Ephrin type-B receptor 4 affinity chromatography: An effective and rapid method studying the active compounds targeting Ephrin type-B receptor 4.

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.