Anti-cancer agents in medicinal chemistry最新文献

{"title":"Computational Optimization and <i>In silico</i> Analysis for the Discovery of New HER2 and CDK4/6 Drug Candidates for Breast Cancer.","authors":"Salma Elmallah","doi":"10.2174/0118715206382065250507114908","DOIUrl":"10.2174/0118715206382065250507114908","url":null,"abstract":"<p><strong>Background: </strong>Breast cancer is an abnormal cell growth that develops in the breast and spreads throughout the body. Despite cancer being the second leading cause of death, survival rates are increasing as a result of progress in cancer screening and therapy. Breast cancer is the most frequently diagnosed cancer type among women, but in most cases, there are no obvious symptoms. Screening mammograms can be used for early detection of cancer. The size of the tumor and the extent of cancer spread determine the type of needed treatment. There are different forms of treatment, where targeted therapy is generally the least harmful. It targets specific characteristics of cancer cells, such as human epidermal growth factor receptor 2 (HER2). Tyrosine kinase inhibitors are effective targeted treatment of HER2 positive breast cancer. A newer class has emerged, cyclin dependent kinase (CDK4/6), which is used to treat metastatic breast cancer.</p><p><strong>Objectives: </strong>Although CDK4/6 inhibitors class of therapy has revolutionized the treatment of metastatic breast cancer, some patients showed resistance and decreased efficacy. This study is the first to propose innovative computational strategies to improve the effectiveness and pharmacokinetic properties of existing HER2/CDK4/6 inhibitors anti-cancer agents. Through computer-aided drug design, the activity of existing breast cancer drug candidates has been tested. Structural modifications have been applied for in-silico optimization of their biological activity.</p><p><strong>Methods: </strong>In this research, twenty-two analogues of the tested compounds have been proposed. Their biological activity and pharmacokinetic properties (ADMET) have been tested using BIOVIA Discovery Studio software.</p><p><strong>Results: </strong>Out of the designed analogous compounds, seven proposed structures demonstrated superior efficacy compared to the original drugs. The research study docking studies revealed that modifications to lapatinib and tucatinib improved binding affinity to HER2 by 15-25%, with docking scores of -18.34 kcal/mol and -1.04 kcal/mol, respectively. Similarly, CDK4/6 inhibitors exhibited enhanced selectivity, with abemaciclib showing the highest binding energy of -13.2 kcal/mol. ADMET predictions suggested improved solubility and reduced toxicity risks compared to the original drugs.</p><p><strong>Conclusion: </strong>The research study results demonstrate that the synthesis of more lipophilic analogues of lapatinib or tucatinib and, likewise designing of fluorinated derivatives of CDK4/6 inhibitors play a crucial role in improving the efficacy of these anti-cancer agents. These findings highlight the potential of the proposed modifications as promising candidates for further pharmacological and <i>in vitro</i> and <i>in vivo</i> clinical validation.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"77-104"},"PeriodicalIF":3.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144075413","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":"Determination of PD-L1 Expression in Circulating Tumor Cells of Hypopharyngeal and Laryngeal Cancers and Correlation with Tissue Detection.","authors":"Chen Li, Hongyu Zhu, Qin Lin, Wei Chen, Xiaoting Huang, Desheng Wang","doi":"10.2174/0118715206340244250605061005","DOIUrl":"10.2174/0118715206340244250605061005","url":null,"abstract":"<p><strong>Background: </strong>PD-L1 plays a pivotal role as an immunoregulatory checkpoint within the immune system, exerting a critical influence on the internal functioning and survival mechanisms of cancer cells. Our study aimed to elucidate the clinical significance of PD-L1 expression in circulating tumor cells (CTCs) derived from individuals afflicted with Hypopharyngeal and Laryngeal Cancers (HLC).</p><p><strong>Objective: </strong>To verify the relationship between the expression of PD-L1 in CTCs in HLC and the consistency in tissue and the preliminary clinical application.</p><p><strong>Methods: </strong>A laboratory-based experimental study was carried out at Fujian Medical University Union Hospital. CTCs were identified using an immunomagnetic positive sorting methodology. Simultaneous detection was conducted on the CTC levels among PD-L1 positive patients, aiming to ascertain the dynamic relationship between real-time CTC fluctuations and the clinicopathological indices of the patients. This investigation encompassed a cohort of 38 individuals, wherein PD-L1 expression analysis was executed to delineate CTC variations in PD-L1- positive patients.