Anti-cancer agents in medicinal chemistry最新文献

{"title":"Exploring the Therapeutic Potential of an Iron(III)-Polysaccharide Complex Derived from Hypsizygus ulmarius.","authors":"Sudha Govindan, Abinaya Nagarajan, Amritha Sukumaran, Prasanna Ramani","doi":"10.2174/0118715206452456260216060400","DOIUrl":"https://doi.org/10.2174/0118715206452456260216060400","url":null,"abstract":"<p><strong>Introduction: </strong>This current research involves the synthesis and biological evaluation of an iron complex derived from the Hypsizygus ulmarius polysaccharide (HUP-Fe(III)), with the aim of determining its potential as an iron supplement and a bioactive agent.</p><p><strong>Methods: </strong>HUP-Fe(III) was characterized using FT-IR, NMR, SEM, XRD, molecular weight analysis, and monosaccharide profiling. Antioxidant capacity was assessed by DPPH, ABTS, hydroxyl radical scavenging, and ferric/cupric ion reduction assays. Antibacterial activity was tested against Gram-positive and Gram-negative strains. Anti-inflammatory effects were evaluated through membrane stabilization and hemolysis inhibition. Coagulation parameters such as Activated Partial Thromboplastin Time (APTT), Thrombin Time (TT), and Prothrombin Time (PT) were measured, and anticancer activity against Triple-Negative Breast Cancer (TNBC) cell lines was analyzed, including effects on cell cycle progression and mitochondrial function.</p><p><strong>Results: </strong>The analysis of HUP-Fe(III) revealed an iron content of 7.56%, and SEM and XRD investigations showed significant morphological changes and reduced crystallinity after Fe³⁺ chelation. FT-IR and XRD patterns point to a β-FeOOH structure, while NMR evidence indicates changes in glycosidic connections in the anomeric region. The anti-oxidant results indicated that HUP-Fe(III) had better radical scavenging activity than native HUP. Antibacterial analysis showed moderate-to-high inhibition. In vitro anti-inflammatory experiments showed that HUP-Fe(III) improved membrane stability and hemolysis prevention. The APTT and TT were significantly prolonged, while PT was unaffected. HUP-Fe(III) strongly inhibited TNBC cell lines by arresting G2/M cell cycle and causing mitochondrial malfunction. These findings indicate that HUP-Fe(III) exhibits promising multifunctional biological activities, suggesting its potential for further investigation as a candidate for iron supplementation.</p><p><strong>Discussion: </strong>Polysaccharide-iron complexes enhanced surface charge may enhance their ability to interact with microbial surfaces and boost their antibacterial activity, especially against Gram-negative bacteria. The HUPFe( III) can improve the protective effects against hemolysis by stabilizing the membrane more effectively, perhaps as a result of iron coordinating with membrane lipids. The HUP-Fe(III) may exert a stronger or prolonged effect on the intrinsic coagulation pathway, potentially through enhanced interaction with clotting factors. The complex exerted enhanced antitumor activity against TNBC cells by reducing viability, inducing cell cycle arrest at the G2/M phase, and collapsing mitochondrial membrane potential, likely through ROS-mediated apoptosis.</p><p><strong>Conclusion: </strong>HUP-Fe(III) is a safe, multifunctional candidate for incorporation into functional foods or therapeutics addressing iron defic","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148257153","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 Meta-Analysis and Systematic Review of the Frequency, Clinicopathological Features, and Diagnostic Potential of CDH1 Methylation in Head and Neck Cancer.","authors":"Mubarak Alqahtani, Abdulmohsin Mohammed Alzuhairi, Osama Hasan Alalmaie, Faisal Nasser Alahmari, Mohammed Nasser Alahmari, Madhawi Abdulaziz Alanazi, Yara Abdullah Alziyad, Mohammed Hamad Alqahtani, Noura Ali Alshahrani, Hossam Abdullah Alawdah, Abdulaziz Awad Alqarni, Faisal Mohammed Bin Libdah, Saud Nayef Salem Aldanyowi, Naif Yaseen Albar, Abdulsalam Mohammed Aleid","doi":"10.2174/0118715206420855251204072123","DOIUrl":"https://doi.org/10.2174/0118715206420855251204072123","url":null,"abstract":"<p><strong>Introduction: </strong>Head and neck cancer (HNC), particularly head and neck squamous cell carcinoma (HNSCC), is a major global health issue. Epigenetic alterations, especially the hypermethylation of tumor suppressor genes (TSGs) such as CDH1, which encodes the E-cadherin protein, play a crucial role in the development and progression of HNC. This meta-analysis aimed to evaluate the role of CDH1 methylation as a potential diagnostic and less invasive biomarker for HNC, assessing its correlation with various clinical, pathological, and lifestyle factors, including tumor size, lymph node involvement, clinical stage, smoking, and alcohol consumption.