Key result
Sulfated lactose-based glycopolymers prolonged activated partial thromboplastin time depending on polymer molecular weight and density, without primarily inhibiting thrombin directly.
Synthesized sulfated lactose-based glycopolymers demonstrate anticoagulant activity that is dependent on molecular weight and sulfation density, likely independent of direct thrombin inhibition.
Glycopolymers prolong aPTT; leaves open their potential as anticoagulants pending in vivo validation.
Cyanoxyl persistent radicals can be used as chain-growth moderators of the statistical copolymerization of a variety of monomers. We report herein the preparation of fully sulfated lactose-based glycopolymers by cyanoxyl (.OC[triple bond]N)-mediated free-radical polymerization of acrylamide derivatized glycomonomers in good yield (60-80%) and low polydispersity (1.1 < M(w)/M(n) < 1.6). Prolongation of the activated partial thromboplastin time (aPTT) was observed, and structure-activity relationships were defined. Specifically, the anticoagulant effect varied in response to both polymer molecular weight and the density of pendant sulfated lactose units. Nonetheless, measured thrombin times were only modestly prolonged suggesting that the observed anticoagulant effect is not primarily related to direct thrombin inhibition.
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Sun et al. (2002) studied this question. Sulfated lactose-based glycopolymers was evaluated on Anticoagulant activity (aPTT and thrombin times). Sulfated lactose-based glycopolymers prolonged activated partial thromboplastin time depending on polymer molecular weight and density, without primarily inhibiting thrombin directly.
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