Xanthones as inhibitors of microsomal lipid peroxidation and TNF-α induced ICAM-1 expression on human umbilical vein endothelial cells (HUVECs)

Abstract

Xanthones bearing different functionalities, namely 1-hydroxyxanthone ( 1), 3-hydroxyxanthone ( 2), 1,4-dihydroxyxanthone ( 3), 2,6-dihydroxyxanthone ( 4), 1,2-diacetoxyxanthone ( 5), 2,6-diacetoxyxanthone ( 6), 3-methoxyxanthone ( 7), 1,3,7-trimethoxyxanthone ( 8) and 1,5-dihydroxy-6-methoxyxanthone ( 9) were synthesised and examined for their effect on nicotinamide adenine dinucleotide phosphate (NADPH)-catalysed liver microsomal lipid peroxidation and on tumour necrosis factor-α (TNF-α) induced expression of intercellular adhesion moledule-1 (ICAM-1) on endothelial cells, with a view to establish structure–activity relationship. Hydroxy- and acetoxyxanthones showed potent inhibitory effects on NADPH-catalysed lipid peroxidation and TNF-α induced expression of ICAM-1 on endothelial cells.