Anti-cancer agents in medicinal chemistry最新文献

{"title":"Synthesis and Evaluation of Optical Properties, SHP2 Inhibitory Activity, and Cellular Imaging for Novel 2-Quinolone Derivatives.","authors":"Chun Zhang, Yuting Yang, Li-Xin Gao, Suya Gan, Jia Li, Xin Wang, Yu-Bo Zhou, Wen-Long Wang","doi":"10.2174/0118715206337347250219112715","DOIUrl":"https://doi.org/10.2174/0118715206337347250219112715","url":null,"abstract":"<p><strong>Introduction: </strong>Although the development of SHP2 inhibitors has made striking progress, there is no inhibitor in clinical evaluation because of the potential side effects induced by poor drug distribution. Fluorescence imaging technology is widely used in the process of diagnosis and treatment of diseases because of the advantages of rapid imaging and non-destructive detection and might provide a new way to explore the mechanism of drug-target interactions in intact tissue.</p><p><strong>Method: </strong>A series of 2-quinolone derivatives as fluorescent inhibitors against SHP2 were designed and synthesized, and their spectral properties and biological activities were evaluated in this report. The representative compound 8A had excellent fluorescence properties (λ : 562 nm, Stokes shift: 170 nm, fluorescence quantum yield: 0.072) and optical stability.</p><p><strong>Results: </strong>Moreover, compound 8A emitted a blue signal in SHP2WT U2OS cells and inhibited the SHP2 enzyme abilities (IC50: 20.16 ± 0.95 μM) without the extra combination of suitable fluorophores, linker, or selectiveactivated molecules.</p><p><strong>Conclusion: </strong>Therefore, we hope that compound 8A could act as a lead to develop novel, convenient, and bifunctional chemical tools to explore the mechanism of drug-target interactions in intact tissue and promote the integrated research progress of diagnosis and treatment of SHP2 related diseases.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-03-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143655881","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":"Gut Microbiota and the Gut-liver Axis in Hepatocellular Carcinoma: A Comprehensive Review of Pathogenesis and Therapeutic Strategies.","authors":"Satyam Yadav, Ranjeet Kumar","doi":"10.2174/0118715206364200250304034753","DOIUrl":"https://doi.org/10.2174/0118715206364200250304034753","url":null,"abstract":"<p><p>Hepatocellular carcinoma (HCC) is among the most prevalent and fatal cancers globally. The gut-liver axis, involving intricate interactions between gut microbiota and the liver, has emerged as a critical pathway in HCC development. This review comprehensively examines the molecular mechanisms by which gut microbiota contribute to hepatocarcinogenesis. It discusses factors that either protect against or promote HCC, such as bacterial translocation, and explores the biological processes that drive carcinogenesis, while addressing clinical and pathophysiological complexities. Special attention is given to the role of toll-like receptors (TLRs) and inflammation in liver cells, where microbial components trigger changes in TLR activation, leading to increased inflammation and fibrosis. Additionally, the review covers obesity-related HCC, highlighting the impact of gut microbiota alterations on this cancer type. It critically assesses current literature on therapeutic interventions targeting gut microbiota in HCC, focusing on strategies like probiotics and antibiotics that could modulate microbial composition to prevent HCC progression. The review also explores gut microbiota-derived biomarkers for early detection and monitoring of HCC and discusses personalized therapies based on individual gut-liver interactions. Finally, it identifies research gaps and suggests future studies to deepen understanding of how gut microbiota can be leveraged as an adjunct therapy in HCC. Overall, the review underscores the pivotal role of gut microbiota in HCC pathogenesis and treatment, pointing to microbiome modulation as a promising therapeutic avenue.