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Potent anti-cancer effects of less polar Curcumin analogues on gastric adenocarcinoma and esophageal squamous cell carcinoma cells.
Alibeiki, Fatemeh; Jafari, Naser; Karimi, Maryam; Peeri Dogaheh, Hadi.
Afiliação
  • Alibeiki F; School of Medicine, Ardabil University of Medical Science, Ardabil, 56197, Iran.
  • Jafari N; School of Medicine, Ardabil University of Medical Science, Ardabil, 56197, Iran. naser.jafari@uky.edu.
  • Karimi M; Markey Cancer Center, University of Kentucky, Lexington, KY, USA. naser.jafari@uky.edu.
  • Peeri Dogaheh H; Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Science, Tehran, 14176, Iran.
Sci Rep ; 7(1): 2559, 2017 05 31.
Article em En | MEDLINE | ID: mdl-28566729
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.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Neoplasias Gástricas / Adenocarcinoma / Curcumina / Carcinoma de Células Escamosas do Esôfago Idioma: En Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Irã

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Neoplasias Gástricas / Adenocarcinoma / Curcumina / Carcinoma de Células Escamosas do Esôfago Idioma: En Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Irã