革皮氏海参皂苷抑制血管新生作用

目的以革皮氏海参中分离得到的三萜皂苷ho-lothurin A1(HA)和24-dehydroechinoside A(DA)为研究对象,比较研究其抗血管新生的作用。方法采用MTT法和AO/EB染色法检测不同剂量HA和DA对人脐静脉内皮细胞(HUVEC)增殖和凋亡的影响;采用小管形成实验观察HA和DA对HUVEC分化形成小管能力的影响;细胞黏附实验比较研究HA和DA对HUVEC与肝癌细胞HepG2的黏附能力的影响;鸡胚绒毛尿囊膜(CAM)血管新生模型,观察HA和DA抑制CAM血管新生的情况。结果 HA和DA均具有抑制HUVEC增殖的活性(48 h的IC50值分别为4.80、3.82μmol.L-1),并能促进内皮细胞的凋亡;在体外能抑制内皮细胞小管形成,可抑制HUVEC与HepG2细胞间(P<0.01)的黏附,能使CAM新生血管明显减少,其中DA抑制血管新生活性优于HA。结论海参皂苷HA和DA具有抑制血管新生的作用,其活性与其结构相关。

Antiangiogenesis effect of holothurin A1 and 24-dehydroechinoside A from Pearsonothria graeffei

Aim To determine the effects of holothurin A1(HA) and 24-dehydroechinoside A(DA) extracted from Pearsonothria graeffe on anti-angiogenesis.Meth-ods Inhibition of angiogenesis was assessed in vitro using proliferation,AO/EB and tubeformation assays in HA and DA treated HUVEC cells.In vivo,CAM assays were used to assess inhibitory effect of HA and DA on physiological angiogenesis.Results HA and DA could inhibit the proliferation of endothelial cells and induce the apoptosis of HUVEC cells.The IC50 were 4.80 μmol·L-1 and 3.82 μmol·L-1 in HA and DA treated HUVEC cells for 48 h respectively.HA and DA could inhibit the tube formation in vitro and decrease the blood vessel growth on the chicken chorioallantoic membrane in vivo.The effect of DA was better than HA,indicating that the hydroxy substituted on C-22 would decrease the anti-tumor and anti-metastasis activity of triterpene glycosides and the carbon bonds on 24(25) would increase the anti-angiogenesis activity of triterpene glycosides.Conclusion Both HA and DA exert significant anti-angiogenic activities relating to their chemical structures.