Anti-cancer agents in medicinal chemistry最新文献

{"title":"Quercetin's Potential Therapeutic Role in Human Colorectal Cancer: An Effective Strategy for Prevention and Treatment.","authors":"Shima Mehrabadi","doi":"10.2174/0118715206354948250226103832","DOIUrl":"https://doi.org/10.2174/0118715206354948250226103832","url":null,"abstract":"<p><strong>Background: </strong>Colorectal cancer (CRC) is a significant global health burden, ranking third in incidence and second in mortality worldwide. The incidence of CRC continues to rise, and drug resistance to conventional therapies such as 5-fluorouracil (5-FU) poses a challenge in treatment. Quercetin, a naturally occurring flavonol, has shown anti-carcinogenic properties and potential in sensitizing cancer cells to chemotherapy.</p><p><strong>Aims and objective: </strong>This review assesses recent animal and clinical studies on the impact of quercetin on CRC treatment and progression and evaluates its potential in combination with conventional therapies.</p><p><strong>Methods: </strong>A comprehensive literature search was conducted to identify relevant studies investigating quercetin's effects on CRC. The search included both animal and clinical studies.</p><p><strong>Results: </strong>Quercetin has been shown to inhibit cancer progression through cell cycle arrest and apoptosis induction. It sensitizes cancer cells to chemotherapy while exhibiting protective effects on normal cells. In CRC, quercetin has demonstrated potential in reducing tumor growth and modulating signaling pathways involved in inflammation and immune responses.</p><p><strong>Conclusion: </strong>Quercetin shows promise as a novel therapeutic agent for CRC, and its combination with conventional therapies may lead to more effective treatment options and improved patient outcomes. Further research is warranted to validate these findings in clinical settings.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-03-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143571654","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Ulvan Microneedles Loaded with Photosensitizer 5-aminolevulinic Acid Inhibits Human Cervical Cancer HeLa cells In vitro.","authors":"Wenxin Hu, Jie Wei, Sen Zheng, Guan Jiang, Bei Zhang, Zhen Liang","doi":"10.2174/0118715206358815250224043946","DOIUrl":"https://doi.org/10.2174/0118715206358815250224043946","url":null,"abstract":"<p><strong>Background: </strong>Cervical cancer encompasses highly invasive and metastatic malignant tumors with poor prognoses. Recently, microneedles have gained significant attention as a novel, non-invasive drug delivery method, offering unique advantages in tumor treatment.</p><p><strong>Objective: </strong>This study aims to develop an ulvan-based microneedle delivery system encapsulating the photosensitizer 5-aminolevulinic acid (5-ALA-UMNs) and to investigate its inhibitory effects on the growth of human cervical cancer Hela cells.</p><p><strong>Methods: </strong>The 5-ALA-UMNs and control microneedles (without photosensitizer) were fabricated using a twostep casting technique. The microneedles' morphology, puncture performance, and mechanical strength were assessed. Hela cells were treated in vitro with 5-ALA-UMNs, and the cellular uptake of the photosensitizer was observed using inverted fluorescence microscopy. Cell viability was determined by the CCK-8 assay to identify the optimal drug concentration. Additionally, the anti-tumor efficacy of 5-ALA-UMNs, induced via photodynamic therapy, was evaluated by Live-Dead staining and flow cytometry.</p><p><strong>Results: </strong>The microneedles exhibited a uniform quadrangular pyramidal shape, orderly arrangement, intact needle tips, and robust mechanical strength. Inverted fluorescence microscopy confirmed the successful uptake of the photosensitizer by Hela cells, which enzymatically converted it to the fluorescent compound protoporphyrin IX. CCK-8 assays demonstrated that 5-ALA-UMNs displayed favorable cytocompatibility and safety. Live-dead staining revealed Hela cell survival rates as follows: 99.55% in the control group, 99.37% in the control microneedle group, 99.41% in the 5-ALA-UMNs group without light exposure, and 57.35% in the 5-ALA-UMNs group with light exposure (all p < 0.05). Flow cytometry results corroborated the live-dead staining findings, confirming the cytotoxic effect of 5-ALA-UMNs on tumor cells.</p><p><strong>Conclusion: </strong>These results indicate that 5-ALA-UMNs hold promise as a tumor-targeting therapeutic.