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Existing clinical and preclinical evidence indicates ART counters cancer through multiple pathways, including inducing apoptosis and autophagy, altering the tumor microenvironment, modulating immune responses, overcoming drug resistance, and suppressing proliferation, migration, invasion, and angiogenesis. The review highlights ART activity across diverse malignancies and discusses how ART-derived DHA drives key molecular effects to support future research directions and clinical expansion.",{"@graph":69,"@context":123},[70,84,106],{"@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/antitumor-mechanism-of-artesunate-review-published-25-october-2024/332720/",{"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/antitumor-mechanism-of-artesunate-review-published-25-october-2024/332720.png","ImageObject",300,407,{"name":92,"@type":93},"Eden","Person",{"url":74,"name":95,"@type":96},"DocShare","Organization","application/pdf","2026-11-04","2026-09-21",true,{"@type":102,"interactionType":103,"userInteractionCount":105},"InteractionCounter",{"@type":104},"ViewAction",13,{"@type":107,"mainEntity":108},"FAQPage",[109,115,119],{"name":110,"@type":111,"acceptedAnswer":112},"Why is artesunate considered relevant for tumor therapy?","Question",{"text":113,"@type":114},"The review states that ART is a classic antimalarial with high efficiency, low toxicity, and good tolerance, and has demonstrated anti-tumor effects across many cancer types.","Answer",{"name":116,"@type":111,"acceptedAnswer":117},"What main mechanisms are highlighted for ART’s anti-tumor action?",{"text":118,"@type":114},"ART is described as acting through inducing apoptosis and autophagy, affecting the tumor microenvironment, regulating immune responses, overcoming drug resistance, and inhibiting tumor proliferation, migration, invasion, and angiogenesis.",{"name":120,"@type":111,"acceptedAnswer":121},"How does the review explain the relationship between ART and DHA in antitumor activity?",{"text":122,"@type":114},"It emphasizes that the antitumor mechanism largely depends on the release of DHA from ART as a prodrug, and summarizes DHA-driven inhibition of tumor progression through signaling and microenvironment modulation.","https://schema.org",{"og:url":83,"og:type":125,"og:title":65,"og:site_name":95,"og:description":67},"article",{"robots":127,"canonical":83},"index,follow",{"doc_id":129,"site_id":62},332720,1790766330,{"code":4,"msg":5,"data":132},{"doc_id":129,"user_id":133,"nickname":92,"user_avatar":134,"doc_module":4,"category_id":39,"category_name":40,"doc_title":65,"doc_description":67,"doc_content":135,"file_id":136,"file_url":137,"file_type":138,"file_size":139,"view_count":105,"is_deleted":4,"is_public":8,"is_downloadable":8,"audit_status":8,"page_count":140,"language":141,"language_code":63,"site_id":62,"html_lang":63,"table_of_contents":142,"faqs":143,"seo_title":144,"seo_description":67,"update_tm":145,"read_time":146,"preview_page_count":4},1374391974468,"https://ap-avatar.wpscdn.com/davatar_29158cc5080c5b710cf443261637dec0","TYPE Review  \nPUBLISHED 25 October 2024  \nDOI 10.3389/fphar.2024.1483049  \nOPEN ACCESS  \nEDITED BY  \nSantanu Kar Mahapatra,  \nMidnapore City College, India  \nREVIEWED BY  \nRuo Wang,  \nShanghai Jiao Tong University, China Simran Sinsinwar,  \nIndian Statistical Institute, India  \n*CORRESPONDENCE  \nBo Li,  \n [lbo@jlu.edu.cn](lbo@jlu.edu.cn)  \nRECEIVED 19 August 2024  \nACCEPTED 14 October 2024  \nPUBLISHED 25 October 2024  \nCITATION  \nFan X, Yan Y, Li Y, Song Y and Li B (2024) Antitumor mechanism of artesunate.  \nFront. Pharmacol. 15:1483049 .  \ndoi: 10.3389/fphar.2024.1483049  \nCOPYRIGHT  \n© 2024 Fan, Yan, Li, Song and Li. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY) . The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.  \nAnti-tumor mechanism of artesunate  \nXiaoyu Fan, Yiming Yan, Yafei Li, Yu Song and Bo Li*  \nDepartment of Oral Anatomy and Physiology, Jilin Provincial Key Laboratory of Oral Biomedical Engineering, Hospital of Stomatology, Jilin University, Changchun, China  \nArtesunate (ART) is a classic antimalarial drug with high efﬁciency, low toxicity and tolerance. It has been shown to be safe and has good anti-tumor effect. Existing clinical studies have shown that the anti-tumor mechanisms of ART mainly include inducing apoptosis and autophagy of tumor cells, affecting tumor microenvironment, regulating immune response, overcoming drug resistance, as well as inhibiting tumor cell proliferation, migration, invasion, and angiogenesis. ART has been proven to ﬁght against lung cancer, hepatocarcinoma, lymphoma, multiple myeloma, leukemia, colorectal cancer, ovarian cancer, cervical cancer, malignant melanoma, oral squamous cell carcinoma, bladder cancer, prostate cancer and other neoplasms. In this review, we highlight the effects of ART on various tumors with an emphasis on its anti-tumor mechanism, which is helpful to propose the potential research directions of ART and expand its clinical application.  \nKEYWORDS  \nartesunate, anti-tumor, mechanism, cancer, drug  \n1 Introduction  \nChemoresistance is an important cause of tumor treatment failure and recurrence. Therefore, it is of great signiﬁcance to ﬁnd effective anti-tumor drugs that can overcome drug resistance. Artesunate (ART), an efﬁcient and relatively safe water-soluble hemisuccinate derivative of dihydroartemisinin (DHA) (an antimalarial drug) (Qian [Y. et](Y. et) al., 2021), is derived from artemisia annua. ART is inherently unstable in an aqueous solution, rapidly hydrolyzes after preparation and injection, and can be used for temporary intravenous administration (Gashe et al., 2022) . At present, it has been found that two-carbon tied artemisinin-isatin complexes have anti-breast cancer potential and the artemisinin-isatin hybrid with ethylene binding system has antilung cancer activity (Wang et al., 2023a; Wang et al., 2023b) . ART is inherently unstable in an aqueous solution, rapidly hydrolyzes after preparation and injection, and can be used for temporary intravenous administration. Recent studies have found that in addition to its speciﬁc anti-malaria effect, ART also has many other biological activities, such as anti-inﬂammatory (Ruwizhi et al., 2022), anti-tumor (Eitae and Park, 2020), anti-viral (Hu Y. J. et al., 2021) and hypoglycemic (Alagbonsi et al., 2021) . Especially in the ﬁeld of anti-tumor, several studies have reported the strong anticancer activity of ART in recent years (Ma et al., 2021; Guan et al., 2023; Zeng et al., 2023) . The antitumor mechanism of ART is largely dependent on the release of DHA from ART as aprodrug. The latest research shows that DHA inhibits tumor progress via blocking ROR1-","cbCaibr50tPD83vi","https://ap.wps.com/l/cbCaibr50tPD83vi","pdf",2937851,15,"English","# Introduction\n# Discovery of ART and its clinical application\n## Antitumor mechanism overview\n# Targeted molecular effects of DHA released from ART","[{\"question\":\"Why is artesunate considered relevant for tumor therapy?\",\"answer\":\"The review states that ART is a classic antimalarial with high efficiency, low toxicity, and good tolerance, and has demonstrated anti-tumor effects across many cancer types.\"},{\"question\":\"What main mechanisms are highlighted for ART’s anti-tumor action?\",\"answer\":\"ART is described as acting through inducing apoptosis and autophagy, affecting the tumor microenvironment, regulating immune responses, overcoming drug resistance, and inhibiting tumor proliferation, migration, invasion, and angiogenesis.\"},{\"question\":\"How does the review explain the relationship between ART and DHA in antitumor activity?\",\"answer\":\"It emphasizes that the antitumor mechanism largely depends on the release of DHA from ART as a prodrug, and summarizes DHA-driven inhibition of tumor progression through signaling and microenvironment modulation.\"}]","Antitumor mechanism of artesunate - Review - Published 25 October 2024 | PDF",1789999201,38]