Development of Approaches to the Study of the Interaction of Biologically Active Thioterpenoids with Model Membranes
BioNanoScience(2017)
摘要
It was shown that the synthesized camphene sulfone, in contrast to acetylsalicylic acid and clopidogrel, completely inhibits the activation of platelets induced by adrenaline and arachidonic acid, and reduces the influence of ADP, collagen, and ristocetin. Detailed NMR studies and molecular dynamics simulations using model SDS membranes indicated that the sulfone is embedded by its bicyclic part inside the SDS micelle, whereas -SO 2 (CH 2 ) 2 OH fragment of sulfone is located on the outer part of the micelle and accessible for solvent. It was ascertained that hemocoagulant activity of sulfone is caused by its capability of inhibition of platelet activation and suppression of catalytic activity of phospholipid surface participating in formation of coagulation complexes of clotting factors.
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关键词
Terpenes,Camphene sulfone,Platelet aggregation,Molecular mechanism of hemocoagulant activity
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