Due to the structural characteristics of isoflavones determines its poor solubility (fat soluble and water soluble), drug oral bioavailability is low, so by structure modification to improve its solubility property and pharmacological activities have become research hotspots. At present, by using the prodrug principle and combination principles, putting the active group in isoflavones sites in order to improve the efficacy has made certain achievements, not only to improve the solubility, but also the partial derivatives of isoflavones pharmacological activity is better than that of matrix. In this paper, the current domestic and international acetoxylation, etherification, esterification and halogenated of isoflavones structure modification research status are reviewed, so as to provide reference for further research and development of this compound.%由于异黄酮本身结构特性决定了其溶解性(脂溶性和水溶性)差,药物口服生物利用度低,故通过结构修饰来改善其溶解性能和药理活性已成为研究的热点.目前利用前药原理及拼合原理在异黄酮的位点上引入活性基团以提高药效已取得了一定的成果,不仅改善了其溶解性,而且部分衍生物的药理活性优于母体.本文对当今国内外异黄酮的酰基化、醚化、酯化、卤化等结构修饰的研究现状进行了综述,以期为该类化合物的进一步研究和开发提供参考.
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