Psammaplin A, a marine natural product, inhibits aminopeptidase N and suppresses angiogenesis in vitro
Psammaplin A, a marine natural product, inhibits aminopeptidase N and suppresses angiogenesis in vitro
复制标题
DOI：
10.1016/j.canlet.2003.08.036
复制
发表时间：
2004-01-20
期刊：
影响因子：
9.7
通讯作者：
Kwon, HJ
中科院分区：
文献类型：
--
作者：
Shim, JS;Lee, HS;Kwon, HJ
Psammaplin A（PsA）是从海绵中分离得到的一种酚类天然产物，对多种肿瘤细胞具有较强的细胞毒活性。本研究发现，PsA可抑制哺乳动物氨肽酶N（APN），而APN在肿瘤细胞侵袭和血管生成中起关键作用。PsA以非竞争性方式抑制APN活性，IC 50为18 μ M。此外，PsA有效地抑制了几种癌细胞和内皮细胞的增殖。有趣的是，PsA的抗增殖作用依赖于APN表达的细胞量。最后，PsA抑制由碱性成纤维细胞生长因子刺激的内皮细胞的侵袭和管形成。这些数据表明，PsA是一种新的APN抑制剂，可以开发为一种新的抗血管生成剂。(C)2003爱思唯尔爱尔兰有限公司保留所有权利。
Psammaplin A (PsA) is a phenolic natural product isolated from a marine sponge, which showed a potent cytotoxicity against several cancer cell lines. In present study, PsA was found to inhibit mammalian aminopeptidase N (APN) that plays a key role in tumor cell invasion and angiogenesis. PsA inhibited the APN activity with an IC50 of 18 muM in a non-competitive manner. Moreover, PsA potently inhibited the proliferation of several cancer and endothelial cells. Interestingly, the anti-proliferative effect of PsA was dependent on the cellular amount of APN expression. Finally, PsA suppressed the invasion and tube formation of endothelial cells stimulated by basic fibroblast growth factor. These data demonstrate that PsA is a new inhibitor of APN and can be developed as a novel anti-angiogenic agent. (C) 2003 Elsevier Ireland Ltd. All rights reserved.