Ephrin type-B receptor 4 affinity chromatography: An effective and rapid method studying the active compounds targeting Ephrin type-B receptor 4
Ephrin type-B receptor 4 affinity chromatography: An effective and rapid method studying the active compounds targeting Ephrin type-B receptor 4
复制标题
Ephrin B 型受体 4 亲和色谱：研究靶向 Ephrin B 型受体 4 的活性化合物的有效且快速的方法
DOI：
10.1016/j.chroma.2018.12.005
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发表时间：
2019-02-08
影响因子：
4.1
通讯作者：
Zhang, Yanmin
中科院分区：
文献类型：
--
作者：
Zhu, Man;Cui, Yuxin;Zhang, Yanmin
促红细胞生成素肝细胞B4（EphB4）最近被报道是一种致癌因子在许多癌症和过度表达在几种类型的肿瘤。因此，EphB4有可能成为这些恶性肿瘤的治疗靶点。高效亲和色谱技术已成为研究药物与受体相互作用的有力工具。在这项研究中，我们构建了一种新的EphB4亲和色谱模型，以研究可以靶向EphB4的活性化合物。用该亲和层析模型对50多种中药粗提物进行了筛选。白屈菜和博落回中的有效成分血根碱以及黄连和黄柏中的小檗碱在EphB4亲和柱上选择性结合。接下来的生物学评价数据显示EphB4在血根碱和小檗碱对癌细胞生长的抑制作用中起关键作用。结果表明，本研究所建立的EphB4亲和层析模型可有效、快速地筛选EphB4靶向活性化合物，尤其是天然产物中的EphB4。(C)2018爱思唯尔B.V.保留所有权利。
Erythropoietin-producing hepatocyte B4 (EphB4) has recently been reported to be an oncogenic factor in many cancers and overexpressed in several types of tumors. Thus, EphB4 has the potential to be a therapeutic target in these malignancies. High-performance affinity chromatography has been a powerful tool to study the interaction between drugs and receptors. In this study, we constructed a novel EphB4 affinity chromatography model to investigate the active compounds which can target EphB4. More than 50 crude extracts of traditional Chinese medicine were screened by this affinity chromatography model. The active ingredients sanguinarine from celandine and macleaya cordata, and berberine from coptis chinensis and phellodendron amurense were found to selectively bind on the EphB4 affinity column. Next biological evaluatation data showed that EphB4 played a critical role in the inhibitory effect of sanguinarine and berberine on cancer cell growth. The results indicated that EphB4 affinity chromatography model constructed in this study can be used to screen the active compounds targeting EphB4 effectively and rapidly, especially in natural products. (C) 2018 Elsevier B.V. All rights reserved.