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-03-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143571669","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Unveiling the Therapeutic Potential of Trigonelline: A Promising Approach in Cancer Prevention and Treatment.","authors":"Yufei Zhu, Danni Ding, Fang Shen, Fang-Yuan Liu, Yang Yu, Feng-Juan Han","doi":"10.2174/0118715206363456250226061713","DOIUrl":"https://doi.org/10.2174/0118715206363456250226061713","url":null,"abstract":"<p><p>With the development of herbal medicine, more and more chemical extracts isolated from natural herbs are being used to treat cancer, and herbal monomers play an important role in treating tumors. There is no doubt that these substances have a powerful ability to address the growing incidence of cancer. Among them, Trigonelline, due to its anti-tumor, hypoglycemic, hypolipidemic, antioxidant, and aphrodisiac properties, has been comprehensively studied for its therapeutic potential. However, there is a lack of a complete and specific review of Trigonelline research. Regarding the information mentioned before, this paper summarizes and describes the literature related to the response mechanisms and therapeutic potential of Trigonelline. This review describes the effects of Trigonelline in inhibiting tumor growth and metastasis, reducing the toxicity of chemotherapeutic agents, decreasing oxidative stress, increasing the sensitivity type of chemotherapeutic agents, and reversing drug resistance. On account of the merits of low cost, safety and efficacy, and few toxic side effects, Trigonelline has the potential to become a new and valuable drug. Furthermore, the in-depth study of this natural substance is yet to be further developed. In addition, by exploiting it more extensively, it is expected to be an effective addition to cancer treatment. We can expect that in the future more and more herbal extracts can be used in clinical practice to prolong the survival and improve the quality of life of patients.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143565833","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Redefining Anthraquinone-based Anticancer Drug Design through Subtle Chemical Modifications.","authors":"Bijayashree Mishra, Pratap Chandra Acharya, Utpal Chandra De","doi":"10.2174/0118715206374787250227064528","DOIUrl":"https://doi.org/10.2174/0118715206374787250227064528","url":null,"abstract":"<p><p>Anthraquinones are well known for their wide spectrum of pharmacological properties. Anthraquinone antibiotics, such as doxorubicin, daunorubicin, epirubicin, and mitoxantrone, have long been used in the clinical management of various tumors. However, their use is limited due to their toxicity effects, especially cardiomyopathy, despite their pronounced therapeutic effects. In recent years, medicinal chemists have explored the possibility of modifying the anthraquinone ring appended with structurally diverse functionality in order to develop better chemotherapeutic agents with fewer adverse effects. The fused polycyclic structure of anthraquinone offers rigidity, planarity, and aromaticity, which helps in double helix DNA intercalation, disruption of G4 DNA, and inhibition of topoisomerase-II enzyme of cancer cells, making them suitable pharmacophore for anticancer drug discovery. Incorporation of suitable functional groups such as amino, hydroxyl, and their derivatives into anthraquinone rings can improve their interactions with biological targets involved in cancer progression. These subtle structural changes produce newer anthraquinone derivatives with improved anticancer properties, increased potency, selectivity, and reduced toxicity, and can overcome multi-drug resistance. On the other hand, the molecular hybrids of the anthraquinone derivatives have been reported to act on multiple targets in cancer cells, as seen in the case of clinical candidates like alectinib, midostaurin, tucatinib, belinostat, and dacinostat. Molecular hybrid has given a new direction for anticancer drug development, which can produce bifunctional drug candidates with reduced toxicity. This review summarizes different structural modifications that have been made to the anthraquinone ring in the last decade with the aim of bringing out potent yet toxicity-free anticancer agents.