Dual-mixed/CMC model for screening target components from traditional Chinese medicines simultaneously acting on EGFR & FGFR4 receptors
Dual-mixed/CMC model for screening target components from traditional Chinese medicines simultaneously acting on EGFR & FGFR4 receptors
复制标题
双混合/CMC模型筛选同时作用于EGFR的中药靶成分
DOI：
10.1016/j.talanta.2018.09.053
复制
发表时间：
2019-01-15
期刊：
影响因子：
6.1
通讯作者：
Han, Shengli
中科院分区：
文献类型：
--
作者：
Fu, Jia;Lv, Yanni;Han, Shengli
丹参（也被称为丹参）是一种受欢迎的中药，具有活血化瘀的作用，据报道具有潜在的抗肿瘤作用。本研究旨在建立一种有效、实用的筛选和鉴定丹参中生物活性物质的方法。本文建立了表皮生长因子受体（EGFR）和成纤维细胞生长因子受体4 （FGFR4）双混合/细胞膜色谱（CMC）联用高效液相色谱-电喷雾电离-离子捕获-飞行时间-多级质谱（HPLC-ESI-IT-TOF-MSn）鉴别丹参有效成分的方法。丹酚酸C （SAC）、丹参酮I （Tan-I）、丹参酮IIA （Tan-IIA）和隐丹参酮（C- tan）被鉴定为具有EGFR和FGFR4活性的生物活性成分。MTT和激酶试验研究了这些化合物对体外EGFR和FGFR4细胞生长的抑制作用。细胞活力和激酶活性均表明隐丹参酮作用于EGFR受体，而丹参酮IIA作用于FGFR4受体。综上所述，EGFR & FGFR4双混合/CMC可以同时从同时作用于EGFR和FGFR4受体的中药中筛选出生物活性成分，从而显著提高了从复杂系统中鉴定特异性生物活性成分的效率。
Radix Salviae Miltiorrhiae (also known as DanShen (DS) in China), a popular herbal drug in traditional Chinese medicine (TCM) for promoting blood circulation and treating blood stasis, has been reported to possess potential anti-tumor effects. The aim of the study was to develop an effective and practical method for screening and identifying bioactive compounds from Radix Salviae Miltiorrhiae. In this work, the epidermal growth factor receptor (EGFR) and fibroblast growth factor receptors 4 (FGFR4) dual-mixed/cell membrane chromatography (CMC) coupled with high performance liquid chromatography-electrospray ionization-ion trap-time of flight-multistage mass spectrum (HPLC-ESI-IT-TOF-MSn) was established and successfully used to identify the active components from Radix Salviae Miltiorrhiae. Salvianolic acid C (SAC), tanshinone I (Tan-I), tanshinone IIA (Tan-IIA), and cryptotanshinone (C-Tan) were identified as bioactive components with EGFR and FGFR4 activities. MTT and kinase assay were performed to investigate inhibitory effects of these compounds against EGFR and FGFR4 cells growth in vitro. Both cell viability and kinase activity showed that cryptotanshinone acting on EGFR receptor and tanshinone IIA acting on FGFR4 receptor. In conclusion, the EGFR & FGFR4 dual-mixed/CMC can simultaneously screen the bioactive components from TCMs that act on both EGFR and FGFR4 receptors, which significantly improve the efficiency of specific bioactive components identification from a complex system.