High-content screening of active components of Traditional Chinese Medicine inhibiting TGF-β-induced cell EMT.
High-content screening of active components of Traditional Chinese Medicine inhibiting TGF-β-induced cell EMT.
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抑制TGF-β诱导的细胞EMT的中药活性成分的高含量筛选
DOI：
10.1016/j.heliyon.2022.e10238
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发表时间：
2022-08
期刊：
影响因子：
4
通讯作者：
Zhu, Qingjun
中科院分区：
文献类型：
--
作者：
Xu, Mengzhen;Cui, Qinghua;Su, Wen;Zhang, Dan;Pan, Jiaxu;Liu, Xiangqi;Pang, Zheng;Zhu, Qingjun
上皮间质转化（EMT）在纤维化疾病和癌症进展中的转移和侵袭中起作用。一些传统中药（TCM）已显示出对EMT的抑制作用。本研究试图建立一种多参数高内涵的方法，通过评估表型变化来筛选具有靶向细胞EMT能力的中药活性单体化合物。采用高容量筛选（HCS）系统从MedChemExpress（MCE）化合物库中筛选出306个单体化合物，鉴定出5个具有抗EMT活性的化合物，包括喜树碱（CPT）、二甲基姜黄素（DMC）、青蒿琥酯（ART）、sinopropyl（SNP）和小檗碱（BER）。为了确认抗EMT活性，通过qRT-PCR和蛋白质印迹法评估EMT标志物的表达，并通过细胞功能测定法测量细胞粘附和迁移。结果显示，CPT、DMC、ART、SNP和BER均能抑制转化生长因子β1（TGF-β1）诱导的波形蛋白和α-SMA表达，上调E-cadherin表达，增强细胞粘附能力，降低细胞迁移能力。综上所述，通过多参数分析量化TGF-β1诱导EMT过程中细胞形态学变化，HCS系统成功筛选出具有抗EMT活性的中药化合物，比传统方法更快速、更经济。高内涵筛选;上皮-间质转化;中药; TGF-β1。
The epithelial mesenchymal transition (EMT) has roles in metastasis and invasion during fibrotic diseases and cancer progression. Some Traditional Chinese Medicines (TCMs) have shown inhibitory effects with respect to the EMT. The current study attempted to establish a multiparametric high-content method to screen for active monomeric compounds in TCM with the ability to target cellular EMT by assessing phenotypic changes. A total of 306 monomeric compounds from the MedChemExpress (MCE) compound library were screened by the high-content screening (HCS) system and 5 compounds with anti-EMT activity, including camptothecin (CPT), dimethyl curcumin (DMC), artesunate (ART), sinapine (SNP) and berberine (BER) were identified. To confirm anti-EMT activity, expression of EMT markers was assessed by qRT-PCR and Western blotting, and cell adhesion and migration measured by cell function assays. The results revealed that CPT, DMC, ART, SNP and BER inhibited transforming growth factor-β1 (TGF-β1)-induced expression of vimentin and α-SMA, upregulated expression of E-cadherin, increased cell adhesion and reduced cell migration. In summary, by quantifying the cell morphological changes during TGF-β1-induced EMT through multi-parametric analysis, TCM compounds with anti-EMT activity were successfully screened using the HCS system, a faster and more economical approach than conventional methods. High-content screening; Epithelial-mesenchymal transition; Traditional Chinese Medicine; TGF-β1.
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影响因子：
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作者：
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5.3
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影响因子：
2.7
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影响因子：
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