Potent anti-cancer effects of less polar Curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells

Abstract Curcumin and its chalcone derivatives inhibit the growth of human cancer cells. It is reported that replacement of two OH groups in curcumin with less polar groups like methoxy increases its anti-proliferative activity. In this study, we explored benzylidine cyclohexanone derivatives with n...

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Autores principales:	Fatemeh Alibeiki, Naser Jafari, Maryam Karimi, Hadi Peeri Dogaheh
Formato:	article
Lenguaje:	EN
Publicado:	Nature Portfolio 2017
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/da91f7701132479294c8a4f369cd69ac
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spelling	oai:doaj.org-article:da91f7701132479294c8a4f369cd69ac2021-12-02T15:06:10ZPotent anti-cancer effects of less polar Curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells10.1038/s41598-017-02666-42045-2322https://doaj.org/article/da91f7701132479294c8a4f369cd69ac2017-05-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-02666-4https://doaj.org/toc/2045-2322Abstract Curcumin and its chalcone derivatives inhibit the growth of human cancer cells. It is reported that replacement of two OH groups in curcumin with less polar groups like methoxy increases its anti-proliferative activity. In this study, we explored benzylidine cyclohexanone derivatives with non-polar groups, to see if they possess increased anti-cancer activity. Novel 2,6-bis benzylidine cyclohexanone analogues of curcumin were synthesized, and their inhibitory effects on gastric adenocarcinoma (AGS) and esophageal squamous cell carcinoma (KYSE30) cancer cells were studied using an MTT assay. Cell apoptosis was detected by EB/AO staining, and cell cycle was analyzed by flow cytometry. Real-time PCR was performed for gene expression analysis. All synthesized analogues were cytotoxic toward gastric and esophageal cancer cells and showed lower IC50 values than curcumin. Treatment with 2,6-Bis-(3-methoxy-4-propoxy-benzylidene)-cyclohexanone (BM2) was 17 times more toxic than curcumin after 48 h incubation. All novel compounds were more effective than curcumin in apoptosis induction and cell cycle arrest at G1 phase. These results suggest that less polar analogues of curcumin have potent cytotoxicity in vitro. However, they need to be investigated further, especially with animal tumor models, to confirm their chemotherapeutic activity in vivo.Fatemeh AlibeikiNaser JafariMaryam KarimiHadi Peeri DogahehNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-9 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Fatemeh Alibeiki Naser Jafari Maryam Karimi Hadi Peeri Dogaheh Potent anti-cancer effects of less polar Curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells
description	Abstract Curcumin and its chalcone derivatives inhibit the growth of human cancer cells. It is reported that replacement of two OH groups in curcumin with less polar groups like methoxy increases its anti-proliferative activity. In this study, we explored benzylidine cyclohexanone derivatives with non-polar groups, to see if they possess increased anti-cancer activity. Novel 2,6-bis benzylidine cyclohexanone analogues of curcumin were synthesized, and their inhibitory effects on gastric adenocarcinoma (AGS) and esophageal squamous cell carcinoma (KYSE30) cancer cells were studied using an MTT assay. Cell apoptosis was detected by EB/AO staining, and cell cycle was analyzed by flow cytometry. Real-time PCR was performed for gene expression analysis. All synthesized analogues were cytotoxic toward gastric and esophageal cancer cells and showed lower IC50 values than curcumin. Treatment with 2,6-Bis-(3-methoxy-4-propoxy-benzylidene)-cyclohexanone (BM2) was 17 times more toxic than curcumin after 48 h incubation. All novel compounds were more effective than curcumin in apoptosis induction and cell cycle arrest at G1 phase. These results suggest that less polar analogues of curcumin have potent cytotoxicity in vitro. However, they need to be investigated further, especially with animal tumor models, to confirm their chemotherapeutic activity in vivo.
format	article
author	Fatemeh Alibeiki Naser Jafari Maryam Karimi Hadi Peeri Dogaheh
author_facet	Fatemeh Alibeiki Naser Jafari Maryam Karimi Hadi Peeri Dogaheh
author_sort	Fatemeh Alibeiki
title	Potent anti-cancer effects of less polar Curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells
title_short	Potent anti-cancer effects of less polar Curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells
title_full	Potent anti-cancer effects of less polar Curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells
title_fullStr	Potent anti-cancer effects of less polar Curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells
title_full_unstemmed	Potent anti-cancer effects of less polar Curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells
title_sort	potent anti-cancer effects of less polar curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells
publisher	Nature Portfolio
publishDate	2017
url	https://doaj.org/article/da91f7701132479294c8a4f369cd69ac
work_keys_str_mv	AT fatemehalibeiki potentanticancereffectsoflesspolarcurcuminanaloguesongastricadenocarcinomaandesophagealsquamouscellcarcinomacells AT naserjafari potentanticancereffectsoflesspolarcurcuminanaloguesongastricadenocarcinomaandesophagealsquamouscellcarcinomacells AT maryamkarimi potentanticancereffectsoflesspolarcurcuminanaloguesongastricadenocarcinomaandesophagealsquamouscellcarcinomacells AT hadipeeridogaheh potentanticancereffectsoflesspolarcurcuminanaloguesongastricadenocarcinomaandesophagealsquamouscellcarcinomacells
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Potent anti-cancer effects of less polar Curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells

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