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An active compound (AT-1), identified as 8-O-acetylharpagide from Ajuga taiwanensis, was evaluated for selective effects on FaDu HPC cells versus periodontal ligament (PDL) cells. AT-1 showed stronger toxicity in FaDu cells, induced dose-dependent G2/M arrest, and promoted necrosis-like fraction and late apoptosis at high concentrations, while PDL cells were comparatively unaffected. AT-1 also enhanced radiosensitivity in FaDu cells, supporting selective efficacy via G2/M arrest, apoptosis, and radiosensitization.",{"@graph":69,"@context":122},[70,84,105],{"@type":71,"itemListElement":72},"BreadcrumbList",[73,77,79,82],{"item":74,"name":75,"@type":76,"position":8},"https://docshare.wps.com","Home","ListItem",{"item":78,"name":9,"@type":76,"position":14},"https://docshare.wps.com/document/",{"item":80,"name":40,"@type":76,"position":81},"https://docshare.wps.com/document/research-report/",3,{"item":83,"name":65,"@type":76,"position":19},"https://docshare.wps.com/document/8-o-acetylharpagide-an-active-compound-isolated-from-ajuga-taiwanensis-selectively-induced-g2m-phase-arrest-and-radiosensitivity-in-hypopharyngeal-cancer-cells/353529/",{"url":83,"name":65,"@type":85,"image":86,"author":91,"headline":65,"publisher":94,"fileFormat":97,"inLanguage":63,"description":67,"dateModified":98,"datePublished":99,"encodingFormat":97,"isAccessibleForFree":100,"interactionStatistic":101},"DigitalDocument",{"url":87,"@type":88,"width":89,"height":90},"https://docshare.wps.com/thumbnails/8-o-acetylharpagide-an-active-compound-isolated-from-ajuga-taiwanensis-selectively-induced-g2m-phase-arrest-and-radiosensitivity-in-hypopharyngeal-cancer-cells/353529.png","ImageObject",300,407,{"name":92,"@type":93},"Patrick","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-09-23","2026-09-22",true,{"@type":102,"interactionType":103,"userInteractionCount":8},"InteractionCounter",{"@type":104},"ViewAction",{"@type":106,"mainEntity":107},"FAQPage",[108,114,118],{"name":109,"@type":110,"acceptedAnswer":111},"What is AT-1 (8-O-acetylharpagide) and where was it isolated from?","Question",{"text":112,"@type":113},"AT-1 is an active compound identified as 8-O-acetylharpagide and isolated from Ajuga taiwanensis.","Answer",{"name":115,"@type":110,"acceptedAnswer":116},"How does AT-1 affect the cell cycle and cell death in FaDu hypopharyngeal cancer cells?",{"text":117,"@type":113},"AT-1 induces significant, dose-dependent G2/M phase arrest in FaDu cells and, at high concentrations, triggers necrosis-like fractions and late apoptosis.",{"name":119,"@type":110,"acceptedAnswer":120},"Does AT-1 work similarly in periodontal ligament (PDL) cells and does it change radiosensitivity?",{"text":121,"@type":113},"AT-1 does not significantly influence cell cycle redistribution or cell death in PDL cells under the same treatment conditions, and it enhances radiosensitivity in FaDu cells rather than PDL cells.","https://schema.org",{"og:url":83,"og:type":124,"og:title":65,"og:site_name":95,"og:description":67},"article",{"robots":126,"canonical":83},"index,follow",{"doc_id":128,"site_id":62},353529,1790194508,{"code":4,"msg":5,"data":131},{"doc_id":128,"user_id":132,"nickname":92,"user_avatar":133,"doc_module":4,"category_id":39,"category_name":40,"doc_title":65,"doc_description":67,"doc_content":134,"file_id":135,"file_url":136,"file_type":137,"file_size":138,"view_count":8,"is_deleted":4,"is_public":8,"is_downloadable":8,"audit_status":8,"page_count":44,"language":139,"language_code":63,"site_id":62,"html_lang":63,"table_of_contents":140,"faqs":141,"seo_title":142,"seo_description":67,"update_tm":143,"read_time":144},549758146520,"https://ap-avatar.wpscdn.com/avatar/80002397d8c0411e94?_k=1775819394049821470","Biochemistry and Biophysics Reports 45 (2026) 102431  \nContents lists available at ScienceDirect  \nBiochemistry and Biophysics Reports  \njournal [homepage:](homepage: www.elsevier.com/locate/bbrep)[ www.elsevier.com/locate/bbrep](homepage: www.elsevier.com/locate/bbrep)  \n| 8-O-acetylharpagide, an active compound isolated from A. taiwanensis selectively induced G2/M phase arrest and radiosensitivity in hypopharyngeal cancer cells\u003Cbr>Wan-Yu Yanga,1, Yung-Cheng Wang b,c,1, Yun-Lian Lind,e, Kuei-Yuan Hou b, Wan-Chun Lif,g,h,i, Yi-Jang Lee a,j,* \u003Cbr>a Department of Biomedical Imaging and Radiological Sciences, National Yang-Ming Chiao Tung University, Taipei, 112, Taiwan b Department of Radiology, Cathay