</p><p><strong>Methods: </strong>A systematic search was conducted across multiple databases (PubMed, Scopus, Web of Science, and Cochrane Library) up to September 2024. Studies that reported the frequency of CDH1 methylation in HNC patients and its association with clinicopathological factors were included. Statistical analysis was performed using Review Manager (RevMan 5.4) software, and diagnostic test accuracy (DTA) was assessed through sensitivity, specificity, and area under the curve (AUC) analyses using MetaDesk software.</p><p><strong>Results: </strong>Forty-three studies, involving 1542 HNC patients and 1532 controls, were included. The pooled analysis showed a significantly higher prevalence of CDH1 methylation in HNC patients compared to controls (OR = 8.09, 95% CI: 5.29-12.36, P < 0.001). Subgroup analysis revealed significant associations in both Asian and Caucasian populations and various tumor subtypes. CDH1 methylation correlated with alcohol consumption and advanced clinical stage, but not with tumor size, lymph node involvement, or metastatic status. The pooled diagnostic odds ratio was 8.18 (95% CI: 5.32-12.58), with an AUC of 0.78, indicating moderate diagnostic accuracy.</p><p><strong>Conclusion: </strong>CDH1 methylation holds promise as a diagnostic biomarker for HNC, demonstrating high specificity but moderate sensitivity. While its association with specific clinicopathological factors is notable, it should be used in conjunction with other diagnostic tools for more effective clinical application.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-06-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148257101","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":"Analysis of the Oncogenic Role of Colony-Stimulating Factor 1 Receptor (CSF1R) in Pancreatic Adenocarcinoma.","authors":"Huiying Cui, Xuezhe Piao, Jiaming Zhang, Zhezhu Han, Qiang Xu","doi":"10.2174/0118715206464495260330052127","DOIUrl":"https://doi.org/10.2174/0118715206464495260330052127","url":null,"abstract":"<p><strong>Introduction: </strong>Based on The Cancer Genome Atlas (TCGA) and Gene Expression Omnibus (GEO), we profiled the role of Colony-Stimulating Factor 1 Receptor (CSF1R) in cancer. We specifically focused on pancreatic ductal adenocarcinoma (PAAD), analysing its regulative function in cancer progression and its usefulness as a potential biomarker and therapeutic target.</p><p><strong>Methods: </strong>Using the TCGA and GEO databases, gene expression, survival prognosis, genetic abnormalities, immune infiltration, and CSF1R-related gene enrichment related to the CSF1R gene in patients with PAAD were studied.</p><p><strong>Results: </strong>CSF1R expression appears to affect the development of PAAD; there is more CSF1R expression in the tumour tissue than in nearby normal tissues. There was no statistical difference in the overall survival or diseasefree survival of CSF1R expression. Analysis of changes in the CSF1R gene showed that PAAD samples had a low mutation frequency, and CSF1R gene amplification was the main reason. It was additionally emphasized that the impact of CSF1R on the tumor microenvironment, as evidenced by an immunological infiltration analysis, showed a strong correlation between the estimated infiltration values of cancer-associated fibroblasts and CSF1R expression in PAAD. This additional evidence was found for CSF1R expression in cancer-associated fibroblasts in PAAD.</p><p><strong>Discussion: </strong>Targeting CSF1R might be a promising strategy for PAAD treatment. Inhibiting CSF1R activity or TGF-β binding to CSF1R inhibits tumour growth and immune escape. Investigating the link between CSF1R, TGF-β, and the immune system leads to new opportunities for combination therapies that integrate targeted medicine with immunotherapy.