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Molecules 2016, 21(10), 1340;

A High Content Screening Assay to Identify Compounds with Anti-Epithelial-Mesenchymal Transition Effects from the Chinese Herbal Medicine Tong-Mai-Yang-Xin-Wan

TCM Research Center, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China
Zhejiang Cancer Research Institute, Zhejiang Cancer Hospital, Hangzhou 310022, China
Department of Nephrology, The Second Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou 310029, China
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
Authors to whom correspondence should be addressed.
Academic Editor: Christopher W.K. Lam
Received: 17 August 2016 / Revised: 29 September 2016 / Accepted: 6 October 2016 / Published: 10 October 2016
(This article belongs to the Collection Herbal Medicine Research)
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Chronic kidney disease (CKD) is a worldwide health problem with growing prevalence in developing countries. Renal tubular epithelial-mesenchymal transition (EMT) is a critical step and key factor in the development of this condition. Renal tubulointerstitial fibrosis is a basic pathological change at the later stages of the disease. Therefore, blocking the development of EMT could be a critical factor in curing CKD. We have established a cell-based high-content screening (HCS) method to identify inhibitors of EMT in human proximal tubular epithelial (HK-2) cells by automatic acquisition and processing of dual-fluorescent labeled images. With the aid of chromatographic separation and mass spectrometry, we achieved the rapid and reliable screening of active compounds from the Chinese herbal medicine Tong-Mai-Yang-Xin-Wan (TMYX) for treating EMT. Five fractions were found to exert anti-EMT activity and were further identified by liquid chromatography coupled with tandem mass spectrometry. Glycyrrhizic acid, glyasperin A, and licorisoflavan A were found to inhibit EMT. The proposed approach was successfully applied to screen active compounds from TMYX on TGF-β1-stimulated HK-2 cells and may offer a new means for identifying lead compounds for treating EMT from registered Chinese herbal medicines. View Full-Text
Keywords: high-content screening; epithelial mesenchymal transition; fluorescence imaging high-content screening; epithelial mesenchymal transition; fluorescence imaging

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Liu, N.; Li, L.; Zhu, X.; Ling, Z.; Feng, J.; Hu, Y.; Wang, Y.; Mou, L.; Wang, Y. A High Content Screening Assay to Identify Compounds with Anti-Epithelial-Mesenchymal Transition Effects from the Chinese Herbal Medicine Tong-Mai-Yang-Xin-Wan. Molecules 2016, 21, 1340.

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