General Hospital, Taipei, 106, Taiwan\u003Cbr>c School of Medicine, Fu Jen Catholic University, Taipei, 242, Taiwan\u003Cbr>d Department of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, China Medical University, Taichung, 40402, Taiwan e Department of Pharmacy, National Taiwan University, Taipei, 10050, Taiwan\u003Cbr>f Institute of Oral Biology, College of Dentistry, National Yang Ming Chiao Tung University, Taipei, Taiwan g Department of Dentistry, College of Dentistry, National Yang Ming Chiao Tung University, Taipei, Taiwan h Oral Medicine Innovation Center (OMIC), National Yang Ming Chiao Tung University, Taipei, Taiwan i Department of Stomatology, Taipei Veterans General Hospital, Taipei, Taiwan\u003Cbr>j Cancer and Immunology Research Center, National Yang Ming Chiao Tung University, Taipei Branch, Taipei, 112, Taiwan |  |  |\n| --- | --- | --- |\n| A R T I C L E I N F O |  | A B S T R A C T |\n| Keywords: Hypopharyngeal cancer AT-1\u003Cbr>8-O-Acetylharpagide G2/M phase arrest Apoptosis Radiosensitivity |  | Hypopharyngeal cancer (HPC) is a rare but most malignant subtype of head and neck squamous cell carcinoma (HNSCC). Conventional chemo-radiotherapy is the primary approach for the treatment of HPC, while the efficacy is limited and complications. Previously, we have isolated an active compound (AT-1) identified as 8-O-acetylharpagide from Ajuga taiwanensis. Because Ajuga extracts are both edible and known for their anti-cancer properties, it is worthwhile to investigate whether AT-1 can inhibit cancers of otolaryngological origin. In this study, we compared the cell killing effects of AT-1 on FaDu HPC cells and periodontal ligament (PDL) cells. The results showed that AT-1 was more toxic on FaDu cells (IC50 = 0.88 mM) than on PDL cells (IC50 = 1.65 mM), yielding a selectivity index (SI) ≈ 1.85. AT-1 caused significant G2/M phase arrest in FaDu cells with a dosedependent manner. Concomitantly, high concentration of AT-1 could induce necrosis-like fraction and late apoptosis in FaDu cells. Notably, AT-1 did not influence the cell cycle redistribution and cell death in PDL cells under the same condition of treatment. Furthermore, AT-1 enhanced the radiosensitivity of FaDu cells rather than PDL cells, suggesting that AT-1 induced G2/M phase arrest remains sensitive to ionizing radiation known asa principle of radiobiology. Taken together, current data indicate that AT-1 raises selectively efficacy on HPC cells by increasing G2/M phase arrest, apoptosis, as well as radiosensitivity. |\n\n1. Introduction  \nHypopharyngeal cancer (HPC) is a rare and aggressive malignancy arising from the hypopharynx, the lower portion of the pharynx that connects the oropharynx to the esophagus. HPC accounts for 2–14 % of whole head and neck squamous cell carcinoma (HNSCC), while it is typically diagnosed at advanced stages with approximately 70 % of  \ncases suffered from lymphatic invasion and poor prognosis after chemoradiotherapy [1–3]. Squamous cell carcinoma (SCC) constitutes over 95 % of HPC based on the histological subtype, and mainly locates the pyriform sinuses [4]. The management of HPC involves a multidisciplinary approach, including surgery, radiation therapy, and systemic chemotherapy. However, treatment of HPC remains a challenge because of ","cbCaihGNpxTLNgGq","https://ap.wps.com/l/cbCaihGNpxTLNgGq","pdf",5671426,"English","# Introduction\n## Hypopharyngeal cancer overview\n## Ajuga taiwanensis and bioactive compounds\n## Study rationale","[{\"question\":\"What is AT-1 (8-O-acetylharpagide) and where was it isolated from?\",\"answer\":\"AT-1 is an active compound identified as 8-O-acetylharpagide and isolated from Ajuga taiwanensis.\"},{\"question\":\"How does AT-1 affect the cell cycle and cell death in FaDu hypopharyngeal cancer cells?\",\"answer\":\"AT-1 induces significant, dose-dependent G2/M phase arrest in FaDu cells and, at high concentrations, triggers necrosis-like fractions and late apoptosis.\"},{\"question\":\"Does AT-1 work similarly in periodontal ligament (PDL) cells and does it change radiosensitivity?\",\"answer\":\"AT-1 does not significantly influence cell cycle redistribution or cell death in PDL cells under the same treatment conditions, and it enhances radiosensitivity in FaDu cells rather than PDL cells.\"}]","8-O-acetylharpagide - an active compound isolated from Ajuga taiwanensis - selectively induced G2/M phase arrest and radiosensitivity in hypopharyngeal cancer cells | PDF",1790105929,23]