甾体化合物是一类生物体中广泛存在并具重要功能的生物分子。其特殊结构使这类化合物具有亲脂性,膜亲合性以及与低密度脂蛋白的特异性结合等性能。利用这些特性设计合成各种药物分子的甾体缀合物,可增加药物分子的脂溶性,提高跨膜渗透能力。在特定组织中的分布以及甾体缀合物自身具有独特的生物活性,对探索新型生物活性分子具有重要意义。本文介绍了近年来在设计合成新型甾体缀合物领域的研究进展,包括甾体药物缀合物、含磷甾体缀合物、作为离子通道和分子载体的缀合物及甾体二聚缀合物等。
Steroids play very important role in the life of animals molecules. Due to their lipophilic character, membrane affinity, and the and plants and are also important biological ability of binding to low density lipoproteins, design and synthesis of steroidal bioconjugates become more important. It should increase lipophilicity and enhance permeability through cell membranes and favorable specific organ distribution. The steroidal bioconjugates have shown many pharmacological activities, such as potent antimicrobial. analgesic, anti-inflammatory, and anti-tumor activities etc. In this review, the recent development of biologically important steroidal bioconjugates is briefly summarized, including steroid-drug conjugates, steroidal derivatives containing phosphorus, ionophores and molecular carriers, and the dimmers of steroids.