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Platelet Aggregation Inhibiting and Anticoagulant Effects of Oligoamines, XXIV: Interactions between Oligosydnone Imines and Albumine or Phospholipids
Author(s) -
Rehse Klaus,
Piechocki Daniela
Publication year - 1994
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19943271103
Subject(s) - chemistry , platelet aggregation , platelet , anticoagulant , pharmacology , biochemistry , stereochemistry , medicine
Oligosydnone imines are strongly bound to albumine (α < 1%) in pure water. In saline, however, this effect is abolished (α ˜ 80%). 4,4′‐Propylene‐bis‐3‐hexyl‐sydnone‐5‐imine hydrochloride ( 1 ) moderately binds to phosphatidylcholine liposomes (PC, α ˜ 34%). This is increased by phosphatidylethanolamine (PE). In PC/PE vesicles α is about 7%. The binding is further enhanced by the incorporation of negatively charged phospholipids (PL) like phosphatidylserine (PS). In PC/PE/PS liposomes complete binding of 1 can be achieved. This holds especially true if the composition of the liposomes is similar to the PL composition of platelet membranes. The results suggest that the antiplatelet activity of 1 is mediated by the bindings to negatively charged PL in the platelet membrane.