</p><p><strong>Conclusion: </strong>Targeting CSF1R might be a PAAD treatment. Inhibiting CSF1R activity or TGF-β binding to CSF1R inhibits tumour growth and immune escape. Investigating the link between CSF1R, TGF-β, and the immune system opens new opportunities for combining targeted medicines with immunotherapy.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-06-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148222585","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":"QSAR Modeling of Camptothecin Derivatives Targeting Topoisomerase I: Structural Insights for Anticancer Drug Design.","authors":"Hossam A Mahmoud, Noha A Elnady, Salma A Elmallah","doi":"10.2174/0118715206389047251115115049","DOIUrl":"https://doi.org/10.2174/0118715206389047251115115049","url":null,"abstract":"<p><strong>Introduction: </strong>This study investigates the quantitative structure-activity relationship (QSAR) of camptothecin derivatives to determine how variations in their structures affect the activity of these derivatives on Topoisomerase I (Top I), a crucial enzyme involved in DNA replication in cancer cells.</p><p><strong>Methods: </strong>A total of 55 camptothecin derivatives were divided into training and test sets, with biological activity (IC50) as the dependent variable. A Partial Least Squares (PLS) Regression model was developed using the calculated molecular descriptors to predict the IC50 values.</p><p><strong>Results: </strong>The R² and Q² values were 0.99852 and 0.249, respectively. QSAR results indicate that molar refractivity, hydrophilicity, molecular weight, and the ether group count highly contribute to the expected activity of camptothecin (CPT) derivatives on Top I.</p><p><strong>Conclusion: </strong>This study presents a computational approach to better understand how the structure of camptothecin derivatives affects their activity against Topoisomerase I, which could inform the future design of more effective anticancer drugs.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-06-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148222658","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":"Targeting CHCHD3 inhibits tumorigenesis of NSCLC by Reprogramming Mitochondrial Metabolism.","authors":"Lili Jin, Jiahao Shen, Xuting Xu, Pingping Niu, Yu Zhou, Shunli Dong, Qibin Shen, Qinhua Gu","doi":"10.2174/0118715206469218260522055432","DOIUrl":"https://doi.org/10.2174/0118715206469218260522055432","url":null,"abstract":"<p><strong>Background: </strong>Mitochondria are essential organelles for cellular metabolism and tumor formation. We discovered that CHCHD3 is an important inner mitochondria membrane protein involved in the proliferation of lung adenocarcinoma (LUAD). However, the molecular pathways through which CHCHD3 contributes to cancer progression remain poorly understood.</p><p><strong>Methods: </strong>Following CHCHD3 knockdown, cell proliferation was assessed by CCK8 assay, colony formation assay, and cell cycle analysis. Apoptosis, intracellular Reactive Oxygen Species (ROS) levels, and mitochondrial membrane potential were evaluated using flow cytometry, JC-1 staining, and Western blot analysis, respectively. Mitochondrial function was measured using a Seahorse analyzer. Immunoprecipitation coupled with mass spectrometry (IP-MS) and Co-immunoprecipitation (CO-IP) were used to identify CHCHD3-interacting proteins.</p><p><strong>Results: </strong>CHCHD3 expression was significantly upregulated in lung cancer tissues, with its overexpression correlating with poor patient survival. In LUAD cells, CHCHD3 knockdown suppressed proliferation, induced G1 cell cycle arrest, and triggered cellular dysfunction, including apoptosis and mitochondrial energy metabolism impairment. IP-MS screening identified several potential CHCHD3-interacting proteins, among which SAMM50 and VDAC1/2 were validated as direct binding partners. Dysregulation of these interactions may underlie the excessive production of ROS observed upon CHCHD3 loss.</p><p><strong>Discussion: </strong>Our results demonstrate that CHCHD3 is highly expressed in lung adenocarcinoma and positively correlates with poor prognosis. Mechanistically, CHCHD3 loss is associated with mitochondrial dysfunction, ROS accumulation, and activation of the intrinsic apoptotic pathway.