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143539981","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Research Progress on Small Molecule Inhibitors of MDM2-p53 Protein-protein Interaction.","authors":"Meiyao Hu, Chang Xu, Mingxin Xu, Siyu He, Dandan Liu","doi":"10.2174/0118715206358340250121060830","DOIUrl":"https://doi.org/10.2174/0118715206358340250121060830","url":null,"abstract":"<p><p>The p53 protein, renowned as the \"anti-cancer protein,\" plays a critical role in regulating the cell cycle, inducing apoptosis, and repairing DNA. Its dysregulation often leads to genomic instability and tumorigenesis. MDM2, a key negative feedback regulator of p53, inhibits both the transcriptional activity and stability of p53, thereby suppressing the anti-cancer effect of p53. With the resolution of the co-crystal structure of the MDM2- p53 complex, using small molecule inhibitors to block their interaction has emerged as a promising cancer treatment strategy. These inhibitors can remove the negative regulation of MDM2 on p53 and allow p53 to function as a \"tumor suppressor protein\". Over recent decades, researchers have designed and synthesized small-molecule inhibitors with diverse structures, showing notable anti-cancer efficacy in preclinical studies. Although several inhibitors have entered clinical trials, none have yet been approved. This review comprehensively summarizes the recent advancements in small-molecule inhibitors of MDM2-p53 protein-protein interaction (PPI) according to different types of structural scaffolds, primarily focusing on imidazolines, spirooxindoles, pyrrolidines, pyrrolones, piperidines, piperidines, purine carboxylic acid derivatives, isoquinolines, pyrazolopyrolidinone analogs, imidazothiazoles, quinolones, and spiroindolines. Additionally, this review focuses on their design, synthesis, and biological evaluation and highlights the structure-activity relationships and ongoing efforts. Despite the progress made, challenges remain. Researchers are exploring strategies to overcome these obstacles in promoting the research on drugs targeting MDM2-p53 PPI with stronger affinity, higher permeability, and a more significant effect.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143522504","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Path to the Formation Mechanism of Propolis Nanoparticles, their Cytotoxicity on 3T3 Fibroblasts, Metastatic Murine B16F10 Cells, and their In vivo Irritability in Animals.","authors":"Jeimmy González-Masís, Rodolfo J Gonzalez-Paz, Yendry Regina Corrales Ureña, Simón Guerrero, Sara González-Camacho, Nohelia Mora-Ugalde, Mónica Baizán-Rojas, Randall Loaiza, José Roberto Vega-Baudrit, Jorge M Cubero-Sesin","doi":"10.2174/0118715206316231250218063957","DOIUrl":"https://doi.org/10.2174/0118715206316231250218063957","url":null,"abstract":"<p><strong>Background: </strong>Natural products, such as propolis, are an important source of biologically active compounds with the potential to treat health disorders. Propolis is a well-known waxy resin recognized for its antimicrobial, immunomodulatory, and cytotoxic effects.</p><p><strong>Objective: </strong>In this study, we aimed to clarify the formation mechanism of propolis nanoparticles from the perspective of their stability and chemical composition. By evaluating the light absorption behaviour of the nanoparticles formed in different media and quantifying the polyphenols, we show that they are superficially hydrophobic nanoparticles with the capacity to encapsulate some polar compounds.</p><p><strong>Methods: </strong>Biological activity was evaluated by in vitro cell viability performed on NIH/3T3 fibroblasts incubated with 10, 100, and 1000 μg/mL of propolis nanoparticles for 48 hours.</p><p><strong>Results: </strong>The results show that nanoparticles are cytocompatible, with a proliferation effect. In contrast, the results of the viability of metastatic murine B16F10 cells indicate that a dose with a concentration of 5 μg/mL in the cell culture media is sufficient to stop the abnormal cell growth, having an antitumor effect. This effect might be related to the flavonoids present in the propolis nanoparticles. In vivo dermal irritability tests on New Zealand rabbits show that propolis nanoparticles' aqueous dissolution was non-irritant.</p><p><strong>Conclusion: </strong>According to the results obtained from this study, reducing the size of raw propolis down to nanoparticles and dispersing them in water solvents enhance its positive effects. The superficially hydrophobic propolis nanoparticles encapsulate active compounds such as polyphenols and flavonoids, which also confirms their ability to generate selective effects on the cells, depending on their nature.