</p><p><strong>Results: </strong>The constructed immunolipid magnetic nano-beads demonstrated pronounced efficacy in capturing CTCs, and the lipid nanoparticles exhibited noteworthy capture efficiency coupled with minimal cytotoxic effects. The assessment of PD-L1 expression consistency between CTCs and tissue specimens revealed a substantial agreement surpassing 70%. Furthermore, inhibition of PD-L1 yielded a significant elevation in the cytokine TNF- α levels, accompanied by a concomitant reduction in IL-10 levels.</p><p><strong>Conclusion: </strong>The CTC sorting system devised in this investigation boasts attributes of remarkable specificity and sensitivity. By virtue of PD-L1 expression analysis, it holds the potential to offer instructive implications for tailoring individualized treatments in clinical scenarios.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"278-288"},"PeriodicalIF":3.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144282033","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":"Phytochemical Profiling and Anticancer Potential of <i>Fagonia cretica</i> L. Extracts on Liver Cancer (HepG2) Cells using <i>In vitro</i> and <i>In silico</i> Approaches.","authors":"Fatima Arshad, Awais Altaf, Ali Raza Arshad, Asia Kiran, Muhammad Sarwar, Sumaira Sharif, Tahir Maqbool, Turki S Abujamel, Absarul Haque, Muhammad Imran Naseer","doi":"10.2174/0118715206377419250527105350","DOIUrl":"10.2174/0118715206377419250527105350","url":null,"abstract":"<p><strong>Background: </strong>Cancer is a complex multifactorial disease charcterized by the progression of genetic and epigenetic changes in human cells. Plant-based derivatives with antioxidant and anticancer properties have been of great interest in treating several human ailments.</p><p><strong>Objective: </strong>This study investigates the in-vitro antioxidative, cytotoxic, and apoptotic activities of different <i>Fagonia cretica L. (F. cretica)</i> leaf extracts.</p><p><strong>Methods: </strong><i>In-vitro</i> DPPH, nitric oxide, superoxide anion, and hydrogen peroxide assays were used to evaluate the antioxidative potential of ethanolic extract of <i>F. cretica</i> (EFC) and hexane extract of <i>F. cretica</i> (HFC). The antiproliferative potential was determined using MTT, crystal violet, and annexin V/PI staining protocols on liver cancer (HepG2) and noncancerous (HEK-293) cell lines. Through <i>in silico</i> analysis, bioactive drug-like phytocompounds identified by GC-MS were evaluated.</p><p><strong>Results: </strong>Higher concentrations of total flavonoid contents (TFCs), total phenolic contents (TPCs), and tannins with strong antioxidant potential were observed in EFC extract as compared to HFC extract. Furthermore, the EFC extract proved to be more cytotoxic with a selective index (SI) of 12.92 than HFC (SI; 5.46) towards experimental cell lines. Moreover, EFC extract showed 82.31% apoptotic induction on HepG2 cells compared to hexane extract and cisplatin (standard drug). From the GC-MS analysis of <i>F. cretica</i>, 32 bioactive compounds were identified from the EFC extract and 21 from the HFC extract. <i>In silico</i> study revealed that 5-(4,5-Dihydro-3Hpyrrol- 2-ylmethylene)-4,4-dimethylpyrrolidine-2-thione showed the highest docking score of -8.9 kcal/mol and - 8.6 kcal/mol against TNF-α and TGF-β, respectively.</p><p><strong>Conclusion: </strong>In conclusion, EFC extract and its bioactive compounds have a scientifically proven role in liver cancer management, but further research is required to validate their therapeutics through clinical trials.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"394-412"},"PeriodicalIF":3.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144214658","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":"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, piperidones, 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":"147-164"},"PeriodicalIF":3.0,"publicationDate":"2026-01-01","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":"Synthesis and Biological Studies of Aurones Derivatives for its Anticancer Potential.","authors":"Kulkarni P Yogesh, Pramod L Ingale","doi":"10.2174/0118715206373750250414155841","DOIUrl":"10.2174/0118715206373750250414155841","url":null,"abstract":"<p><strong>Background: </strong>Aurone based compounds exhibited antioxidant and anti-inflammatory potential and documented for their anticancer potential. The anticancer potential of aurone derivatives AU3, AU4, AU5, AU7, and AU10 is yet to be studied against breast cancer.</p><p><strong>Objective: </strong>The present work was undertaken to evaluate the anticancer potential of aurone based test compounds AU3, AU4, AU5, AU7, and AU10 in breast cancer cell lines MCF-7.</p><p><strong>Methods: </strong>The azaindole based aurones were synthesized by the condensing 4,6-dimethoxybenzofuran-3(2H)-one derivative with various indole aldehydes in the presence of sodium hydroxide. The MCF-7 breast cancer cell line was used to assess the cytotoxic effects of these compounds. Molecular docking studies of the synthesized compounds against the Cyclin-dependent kinase 2 (CDK2)/Cyclin A complex were conducted.