三种冬凌草素和毛萼乙素体外对人血管生成的影响

目的：研究4种二萜化合物（冬凌草甲素、信阳冬凌草甲素、冬凌草乙素、毛萼乙素,分别简称为SH-A、SX-A、SH-B、ER-B）在体外对血管生成的影响，为发现新的抗肿瘤药物提供线索。方法：采用人脐静脉内皮细胞ECV304增殖、迁移试验及小管形成试验研究了4种化合物对血管生成的影响。结果：4种二萜化合物对ECV304（人脐静脉内皮细胞系）的增殖、迁移、小管形成具有不同程度的抑制作用，IC50值分别在1.47×10-5~3.76×10-5mol·L-1（抑制作用SX-A＞SH-A＞SH-B＞ER-B）、8.01×10-7~5.41×10-6mol·L-1（抑制作用SH-B最强,而SH-A、SX-A和ER-B相仿）和4.25×10-7~2.80×10-6mol·L-1内（抑制作用SH-B＞SH-A＞SX-A＞ER-B），抑制血管迁移、小管形成的IC50值均低于抑制增殖的IC50。结论：4种二萜化合物在体外对人脐静脉内皮细胞系血管形成均有不同程度的抑制作用，值得作为抗肿瘤药物的候选物进一步深入研究。

OBJECTIVE: To investigate the effect of Oridonin (SH-A), Xindonqnin A (SX-A), Ponicidin (SH-B) and Eriocalyxin B (ER-B) on angiogenesis in vitro. METHODS: The effects of 4 compounds on angiogenesis in vitro were measured by the proliferation, migration and tube formation assay using ECV304 (human umbilical vein endothelial cell). RESULTS: SH-A, SH-B, SX-A and ER-B had inhibitory effects on the proliferation of ECV304. Their IC₅₀ to ECV304 were fell in the range of 1.47 × 10^-5 -3.76 × 10^-5 mol·L^-1, which showed similarity of inhibition. Four ent-Kaurenoids had different effects on the migration of ECV304 and their IC₅₀ were in the range of 8.01 × 10^-7 -5.41 × 10^-6 mol·L^-1. SH-B was much stronger than the other three. All the four ent-Kaurenoids inhibited the tube formation with IC₅₀ between 4.25 × 10^-7 -2.80 × 10 ^-6 mol·L^-1. SX-A was weaker than the other three. CONCLUSION: Four ent-Kaurenoids could inhibit the migration and tube formation of ECV304 at lower concentrations, and they have no effect on the proliferation of ECV304.