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Abstract
Aseries of obtusatic acid analogues has been synthesized and evaluated as inhibitors
of leukotriene B(4) (LTB(4)) biosynthesis and as antiproliferative agents. The 4-O-benzylated
and the 4-O-demethylated congeners were the most potent inhibitors of LTB(4) production
of the depside class of compounds, with IC(50) values in the submicromolar range.
Furthermore, these compounds do not function as redox-based inhibitors because they
were not reactive against a stable free radical, 2,2-diphenyl-1-picrylhydrazyl, and
did not produce appreciable amounts of deoxyribose degradation as a measure of their
potency to generate hydroxyl radicals. Some obtusatic acid congeners were also potent
inhibitors of keratinocyte growth. Growth inhibition was not mediated by damage to
the cell membrane, as the activity of lactate dehydrogenase released from the cytoplasm
was in the control range.