</p><p><strong>Results: </strong>Our experimental findings demonstrated that AU3, AU4, AU5, AU7, and AU10 elicited significant effects on MCF-7 by virtue of its minimum cell viability, with IC50 values of 70.14 μM, 87.85 μM, 133.21 μM, 52.79 μM, and 99.55 μM, respectively, thus, exhibits potential anticancer action. Further, to corroborate the anticancer potential, we investigated mechanisms of action through molecular docking studies with the CDK2/Cyclin A complex (PDB: 6GUC) and their findings demonstrated that test compounds showed robust binding through various interactions, including hydrogen bonds, Pi-interactions, and Alkyl bonds with key residues such as Lys129, Asp127, Gln131, and Asp145. Test compounds AU3 and AU7, exhibited better binding affinities and diverse interaction profiles, suggesting a potent disruption of CDK2/Cyclin A activity.</p><p><strong>Conclusion: </strong>Thus, in conclusion, our findings revealed that AU3, AU4, AU5, AU7, and AU10 elicited anticancer action and their effects through CDK2/Cyclin A disruption.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"61-69"},"PeriodicalIF":3.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143958783","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":"Analytical Techniques as Indicators of Biomarkers in Proteomics Cancer Diagnosis.","authors":"Pawan Kumar Goswami, Ranjeet Kumar, Dharmendra Kumar, Shubham Dhiman","doi":"10.2174/0118715206377391250526054417","DOIUrl":"10.2174/0118715206377391250526054417","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Background: &lt;/strong&gt;Cancer is a complex disease marked by changes in the levels and functions of key cellular proteins, including oncogenes and tumor suppressors. Proteomics technology enables the identification of crucial protein targets and signaling pathways involved in cancer cell proliferation and metastasis. Various proteomics techniques have been employed to investigate the molecular mechanisms of cancer, aiding in the confirmation and characterization of heritable disorders.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;A comprehensive literature search was conducted using PubMed, ScienceDirect, and Google Scholar with search terms like \"Cancer and proteomics\" and \"Mass spectrometry in oncology,\" utilizing Boolean operators for refinement. Selection criteria included peer-reviewed articles in English on MS-based biomarker detection, tumor-specific proteins, and drug resistance markers, excluding non-peer-reviewed works and pre-2000 publications unless foundational. Extracted data focused on MS methodologies, biomarker sensitivity, and clinical applications, particularly advances in detecting low-abundance biomarkers and monitoring treatment response. Methodological quality was assessed using PRISMA, evaluating study design, sample size, reproducibility, and statistical analysis. Ethical approval was not required, but adherence to systematic review guidelines and proper citation were ensured.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;In this review, we highlighted the advanced analytical technique for cancer diagnosis and management of cancer, and described the objective of novel cancer biomarkers. Mass spectrometry (MS) is transforming cancer diagnostics and personalized medicine by enabling precise biomarker detection and monitoring. Unlike traditional antibody-based methods, MS provides high-throughput, quantitative analysis of tumor-specific proteins in clinical samples like blood and tissue. Advanced MS techniques improve sensitivity, allowing for the identification of low-abundance biomarkers and tumor-associated proteoforms, including post-translational modifications and drug resistance markers. In research, MS-based proteomics supports multi-center biomarker validation studies with standardized protocols, enhancing reproducibility. The integration of proteomic data with genomic and transcriptomic datasets through proteogenomics is refining precision oncology strategies. These advancements are bridging the gap between research and clinical application, making MS a critical tool for early cancer detection, prognosis, and therapy selection.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;Advancements in technology and analytical techniques have helped to produce more accurate and sensitive cancer-specific biomarkers. These methods are advancing rapidly, and developing high-throughput platforms has yielded great results. However, the substantial variation in protein concentrations makes cancer protein profiling extremely complicated. This shows that more techn","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"186-201"},"PeriodicalIF":3.