磷酸二酯酶天然抑制剂的研究进展

Research progress on natural inhibitors towards phosphodiesterases

磷酸二酯酶(PDEs)是一类多基因大家族酶,包括11型,可以通过水解细胞内第二信使环磷酸腺苷和环磷酸鸟苷调节细胞内的多种信号传递和生理活动。研究表明,PDEs参与了炎症、抑郁、哮喘等多种病理过程的发生发展,是新药研究的热门靶点。近年来,从天然产物中发现了一些特异性强、活性高的PDEs抑制成分。对PDEs各家族的生物学特点、生理病理学意义及其天然抑制剂的研究进展进行综述,以期为PDEs抑制剂新药的研发提供参考。

Phosphodiesterases（PDEs） represent an important enzyme class constituted by 11 isozymes（PDE1 to PDE11）. They can regulate gene expression and nucleotide signaling pathway through the hydrolysis of c AMP and c GMP. Studies showed that PDEs have become one of the most popular research topics in the new drug development because they involved in the development of many pathological processes, such as inflammation, depression, asthma and so on. In recent years, many specific and efficient PDEs inhibitors derived from natural products have been reported. This paper reviews the biochemical properties, physiological functions, and their natural inhibitors of the PDEs families for providing a solid support for the further new drug development of selective PDEs inhibitors.