Novel indolyl-chalcone derivatives inhibit A549 lung cancer cell growth through activating Nrf-2/HO-1 and inducing apoptosis in vitro and in vivo

Abstract Increasing evidence indicates that Nrf-2, named the nuclear factor-erythroid 2-related factor, may perform anticancer function. In this study, a series of novel substituted phenyl- (3-methyl-1H-indol-2-yl)-prop-2-en-1-one (indolyl-chalcone) derivatives were synthesized and their effects on...

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Autores principales:	Xuan Zhao, WenLiang Dong, YuanDi Gao, Dong-Shoo Shin, Qing Ye, Le Su, Fan Jiang, BaoXiang Zhao, JunYing Miao
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2017
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/096f1f9f54a845be8fc892dc518dcd89
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spelling	oai:doaj.org-article:096f1f9f54a845be8fc892dc518dcd892021-12-02T12:32:29ZNovel indolyl-chalcone derivatives inhibit A549 lung cancer cell growth through activating Nrf-2/HO-1 and inducing apoptosis in vitro and in vivo10.1038/s41598-017-04411-32045-2322https://doaj.org/article/096f1f9f54a845be8fc892dc518dcd892017-06-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-04411-3https://doaj.org/toc/2045-2322Abstract Increasing evidence indicates that Nrf-2, named the nuclear factor-erythroid 2-related factor, may perform anticancer function. In this study, a series of novel substituted phenyl- (3-methyl-1H-indol-2-yl)-prop-2-en-1-one (indolyl-chalcone) derivatives were synthesized and their effects on Nrf-2 activity were observed. We found that compounds 3a-3d and 6c elevated Nrf-2 activity. Then we evaluated their anticancer activities in vitro and in vivo by utilizing human lung cancer cell line A549. The in vitro results showed that among the compounds, 3d performed effectively anti-growth activity by inducing A549 lung cancer cell apoptosis and activating Nrf-2/HO-1 (heme oxygenase-1) pathway. In vivo, we proved that compound 3d inhibited the tumor growth effectively through inducing cell apoptosis without affecting CAM normal angiogenesis. These data suggest that our discovery of a novel Nrf-2 activator compound 3d would provide a new point of human lung cancer treatment.Xuan ZhaoWenLiang DongYuanDi GaoDong-Shoo ShinQing YeLe SuFan JiangBaoXiang ZhaoJunYing MiaoNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-11 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Xuan Zhao WenLiang Dong YuanDi Gao Dong-Shoo Shin Qing Ye Le Su Fan Jiang BaoXiang Zhao JunYing Miao Novel indolyl-chalcone derivatives inhibit A549 lung cancer cell growth through activating Nrf-2/HO-1 and inducing apoptosis in vitro and in vivo
description	Abstract Increasing evidence indicates that Nrf-2, named the nuclear factor-erythroid 2-related factor, may perform anticancer function. In this study, a series of novel substituted phenyl- (3-methyl-1H-indol-2-yl)-prop-2-en-1-one (indolyl-chalcone) derivatives were synthesized and their effects on Nrf-2 activity were observed. We found that compounds 3a-3d and 6c elevated Nrf-2 activity. Then we evaluated their anticancer activities in vitro and in vivo by utilizing human lung cancer cell line A549. The in vitro results showed that among the compounds, 3d performed effectively anti-growth activity by inducing A549 lung cancer cell apoptosis and activating Nrf-2/HO-1 (heme oxygenase-1) pathway. In vivo, we proved that compound 3d inhibited the tumor growth effectively through inducing cell apoptosis without affecting CAM normal angiogenesis. These data suggest that our discovery of a novel Nrf-2 activator compound 3d would provide a new point of human lung cancer treatment.
format	article
author	Xuan Zhao WenLiang Dong YuanDi Gao Dong-Shoo Shin Qing Ye Le Su Fan Jiang BaoXiang Zhao JunYing Miao
author_facet	Xuan Zhao WenLiang Dong YuanDi Gao Dong-Shoo Shin Qing Ye Le Su Fan Jiang BaoXiang Zhao JunYing Miao
author_sort	Xuan Zhao
title	Novel indolyl-chalcone derivatives inhibit A549 lung cancer cell growth through activating Nrf-2/HO-1 and inducing apoptosis in vitro and in vivo
title_short	Novel indolyl-chalcone derivatives inhibit A549 lung cancer cell growth through activating Nrf-2/HO-1 and inducing apoptosis in vitro and in vivo
title_full	Novel indolyl-chalcone derivatives inhibit A549 lung cancer cell growth through activating Nrf-2/HO-1 and inducing apoptosis in vitro and in vivo
title_fullStr	Novel indolyl-chalcone derivatives inhibit A549 lung cancer cell growth through activating Nrf-2/HO-1 and inducing apoptosis in vitro and in vivo
title_full_unstemmed	Novel indolyl-chalcone derivatives inhibit A549 lung cancer cell growth through activating Nrf-2/HO-1 and inducing apoptosis in vitro and in vivo
title_sort	novel indolyl-chalcone derivatives inhibit a549 lung cancer cell growth through activating nrf-2/ho-1 and inducing apoptosis in vitro and in vivo
publisher	Nature Portfolio
publishDate	2017
url	https://doaj.org/article/096f1f9f54a845be8fc892dc518dcd89
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Novel indolyl-chalcone derivatives inhibit A549 lung cancer cell growth through activating Nrf-2/HO-1 and inducing apoptosis in vitro and in vivo

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