Key result
Trans-2S,5S neolignan enantiomers exhibit ~10-200 times greater in vitro PAF receptor antagonism than corresponding isomers.
Why the study?
The biological justification for concomitant inhibition of both PAF receptor and 5-lipoxygenase in inflammation is well recognized, motivating development of novel PAF receptor antagonists.
Lignan analogs demonstrate potent, stereospecific antagonism of the PAF receptor, with potential for dual inhibition of PAF and 5-lipoxygenase in inflammation.
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Trans-2S,5S neolignan enantiomers may guide stereoselective PAF antagonist design; leaves open therapeutic potential pending in vivo studies.
T. Y. Shen (1991) studied this question. Lignan analogs (2,5-diaryl tetrahydrofuran type neolignans) was evaluated on In vitro potency as platelet-activating factor (PAF) antagonists. Trans-2S,5S enantiomers of 2,5-diaryl tetrahydrofuran neolignans were 10-200 times more potent in vitro as PAF receptor antagonists than their corresponding cis or trans-2R,5R isomers.
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