Current pharmaceutical design最新文献

{"title":"Anti-hypertensive Function of Plant-derived Bioactive Peptides: A Review.","authors":"Monalisa Gochhi, Priyanka Dash, Biswakanth Kar, Deepak Pradhan, Jitu Halder, Chandan Das, Vineet Kumar Rai, Saroj Kumar Rout, Goutam Ghosh, Goutam Rath","doi":"10.2174/0113816128386781250415105515","DOIUrl":"https://doi.org/10.2174/0113816128386781250415105515","url":null,"abstract":"<p><p>Hypertension is considered to be a crucial factor in the development of chronic diseases like obesity, diabetes, and Cardiovascular Disease (CVD). Several conventional medications are frequently used to manage hypertension. However, they have certain adverse effects that limit their use. Therefore, alternative medications, including bioactive peptides, could be valuable in managing CVD because they are safer, less expensive, and more effective. In light of this, this article aimed to explore the potential application of plantderived peptides for their efficient role in ameliorating hypertension. In particular, the authors summarise the current understanding of the anti-hypertensive function of plant-derived bioactive peptides, focusing on the source, isolation technique, purification process, and potential CVD applications. The potential antihypertensive peptides are highlighted in particular, and their molecular mechanisms, such as ACE inhibition, renin inhibition, and CCB blockers, are highlighted in terms of in vitro, in vivo, and in-silico models. Recent literature evidence revealed that plant peptides with low molecular weight show better potential for inhibiting ACE and renin. Moreover, the molecular structure, solubility, and types of amino acids play an important role in determining antihypertensive activity. This review will improve the understanding of plant-derived bioactive peptides and provide some constructive inspiration for further research and industrial application in cardiovascular disorders.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143988888","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 MicroRNAs, CircRNAs, and LncRNAs in Chronic Lymphocytic Leukemia.","authors":"Nan Chen, Yaping Zhang, Yongning Jiang, Guangcan Gao, Jianyong Li, Wenyu Shi","doi":"10.2174/0113816128361848250401200001","DOIUrl":"https://doi.org/10.2174/0113816128361848250401200001","url":null,"abstract":"<p><p>Chronic lymphocytic leukemia (CLL) constitutes a heterogeneous hematological malignancy, often correlated with disruptions in various signaling pathways, chromosomal deletions, and gene mutations. A comprehensive grasp of CLL pathogenesis and its associated risk factors remains vital for the development of more efficacious treatment strategies. Although non-coding RNAs (ncRNAs) do not encode proteins, they possess substantial regulatory influence over target genes. These ncRNAs govern a multitude of target genes implicated in the pathogenesis of CLL. Furthermore, some ncRNAs serve as prognostic markers in CLL and might contribute to overcoming chemotherapy resistance. This review determines the association between ncRNAs and the molecular mechanisms driving the onset and advancement of CLL, with particular emphasis on the roles of these ncRNAs in modulating signaling pathways, encompassing NF-κB/PI3K-AKT/TNF and P53 in CLL. It also underscores their relevance as significant biomarkers and their potential as therapeutic targets in clinical CLL settings.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143972321","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":"Nano Selenium: A Promising Solution for Infectious Diseases - Current Status and Future Prospects.","authors":"Shaheen Husain, Rania Mohammad Sabri Sultan, Kirti Saxena, Fareha Bano, Rajat Goyal, Shivani Chopra, Hitesh Chopra, Suresh K Verma","doi":"10.2174/0113816128346637250401090138","DOIUrl":"https://doi.org/10.2174/0113816128346637250401090138","url":null,"abstract":"<p><strong>Background: </strong>Due to increasing antibiotic resistance, researchers are investigating the medicinal potential of nanoparticles, particularly their antibacterial and antiviral properties. Among other things, this concern mandates the journey for novel and more potent antibacterial drugs. The crucial role of nanoparticles in the treatment of various microbial diseases has been demonstrated in several research studies.</p><p><strong>Aim & objective: </strong>This study focuses on the role of Selenium nanoparticles (SeNPs) against infectious diseases, with an emphasis on exploring their probable mechanisms of action.</p><p><strong>Methodology: </strong>Nanoparticles have been exploited as delivery mechanisms and broad-spectrum inhibitors in viral and microbial studies. Their significant therapeutic potential stems from their high surface area to volume ratio, which enables diverse applications. Various materials have been employed in the synthesis of nanoparticles, each tailored to meet specific therapeutic requirements. The unique combination of biological relevance, environmental friendliness, and versatile applications makes SeNPs a promising alternative to other nanoparticles in various fields.