亲和超滤-液质联用技术筛选补骨脂治疗子宫内膜癌的有效成分

Screening of effective components of Psoralea Fructus for endometrial cancer by affinity ultrafiltration chromatography-mass spectrometry

目的采用亲和超滤-液质联用技术筛选补骨脂Psoralea Fructus中治疗子宫内膜癌的潜在活性成分。方法以表皮生长因子受体(epidermal growth factor receptor erbB1,EGFR)为靶蛋白,将补骨脂水提液和EGFR蛋白液共同孵育,利用基于亲和超滤原理的超速离心法和解离剂对活性配体进行分离和筛选,借助超高效液相色谱-四级杆飞行质谱技术对与EGFR蛋白亲和的补骨脂化学成分进行鉴定,并通过计算结合变化率比较活性成分与蛋白之间的结合能力。结果共筛选得到4种与EGFR亲和的补骨脂活性成分,通过对结合变化率进行比较,发现psorachalcone A与EGFR蛋白结合变化率最大。结论该研究为补骨脂防治子宫内膜癌的药效物质基础和作用机制研究提供了理论依据。

Objective To screen the active components in the extract of Buguzhi(Psoraleae Fructus) for the treatment of endometrial cancer by ultra-filtration affinity-liquid chromatography-mass spectrometry.Methods With epidermal growth factor receptor erbB1(EGFR) as the target protein,the aqueous extract of Psoralea Fructus and EGFR protein were incubated together,and the active ligands were separated and screened by ultracentrifugation and dissociation agent based on affinity ultrafiltration principle.The chemical components of Psoralea Fructus which are compatible with EGFR protein were identified,and the binding ability between active components and protein was compared by calculating the binding change rate.Results The result showed that four active components with EGFR affinity were screened out.By comparing the binding change rate,psorachalcone A has the largest binding change rate with EGFR protein.Conclusion Our work provides a theoretical basis for the study of the material basis and mechanism of Psoralea Fructus in preventing and treating endometrial cancer.