RGD-Tachyplesin inhibits tumor growth.
RGD-Tachyplesin inhibits tumor growth.
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DOI：
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发表时间：
2001-03
期刊：
影响因子：
11.2
通讯作者：
Yixin Chen;Xue-Ming Xu;Shuigen Hong;Jinguo Chen;Ningfei Liu;Charles B. Underhill;Karen Creswell;Lurong Zhang
中科院分区：
文献类型：
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作者：
Yixin Chen;Xue-Ming Xu;Shuigen Hong;Jinguo Chen;Ningfei Liu;Charles B. Underhill;Karen Creswell;Lurong Zhang
河蟹素是一种存在于中华绒螯蟹白细胞中的抗菌肽。在这项研究中，合成了一种与整合素归巢结构域RGD偶联的血栓素，并对其抗肿瘤活性进行了测试。体外实验结果表明，RGD-Tachyplesin对培养的肿瘤细胞和血管内皮细胞的增殖均有抑制作用，并能减少TSU前列腺癌细胞的集落形成。FITC-Annexin V、JC-1、Yo-PRO-1和FITC-葡聚糖荧光探针染色表明，RGD-tachyplesin可诱导肿瘤细胞和血管内皮细胞的凋亡。Western blotting结果显示，RGD-tachyplesin可激活caspase9、caspase8和caspase3，并增加Fas配体、Fas相关死亡结构域、caspase7和caspase6的表达，提示线粒体和Fas依赖途径共同参与了细胞凋亡的诱导。体内实验表明，RGD-Tachyplesin对鸡胚绒毛尿囊膜和同系小鼠的肿瘤生长均有抑制作用。
Tachyplesin is an antimicrobial peptide present in leukocytes of the horseshoe crab (Tachypleus tridentatus). In this study, a synthetic tachyplesin conjugated to the integrin homing domain RGD was tested for antitumor activity. The in vitro results showed that RGD-tachyplesin inhibited the proliferation of both cultured tumor and endothelial cells and reduced the colony formation of TSU prostate cancer cells. Staining with fluorescent probes of FITC-annexin V, JC-1, YO-PRO-1, and FITC-dextran indicated that RGD-tachyplesin could induce apoptosis in both tumor and endothelial cells. Western blotting showed that treatment of cells with RGD-tachyplesin could activate caspase 9, caspase 8, and caspase 3 and increase the expression of the Fas ligand, Fas-associated death domain, caspase 7, and caspase 6, suggesting that apoptotic molecules related to both mitochondrial and Fas-dependent pathways are involved in the induction of apoptosis. The in vivo studies indicated that the RGD-tachyplesin could inhibit the growth of tumors on the chorioallantoic membranes of chicken embryos and in syngenic mice.