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Application of SNAP-tag-EGFR cell membrane chromatography model in screening antitumor active components of Silybum marianum (L.) Gaertn
Journal of Pharmaceutical and Biomedical Analysis ( IF 3.1 ) Pub Date : 2023-10-26 , DOI: 10.1016/j.jpba.2023.115816 Xin Zhang 1 , Yuhan Jiang 1 , Na Guo 1 , Yifan Ding 1 , Jingting Feng 1 , Chenyang Miao 1 , Yanni Lv 1
Journal of Pharmaceutical and Biomedical Analysis ( IF 3.1 ) Pub Date : 2023-10-26 , DOI: 10.1016/j.jpba.2023.115816 Xin Zhang 1 , Yuhan Jiang 1 , Na Guo 1 , Yifan Ding 1 , Jingting Feng 1 , Chenyang Miao 1 , Yanni Lv 1
Affiliation
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The SNAP-tag-epidermal growth factor receptor (SNAP-tag-EGFR) cell membrane chromatography (CMC) model is a powerful tool for investigating ligand-receptor interactions and screening active ingredients in traditional Chinese medicine. Most tyrosine kinase inhibitors (TKIs) target epidermal growth factor receptors. However, TKIs associated with significant side effects and drug resistance must be addressed immediately. Therefore, there is an urgent need to develop new TKIs with high efficiency and low toxicity. Because of its low toxicity and side effects, traditional Chinese medicine has been widely employed to treat various diseases, including cancer. Hence, this study aimed to use the SNAP-tag-EGFR/CMC-high-performance liquid chromatography-mass spectrometry (HPLC-MS) two-dimensional system model as the research tool to screen and identify potential EGFR antagonists from the Chinese medicine . The applicability of the system was verified using the positive control drug osimertinib. Four potential EGFR antagonists were screened from the Chinese medicine . They were identified as silydianin, silychristin, silybin, and isosilybin. Additionally, their pharmacological activity was preliminarily verified using a CCK-8 assay. The kinetic parameters of the four active ingredients interacting with EGFR and their binding modes with EGFR were analyzed using nonlinear chromatography (NLC) and molecular docking. This study identified silydianin, silychristin, silybin, and isosilybin from and verified their potential antitumor effects on EGFR.
中文翻译：
SNAP-tag-EGFR细胞膜层析模型在筛选水飞蓟抗肿瘤活性成分中的应用
SNAP-标签-表皮生长因子受体（SNAP-tag-EGFR）细胞膜色谱（CMC）模型是研究配体-受体相互作用和筛选中药活性成分的有力工具。大多数酪氨酸激酶抑制剂 (TKI) 以表皮生长因子受体为目标。然而，必须立即解决与显着副作用和耐药性相关的 TKI 问题。因此，迫切需要开发高效、低毒的新型TKI。中药因其毒副作用低，被广泛应用于治疗包括癌症在内的多种疾病。因此，本研究旨在以SNAP-tag-EGFR/CMC-高效液相色谱-质谱（HPLC-MS）二维系统模型为研究工具，筛选和鉴定中药中潜在的EGFR拮抗剂。使用阳性对照药奥希替尼验证了该系统的适用性。从中药中筛选出四种潜在的EGFR拮抗剂。它们被鉴定为水飞蓟宁、水飞蓟亭、水飞蓟宾和异水飞蓟宾。此外，它们的药理活性通过CCK-8测定进行了初步验证。采用非线性色谱（NLC）和分子对接分析了四种活性成分与EGFR相互作用的动力学参数及其与EGFR的结合模式。本研究从 EGFR 中鉴定出水飞蓟宁、水飞蓟亭、水飞蓟宾和异水飞蓟宾，并验证了它们对 EGFR 的潜在抗肿瘤作用。
更新日期：2023-10-26
中文翻译：
SNAP-tag-EGFR细胞膜层析模型在筛选水飞蓟抗肿瘤活性成分中的应用
SNAP-标签-表皮生长因子受体（SNAP-tag-EGFR）细胞膜色谱（CMC）模型是研究配体-受体相互作用和筛选中药活性成分的有力工具。大多数酪氨酸激酶抑制剂 (TKI) 以表皮生长因子受体为目标。然而，必须立即解决与显着副作用和耐药性相关的 TKI 问题。因此，迫切需要开发高效、低毒的新型TKI。中药因其毒副作用低，被广泛应用于治疗包括癌症在内的多种疾病。因此，本研究旨在以SNAP-tag-EGFR/CMC-高效液相色谱-质谱（HPLC-MS）二维系统模型为研究工具，筛选和鉴定中药中潜在的EGFR拮抗剂。使用阳性对照药奥希替尼验证了该系统的适用性。从中药中筛选出四种潜在的EGFR拮抗剂。它们被鉴定为水飞蓟宁、水飞蓟亭、水飞蓟宾和异水飞蓟宾。此外，它们的药理活性通过CCK-8测定进行了初步验证。采用非线性色谱（NLC）和分子对接分析了四种活性成分与EGFR相互作用的动力学参数及其与EGFR的结合模式。本研究从 EGFR 中鉴定出水飞蓟宁、水飞蓟亭、水飞蓟宾和异水飞蓟宾，并验证了它们对 EGFR 的潜在抗肿瘤作用。
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