Xanthohumol modulate autophagy and ER stress to counteract stemness and enhance cisplatin efficacy in head and neck squamous cell carcinoma

Abstract Natural compounds have been increasingly investigated for their efficient anti-cancer activity. Xanthohumol (XN), a flavonoid derived from hops, has shown promise in preclinical studies for various cancers due to its unique biological properties. This study investigates the effects of XN an...

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Main Authors: Vitale Del Vecchio, Ibone Rubio Sanchez-Pajares, Sameer Kumar Panda, Ayesha Rehman, Vincenzo De Falco, Aditya Nigam, Laura Mosca, Diana Russo, Claudia Arena, Maria Maddalena Nicoletti, Vincenzo Desiderio, Gianpaolo Papaccio, Luigi Mele, Luigi Laino
Format: Article
Language:English
Published: Nature Portfolio 2025-04-01
Series:Scientific Reports
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Online Access:https://doi.org/10.1038/s41598-025-98003-1
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author Vitale Del Vecchio
Ibone Rubio Sanchez-Pajares
Sameer Kumar Panda
Ayesha Rehman
Vincenzo De Falco
Aditya Nigam
Laura Mosca
Diana Russo
Claudia Arena
Maria Maddalena Nicoletti
Vincenzo Desiderio
Gianpaolo Papaccio
Luigi Mele
Luigi Laino
author_facet Vitale Del Vecchio
Ibone Rubio Sanchez-Pajares
Sameer Kumar Panda
Ayesha Rehman
Vincenzo De Falco
Aditya Nigam
Laura Mosca
Diana Russo
Claudia Arena
Maria Maddalena Nicoletti
Vincenzo Desiderio
Gianpaolo Papaccio
Luigi Mele
Luigi Laino
author_sort Vitale Del Vecchio
collection DOAJ
description Abstract Natural compounds have been increasingly investigated for their efficient anti-cancer activity. Xanthohumol (XN), a flavonoid derived from hops, has shown promise in preclinical studies for various cancers due to its unique biological properties. This study investigates the effects of XN and a cost-effective hop extract (HOP EX) on head and neck squamous cell carcinoma (HNSCC), focusing on their potential to modulate cancer stemness and enhance the efficacy of Cisplatin chemotherapy. Using a combination of flow cytometry, qPCR, and cellular assays, we assessed the impact of XN and HOP EX on cell viability, stemness, and chemoresistance in HNSCC cell lines. Further, we explored the underlying mechanisms by examining the induction of apoptosis, ER stress, and autophagy activation. Our findings demonstrate that both XN and HOP EX significantly decrease cell viability and stemness in HNSCC cells and enhance the cytotoxic effects of Cisplatin, suggesting a synergistic interaction. Mechanistically, we identified that the induction of ER stress and subsequent activation of the unfolded protein response (UPR) promote autophagy, leading to increased apoptosis. By modulating key cellular pathways such as ER stress and autophagy, these natural compounds could be developed into supportive treatments for HNSCC.