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144198134","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":"Exploring the Therapeutic Potential of <i>Ocimum sanctum</i> and <i>Phanera variegata</i> in Breast Cancer Treatment: A Promising Natural Approach.","authors":"Tohfa Siddiqui, Md Nasar Mallick, Vikram Sharma","doi":"10.2174/0118715206375507250603074251","DOIUrl":"10.2174/0118715206375507250603074251","url":null,"abstract":"<p><p>Breast cancer is one of the most common malignancies affecting women worldwide. It is a complex, heterogeneous disease, classified into several subtypes, including hormone receptor-positive and triple-negative breast cancer (TNBC), each with distinct therapeutic challenges. TNBC, in particular, is characterized by its aggressive nature and lack of targeted therapies due to the absence of estrogen, progesterone, and HER2 receptors. This review explores the potential of natural plant-based compounds, especially focusing on Clove Basil (Ocimum sanctum) and <i>Phanera variegata</i>, in combating breast cancer. These plants have been traditionally used for their medicinal properties and are now being studied for their anticancer effects. <i>Ocimum sanctum</i> has demonstrated significant antiproliferative and pro-apoptotic effects against breast cancer cells, particularly the MCF-7 line, through mitochondrial pathway activation and gene regulation. Similarly, Phanera variegata exhibits potential through its rich content of flavonoids and other bioactive compounds, which have been shown to induce apoptosis, reduce tumor growth, and offer antioxidant benefits. The review highlights how these plant extracts, with their multiple mechanisms, including immune modulation and direct cytotoxic effects, hold promise as adjunctive or alternative therapies in breast cancer treatment, particularly for hard-to-treat subtypes like TNBC. Continued research into their molecular pathways and therapeutic efficacy could lead to new, less toxic treatment options.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"239-253"},"PeriodicalIF":3.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144282034","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 Role of Kinase Inhibitors in Cancer Neuroscience: Mechanisms, Therapeutic Potential, and Future Directions.","authors":"Manos C Vlasiou","doi":"10.2174/0118715206387712250711132221","DOIUrl":"10.2174/0118715206387712250711132221","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Introduction: &lt;/strong&gt;Cancer progression is increasingly understood to be influenced by neural mechanisms, including neurotransmitter signaling, neurotrophic factor activity, neuroinflammation, and neurogenic inflammation. These neurobiological interactions contribute to tumor proliferation, angiogenesis, and metastasis. Kinase inhibitors, a class of targeted therapies that block dysregulated kinase activity, have demonstrated promise not only in direct tumor suppression but also in modulating neural pathways associated with cancer progression.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;This review examines the role of kinase inhibitors in modulating cancer-associated neural mechanisms. A comprehensive literature search was conducted to identify studies exploring the effects of kinase inhibition on: (1) neurotransmitter signaling pathways; (2) neurotrophic factors such as nerve growth factor (NGF) and brain-derived neurotrophic factor (BDNF); (3) neuroinflammation through glial cell modulation; and (4) neurogenic inflammation. Additionally, we assessed the impact of kinase inhibitors on tumor-induced axonogenesis and stress-related signaling. Clinical relevance was evaluated through analysis of preclinical models, human case studies, and outcomes from relevant clinical trials.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;Kinase inhibitors were found to significantly modulate neural factors that facilitate tumor growth. Specifically, they can suppress neurotrophic signaling (e.g., NGF/TrkA, BDNF/TrkB), inhibit glial activation, reduce pro-inflammatory cytokine production, and block neurotransmitter-induced proliferation. Inhibition of stress-responsive kinases such as p38 MAPK and JNK also disrupted tumor-associated axonogenesis and inflammation. Clinical trials demonstrate improved outcomes in cancers such as glioblastoma, breast cancer, and pancreatic cancer when kinase inhibitors are employed with consideration of neural mechanisms.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Discussion: &lt;/strong&gt;These findings support the emerging concept of targeting the neural tumor microenvironment as a therapeutic strategy. Kinase inhibitors represent a dual-action approach, suppressing both cancer cell intrinsic growth pathways and the neural factors that sustain them. However, several challenges persist, including resistance mechanisms, variability in patient neural profiles, and off-target effects. Future research should focus on the development of neural-specific kinase inhibitors, the use of neural biomarkers for therapy selection, and the integration of neuro-oncology into personalized treatment plans.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;Kinase inhibitors offer a promising frontier in cancer treatment by targeting neural mechanisms that contribute to tumor progression. While current evidence is encouraging, further investigation is required to optimize their use within neuro-oncology. Personalized approaches and novel targets within the neural-cancer axis will be essential for translating thi","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"1-11"},"PeriodicalIF":3.