</p><p><strong>Results: </strong>The therapeutic potential of nanoparticles, especially Selenium nanoparticles (SeNPs), is significant and warrants further exploration. They have shown promise as delivery agents and potent materials for combating infectious diseases, making them a valuable asset in the fight against antibiotic resistance.</p><p><strong>Conclusion: </strong>Selenium nanoparticles (SeNPs) are potential biological prospects because of their biocompatibility, bioavailability, and low toxicity. Size, shape, and synthesis affect SeNP uses in biological systems. SeNPs are chemopreventive, anti-inflammatory, and antioxidant medicines that may cure fungal, bacterial, and parasite infections, cancer, and diabetes. They have better absorption, bioavailability, and antibacterial action than micron-size particles. Their large surface area facilitates biological contact and bioactive chemical functionalization. Functionalized SeNPs are less cytotoxic than other seleniums. They prevent DNA oxidation, detoxify heavy metals, and inhibit hydroxyl radicals. In conclusion, selenium nanoparticles have considerable promise for medication delivery, antimicrobials, and cancer and diabetes treatment. They are attractive nanomedicine prospects due to their low toxicity, biocompatibility, and high bioavailability.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143982636","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 killer in disguise: Button battery ingestions in acute care.","authors":"Canan Akman, Ozgur Karcioglu, Göksu Afacan Ozturk, Asli Bahar Ucar","doi":"10.2174/0113816128361865250411045020","DOIUrl":"https://doi.org/10.2174/0113816128361865250411045020","url":null,"abstract":"<p><p>Ingestion of button batteries (BB) represents a substantial health hazard, causing more common and severe complications than most other ingested objects. While the primary mechanism of injury is alkaline caustic injury (mediated by hydroxide ions produced through electrolysis at the site of the button battery), additional pathophysiological processes include pressure-induced necrosis, accumulation of hydroxide compounds at the battery's negative pole, direct caustic tissue injury, and potential heavy metal toxicity. Full-thickness burns, esophageal perforation, tracheoesophageal and aortoesophageal fistulas are encountered shortly after exposure. Vocal cord paralysis due to BB ingestion appears to be an early sign to predict the severity of the condition. Besides expedient removal, mitigation strategies are the key to the management. Pre-BB removal using honey or sucralfate and post-removal sterile acetic acid irrigation in the operation room can alleviate complication rates. This review is intended to cover and summarize all aspects of these incidents to provide information to clinicians and healthcare personnel.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143965270","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":"Nanoemulsion Technology in Oral Drug Delivery: A Path to Enhanced Solubility and Bioavailability.","authors":"Akash Vikal, Rashmi Maurya, Preeti Patel, Balak Das Kurmi","doi":"10.2174/0113816128370159250401012611","DOIUrl":"https://doi.org/10.2174/0113816128370159250401012611","url":null,"abstract":"<p><p>Nanoemulsions (NEs) are submicron-sized colloidal dispersions (20-500 nm) consisting of oil and aqueous phases stabilized by surfactants and cosurfactants. Despite their thermodynamic instability, NEs maintain kinetic stability, preventing separation and aggregation. This stability distinguishes them from microemulsions, which are thermodynamically stable and formed spontaneously. The emulsification process involves a reduction in Gibbs surface free energy facilitated by emulsifiers that lower interfacial tension, crucial for compensating for the high surface area associated with small droplet sizes. The Gibbs free energy reduction is vital as it helps in stabilizing nanoemulsions, while Laplace pressure, resulting from the curvature of the droplets, affects the stability and uniformity of the system. High Laplace pressures in smaller droplets can lead to coalescence, but the proper formulation with suitable surfactants can help mitigate this effect. This review investigates the hypothesis that NEs can significantly enhance the solubility and bioavailability of hydrophobic drugs by optimizing their formulation and stability. We focus on the role of emulsification techniques in creating stable nanoemulsions, with particular attention to the impact of hydrophilic-lipophilic balance (HLB) and critical packing parameters (CPP) on droplet size and stability. Furthermore, we provide a detailed comparison of various preparation methods, including ultrasonication and high-pressure homogenization, emphasizing their influence on droplet size, stability, and scalability. Experimental data from in vitro and in vivo studies illustrate the advantages of NEs for oral drug delivery, with findings showing significant improvements in bioavailability for poorly soluble drugs, such as paclitaxel and curcumin, under optimized formulation conditions. This review highlights the potential of NEs to overcome the limitations of traditional drug delivery systems and provides a roadmap for future research to improve their commercial viability and therapeutic outcomes.