New oleoyl hybrids of natural antioxidants: Synthesis and in vitro evaluation as inducers of apoptosis in colorectal cancer cells

Carullo G, Mazzotta S, Koch AM, Hartmann K, Friedrich O, Gilbert D, Vega-Holm M, Schneider-Stock R, Aiello F (2020)

Publication Type: Journal article

Publication year: 2020

Journal

Antioxidants MDPI AG

Book Volume: 9

Pages Range: 1-16

Article Number: 1077

Journal Issue: 11

DOI: 10.3390/antiox9111077

Abstract

Nowadays, the beneficial role of a healthy lifestyle, particularly emphasizing the quality of foods and cancer management, is accepted worldwide. Polyphenols and oleic acid play a key role in this context, but are still scarcely used as anti-cancer agents due to their bio-accessibility limits. Therefore, we aimed to synthesize a set of new oleoyl-hybrids of quercetin, morin, pinocembrin, and catechin to overcome the low bioavailability of polyphenols, throughout a bio-catalytic approach using pancreatic porcine lipase as a catalyst. The in vitro assays, using a wide panel of human cancer cell lines showed, mainly for two novel regioisomer oleoyl-hybrids of quercetin, a remarkable increase in apoptotic cell populations. We suggested that the DNA damage shown as GH2AX signals might be the major cause of apoptotic cell death. Finally, we demonstrated convincing data about two novel polyphenol-based hybrids displaying a highly selective anti-cancer cytotoxicity and being superior compared to their reference/parental compounds.

Authors with CRIS profile

Anna Maria Koch Department of Paediatric Cardiac Surgery Kristin Hartmann Lehrstuhl für Medizinische Biotechnologie (MBT) Oliver Friedrich Lehrstuhl für Medizinische Biotechnologie (MBT) Daniel Gilbert Lehrstuhl für Medizinische Biotechnologie (MBT) Regine Schneider-Stock Professur für Experimentelle Tumorpathologie

Involved external institutions

Università della Calabria (UNICAL) IT Italy (IT) University of Seville / Universidad de Sevilla ES Spain (ES) Università degli Studi di Siena (UNISI) / University of Siena IT Italy (IT)

How to cite

APA:

Carullo, G., Mazzotta, S., Koch, A.M., Hartmann, K., Friedrich, O., Gilbert, D.,... Aiello, F. (2020). New oleoyl hybrids of natural antioxidants: Synthesis and in vitro evaluation as inducers of apoptosis in colorectal cancer cells. Antioxidants, 9(11), 1-16. https://doi.org/10.3390/antiox9111077

MLA:

Carullo, Gabriele, et al. "New oleoyl hybrids of natural antioxidants: Synthesis and in vitro evaluation as inducers of apoptosis in colorectal cancer cells." Antioxidants 9.11 (2020): 1-16.

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