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. 2020 Nov 20:7:1588-1591.
doi: 10.1016/j.toxrep.2020.11.004. eCollection 2020.

Cytokinesis-block micronucleus assay of celecoxib and celecoxib derivatives

Hauke Reimann  1 , Quoc Anh Ngo  2 , Helga Stopper  1 , Henning Hintzsche  1   3
Affiliations

Cytokinesis-block micronucleus assay of celecoxib and celecoxib derivatives

Hauke Reimann et al. Toxicol Rep. .

Abstract

Celecoxib is used widely for the acute treatment of pain and for pain relief in various diseases. Furthermore, it shows potential in chemoprevention, although chronic treatment with celecoxib could lead to adverse effects like cardiovascular events. New derivatives of celecoxib were synthesised that may be suitable as chemopreventive agent without inducing adverse effects. Critical endpoint for a safe use of pharmaceuticals is genotoxicity after application. A standard test for the assessment of genotoxicity is the cytokinesis-block micronucleus assay, that evaluates the number micronuclei after treatment of cells with a test compound as biomarker for DNA damage. Various promising derivatives of celecoxib have been assessed with the cytokinesis-block micronucleus assay in HeLa-H2B-GFP cells. It could be demonstrated, that neither celecoxib nor its derivatives were genotoxic in this assay and therefore celecoxib derivatives could be developed further for a safe use as chemopreventive agent.

Keywords: Celecoxib; Chemoprevention; DNA damage; Micronucleus test.

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Conflict of interest statement

The authors report no declarations of interest.

Figures

Fig. 1
Fig. 1
Test materials used for genotoxicity testing. A) Structure of celecoxib. B) Structure of the 3,4,5-trimethoxyphenyl analogue of celecoxib. C) Structure of ethyl 1,4,5-triaryl-1H-pyrazole-3-carboxylate. D) Structure of derivative 2-4.
Fig. 2
Fig. 2
Micronucleus test of celecoxib. Micronucleus frequency (grey bar) per 1000 binucleated cells (BNC) and cytokinesis-block proliferation index (CBPI, black line). Mean of three independent experiments ± standard error. Asterisk represent p ≤ 0.05 compared to treatment with 1% DMSO (Mann-Whitney-U-test).
Fig. 3
Fig. 3
Micronucleus test of celecoxib derivatives 1-4 (A-D). Micronucleus frequency (grey bar) per 1000 binucleated cells (BNC) and cytokinesis-block proliferation index (CBPI, black line) were shown. Mean of three independent experiments ± standard error. Asterisk represent p ≤ 0.05 compared to treatment with 1% DMSO (Mann-Whitney-U-test).
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