30-hydroxygambogic acid increases the efficacy of cisplatin in an HPV+ head and neck cancer in vivo model

Abstract Background Head and neck squamous cell carcinoma (HNSCC) affects more than half a million people annually, and nearly 80% of oropharyngeal cancer cases are caused by human papillomavirus (HPV). Current treatments include chemo- and radiotherapy, though the effectiveness of these therapies i...

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Main Authors: Sonia N. Whang, Valeria Rodarte, Trevor Lohman, Josh Barforough, Lennox Chitsike, Gina N. Lucas, David Lee, Caleb Ruiz-Jimenez, Yan Chen Wongworawat, Rouba Ali-Fehmi, Marya Wahidi, Juli Unternaehrer, Valery Filippov, Penelope J. Duerksen-Hughes
Format: Article
Language:English
Published: BMC 2025-08-01
Series:BMC Cancer
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Online Access:https://doi.org/10.1186/s12885-025-14638-3
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author Sonia N. Whang
Valeria Rodarte
Trevor Lohman
Josh Barforough
Lennox Chitsike
Gina N. Lucas
David Lee
Caleb Ruiz-Jimenez
Yan Chen Wongworawat
Rouba Ali-Fehmi
Marya Wahidi
Juli Unternaehrer
Valery Filippov
Penelope J. Duerksen-Hughes
author_facet Sonia N. Whang
Valeria Rodarte
Trevor Lohman
Josh Barforough
Lennox Chitsike
Gina N. Lucas
David Lee
Caleb Ruiz-Jimenez
Yan Chen Wongworawat
Rouba Ali-Fehmi
Marya Wahidi
Juli Unternaehrer
Valery Filippov
Penelope J. Duerksen-Hughes
author_sort Sonia N. Whang
collection DOAJ
description Abstract Background Head and neck squamous cell carcinoma (HNSCC) affects more than half a million people annually, and nearly 80% of oropharyngeal cancer cases are caused by human papillomavirus (HPV). Current treatments include chemo- and radiotherapy, though the effectiveness of these therapies is limited by the viral oncoprotein E6, which disrupts apoptotic pathways by binding and accelerating the degradation of molecules such as E6AP and caspase-8. Our lab has identified an E6 inhibitor, 30-hydroxygambogic acid (GA-OH), that is able to maintain these apoptotic signaling molecules. Method To further explore the therapeutic potential of this small molecule, we determined its antitumor efficacy in vivo. We developed an optimized xenograft model for HPV+ HNSCC, assessed GA-OH’s toxicity, and evaluated the effectiveness of GA-OH in combination with chemotherapy utilizing the optimized concentration of 0.6 mg/kg. Results GA-OH significantly increases (* p = 0.0105) cisplatin’s efficacy in HPV+ HNSCC in vivo without overt clinical manifestations. The only toxicities noted were a 4-fold increase in creatine kinase (**** p < 0.0001) and a 2.4-fold increase in aspartate aminotransferase (** p = 0.0057) in the cisplatin and GA-OH combination group compared to the vehicle group. Conclusion The small molecule GA-OH was tolerable in our murine model, significantly amplifying the efficacy of cisplatin treatment.
