Effect of marchantins and related compounds on 5-lipoxygenase and cyclooxygenase and their antioxidant properties: a structure activity relationship study

摘要: Summary Marchantins and related compounds, isolated from different species of liverworts, were investigated for their inhibitory potential on cyclooxygenase (COX) 5-lipoxygenase 5-(LOX), the key enzymes arachidonic acid cascade, additionally in a cell-free lipid-peroxidation system. The results compared with rate constants obtained pulse-radiolytic studies. All substances tested showed significant COX 5-LOX-activity. Marchantin B two catechol moieties, as NDGA, exerted an enhanced effect all test systems. most active compound 5-LOX-test was Perrottetin D (IC 50 = 0.66 μM), which also effective assay. While constant determined by pulse radiolysis rather low, EPR studies at elevated temperatures demonstrated perrottetin presence pyrogallol-type radical, generated furan-ring opening reaction. In conclusion, compounds liverworts possess antiinflammatory activities. let us suggest that these phenolic can be considered promising leads due to strong radical scavenger potential.