Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.11861/7442
Title: Econazole nitrate inhibits PI3K activity and promotes apoptosis in lung cancer cells
Authors: Dong, Chao 
Yang, Runxiang 
Li, Hongjian 
Ke, Kunbin 
Luo, Chunxiang 
Yang, Fang 
Shi, Xi-Nan 
Zhu, Ying 
Liu, Xu 
Wong, Man-Hon 
Lin, Guimiao 
Wang, Xiaomei 
Prof. LEUNG Kwong Sak 
Kung, Hsiang-Fu 
Chen, Ceshi 
Lin, Marie Chia-mi 
Issue Date: 2017
Source: Scientific Reports, 2017, vol. 7, Article number: 17987
Journal: Scientific Reports 
Abstract: The phosphatidylinositol-3-kinase (PI3K)/AKT signaling pathway plays a pivotal role in many cellular processes, including the proliferation, survival and differentiation of lung cancer cells. Thus, PI3K is a promising therapeutic target for lung cancer treatment. In this study, we applied free and open-source protein-ligand docking software, screened 3167 FDA-approved small molecules, and identified putative PI3Kα inhibitors. Among them, econazole nitrate, an antifungal agent, exhibited the highest activity in decreasing cell viability in pathological types of NSCLC cell lines, including H661 (large cell lung cancer) and A549 (adenocarcinoma). Econazole decreased the protein levels of p-AKT and Bcl-2, but had no effect on the phosphorylation level of ERK. It inhibited cell growth and promote apoptosis in a dose-dependent manner. Furthermore, the combination of econazole and cisplatin exhibited additive and synergistic effects in the H661 and A549 lung cancer cell lines, respectively. Finally, we demonstrated that econazole significantly suppressed A549 tumor growth in nude mice. Our findings suggest that econazole is a new PI3K inhibitor and a potential drug that can be used in lung cancer treatment alone or in combination with cisplatin.
Type: Peer Reviewed Journal Article
URI: http://hdl.handle.net/20.500.11861/7442
DOI: 10.1038/s41598-017-18178-0
Appears in Collections:Applied Data Science - Publication

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