</p><p><strong>Conclusion: </strong>Our study identifies CHCHD3 as a mitochondrial protein upregulated in lung cancer that contributes to tumor cell proliferation and survival.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-06-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148203270","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":"Immunohistochemical Evaluation of PD-L1 Expression in Complex Atypical Hyperplasia and Early-Stage Endometrial Cancer.","authors":"Levent Akman, Mert Acar, Gurdeniz Serin, Lena Tureyici, Nuri Yildirim, Osman Zekioglu, Burcak Karaca, Mustafa Cosan Terek","doi":"10.2174/0118715206478683260521063609","DOIUrl":"https://doi.org/10.2174/0118715206478683260521063609","url":null,"abstract":"<p><strong>Introduction: </strong>The study aims to evaluate programmed cell death ligand-1 (PD-L1) expression in complex atypical hyperplasia and early-stage endometrial cancer and to assess its association with tumor grade.</p><p><strong>Materials and methods: </strong>This retrospective study was conducted at a single tertiary university hospital and included hysterectomy specimens obtained between 2010 and 2020. A total of 80 cases were analyzed: 20 with complex atypical hyperplasia and 60 with Stage IA endometrioid endometrial cancer, comprising 20 Grade 1, 20 Grade 2, and 20 Grade 3 tumors. All specimens underwent immunohistochemical staining with the PD-L1 (22C3) antibody, and PD-L1 expression was assessed using the combined positive score.</p><p><strong>Results: </strong>PD-L1 expression was absent in complex atypical hyperplasia but present in 4 of 20 Grade 1 cases (20%), 6 of 20 Grade 2 cases (30%), and 16 of 20 Grade 3 cases (80%). PD-L1 positivity increased significantly with higher tumor grade (p < 0.001). No significant associations were identified between PD-L1 expression and patient age, tumor diameter, depth of myometrial invasion, endometrial confinement, or lymphovascular invasion.</p><p><strong>Discussion: </strong>PD-L1 expression appears to be detectable in early-stage endometrioid endometrial cancer and may increase with tumor grade, suggesting early immune checkpoint activity.</p><p><strong>Conclusion: </strong>PD-L1 expression may be associated with tumor grade in early-stage endometrioid endometrial cancer. However, its clinical significance remains unclear. These findings may be relevant in the context of fertility- preserving management and require further investigation.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-06-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148203916","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":"Marine-Derived Dual BTK-FGFR Inhibitors: Pioneering a New Era of Precision Oncology Therapeutics.","authors":"Sonam Kundral, Anoop Kumar, Puneet Gupta, Ramesh Bodla, Dharmendra Kumar","doi":"10.2174/0118715206464059260420095736","DOIUrl":"https://doi.org/10.2174/0118715206464059260420095736","url":null,"abstract":"<p><strong>Introduction: </strong>The secondary metabolites produced under the extreme and competitive conditions in the ocean represent a rich and varied source of structurally diverse and biologically active compounds, which have tremendous therapeutic potential. Among others, marine invertebrates continue to yield numerous MNPs with notable anticancer properties. Most of these compounds remain an underexplored reservoir for novel drug discovery.</p><p><strong>Methods: </strong>This study covers indepth literature study (2015-2025) on Marine-Derived Dual BTK-FGFR Inhibitors. Relevant studies were retrieved from databases including ScienceDirect, PubMed, and Google Scholar. Closely related 110 studies on Marine-Derived Dual BTK-FGFR Inhibitors were included, while unrelated works were excluded.</p><p><strong>Results: </strong>Marine-derived compounds with functional groups, including peptides, terpenoids, alkaloids, and polyketides, have also been shown to inhibit the BTK/FGFR pathway. Several compounds are currently in the preclinical or early-phase of clinical development and show cytotoxicity against multiple cancer cell lines. Computational simulations have predicted bioactivity, refined the model of molecular interactions, and assisted in identifying scaffolds for use in the development of targeted therapies.