Abstract
The stereochemistry of new acetophenones, cynandione B–D ( 2– 4), isolated from Cynanchum taiwanianum, elucidated by computer modelling calculation and NOESY spectrum. It establishes the absolute configurations of cynandiones B–D ( 2– 4) as 7R; 7″S, 7S; 7″S and 7R; 7″R, respectively. Cynandione B ( 2) strongly inhibited the release of β-glucuronidase and lysozyme in formyl–methionyl–leucyl–phenylalanine (fMLP)-stimulated rat neutrophils in a concentration-dependent manner with IC 50 values of 1.5±0.2 and 1.6±0.2 μM, respectively. 2,5-Dihydroxyacetophenone ( 6) strongly inhibited the aggregation of washed rabbit platelets induced by arachidonic acid in a concentration-dependent manner with an IC 50 value of about 4.8 μM. In human citrated platelet-rich plasma, 2,5-dihydroxyacetophenone ( 6) inhibited the secondary phase, but not the primary phase, of aggregation induced by adrenaline and ADP. These results suggest that the antiplatelet effect of 2,5-dihydroxyacetophenone ( 6) is due to inhibition of the formation of thromboxane A 2.
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Schedule a callMore From: Biochimica et Biophysica Acta (BBA) - General Subjects
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