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spelling doaj-art-9e02308a4f55486aa8a7f30f55b73ba32025-08-20T03:05:09ZengBMCBMC Cancer1471-24072025-08-0125111510.1186/s12885-025-14638-330-hydroxygambogic acid increases the efficacy of cisplatin in an HPV+ head and neck cancer in vivo modelSonia N. Whang0Valeria Rodarte1Trevor Lohman2Josh Barforough3Lennox Chitsike4Gina N. Lucas5David Lee6Caleb Ruiz-Jimenez7Yan Chen Wongworawat8Rouba Ali-Fehmi9Marya Wahidi10Juli Unternaehrer11Valery Filippov12Penelope J. Duerksen-Hughes13Department of Basic Science, School of Medicine, Loma Linda UniversityDepartment of Basic Science, School of Medicine, Loma Linda UniversitySchool of Allied Health Professions, Loma Linda UniversityDepartment of Basic Science, School of Medicine, Loma Linda UniversityDepartment of Basic Science, School of Medicine, Loma Linda UniversityDepartment of Basic Science, School of Medicine, Loma Linda UniversityDepartment of Basic Science, School of Medicine, Loma Linda UniversityDepartment of Basic Science, School of Medicine, Loma Linda UniversityDepartment of Pathology and Human Anatomy, Loma Linda University Medical CenterDepartment of Pathology, Michigan Medicine, University of MichiganDepartment of Pathology, Michigan Medicine, University of MichiganDepartment of Basic Science, School of Medicine, Loma Linda UniversityDepartment of Basic Science, School of Medicine, Loma Linda UniversityDepartment of Basic Science, School of Medicine, Loma Linda UniversityAbstract Background Head and neck squamous cell carcinoma (HNSCC) affects more than half a million people annually, and nearly 80% of oropharyngeal cancer cases are caused by human papillomavirus (HPV). Current treatments include chemo- and radiotherapy, though the effectiveness of these therapies is limited by the viral oncoprotein E6, which disrupts apoptotic pathways by binding and accelerating the degradation of molecules such as E6AP and caspase-8. Our lab has identified an E6 inhibitor, 30-hydroxygambogic acid (GA-OH), that is able to maintain these apoptotic signaling molecules. Method To further explore the therapeutic potential of this small molecule, we determined its antitumor efficacy in vivo. We developed an optimized xenograft model for HPV+ HNSCC, assessed GA-OH’s toxicity, and evaluated the effectiveness of GA-OH in combination with chemotherapy utilizing the optimized concentration of 0.6 mg/kg. Results GA-OH significantly increases (* p = 0.0105) cisplatin’s efficacy in HPV+ HNSCC in vivo without overt clinical manifestations. The only toxicities noted were a 4-fold increase in creatine kinase (**** p < 0.0001) and a 2.4-fold increase in aspartate aminotransferase (** p = 0.0057) in the cisplatin and GA-OH combination group compared to the vehicle group. Conclusion The small molecule GA-OH was tolerable in our murine model, significantly amplifying the efficacy of cisplatin treatment.https://doi.org/10.1186/s12885-025-14638-3Human papillomavirus (HPV)Head and neck cancerHead and neck squamous cell carcinoma (HNSCC)30-hydroxygambogic acid (GA-OH)HPV+ mouse xenograftCombination therapy
spellingShingle Sonia N. Whang
Valeria Rodarte
Trevor Lohman
Josh Barforough
Lennox Chitsike
Gina N. Lucas
David Lee
Caleb Ruiz-Jimenez
Yan Chen Wongworawat
Rouba Ali-Fehmi
Marya Wahidi
Juli Unternaehrer
Valery Filippov
Penelope J. Duerksen-Hughes
30-hydroxygambogic acid increases the efficacy of cisplatin in an HPV+ head and neck cancer in vivo model
BMC Cancer
Human papillomavirus (HPV)
Head and neck cancer
Head and neck squamous cell carcinoma (HNSCC)
30-hydroxygambogic acid (GA-OH)
HPV+ mouse xenograft
Combination therapy
title 30-hydroxygambogic acid increases the efficacy of cisplatin in an HPV+ head and neck cancer in vivo model
title_full 30-hydroxygambogic acid increases the efficacy of cisplatin in an HPV+ head and neck cancer in vivo model
title_fullStr 30-hydroxygambogic acid increases the efficacy of cisplatin in an HPV+ head and neck cancer in vivo model
title_full_unstemmed 30-hydroxygambogic acid increases the efficacy of cisplatin in an HPV+ head and neck cancer in vivo model
title_short 30-hydroxygambogic acid increases the efficacy of cisplatin in an HPV+ head and neck cancer in vivo model
title_sort 30 hydroxygambogic acid increases the efficacy of cisplatin in an hpv head and neck cancer in vivo model
topic Human papillomavirus (HPV)
Head and neck cancer
Head and neck squamous cell carcinoma (HNSCC)
30-hydroxygambogic acid (GA-OH)
HPV+ mouse xenograft
Combination therapy
url https://doi.org/10.1186/s12885-025-14638-3
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