate the effect of a novel genistein analog, 2,4,6-trihydroxy-alpha -p-methoxyphenylacetopheno ne, with antioxidant property (compound D-58), on UVB-induced inflammatory responses. Methods: Epidermal cell cultures were irradiated with UVB both i n the presence and absence of compound D-58 and the PGE(2) released in the medium was determined by ELISA. For in vivo studies, skin inflammation was induced in mice either by carrageenan challenge of the air pouch or by an a cute exposure of skin to UVB radiation, The resulting inflammatory mediator release, skin edema and the histological changes of the skin were determin ed both in the presence and absence of compound D-58, Results: Compound D-5 8 treatment effectively inhibited the development of edema and histological changes in the skin of UVB-irradiated mice as well as the release of PGE(2 ) in vitro as well as in vivo. Conclusion: Compound D-58 (2,4,6-trihydroxy- alpha -p-methoxyphenyl-acetophenone) has potent anti-inflammatory propertie s. Copyright (C) 2000 S. Karger AG, Basel.