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Vol. 64 No. 7: Issue 7

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Cytotoxic effect of 2, 5-dimethyl-celecoxib as a structural analog of celecoxib on human colorectal cancer (HT-29) cell line

https://doi.org/10.14715/cmb/2018.64.7.2
Saba Nikanfar
epartment of biochemistry, Faculty of Medicine, Cellular and Molecular Research Center, Urmia University of Medical Sciences, Urmia, Iran
Somayeh Atari-hajipirloo
epartment of biochemistry, Faculty of Medicine, Cellular and Molecular Research Center, Urmia University of Medical Sciences, Urmia, Iran
Fatemeh Kheradmand
Department of biochemistry, Faculty of Medicine, Solid Tumor and Cellular and Molecular Research Center, Urmia University of Medical Sciences, Urmia, Iran
Jalil Rashedi
Department of laboratory sciences, Faculty of Paramedicine, Tabriz University of Medical Sciences, Tabriz, Iran
Amir Heydari
Department of Pharmacology, Faculty of Pharmacy, Urmia University of Medical Sciences, Urmia, Iran

Corresponding Author(s) : Fatemeh Kheradmand

fkheradmand@yahoo.com

Cellular and Molecular Biology, Vol. 64 No. 7: Issue 7

Abstract

Dimethyl-celecoxib (DMC), a close derivative of celecoxib (CXB) with a low COX-2 inhibitory function, exhibits signiï¬cant anti-neoplastic properties. In this study, we have investigated the effect of CXB and DMC on the human HT-29 cell line. The cellular viability, caspase-3 activity, and VEGF, NF-κB, and COX-2 genes expressions were assessed respectively with MTT, colorimetric, and real-time RT-PCR methods. DMC, a close analogue of CXB, was more potent in inhibiting the growth of cells (IC50: 23.45 µM at 24 hr) than CXB (IC50: 30.41 µM at 24 hr). Both CXB and DMC caused a significant difference in caspase-3 activity compared to the control group. DMC significantly decreased the NF-κB expression. Down-regulation of the COX-2 mRNA expression in the celecoxib-treated group was significant compared with that in the DMC-treated group. Alterations in the mRNA expression of VEGF were not significant between the groups. Owing to the more potent growth inhibitory effects of DMC compared to that of celecoxib, it may be important to conduct research on the anticancer application of this compound, which can reduce the side effects relating to COX2 inhibition.

 

Keywords

Celecoxib Colorectal Cyclooxygenase2 NF-κB 2 5-Dimethyl-celecoxib.
Nikanfar, S., Atari-hajipirloo, S., Kheradmand, F., Rashedi, J., & Heydari, A. (2018). Cytotoxic effect of 2, 5-dimethyl-celecoxib as a structural analog of celecoxib on human colorectal cancer (HT-29) cell line. Cellular and Molecular Biology, 64(7), 8–13. https://doi.org/10.14715/cmb/2018.64.7.2
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