磷酸二酯酶-4抑制剂的研究进展

Advances in research of phosphodiesterase-4 inhibitors

目的综述磷酸二酯酶-4(phosphodiesterase-4,PDE-4)的生理活性及其抑制剂的研究进展。方法查阅近年来国内外相关文献31篇,对其进行归纳、总结和分析。结果 PDE-4抑制剂通过对PDE-4的抑制作用,阻止环磷酸腺苷的水解,在哮喘和慢性阻塞性肺炎等炎症疾病方面作用显著。目前,罗氟司特已经通过美国FDA批准上市,许多活性较强、不良反应较少的PDE-4抑制剂相继进入了临床阶段。结论 PDE-4作为重要的炎症靶点之一得到了深入的研究,其抑制剂发展迅速,具有良好的开发前景。

Objective To review PDE-4′s physiological activity and its inhibitors′ research progress.Methods The relevant 31 papers on PDE-4 inhibitors were summarized and analyzed.Results PDE-4 were inhibited by PDE-4 inhibitors which can prevent the hydrolysis of cAMP and applied in the field of anti-asthma,anti-chronic obstructive pulmonary disease and other inflammatory diseases.Roflumilast had been approved by the FDA and many PDE-4 inhibitors which have strong activities and fewer adverse effects were under clinical tests.Conclusions As one of the important inflammatory targets,PDE-4 has been studied deeply and its inhibitors develop rapidly which have a brilliant prospect.