关键词: 柚皮素, 区域选择性酰化, 水溶性, 抗血小板聚集

Abstract: To improve the water solubility without affecting the anti-platelet aggregation activity of naringenin,two acylated derivatives of naringenin,namely naringenin-7-O-acylate,naringenin-7-O-propionate were synthesized by a four step synthesis route,benzylation-hydrolysis-acylation-hydrogenation,with naringin as raw material.The water solubility of naringenin-7-O-acylate and naringenin-7-O-propionate were 637.34 ± 53.23 μg/mL and 59.74 ± 4.81 μg/mL,respectively,both of which were higher than that of naringenin.These two derivatives inhibited platelet aggregation induced by adenosine diphosphate both in vitro and in vivo, and both showed higher anti-platelet aggregation activity than naringenin.The results suggested that the acylation of hydroxyl group at C7 of naringrnin with aliphatic acyl donors containing two or three carbons not only provided the suitable water solubility but also improved the anti-platelet aggregation activity of naringrnin.

Key words: naringenin, regioselective acylation, water solubility, anti-platelet aggregation