Nguyen M, Eilber F R, Defrees S
UCLA School of Medicine 90095, USA.
Biochem Biophys Res Commun. 1996 Nov 21;228(3):716-23. doi: 10.1006/bbrc.1996.1722.
Selectins have been shown to play an important role in angiogenesis. We have set out to synthesize multiple analogs of the selectin ligand sialyl Lewis X. We show here that analogs of sialyl Lewis X at concentrations of 50 micrograms/ml or greater significantly inhibited angiogenesis in in vitro assays of endothelial cell migration and proliferation (p < 0.05). These analogs also exerted significant inhibitory effects in in vivo angiogenesis assays using the chick chorioallantoic membrane at doses of 2 mg/chick or greater (p < 0.05). In contrast, the related carbohydrate Lewis X did not inhibit angiogenesis in both in vitro and in vivo assays. These data indicate that angiogenesis can be inhibited specifically by synthetic analogs of sialyl Lewis X. These analogs may potentially be useful in the treatment of angiogenesis-related diseases.
选择素已被证明在血管生成中起重要作用。我们已着手合成选择素配体唾液酸化路易斯X的多种类似物。我们在此表明，浓度为50微克/毫升或更高的唾液酸化路易斯X类似物在体外内皮细胞迁移和增殖测定中显著抑制血管生成（p < 0.05）。这些类似物在使用鸡胚绒毛尿囊膜的体内血管生成测定中，以2毫克/只或更高剂量时也发挥了显著的抑制作用（p < 0.05）。相比之下，相关碳水化合物路易斯X在体外和体内测定中均未抑制血管生成。这些数据表明，唾液酸化路易斯X的合成类似物可特异性抑制血管生成。这些类似物可能在治疗血管生成相关疾病中具有潜在用途。
