Tebrophen — An Old Polyphenol Drug with Anticancer Potential †
Abstract
:Abbreviations
BDE | bond dissociation enthalpy |
HAT | hydrogen atom transfer |
HTS | high-throughput screening |
IP | ionization potential |
PDs | population doublings |
PMA | phorbol-12-myristate acetate |
RSA | radical scavenging activity |
SET | single electron transfer |
TEB | tebrophen |
1. Introduction
2. Results
2.1. Docking Pose of Tebrophen within DPPIV Catalytic Site
2.2. In Vitro Inhibition of ZAP-70, Lck kinase and DPPIV
2.3. Oxidative Burst
2.4. Cytotoxicity Assay
2.5. The Effects of Tebrophenon on Cell Cultures Proliferation
2.5.1. Normal Human Skin Fibroblasts NF (Primary Cells)
2.5.2. Neonatal Foreskin Fibroblasts MJ90 (Primary Cells)
2.5.3. Breast Adenocarcinoma MDA-MB-231 Cell Line
2.5.4. Strong Inhibitory Effect of Tebrophen on Proliferation of Prostate PC3 Cell Line
2.5.5. Bone Osteosarcoma U2OS Cell Line
2.5.6. Cervical Adenocarcinoma HeLa Cell Line
2.6. Radical Scavenging Activity of Tebrophen
Species | BDE | IP | Acidity | ABTS+ assay (TEAC, mM) b |
---|---|---|---|---|
ortho-Tebrophen | 82.37 | 169.6 | 326.3 | NA |
para-Tebrophen | 81.98 | 169.6 | 324.9 | NA |
Apigenin | 82.2 | 176.0 | 321.3 | 0.086 |
Kaempferol | 80.9 | 168.0 | 322.7 | 1.59 |
Luteolin | 74.5 | 174.4 | 2.18 | |
Quercetin | 72.3 | 166.1 | 316.5 | 4.42 |
Resveratrol | 77.3 | 161.3 | 327.5 | 2.14 |
3. Discussion
4. Experimental
4.1. Tebrophen
4.2. In Silico
4.2.1. Molecular Docking
4.2.2. Quantum-Chemical Calculations
4.3. In Vitro ZAP-70 and Lck Kinase, and DPPIV Inhibition Protocols
4.4. Cytotoxicity Assay
4.5. Oxidative Burst Assay
4.6. Functional Assays
4.6.1. Cell Culture
4.6.2. SA-β-galactosidase Staining and 3H-Thymidine Labeling Index
4.6.3. DiI Staining and Flow Cytometry
5. Conclusions
Conflict of Interest
Acknowledgements
- Sample Availability: Sample of the compound is available from the authors.
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Rubelj, I.; Stepanić, V.; Jelić, D.; Vidaček, N.Š.; Kalajžić, A.Ć.; Ivanković, M.; Nujić, K.; Matijašić, M.; Verbanac, D. Tebrophen — An Old Polyphenol Drug with Anticancer Potential †. Molecules 2012, 17, 7864-7886. https://doi.org/10.3390/molecules17077864
Rubelj I, Stepanić V, Jelić D, Vidaček NŠ, Kalajžić AĆ, Ivanković M, Nujić K, Matijašić M, Verbanac D. Tebrophen — An Old Polyphenol Drug with Anticancer Potential †. Molecules. 2012; 17(7):7864-7886. https://doi.org/10.3390/molecules17077864
Chicago/Turabian StyleRubelj, Ivica, Višnja Stepanić, Dubravko Jelić, Nikolina Škrobot Vidaček, Andrea Ćukušić Kalajžić, Milena Ivanković, Krunoslav Nujić, Mario Matijašić, and Donatella Verbanac. 2012. "Tebrophen — An Old Polyphenol Drug with Anticancer Potential †" Molecules 17, no. 7: 7864-7886. https://doi.org/10.3390/molecules17077864