</p><p><strong>Discussion: </strong>The marine-derived metabolites display unusual chemical scaffold structures that modify BTK and FGFR activity in a very effective manner and decrease the growth of cancer cells. They were selected as potential lead candidates for precision oncology therapies based on computational analyses and newly developing evidence supporting their efficacy as kinase inhibitors.</p><p><strong>Conclusion: </strong>Marine invertebrates may provide an exciting source for developing anticancer therapies, as their metabolites are selective modifiers of the BTK and FGFR pathways. Furthermore, when coupled with computational approaches, the integration of marine pharmacology can expedite the identification of strong marinebased therapeutic agents.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-06-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148203944","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":"Synergistic Anticancer and Antibacterial Activities of Marine Sponge Extracts Combined with Fungal-Synthesized Silver Nanoparticles from Aspergillus flavus.","authors":"Moath Alqaraleh, Ali Al-Samydai, Simone Carradori, Khaled M Khleifat, Belal O Al-Najjar, Salameh Alqaraleh, Jehad F Alhmoud, Futoon Abedrabbu Al-Rawashde","doi":"10.2174/0118715206391677250818074408","DOIUrl":"https://doi.org/10.2174/0118715206391677250818074408","url":null,"abstract":"<p><strong>Introduction: </strong>This study explores the cytotoxic efficacy of combining Dysidea tuapokere or Agelas conifera extract with silver nanoparticles (AgNPs) synthesized from Aspergillus flavus on various cancer cell lines and pathogenic bacteria.</p><p><strong>Methods: </strong>AgNPs were characterized using zeta potential, dynamic light scattering, and scanning electron microscopy. The chemical composition of the marine sponge extracts was analyzed using LC-MS/MS. Cancer cell lines (PANC-1, A549, MCF-7, and HT-29) and normal HUVEC cells were tested for cytotoxicity using MTT assays to calculate selectivity indices (SI). Antibacterial activity was assessed against antibiotic-resistant strains. Docking studies were conducted to investigate the binding of sponge-derived compounds to EGFR and TrkA receptors.</p><p><strong>Results: </strong>Characterization of AgNPs revealed a mean particle size of 69.455 nm, a zeta potential of -28 mV, and a polydispersity index (PDI) of 0.177. After lyophilization, the particle size increased to 144.555 nm and the PDI to 0.335. SEM showed silver particles below 0.5 μm. Combining Dysidea tuapokere or Agelas conifera extracts with AgNPs enhanced antiproliferative activity. This activity was relatively selective for cancer cells over HUVEC cells, particularly for PANC-1 (SI: 254.74) and A549 (SI: 204.85). LC-MS/MS identified bioactive components. Docking showed favorable binding to EGFR and TrkA. Dysidea tuapokere extract with AgNPs significantly enhanced the inhibition of S. xylosus, K. oxytoca, and P. aeruginosa.</p><p><strong>Discussion: </strong>The synergistic antiproliferative effect selectively targets cancer cells. The combined treatment may have broad-spectrum bioactivity.</p><p><strong>Conclusion: </strong>This study highlights the synergistic potential of marine sponge extracts combined with AgNPs.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-05-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148136591","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":"Design and Development of Chitosan-Based Nanocomposite Films Enriched with Tailored AgNPs Derived from Cassia fistula Flower Extract for Biotherapeutic Applications.","authors":"Shivanjali Esther Arland, Jyotsna Kumar","doi":"10.2174/0118715206394506260219214624","DOIUrl":"https://doi.org/10.2174/0118715206394506260219214624","url":null,"abstract":"<p><strong>Introduction: </strong>Chitosan (CS) is a natural biopolymer widely appreciated for its versatile biological attributes, such as biocompatibility and biodegradability, making it an alternative for biomedical applications. The recent trend in nanotechnology has led to the development of CS based composite biomaterials by incorporating the phytochemicals and biosynthesized silver nanoparticles (AgnPs). These modifications to the CS backbone broaden its biomedical applications.