147249-33-0Relevant articles and documents
Synthesis and antiplatelet effects of the new antithrombotic agent aspalatone with low ulcerogenicity
Han,Suh,Yang,Park,Kang,Kim
, p. 1122 - 1126 (2007/10/02)
A new compound, aspalatone (acetylsalicylic acid maltol ester), was synthesized by esterification of acetylsalicylic acid (ASA) and maltol, an antioxidant, and studied for its bleeding time prolongation effect in rats for its antiplatelet aggregation activity in vitro and ex vitro in rats, and for its antithrombotic activity in vivo using the mouse thromboembolism test. Aspalatone treatment (15 mg/kg p.o.) for 10 days prolonged bleeding time by 57% (p 50 of 1.8 x 10-4 mol/l, but, similar to ASA, did not significantly inhibit ADP-induced aggregation. The ability of oral aspalatone to inhibit platelet aggregation in rats ex vivo was compared with other reference antiplatelet drugs. Relative potency was ASA > dipyridamole ? aspalatone > ticlopidine. A single dose of asplatone potently prevented death due to collagen-induced platelet aggregation in mice in vivo with ED50 value of 32 mg/kg p.o., but failed to prevent death due to ADP-induced platelet aggregation. When given for 10 days, aspalatone prevented collagen-induced death by 90% (p 50 values for malondialdehyde degeneration in vitro were 1.1 x 10-4 mol/l and 8.4 x 10-5 mol/l, respectively. These results suggest that aspalatone might be a potential antithrombotic agent with low ulcerogenicity.