Apicularen A, a Macrolide from Chondromyces sp., Inhibits Growth Factor Induced In Vitro Angiogenesis
Apicularen A, a Macrolide from Chondromyces sp., Inhibits Growth Factor Induced In Vitro Angiogenesis
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Apularen A 是一种来自软骨菌属的大环内酯，可抑制生长因子诱导的体外血管生成
DOI：
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发表时间：
2002
期刊：
影响因子：
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通讯作者：
Jong
中科院分区：
文献类型：
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作者：
H. Kwon;Dong Hoon Kim;J. Shim;Jong
Apicularen A（API A）是近年来从软骨菌属中分离得到的一种具有抗肿瘤活性的化合物。由于其独特的化学结构，具有高度不饱和酰胺侧链的大环内酯，以及在各种癌细胞系中的强效生长抑制作用，API A目前正在进行癌症治疗的临床试验。本研究观察了API A对体外培养的牛主动脉内皮细胞（BAECs）血管生成的影响。API对BAECs增殖有明显的抑制作用，且呈剂量依赖性。用高达10 ng/ml的化合物处理内皮细胞未显示出任何细胞毒性。此外，它抑制碱性成纤维细胞生长因子（bFGF）诱导的BAECs的侵袭和毛细血管形成的浓度为2-5 ng/ml。因此，这些结果表明，API A是一种新的抗血管生成剂，并可能抑制肿瘤的生长，至少部分，通过抑制新血管形成。
Apicularen A (Api A) was recently isolated from Chondromyces sp. as a potent antitumor agent. Because of its unique chemical structure, a macrolide with a highly unsaturated amide side chain, and potent growth inhibitory effect in various cancer cell lines, Api A is currently in clinical trial for cancer therapy. In the present study, the effect of Api A on in vitro angiogenesis of bovine aortic endothelial cells (BAECs) was investigated. Api A potently inhibited the proliferation of BAECs in a dose-dependent manner. Treatment of the endothelial cells with up to 10 ng/ml of the compound did not show any cytotoxicity. In addition, it inhibited basic fibroblast growth factor (bFGF)-induced invasion and capillary tube formation of BAECs at concentrations of 2-5 ng/ml. These results, therefore, demonstrate that Api A is a novel antiangiogenic agent and may suppress the growth of tumors, at least in part, by the inhibition of neovascularization.