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144688613","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":"Evaluation of Anticancer Potential in Human Colorectal Carcinoma <i>HCT-116</i> Cells by Fungal-Mediated Zinc Oxide Nanoparticles.","authors":"Yaser E Alqurashi, Sami G Almalki, Ibrahim M Ibrahim, Aisha O Mohammed, Amal E Abd El Hady, Mehnaz Kamal, Faria Fatima, Danish Iqbal","doi":"10.2174/0118715206395334250707063019","DOIUrl":"10.2174/0118715206395334250707063019","url":null,"abstract":"<p><strong>Introduction: </strong>Chemotherapy faces limitations such as toxicity and resistance, necessitating novel cancer treatments. Green-synthesized zinc oxide nanoparticles (ZnO-NPs) have attracted attention for their safety, biocompatibility, and therapeutic potential. This study investigates the anticancer efficacy of ZnO-NPs synthesized using the extracellular matrix of <i>Aspergillus biplanus</i> against colorectal cancer cell lines <i>(HCT-116)</i>.</p><p><strong>Methods: </strong>ZnO-NPs were synthesized extracellularly using <i>A. biplanus</i> fungal extract. The nanoparticles were characterized through UV-Vis spectrophotometry, showing an absorbance peak at 375 nm, and scanning electron microscopy (SEM), which determined their morphology and size. The anticancer activity was evaluated in vitro using <i>HCT-116</i> cells. Reactive oxygen species (ROS) generation and mitochondrial membrane potential (MMP) were assessed to understand the mechanism of cytotoxicity. <i>In vivo</i> studies were proposed for further validation.</p><p><strong>Results: </strong>The synthesized ZnO-NPs appeared pale white and exhibited a characteristic absorbance at 375 nm. SEM revealed spherical particles ranging from 35-150 nm. The ZnO-NPs showed strong anticancer activity with an IC₅₀ value of 40.6 μg/mL. ROS levels increased significantly in treated cells, while the MMP decreased to 77.25% compared to 100% in controls.</p><p><strong>Discussion: </strong>ZnO-NPs exerted cytotoxic effects via ROS generation and mitochondrial dysfunction. These results underscore the nanoparticles' ability to induce apoptosis in cancer cells through oxidative stress pathways.</p><p><strong>Conclusion: </strong>Biogenically synthesized ZnO-NPs from A. biplanus show promise as eco-friendly anticancer agents. Further in vivo studies are recommended to confirm their therapeutic potential.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"313-322"},"PeriodicalIF":3.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144999407","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":"Jianpi Yiwei Granules for Chemotherapy-Induced Gastrointestinal Reactions: A Randomized Double-Blind Placebo-Controlled Trial.","authors":"Kerun Cai, Jiayang Chen, Nuo Li, Li Feng","doi":"10.2174/0118715206427314251002153843","DOIUrl":"10.2174/0118715206427314251002153843","url":null,"abstract":"<p><strong>Introduction: </strong>Chemotherapy-induced gastrointestinal reactions are common in non-small cell lung cancer (NSCLC) patients undergoing carboplatin-based chemotherapy. Jianpi Yiwei granules (JPYW), a traditional Chinese medicine (TCM) formula, can alleviate these symptoms.</p><p><strong>Materials and methods: </strong>This multi-center, randomized, double-blind, placebo-controlled trial enrolled 136 NSCLC patients scheduled for carboplatin-based chemotherapy. Participants were randomly assigned to the treatment group (JPYW with standard antiemetic drugs) and the control group (placebo with standard antiemetic drugs). The complete control rate of nausea and vomiting was assessed using the Visual Analog Scale (VAS) and patient diaries. Control of anorexia, bloating, constipation, and quality of life was measured using the Functional Living Index-Emesis scale and the Brief Fatigue Inventory (BFI).</p><p><strong>Results: </strong>The primary objective of this study was to assess the efficacy of JPYW in alleviating non-vomiting digestive symptoms, such as nausea and anorexia, in NSCLC patients receiving carboplatin-based chemotherapy. The secondary objective was to evaluate its effect on improving bloating, constipation, quality of life, and safety.</p><p><strong>Discussion: </strong>Previous studies have shown that Chinese herbs, such as ginger, are effective in treating chemotherapy- induced nausea and vomiting (CINV). JPYW, a multi-component TCM formula, contains active compounds from <i>Codonopsis pilosula</i> and <i>Atractylodes macrocephala</i>. JPYW exerts anti-inflammatory and prokinetic effects that can synergistically regulate gastrointestinal functions. Preliminary observations confirmed the safety of JPYW combined with standard chemotherapy.</p><p><strong>Conclusion: </strong>The current findings contribute to the treatment of adverse reactions to tumor chemotherapy and are expected to improve the quality of life for chemotherapy patients.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"217-224"},"PeriodicalIF":3.0,"publicationDate":"2026-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145328053","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}