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Platelet activating factor (PAF) is a potent phospholipid mediator produced by different cell types, showing a well-characterized role in allergy, inflammation and cardiovascular disorders. Using the PAF-induced platelet aggregation as a guide, the potent and specific PAF receptor antagonist, kadsurenone along with 40 compounds were isolated from Piper medicinal plant spp. as well as Kadsura heteroclita and Arctium lappa. By the spectroscopic analysis, the structures of all the isolates were identified as lignans and neolignans. These compounds were tested on the 3H PAF receptor binding assay. Bicyclo [3, 2, 1] octane neolignans demonstrated potent PAF antagonistic properties. The 8.3’ and 8.0.4’ neolignan analogic were also found to be active. The structure-activity relationships were discussed.
Platelet activating factor (PAF) is a potent phospholipid mediator produced by different cell types, showing a well-characterized role in allergy, inflammation and cardiovascular disorders. Using the PAF-induced platelet aggregation as a guide, the potent and specific PAF receptor antagonist, Kadsurenone along with 40 compounds were isolated from Piper medicinal plant spp. as well as Kadsura heteroclita and Arctium lappa. By the spectroscopic analysis, the structures of all the isolates were identified as lignans and neolignans. these compounds were tested on the 3H PAF receptor binding Assay. Bicyclo [3, 2, 1] octane neolignans demonstrated potent PAF antagonistic properties. The 8.3’ and 8.0.4’ neolignan analogic were also found to be active. The structure-activity classes were discussed.