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143717927","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":"New Radiopharmaceutical Tracers in Breast Cancer Diagnosis and Therapy.","authors":"Hiva Rahmati, Seyed Mehdi Mousavi, Zobin Souri, Soghra Farzipour, Amin Ebrahimi Tavani, Fatemeh Jalali-Zefrei","doi":"10.2174/0118715206357095250306051714","DOIUrl":"https://doi.org/10.2174/0118715206357095250306051714","url":null,"abstract":"<p><p>Breast cancer (BC) remains a predominant cause of mortality among women, with early diagnosis and ongoing monitoring being crucial for effective management. Integrating nuclear medicine with radiological modalities offers non-invasive anatomical and functional information, enabling precise target localization and quantification. This approach guided the selection of the most appropriate personalized treatment and predicted its efficacy, reducing the use of unnecessary drugs and lowering patient management costs. Since 2020, significant breakthroughs have been made in the development of radiopharmaceuticals, which are different in importantly targeting agents and radionuclides, with a focus on their efficacy in preclinical studies. This review accentuates the central role of radiopharmaceuticals in recent advancements for both imaging and therapeutic applications in BC. We discussed various receptor-targeted radiopharmaceutical therapy (RPT) agents currently utilized in clinical and preclinical settings with their chemical structures, along with the challenges faced in their implementation, including angiotensin II type 1 receptor (AT1 receptor), integrins αvβ3, chemokine receptor (CXCR4), and trophoblast cell-surface antigen-2 (TROP2), cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor, and epithelial cell adhesion molecule (EpCAM)-targeted, epidermal growth factor receptor (EGFR), vascular endothelial growth factor receptor (VEGFR), fibroblast activation protein inhibitor (FAPI), and mucin 1 (MUC1). While numerous promising RPT agents were still in preclinical stages, this review underscored the potential of tailored radiopharmaceuticals to enhance BC diagnosis and treatment, providing novel avenues for personalized medicine.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143717928","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":"Bacteriocins from Lactic Acid Bacteria Could Modulate the Wnt Pathway: A Possible Therapeutic Candidate for the Management of Colorectal Cancer- An In silico Study.","authors":"Sherlin Rosita Arokiaraj, Ragothaman Prathiviraj, Chaiyavat Chaiyasut, Bhagavathi Sundaram Sivamaruthi","doi":"10.2174/0118715206367950250228100833","DOIUrl":"https://doi.org/10.2174/0118715206367950250228100833","url":null,"abstract":"<p><strong>Introduction: </strong>Colorectal cancer (CRC) is a type of cancer that develops due to abnormal cell growth in the colon and rectum. Existing conventional CRC treatment strategies have side effects. Hence, exploring new and advanced techniques for bacterial CRC therapy is crucial. Bacteriocins are peptides produced by bacteria, including lactic acid bacteria (LAB), that have bactericidal effects. In the present study, we have focused on searching for effective and safe bacteriocins from LAB as alternatives to clinical therapeutics for treating CRC, leaving healthy cells unaffected.</p><p><strong>Methods: </strong>We selected nine bacteriocin-like peptides that are effective in the human gut microbiome. These peptides were derived from LAB species using online database resources. We then conducted an in silico phylogenetic analysis of other LAB species present in the gut microbiome using the KEGG Genome database. We established the phylogenetic relationship of these LAB species with others observed in the database to determine their closeness and similarity. Further, the bacteriocin-like peptides were modeled and refined to interact with the plausible target. The systematic network analysis was performed to find the highly interconnected targets involved in the Wnt target genes of CRC.</p><p><strong>Results: </strong>The network analysis observed that the genes CTNNB1 and LRP5 were found as hub genes to upregulate CRC. In silico protein-peptide docking between the target bacteriocins like peptides and the therapeutic targets of CRC was performed, significantly our findings revealed that the peptide PE4 and PE9 (Lactacin F and Lactacin B) exhibited better binding affinity with CTNNB1. In contrast, the peptides PE7 and PE9 (Doderlin and Lactacin B) revealed better binding affinity with LRP5. Furthermore, we conducted molecular dynamics (MD) simulations to confirm the stability and bonding interactions of the bacteriocins derived from the LAB species.</p><p><strong>Conclusion: </strong>Our findings indicate that bacteriocins (Lactacin B, Lactacin F and Doderlin) may have significant potential as therapeutics for CRC.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-03-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143612930","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":"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}