PMEDAP的药理活性研究进展

9-(2-磷酸甲氧乙基)-2,6-二氨基嘌呤(PMEDAP)是无环核苷酸类化合物,结构上与9-(2-磷酸甲氧乙基)腺嘌呤(PMEA)相似,具有更广更强的抗病毒活性,尽管其有一定的细胞毒性,在抗病毒感染及抗肿瘤等领域仍具有开发前景。本文概括了近20年来PMEDAP及其部分取代的衍生物在抗逆转录病毒(如艾滋病毒等)、肝炎病毒(如人和鸭乙肝病毒等)、疱疹病毒(如简单疱疹病毒1型和2型、人类疱疹病毒6、7、8型等)和其他动植物病毒(如香蕉条纹病毒、腺病毒等)活性的研究进展。PMEDAP在具有广谱抗病毒作用的同时,具有一定的细胞毒性,在抗肿瘤方面有很高的研究意义。本文综述了PMEDAP在抗肿瘤方面的研究进展及其可能的作用机制,并根据现有的构效研究对PMEDAP在抗病毒和抗肿瘤两个方向的进一步研究提出了展望。

Pharmacological Activity Research Progress of Pmedap

9- 2- (phosphonomethoxy)ethyl]-2,6-diaminopurine (PMEDAP),chemically similar to 9- 2- (phosphonomethoxy) ethyl]adenine (PMEA),belongs to acyclic nucleoside phosphonate compound.PMEDAP was found to have broader and better antiviral activity profile than PMEA,and was reported that PMEDAP was tested as a promising antiviral and antitumour drug in spite of its serious toxicity.We summed up the antiviral activity profile research of PMEDAP and some derivates in the past twenty years,which encom- passes retroviridae e.g.human immunodeficiency virus (HIV)],hepadnaviridae e.g.human hepatitis B virus (HHBV) and duck hepatitis B virus (DHBV)],herpesviridae e.g.herpes simplex virus (HSV-1,HSV-2) and Human Herpes Virus (HHV-6,HHV-7,HHV-8)] and other viruse.g,banana streak virus (BSV) and adenovirus].Besides its broad-spectrum antiviral activities,the cytotoxicity of PMEDAP may make sense in the aspect ofantitumor activity.In this paper,we overviewed the research progress of PMEDAP so far and tried to ex- plain the mechanism of its antitumor action.And we made further prospect over their potential research of antiviral and antitumor activi- ties based on reported structure-function relationship studies.