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143514456","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preliminary Investigations on Acyl Hydrazones Bearing Sulfonamides as Inhibitors of the Human Carbonic Anhydrase Isoforms I, II, IX, and XII.","authors":"Efe Doğukan Dincel, Ebru Didem Kuran, Abdulilah Ece, Faika Başoğlu-Ünal, Gioele Renzi, Gloria Badii, Fabrizio Carta, Cladiu T Supuran, Nuray Ulusoy-Güzeldemirci","doi":"10.2174/0118715206356980250113074705","DOIUrl":"https://doi.org/10.2174/0118715206356980250113074705","url":null,"abstract":"<p><strong>Aim: </strong>The present study aims to identify the synthesis and structural characterization of acyl hydrazone- sulfonamide-containing compounds that were tested in vitro on human carbonic anhydrase (hCA) isoforms I, II, IX, and XII.</p><p><strong>Methods: </strong>Herein, acyl hydrazone derivatives containing the primary sulfonamide moiety were synthesized via a three-step synthetic pathway starting from the commercially available 4-sulfamoyl benzoic acid. Structural characterizations of the final compounds were assessed through IR IR, 1H-NMR, 13C-NMR, and elemental analyses. The in vitro profiling activity of the final compounds on the Carbonic Anhydrases (CAs; EC 4.2.1.1) I, II, IX, and XII were performed by means of the stopped-flow technique and revealed nanomolar inhibitory potencies on the selected targets. Molecular docking and molecular dynamic simulations afforded a detailed understanding of the binding modes of the most effective compounds.</p><p><strong>Results: </strong>We reported the synthesis and structural characterization of 25 acyl hydrazone-sulfonamide-containing compounds that were tested in vitro on the hCAs I, II, IX, and XII isoforms for their inhibitory features. Overall, all compounds showed nanomolar inhibition potencies on the panel of hCAs considered, and their binding modes were deciphered by means of in-silico studies. Molecular docking followed by MD simulations confirmed the stability of 4l-hCA I, 4n-hCA II, 4t-hCA II, 4v-hCA XII, and 4w-hCA XII complexes.</p><p><strong>Conclusion: </strong>This study presents a deep understanding of the structural determinants influencing the affinity and selectivity of the designed compounds towards different hCAs, thus offering valuable insights for further optimization and development in the field.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-02-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143514421","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Melittin, A Potential Game-changer in the Fight Against Breast Cancer: A Systematic Review.","authors":"Gilles Prince, Ahmad Assi, Marc Aoude, Hampig Raphael Kourie, Fadi Haddad","doi":"10.2174/0118715206347581250217045306","DOIUrl":"https://doi.org/10.2174/0118715206347581250217045306","url":null,"abstract":"<p><strong>Introduction: </strong>Breast cancer is the most common cancer in women. Traditional treatments include endocrine therapy, chemotherapy, surgery, radiation, and immunotherapy. Recent studies suggest melittin, a component of bee venom, as a promising breast cancer treatment due to its anticancer properties: inducing cytotoxicity, apoptosis, and gene regulation.</p><p><strong>Method: </strong>This manuscript aims to review melittin's potential therapeutical and future implications in treating breast cancer. An extensive literature search was conducted on MEDLINE and Cochrane databases up to July 2024 using Boolean operators with a combination of keywords. After screening, data extraction, and descriptive analysis, 40 articles were retained.</p><p><strong>Results: </strong>Experimental data and different therapeutical strategies were collected. Melittin disrupts tumor cell membranes and modulates key apoptotic pathways. Advanced delivery systems enhance their effectiveness and reduce toxicity. Combining melittin with chemotherapy shows synergistic effects, improving outcomes. Thus, melittin could be a valuable addition to breast cancer therapies.</p><p><strong>Conclusion: </strong>Further clinical trials are essential to validate its potential and establish its role in breast cancer therapy.