Screening active components targeting membrane proteins is important for drug discovery from traditional Chinese medicine. Cell membrane chromatography (CMC) has achieved a wide application in screening active components on pathological cells due to its high sensitivity and effectiveness. However, it is hard to clarify the specific target protein through simply using pathological and normal cells. In this study, a novel comparative two-dimensional (2D) cell membrane chromatography system was established. Based on the construction of hepatocellular carcinoma cell line SK-Hep1-GPC3 with high expression of protein Glypican-3 (GPC3), SK-Hep1-GPC3/CMC column was loaded to screen selective antitumor components from Scutellariae Radix according to the retention behaviors on column. Viscidulin I was retained on SK-Hep1-GPC3/CMC column, and showed 4.33 μM affinity to GPC3 according to surface plasmon resonance (SPR). The IC₅₀ of viscidulin I on SK-Hep1-GPC3 cells was 18.01 μM in cell proliferation assay. Thus, this method can be applied to screen complex herbal medicines for ligands bound to specific target protein receptor related to hepatic carcinoma.

筛选靶向膜蛋白的活性成分对于从中药中发现药物很重要。细胞膜色谱法（CMC）具有很高的灵敏度和效率，因此在筛选病理细胞上的活性成分方面已获得了广泛的应用。但是，仅通过使用病理细胞和正常细胞很难明确特定的靶蛋白。在这项研究中，建立了一种新型的比较二维（2D）细胞膜色谱系统。基于高表达蛋白Glypican-3（GPC3）的肝癌细胞株SK-Hep1-GPC3的构建，根据其保留行为，加载SK-Hep1-GPC3 / CMC柱从黄cut中筛选选择性抗肿瘤成分。柱。Viscidulin I保留在SK-Hep1-GPC3 / CMC柱上，显示4。根据表面等离子体共振（SPR），与GPC3的亲和力为33μM。集成电路在细胞增殖测定中，SK-Hep1-GPC3细胞上的粘蛋白I的_50个为18.01μM。因此，该方法可用于筛选复杂的草药中与肝癌相关的特异性靶蛋白受体结合的配体。