School of Medicine, Xi'an Jiaotong University, Xi'an, Shaanxi Province, PR China.
Biomed Pharmacother. 2012 Oct;66(7):499-505. doi: 10.1016/j.biopha.2012.05.002. Epub 2012 Jun 19.
In order to investigate the anti-angiogenesis potential and related mechanisms of Ta1722 (a novel taspine derivative compound), a series of experiments in vivo and in vitro were carried out. The proliferation on human cell lines of SMMC-7721, A549, MCF-7, Lovo, and ECV304 was examined by MTT. Angiogenesis inhibition was examined by chick embryo chorioallantoic membrane (CAM) angiogenesis and tube formation assays. Related angiogenesis proteins and their mRNA expression were determined by western blotting and RT-PCR. In addition, the SMMC-7721 nude mouse xenotransplant model was used to evaluate the inhibition of tumor growth. The results showed that Ta1722 inhibited cell proliferation, angiogenesis of CAM and tube formation, and downregulated related positive angiogenesis proteins. The above indicated Ta1722 could serve as a promising candidate of angiogenesis inhibitors by interrupting the VEGF/VEGFR-2 pathway.
为了研究 Ta1722（一种新型紫杉烷衍生物化合物）的抗血管生成潜力及其相关机制，我们进行了一系列体内和体外实验。通过 MTT 法检测 Ta1722 对人肝癌细胞株 SMMC-7721、人肺腺癌细胞株 A549、人乳腺癌细胞株 MCF-7、人结肠癌细胞株 Lovo、人脐静脉内皮细胞株 ECV304 的增殖抑制作用；通过鸡胚尿囊膜血管生成实验和管腔形成实验检测 Ta1722 的抗血管生成作用；通过 Western blot 和 RT-PCR 检测相关血管生成蛋白及其 mRNA 的表达情况。此外，我们还构建了人肝癌 SMMC-7721 裸鼠移植瘤模型，评估 Ta1722 对肿瘤生长的抑制作用。结果表明，Ta1722 能够抑制细胞增殖、CAM 血管生成和管腔形成，并下调相关阳性血管生成蛋白。以上结果表明，Ta1722 可能通过阻断 VEGF/VEGFR-2 通路成为一种有前途的血管生成抑制剂候选药物。
