目的 以革皮氏海参中分离得到的三萜皂苷holothurin 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、3.82 μmol·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.%Aim To determine the effects of holothurin Al( HA ) and 24-dehvdroechinoside A( DA ) extracted from Pearsonothria graeffe on anti-angiogenesis. Methods Inhibition of angiogenesis was assessed in vitro using proliferation, AO/EB and tubeformation assaysin HA and DA treated HUVEC cells. In vivo, CAM as-says were used to assess inhibitory effect of HA and DAon physiological angiogenesis. Results HA and DAcould inhibit the proliferation of endothelial cells andinduce the apoptosis of HUVEC cells. The ICso were4. 80 μmol·L-1 and 3. 82 μmol · L-1 in HA and DAtreated HUVEC cells for 48 h respectively. HA andDA could inhibit the tube formation in vitro and de-crease the blood vessel growth on the chicken chorioal-lantoic membrane in vivo. The effect of DA was betterthan HA,indicating that the hydroxy substituted on C-22 would decrease the anti-tumor and anti-metastasisactivity of triterpene glycosides and the carbon bondson 24( 25 ) would increase the anti- angiogenesis activ-ity of triterpene glycosides. Conclusion Both HA andDA exert significant anti-angiogenic activities relatingto their chemical structures.
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