Cha B C, Lee S B
Department of Applied Animal Sciences, College of Life Sciences and Natural Resources, Sangji University, Wonju, Korea.
Arch Pharm Res. 2000 Apr;23(2):116-20. doi: 10.1007/BF02975499.
Aspirin has been widely used as analgesic and anti-inflammatory drug. Recently, it was elucidated that aspirin have anti-coaggregatory effect in low dose. This study was carried out to investigate the synthesis of aspirin derivatives from aspirin and aromatic compound of antioxidant and its biological activities. Synthesis of aspirin derivatives was prepared by esterification in the presence of 1,1-carbonyldiimidazole. Biological activities was examined using effect of anti-coagulant on bleeding time, effect of antioxidant and effect of anti-platelet aggregation. As a result, SJ-101 showed strong antioxidative activity and anti-coagulant activity among four compounds. Anti-platelet aggregation of SJ-101 was examined by collagen, ADP, PAF method. SJ-101 exhibited more stronger activity to aspirin at collagen aggregation reaction. These finding demonstrates that SJ-101 is useful as care drug of aging and old-disease because of its has antioxidant activity, anti-coagulant activity and anti-platelet activity.
阿司匹林一直被广泛用作镇痛和抗炎药物。最近，有研究表明阿司匹林在低剂量时具有抗凝血聚集作用。本研究旨在探讨由阿司匹林与抗氧化剂芳香族化合物合成阿司匹林衍生物及其生物活性。阿司匹林衍生物的合成是在1,1-羰基二咪唑存在下通过酯化反应制备的。使用抗凝血剂对出血时间的影响、抗氧化剂的作用和抗血小板聚集的作用来检测生物活性。结果，SJ-101在四种化合物中表现出较强的抗氧化活性和抗凝血活性。通过胶原蛋白、ADP、PAF方法检测了SJ-101的抗血小板聚集作用。在胶原蛋白聚集反应中，SJ-101对阿司匹林表现出更强的活性。这些发现表明，SJ-101因其具有抗氧化活性、抗凝血活性和抗血小板活性，可用作抗衰老和老年疾病的保健药物。
