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Dequalinium, a topical antimicrobial agent, displays anticarcinoma activity based on selective mitochondrial accumulation.
Open accessAbstract
Positively charged lipophilic compounds, such as rhodamine 123, localize in mitochondria and are selectively accumulated and retained by carcinoma cells. It has been suggested that this phenotype may be exploited for selective killing of carcinoma cells by lipophilic cations. Here we report that doubly positively charged dequalinium, which has been used for 30 years as an antimicrobial agent in over-the-counter mouthwashes, lozenges, ointments, and paints, exhibits significant anticarcinoma activity. Dequalinium is more effective than seven of eight established anticancer drugs in prolonging the survival of mice with intraperitoneally implanted mouse bladder carcinoma MB49. Dequalinium also inhibits the growth of subcutaneously implanted human colon carcinoma CX-1 in nude mice and recurrent rat colon carcinoma W163 in rats. Lipophilic cationic compounds, such as dequalinium, could comprise a unique class of anticarcinoma agents.
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Cited by
Zielonka, J., Joseph, J., Sikora, A., Hardy, M., Ouari, O., Vasquez-Vivar, J., Cheng, G., Lopez, M., & Kalyanaraman, B. (2017) · Chemical Reviews · doi:10.1021/acs.chemrev.7b00042 · Cited by 1,683
Inhibition of mitochondrial beta-oxidation as a mechanism of hepatotoxicity
Fromenty, B., & Pessayre, D. (1995) · Pharmacology & Therapeutics · doi:10.1016/0163-7258(95)00012-6 · Cited by 665
Quaternary ammonium salts and their antimicrobial potential: targets or nonspecific interactions
Tischer, M., Pradel, G., Ohlsen, K., & Holzgrabe, U. (2012) · ChemMedChem · doi:10.1002/cmdc.201100404 · Cited by 357
Pierroz, V., Joshi, T., Leonidova, A., Mari, C., Schur, J., Ott, I., Spiccia, L., Ferrari, S., & Gasser, G. (2012) · Journal of the American Chemical Society · doi:10.1021/ja307288s · Cited by 296
ROS as a novel indicator to predict anticancer drug efficacy
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Metadata
- Authors
- Weiss, M. J., Wong, J. R., Ha, C. S., Bleday, R., Salem, R. R., Steele, G. D., & Chen, L. B.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1987-08
- Volume
- 84
- Issue
- 15
- Pages
- 5444-5448
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W1987885263
- Cited by
- 240
- References
- 0
- FWCI
- 3.58
- Type
- journal article
- Language
- en
- Open access
- green
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- Weiss, M. J., Wong, J. R., Ha, C. S., Bleday, R., Salem, R. R., Steele, G. D., & Chen, L. B. (1987). Dequalinium, a topical antimicrobial agent, displays anticarcinoma activity based on selective mitochondrial accumulation. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.84.15.5444
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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