Anticancer Potential of a Synthetic Quinoline, 9IV-c, by Inducing Apoptosis in A549 Cell and In vivo BALB/c Mice Models


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Abstract

Background:In a previous work from the author of this study, the compound of 9IV-c, ((E)-2-(3,4- dimethoxystyryl)-6,7,8-trimethoxy-N-(3,4,5-trimethoxyphenyl)quinoline-4-amine) was synthesized, and the effects of potent activity on the multiple human tumor cell lines were evaluated considering the spindle formation together with the microtubule network.

Methods:Accordingly, cytotoxic activity, apoptotic effects, and the therapeutic efficiency of compound 9IV-c on A549 and C26 cell lines were investigated in this study.

Results:The compound 9IV-c demonstrated high cytotoxicity against A549 and C26 cell lines with IC50 = 1.66 and 1.21 µM, respectively. The flow cytometric analysis of the A549 cancer cell line treated with compounds 9IV-c showed that these compounds induced cell cycle arrest at the G2/M phase and apoptosis. Western blotting analysis displayed that compound 9IV-c also elevated the Bax/Bcl-2 ratio and increased the activation of caspase- 9 and -3 but not caspase -8.

Conclusion:These data presented that the intrinsic pathway was responsible for 9IV-c -induced cell apoptosis. In vivo studies demonstrated that treatment with the compound of 9IV-c at 10 mg/kg dose led to a decrease in tumor growth compared to the control group. It was found that there was not any apparent body weight loss in the period of treatment. Also, in the vital organs of the BALB/c mice, observable pathologic changes were not detected.

About the authors

Salimeh Mirzaei

Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences

Email: info@benthamscience.net

Farhad Eisvand

Department of Pharmacodynamics and Toxicology, School of Pharmacy, Mashhad University of Medical Sciences

Email: info@benthamscience.net

Mojgan Nejabat

Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences

Email: info@benthamscience.net

Razieh Ghodsi

Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences,

Email: info@benthamscience.net

Farzin Hadizadeh

Department of Medicinal Chemistry, School of Pharmacy, Mashhad University of Medical Sciences

Author for correspondence.
Email: info@benthamscience.net

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