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目的:研究确定磷酸二脂酶(phosphodiesterase,PDE)抑制剂对内皮细胞增殖、迁移以及在体内血管生成中的作用。方法:分别以人静脉内皮细胞(HUVEC)及C57BL/N6纯系小鼠为体外、体内研究对象,通过酶联免疫方法检测PDE2(ENHA)、PDE4(RP705)抑制剂对HUVEC中cAMP的含量的影响,及其与细胞增殖和迁移的关系。ENHA和RP705联合应用在C57BL/N6小鼠中的抑瘤作用。结果:PDE2选择性抑制剂EHNA(25μmol/L)和PDE4选择性抑制RP705(15μmol/L)均能够抑制由VEGF刺激的HUVEC增殖和迁移,并能增加HUVEC内cAMP含量,实验结果还显示PDE2和PDE4抑制剂的联合应用能够抑制体内血管生成,对C57BL/6N小鼠的抑瘤率达45.50%。结论:上述结果充分提示在病理性血管生成中PDE2和PDE4可能是新的潜在性的治疗靶点。
AIM: To determine the role of phosphodiesterase (PDE) inhibitors in endothelial cell proliferation, migration and in vivo angiogenesis. Methods: HUVECs and C57BL / N6 mice were used as in vitro and in vivo. Enzyme linked immunosorbent assay (ELISA) was used to examine the effect of PDE2 (ENHA) and PDE4 (RP705) Influence, and its relationship with cell proliferation and migration. Antitumor effect of ENHA combined with RP705 in C57BL / N6 mice. Results: PDE2 selective inhibitor EHNA (25μmol / L) and PDE4 selective RP705 (15μmol / L) inhibited the proliferation and migration of VEGF-stimulated HUVECs and increased the cAMP content in HUVECs. The results also showed that PDE2 and The combination of PDE4 inhibitors can inhibit angiogenesis in vivo, and the inhibition rate to C57BL / 6N mice was 45.50%. Conclusion: These results suggest that PDE2 and PDE4 may be potential new therapeutic targets in pathological angiogenesis.