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靛玉红衍生物 E804 抑制血管生成。

Indirubin derivative E804 inhibits angiogenesis.

机构信息

Center for Efficacy Assessment and Development of Functional Foods andDrugs, Hallym University, Chuncheon, Republic of Korea.

出版信息

BMC Cancer. 2012 May 3;12:164. doi: 10.1186/1471-2407-12-164.

DOI:10.1186/1471-2407-12-164
PMID:22554053
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3488320/
Abstract

BACKGROUND

It has previously been shown that indirubin derivative E804 (IDR-E804) blocks signal transducer and activator of transcription-3 signaling in human breast and prostate cancer cells and inhibits Src kinase activity. To further establish its role in angiogenesis, we tested its potential using human umbilical vein endothelial cells (HUVECs) and analyzed the effects of IDR-E804 on cellular and molecular events related to angiogenesis.

METHODS

The anti-angiogenic effects of IDR-E804 were examined by assessing the proliferation, migration and capillary tube formation of HUVECs were induced by vascular endothelial growth factor (VEGF) with or without various concentrations of IDR-E804. The inhibitory effect of IDR-E804 angiogenesis and tumor growth in vivo was also investigated in Balb/c mice subcutaneously transplanted with CT-26 colon cancer cells.

RESULTS

IDR-E804 significantly decreased proliferation, migration and tube formation of vascular endothelial growth factor VEGF-treated HUVECs. These effects were accompanied by decreased phosphorylation of VEGF receptor (VEGFR)-2, AKT and extracellular signal regulated kinase in VEGF-treated HUVECs. Intratumor injections of IDR-E804 inhibited the growth of subcutaneously inoculated CT-26 allografts in syngenic mice. Immunohistochemistry revealed a decreased CD31 microvessel density index and Ki-67 proliferative index, but an increased apoptosis index in IDR-E804-treated tumors.

CONCLUSIONS

These data revealed that IDR-E804 is an inhibitor of angiogenesis and also provide evidence for the efficacy of IDR-E804 for anti-tumor therapies.

摘要

背景

先前的研究表明，靛玉红衍生物 E804（IDR-E804）可阻断人乳腺癌和前列腺癌细胞中的信号转导子和转录激活子 3 信号通路，并抑制Src 激酶活性。为了进一步确定其在血管生成中的作用，我们使用人脐静脉内皮细胞（HUVEC）进行了测试，并分析了 IDR-E804 对与血管生成相关的细胞和分子事件的影响。

方法

通过评估血管内皮生长因子（VEGF）诱导的 HUVEC 的增殖、迁移和毛细血管管形成，来检测 IDR-E804 的抗血管生成作用，同时还检测了不同浓度的 IDR-E804 对其的影响。还在皮下接种 CT-26 结肠癌细胞的 Balb/c 小鼠中研究了 IDR-E804 对体内血管生成和肿瘤生长的抑制作用。

结果

IDR-E804 显著降低了 VEGF 处理的 HUVEC 的增殖、迁移和管形成。这些作用伴随着 VEGF 处理的 HUVEC 中 VEGF 受体（VEGFR）-2、AKT 和细胞外信号调节激酶的磷酸化减少。IDR-E804 瘤内注射抑制了同基因小鼠皮下接种 CT-26 同种移植物的生长。免疫组织化学显示 IDR-E804 治疗的肿瘤中 CD31 微血管密度指数降低和 Ki-67 增殖指数升高，但凋亡指数升高。

结论

这些数据表明，IDR-E804 是一种血管生成抑制剂，并为 IDR-E804 用于抗肿瘤治疗的疗效提供了证据。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/c01b60ba0f3a/1471-2407-12-164-5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/4430d2d2e974/1471-2407-12-164-1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/1d78c32908d0/1471-2407-12-164-2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/d336aff4934c/1471-2407-12-164-3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/80f4ccb31c67/1471-2407-12-164-4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/c01b60ba0f3a/1471-2407-12-164-5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/4430d2d2e974/1471-2407-12-164-1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/1d78c32908d0/1471-2407-12-164-2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/d336aff4934c/1471-2407-12-164-3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/80f4ccb31c67/1471-2407-12-164-4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cd0c/3488320/c01b60ba0f3a/1471-2407-12-164-5.jpg

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