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spelling doaj-art-6098369692b249a59c1be4e4d3b8f78f2025-08-20T02:17:57ZengNature PortfolioScientific Reports2045-23222025-04-0115111310.1038/s41598-025-98003-1Xanthohumol modulate autophagy and ER stress to counteract stemness and enhance cisplatin efficacy in head and neck squamous cell carcinomaVitale Del Vecchio0Ibone Rubio Sanchez-Pajares1Sameer Kumar Panda2Ayesha Rehman3Vincenzo De Falco4Aditya Nigam5Laura Mosca6Diana Russo7Claudia Arena8Maria Maddalena Nicoletti9Vincenzo Desiderio10Gianpaolo Papaccio11Luigi Mele12Luigi Laino13Department of Experimental Medicine, University of Campania “Luigi Vanvitelli”Department of Experimental Medicine, University of Campania “Luigi Vanvitelli”Department of Experimental Medicine, University of Campania “Luigi Vanvitelli”Department of Experimental Medicine, University of Campania “Luigi Vanvitelli”Department of Experimental Medicine, University of Campania “Luigi Vanvitelli”Department of Experimental Medicine, University of Campania “Luigi Vanvitelli”Department of Life Sciences, Health and Health Professions, Link Campus UniversityMultidisciplinary Department of Medical-Surgical and Dental Specialties, University of Campania “L. Vanvitelli”Multidisciplinary Department of Medical-Surgical and Dental Specialties, University of Campania “L. Vanvitelli”Multidisciplinary Department of Medical-Surgical and Dental Specialties, University of Campania “L. Vanvitelli”Department of Experimental Medicine, University of Campania “Luigi Vanvitelli”Department of Experimental Medicine, University of Campania “Luigi Vanvitelli”Department of Health Sciences, University of BasilicataDermatology Unit, University of Campania “L.Vanvitelli”Abstract Natural compounds have been increasingly investigated for their efficient anti-cancer activity. Xanthohumol (XN), a flavonoid derived from hops, has shown promise in preclinical studies for various cancers due to its unique biological properties. This study investigates the effects of XN and a cost-effective hop extract (HOP EX) on head and neck squamous cell carcinoma (HNSCC), focusing on their potential to modulate cancer stemness and enhance the efficacy of Cisplatin chemotherapy. Using a combination of flow cytometry, qPCR, and cellular assays, we assessed the impact of XN and HOP EX on cell viability, stemness, and chemoresistance in HNSCC cell lines. Further, we explored the underlying mechanisms by examining the induction of apoptosis, ER stress, and autophagy activation. Our findings demonstrate that both XN and HOP EX significantly decrease cell viability and stemness in HNSCC cells and enhance the cytotoxic effects of Cisplatin, suggesting a synergistic interaction. Mechanistically, we identified that the induction of ER stress and subsequent activation of the unfolded protein response (UPR) promote autophagy, leading to increased apoptosis. By modulating key cellular pathways such as ER stress and autophagy, these natural compounds could be developed into supportive treatments for HNSCC.https://doi.org/10.1038/s41598-025-98003-1XanthohumolHNSCCUPRCancer stem cellsEndoplasmic reticulum stressAutophagy
spellingShingle Vitale Del Vecchio
Ibone Rubio Sanchez-Pajares
Sameer Kumar Panda
Ayesha Rehman
Vincenzo De Falco
Aditya Nigam
Laura Mosca
Diana Russo
Claudia Arena
Maria Maddalena Nicoletti
Vincenzo Desiderio
Gianpaolo Papaccio
Luigi Mele
Luigi Laino
Xanthohumol modulate autophagy and ER stress to counteract stemness and enhance cisplatin efficacy in head and neck squamous cell carcinoma
Scientific Reports
Xanthohumol
HNSCC
UPR
Cancer stem cells
Endoplasmic reticulum stress
Autophagy
title Xanthohumol modulate autophagy and ER stress to counteract stemness and enhance cisplatin efficacy in head and neck squamous cell carcinoma
title_full Xanthohumol modulate autophagy and ER stress to counteract stemness and enhance cisplatin efficacy in head and neck squamous cell carcinoma
title_fullStr Xanthohumol modulate autophagy and ER stress to counteract stemness and enhance cisplatin efficacy in head and neck squamous cell carcinoma
title_full_unstemmed Xanthohumol modulate autophagy and ER stress to counteract stemness and enhance cisplatin efficacy in head and neck squamous cell carcinoma
title_short Xanthohumol modulate autophagy and ER stress to counteract stemness and enhance cisplatin efficacy in head and neck squamous cell carcinoma
title_sort xanthohumol modulate autophagy and er stress to counteract stemness and enhance cisplatin efficacy in head and neck squamous cell carcinoma
topic Xanthohumol
HNSCC
UPR
Cancer stem cells
Endoplasmic reticulum stress
Autophagy
url https://doi.org/10.1038/s41598-025-98003-1
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