Journal Articles

Non-conventional rottlerin anticancer properties

April 05, 2018

Maioli, E; Daveri, E; Maellaro, E; Ietta, F; Cresti, L; Valacchi, G (2018). Non-conventional rottlerin anticancer properties. Archives of Biochemistry and Biophysics, vol. 645 (50-53).

Author Affiliations

Dipartimento di Scienze della Vita, Universita’ di Siena, Via A. Moro, 53100, Siena, Italy

University of California Davis, Department of Nutrition and Environmental Toxicology, 2251 Meyer Hall, 450 Bioletti Way, 95616-5270, Davis, CA, USA

Dipartimento di Medicina Molecolare e dello Sviluppo, Universita’ di Siena, Via A. Moro, 53100, Siena, Italy

Dipartimento di Scienze della Vita e Biotecnologie, Universita’ di Ferrara, Via Borsari 46, Ferrara, 44121, Italy

NC State University, Plants for Human Health Institute, Animal Science Dept. NC Research Campus, 600 Laureate Way, Kannapolis, NC, 28081, USA


In the past few years, we focused the interest on rottlerin, an old/new natural substance that, over the time, has revealed a number of cellular and molecular targets, all potentially implicated in the fight against cancer. Past and recent literature well demonstrated that rottlerin is an inhibitor of enzymes, transcription factors and signaling molecules that control cancer cell life and death. Although the rottlerin anticancer activity has been mainly ascribed to apoptosis and/or autophagy induction, recent findings unveiled the existence of additional mechanisms of toxicity. The major novelties highlighted in this mini review are the ability to bind and inhibit key molecules, such as ERK and mTOR, directly, thus independently of upstream signaling cascades, and to cause a profound dysregulation of cap-dependent protein translation through the mTORC1/4EBP1/eIF4E axis and by inhibition of eIF2, an initiation factor of translation that is negatively regulated by endoplasmic reticulum (ER) stress. These last mechanisms, proved to be lethal in cancer cell lines derived from breast and skin, strongly enforce the potential of rottlerin as a promising natural lead compound for the development of novel therapeutic approaches.

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