Biological evaluation of 2-arylidene-4, 7-dimethyl indan-1-one (FXY-1): a novel Akt inhibitor with potent activity in lung cancer

Cancer Chemotherapy and Pharmacology
Prasanna RajagopalanHarish C Chandramoorthy

Abstract

Human lung cancer is contributed to be a major mortality factor in the cancer-related deaths. Arylidene indan-ones constitute a new class of potential anti-tumor compounds. Herein, we report the biological efficacy of the 2-arylidene-4, 7-dimethyl indan-1-one (FXY-1), a potential lead molecule of arylidene indan-ones in lung cancer models. We previously described anticancer activity of FXY-1 against human breast adenocarcinoma. FXY-1 efficacy was assessed by standard anticancer screening in NCI-H 460, A549, NCI-H 1975 and NCI-H 2170 cells. Initial molecular docking analysis was performed to check the interaction of compound to Akt enzyme. Anti-proliferation, anti-metastatic and transendothelial cell migration were performed to check efficacy of the drug. Western blot analysis was performed to understand the regulation of pro-apoptotic and anti-apoptotic proteins by the compound. The effect of FXY-1 on caspase induction and Akt phosphorylation were checked using Western blot analysis. Flow cytometry was used to reveal the cell cycle changes and apoptosis-inducing properties of FXY-1 in the lung cancer cells. In-vitro Akt inhibition property of the compound was studied using a fluorescence-based, coupled-enzyme reaction. The in-v...Continue Reading

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Citations

Feb 19, 2020·Biotechnology and Applied Biochemistry·Meenakshisundaram BalasubramaniamPrasanna Rajagopalan
Jul 30, 2019·Journal of Food Biochemistry·Ayed Dera, Prasanna Rajagopalan
Jun 28, 2017·Cancer Chemotherapy and Pharmacology·Samira ValiyariSaeid Bouzari
Jul 30, 2019·Journal of Food Biochemistry·Prasanna RajagopalanHarish C Chandramoorthy

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