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143978053","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":"Phytoestrogens: A Promising Therapeutic Approach for Endometriosis Management, Insights from Preclinical and Clinical Studies.","authors":"Marzieh Neykhonji, Abdulridha Mohammed Al-Asady, Souad Al Okla, Nasser Al-Nazwani, Amir Avan, Majid Khazaei, Seyed Mahdi Hassanian","doi":"10.2174/0113816128364775250326161410","DOIUrl":"https://doi.org/10.2174/0113816128364775250326161410","url":null,"abstract":"<p><strong>Introduction: </strong>Endometriosis is a prevalent gynecological disorder characterized by the growth of endometrial tissue outside the uterine cavity. The disease often involves internal organs and leads to chronic pelvic pain and infertility. While its pathogenesis remains incompletely understood, the disease is considered estrogen-dependent, and reducing estrogen levels is a primary clinical treatment strategy. Despite extensive research and diverse treatment modalities, including surgery and pharmacotherapy, current treatments are associated with significant complications and recurrence. This review aims to explore recent studies on phytoestrogens' therapeutic potential in endometriosis treatment by examining the underlying mechanisms contributing to their efficacy.</p><p><strong>Methods: </strong>An extensive evaluation of Google Scholar and PubMed, utilizing relevant keywords including \"Endometriosis, Phytoestrogen, Estrogen, inflammation, pelvic pain, and Infertility\" was carried out to assess the potential therapeutic efficacy of phytoestrogens in managing endometriosis, based on recent research findings. This review considered a wide range of studies, including in-vitro, in-vivo, and clinical studies, as well as reviews and research articles, to provide a comprehensive overview of the current state of knowledge on this topic.</p><p><strong>Results: </strong>Phytoestrogens, with their structural similarity to estrogen, have emerged as a novel therapeutic approach. These compounds compete for estrogen receptor binding, displaying anti-estrogenic or weak proestrogenic properties upon binding.</p><p><strong>Conclusion: </strong>Exhibiting anti-proliferative, antioxidant, anti-angiogenic, and pro-apoptotic properties, phytoestrogens have demonstrated substantial therapeutic potential in endometriosis management. Extensive cellular, animal, and clinical investigations support their therapeutic efficacy.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-04-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143984784","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 Randomized Comparative Study of Luteolin-Based Herbal Unani Formulations versus Nitrofurantoin in Women with Uncomplicated Urinary Tract Infections.","authors":"Arshiya Sultana, Khaleequr Rahman, Saiyad Shah Alam","doi":"10.2174/0113816128389673250415101004","DOIUrl":"https://doi.org/10.2174/0113816128389673250415101004","url":null,"abstract":"<p><strong>Background: </strong>Urinary tract infection (UTI) is a common infection, particularly among reproductive- age and elderly women. While antibiotics remain the primary treatment, antimicrobial resistance is a growing global concern, necessitating effective non-antibiotic alternatives.</p><p><strong>Objectives: </strong>This study determines the safety and efficacy of herbal formulation compared to nitrofurantoin in treating uncomplicated UTI and its impact on health-related quality of life (HRQoL) in women.</p><p><strong>Methodology: </strong>A randomized, standard-controlled study was conducted involving 66 women diagnosed with uUTI. Participants were randomly assigned to either the Unani Herbal Formulations group (UHF) or the nitrofurantoin group (NG). The UHF group (n=33) received a Unani herbal formulation (3.5 g powder of Cucumis sativus L., Lagenaria siceraria, Portulaca oleracea L., Malva sylvestris L., and Adiantum capillus-veneris L.) along with 25 ml of Viola odorata L. syrup, administered twice daily for 8 days. The NG (n=33) received nitrofurantoin (100 mg) twice daily for 7 days. The primary outcome was the Urinary Tract Infection Symptom Assessment (UTISA) questionnaire. The secondary outcomes were symptom severity, urine dipstick test, urine culture and sensitivity, SF-12 HRQoL survey, and safety evaluation. Standardization, in vitro, and phytochemical analyses of the herbal formulation were also conducted.