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-02-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143514458","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Kinesin Eg5 Inhibitor K858 Enhances Radiosensitivity in Esophageal Squamous Cell Carcinoma and Affects the Expression of Epithelial-mesenchymal Transition Related Markers: In vitro and In vivo Studies.","authors":"Ruixue Liu, Zhijun Yu, Wenbin Shen, Shuchai Zhu","doi":"10.2174/0118715206373782250211104402","DOIUrl":"https://doi.org/10.2174/0118715206373782250211104402","url":null,"abstract":"<p><strong>Background: </strong>Radioresistance is the primary cause of treatment failure in esophageal squamous cell carcinoma, emphasizing the importance of identifying effective radiosensitizers.</p><p><strong>Objectives: </strong>This study aimed to explore the effects and potential mechanisms of Eg5 inhibitor K858 on the radiosensitivity of esophageal squamous cell carcinoma TE-1 and KYSE150 cell lines, as well as xenografts (TE-1 cells).</p><p><strong>Methods: </strong>Cellular function was assessed using CCK8, wound healing, and transwell invasion assays. Radiosensitivity parameters were derived from colony formation assays. Cell apoptosis and cell cycle were assessed using flow cytometry, whereas protein expression levels were detected using western blotting and immunohistochemistry. The xenograft model was used to observe the growth of tumors.</p><p><strong>Results: </strong>K858 inhibited the malignant functions of TE-1 and KYSE150 cell lines. Radiosensitivity parameters were reduced after K858 treatment. The combination of K858 and irradiation markedly suppressed cell proliferation, induced apoptosis, and stimulated cell cycle arrest during the irradiation-sensitive phase. Additionally, K858, combined with irradiation, significantly increased the expression of the epithelial-mesenchymal transition marker E-cadherin and decreased the expression of N-cadherin, vimentin, MMP2, and MMP9. K858, combined with irradiation, significantly inhibited tumor growth in xenograft models.</p><p><strong>Conclusion: </strong>K858 enhanced the radiosensitivity of esophageal squamous cell carcinoma and affected the expression of epithelial-mesenchymal transition-related markers.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-02-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143490537","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Atractylenolide I Inhibits the Growth of Esophageal Cancer Cells by Inhibiting the Wnt/Β-Catenin Pathway.","authors":"Maowei Lian, Yunxiang Zhang, Xu Li, Na Niu, Dong Tang, Lihua Cao, Yong Li, Xiaocong Xiang, Chunlei Yu","doi":"10.2174/0118715206366543250213071529","DOIUrl":"https://doi.org/10.2174/0118715206366543250213071529","url":null,"abstract":"<p><strong>Background: </strong>Esophageal cancer is a highly lethal cancer with a rapidly increasing incidence and a poor prognosis. Atractylenolide I is a natural sesquiterpene lactone extracted from the rhizome of the Asteraceae plant, which has a variety of pharmacological effects, such as anti-inflammatory and immunomodulatory. Still, its impact on esophageal cancer has not been reported. Therefore, this study investigated the in vitro and in vivo effects of Atractylenolide I on the growth and proliferation of esophageal cancer and explored its possible mechanisms.</p><p><strong>Methods: </strong>To evaluate the effect of atractylenolide I on esophageal cancer cells, apoptosis assay and cell cycle assay tests were performed. Atractylenolide I was used to treat esophageal cancer cells for 48 hours, and flow cytometry detects apoptosis and cell cycle. The Wnt/β-catenin-related pathway proteins were then detected by Western blotting. For in vivo studies, an esophageal cancer graft tumor model was established subcutaneously in BALB/c nude mice, which were given Atractylenolide I treatment for 2 weeks.</p><p><strong>Result: </strong>The result shows that Atractylenolide I inhibited the proliferation and induced apoptosis of esophageal squamous carcinoma and adenocarcinoma cells. Further research shows that Atractylenolide I inhibited the Wnt/β-catenin signaling pathway, decreased the expression of CCND1, MYC, and FN1 genes, and thus increased the apoptosis of esophageal cancer cells and blocked the cell cycle in G0/G1 phase, hence exerting the role of inhibiting esophageal cancer cells in vivo and in vitro.</p><p><strong>Conclusion: </strong>This study indicates that Atractylenolide I is an efficient lead compound for the treatment of esophageal cancer, providing a theoretical basis for further clinical development and application of Atractylenolide I.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-02-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143466796","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}