Within the huge class of plant secondary metabolites, resveratrol-derived stilbenoids show wide structural diversity and mediate a great number of biological responses relevant for human health, including cancer prevention and cytotoxicity. Resveratrol is known to modulate several pathways directly linked to cancer progression, as well as its analogue pterostilbene, characterized by an increased metabolic stability and significant pharmacological activities. To study the potential anticancer activity of other stilbenoids, a home-made collection of resveratrol dimers and simplified analogues was tested on melanoma A375, non-small cell lung cancer H460 and PC3 prostate cancer cell lines. The structural determinants responsible for the antiproliferative activity have been highlighted. Moreover, to investigate the DNA damage ability of the selected molecules, the expression of the gamma-H2AX after compound exposure was evaluated.

Cytotoxicity of Benzofuran-Containing Simplified Viniferin Analogues / S. Princiotto, C. Pinna, L.M. Mattio, F. Annunziata, G.L. Beretta, A. Pinto, S. Dallavalle. - In: PHARMACEUTICALS. - ISSN 1424-8247. - 17:8(2024 Aug 01), pp. 1-7. [10.3390/ph17081012]

Cytotoxicity of Benzofuran-Containing Simplified Viniferin Analogues

S. Princiotto
Primo
;
C. Pinna
Secondo
;
L.M. Mattio;F. Annunziata;A. Pinto
Penultimo
;
S. Dallavalle
Ultimo
2024

Abstract

Within the huge class of plant secondary metabolites, resveratrol-derived stilbenoids show wide structural diversity and mediate a great number of biological responses relevant for human health, including cancer prevention and cytotoxicity. Resveratrol is known to modulate several pathways directly linked to cancer progression, as well as its analogue pterostilbene, characterized by an increased metabolic stability and significant pharmacological activities. To study the potential anticancer activity of other stilbenoids, a home-made collection of resveratrol dimers and simplified analogues was tested on melanoma A375, non-small cell lung cancer H460 and PC3 prostate cancer cell lines. The structural determinants responsible for the antiproliferative activity have been highlighted. Moreover, to investigate the DNA damage ability of the selected molecules, the expression of the gamma-H2AX after compound exposure was evaluated.
DNA damage; antiproliferative activity; benzofuran nucleus; dimeric stilbenoids; viniferin derivatives;
Settore CHEM-05/A - Chimica organica
Settore CHEM-07/A - Chimica farmaceutica
   Exploiting synergy in molecular targeted anticancer chemotherapy: synthesis, optimization, mechanism of action determination and biological validation in cellular and animal models of novel molecules targeting convergent metabolic pathways in cancer
   MINISTERO DELL'ISTRUZIONE E DEL MERITO
   2017SA5837_005
1-ago-2024
Article (author)
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/1101128
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