</p><p><strong>Methods: </strong>The CS embedded nanocomposite film (CS_CFF_AgNPs) was developed via the incorporation of silver nanoparticles (AgNPs) derived from Cassia fistula flower extracts. The developed nanofilm was characterized using multiple analytical techniques. Different parameters of physicochemical properties were studied. The films underwent in vitro biological assays of antioxidant potential via DPPH, and antimicrobial efficacy via agar well diffusion method. Additionally, cytotoxicity and scratch assays were performed to determine its woundhealing capabilities.</p><p><strong>Results: </strong>The CS_CFF_AgNPs nanocomposite film exhibited distinct, well-defined physicochemical properties and biotherapeutic activity. FTIR, XRD, and TGA techniques confirmed its successful fabrication, and enhanced antioxidant activity and notable antibacterial efficacy were observed. Cytotoxicity and scratch assays revealed high cell viability and accelerated cell migration, supporting its regenerative potential.</p><p><strong>Discussion: </strong>The improved therapeutic activity of the developed CS_CFF_AgNPs nanocomposite is likely due to the synergistic effects of CS, CFF phytochemicals and biogenic AgNPs, as evidenced by improved DPPH and ZOI along with accelerated wound healing.</p><p><strong>Conclusion: </strong>Overall, this study displays the promising potential of the CS_CFF_AgNPs nanocomposite as a sustainable and effective functional biomaterial. The observed enhanced antioxidant, antimicrobial, and woundhealing properties supports its viable candidature for advanced biomedical applications, especially in regenerative medicine and infection management.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148142540","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":"Pyruvate Kinase M2 in Glioblastoma: A Dual Role in Tumor Metabolism and Nuclear Regulation with Therapeutic and Medicinal Chemistry Insights.","authors":"Rahul Kumar, Prem Shankar Mishra, Sakshi Patel","doi":"10.2174/0118715206458405260508040647","DOIUrl":"https://doi.org/10.2174/0118715206458405260508040647","url":null,"abstract":"<p><strong>Introduction: </strong>Glioblastoma (GBM) is a high-grade primary brain tumor with a high proliferation rate, metabolic reprogramming, and unresponsiveness to existing therapeutic interventions. One of the most important glycolytic enzymes is pyruvate kinase M2 (PKM2), which plays two roles in GBM: controlling tumor metabolism and nuclear gene expression. The complexity of PKM2 functions is important in the formulation of effective targeted treatments against GBM.</p><p><strong>Methods: </strong>A comprehensive search of electronic databases such as PubMed, Scopus, Web of Science, and Google Scholar was conducted from inception until 2025. The keywords used were PKM2, glioblastoma, cancer metabolism, and therapeutic targeting. The screening and selection of studies were based on their relevance to the molecular biology of PKM2, its metabolic and nuclear functions, and GBM therapeutic approaches.</p><p><strong>Results: </strong>The outcomes show that PKM2 enhances the Warburg effect in GBM, maintaining glycolytic flux and biosynthetic pathways that support tumor growth under hypoxic conditions. Moreover, PKM2 is associated with proliferation-, stemness-, and immune-evasion-related gene expression. Small-molecule activators and inhibitors, RNA-based therapies, and advanced drug-delivery systems that bypass the blood-brain barrier are therapeutic approaches for targeting PKM2. Medicinal chemistry initiatives have optimized PKM2 modulators, but challenges remain regarding isoform selectivity and effective brain penetration.</p><p><strong>Discussion: </strong>The discussion of PKM2 reveals that it has both metabolic and nuclear functions, making it a promising therapeutic target. However, the difficulties in specific targeting and delivery require combined solutions using molecular, pharmacological, and nanotechnological methods.</p><p><strong>Conclusion: </strong>In general, the bifunctional metabolic and nuclear characteristics of PKM2 indicate its relevance as a therapeutic target in glioblastoma, suggesting that combined approaches are needed to support clinical translation.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148142462","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}