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Caulerpenyne and related bis-enol esters are novel-type inhibitors of human 5-lipoxygenase

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Richter, P., Schubert, G., Schaible, A. M., Cavas, L., Werz, O., & Pohnert, G. (2014). Caulerpenyne and related bis-enol esters are novel-type inhibitors of human 5-lipoxygenase. ChemMedChem, 9(8), 1655-1659. doi:10.1002/cmdc.201402065.


Cite as: http://hdl.handle.net/21.11116/0000-0003-7D38-3
Abstract
Caulerpenyne (CYN) is a sesquiterpene from green algae with known inhibitory properties against soybean lipoxygenase. Here we introduce a detailed structure-activity study elucidating the inhibitory effects of CYN and a library of six synthetic CYN analogues on isolated human 5-lipoxygenase (5-LO) and cellular 5-LO in polymorphonuclear leukocytes. Essential structural elements are identified and a structurally simplified inhibitor is introduced. The modes of 5-LO inhibition by CYN and the synthetic inhibitors cannot be assigned to any of the known categories of lipoxygenase inhibitors. These compounds clearly interfere directly with 5-LO and represent rather small and flexible molecules, with unique structures among 5-LO inhibitors identified thus far.