</p><p><strong>Results: </strong>UTISA scores significantly improved within both groups (p<0.001). The UTISA total score from 14.21 ± 3.43 and 14.18 ± 3.36 was reduced to 3.12 ± 4.65 and 1.61 ± 3.10 in the UHF and NG, respectively, on the 9th day. On the 9th day, 81.81% (UHF) and 87.87% (NG) had negative cultures. HRQoL scores showed significant within-group improvements (p < 0.001), with no significant difference between groups (p > 0.05). No adverse effects were reported. HPLC analysis confirmed the presence of Luteolin, a bioactive antimicrobial metabolite.</p><p><strong>Conclusion: </strong>The herbal formulations were as effective as nitrofurantoin in treating bacterial uUTIs, with no adverse effects and enhanced HRQoL. The presence of Luteolin supports its antimicrobial potential, offering a favourable non-antibiotic alternative for UTI management.</p><p><strong>Trial registration: </strong>The research project is registered at the Clinical Trial Registry of India, ICMR with No: CTRI/2021/09/036138 dated 01/09/2021. The protocol can be retrieved from CTRI.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143969233","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":"Unraveling the Therapeutic Potential of Scutellarin for Clear Cell Renal Cell Carcinoma: A Comprehensive Molecular Analysis.","authors":"Yangyang Bai, Yilin Guo, Ruiting Chen, Jijian Sun, Ranlu Liu","doi":"10.2174/0113816128340451241224055536","DOIUrl":"https://doi.org/10.2174/0113816128340451241224055536","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Background: &lt;/strong&gt;Clear cell renal cell carcinoma (ccRCC), the most common subtype of renal cell carcinoma, is a significant global health issue. Despite advancements in surgery and systemic therapies, drug resistance remains a challenge, and more effective treatments are needed. Scutellarin, a natural flavonoid with anticancer properties, is a promising therapeutic option for ccRCC.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;This present study identified the potential target genes of scutellarin by searching four databases and utilized the TCGA-KIRC and GSE53757 datasets to identify ccRCC features genes. Protein-protein interaction networks and molecular complex detection analyses determined the hub genes through which scutellarin acts on ccRCC. Differential expression, receiver operating characteristic analysis, survival, and immune cell infiltration analyses were conducted successively on these hub genes in tumor and normal tissues to verify their clinical significance. The intracellular mechanism of the hub genes was explored using a single-cell dataset (GSE222703) to elucidate the intracellular pathway through which scutellarin exerts its anti-ccRCC effects. At last, molecular docking and molecular dynamics simulations were performed to confirm the stability of the receptor protein of the hub gene binding to scutellarin.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;158 scutellarin targets were collected and identified through database searches. Analyzing the TCGA-KIRC and GSE53757 data separately identified finally 132 ccRCC feature genes through differential expression analysis and WGCNA. Protein-protein interaction network and molecular complex detection analyses revealed 26 hub genes potentially involved in hinge pathways of scutellarin in ccRCC. Differential expression analysis revealed significant differences in the expression of these hub genes between tumor and normal tissues. Receiver operating characteristic analysis demonstrated the fine diagnostic efficacy of these hub genes. Survival analysis indicated that the hub genes TYMS and CDCA2 were associated with a better prognosis, whereas the remaining hub genes had a poorer prognosis. Enrichment analysis revealed that hub genes mainly involved oxidative stress and cell cycle regulation. Single-cell RNA sequencing analysis suggested that most hub genes exert their effects on T helper cells. Molecular docking results showed stable docking of hub genes with scutellari, except for SPAG5 and ASPM. Molecular dynamics simulations of the most stable docking sites, KIF20A, TYMS, and KIF18B, indicated stable complex formation compared with that of the internal reference protein GAPDH.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;This integrated study provides a comprehensive analysis of the molecular targets and pathways affected by scutellarin in ccRCC. The identified hub genes and their related pathways present exciting prospects for therapeutic intervention and highlight the potential of scutellarin as a novel","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143994022","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 Promising PARP12 Inhibitors through Virtual Screening for Cancer Therapy.","authors":"Sara Seifeldin, Mohd Saeed, Hanan Ali Alatawi, Khalid Alshaghdali, Samra Siddiqui, Amal Abu Sabaa, Hatem Rabie, Ankit Srivastava, Dharmendra Kumar Yadav, Amir Saeed","doi":"10.2174/0113816128369323250322044605","DOIUrl":"https://doi.org/10.2174/0113816128369323250322044605","url":null,"abstract":"<p><strong>Background: </strong>Poly (ADP-ribose) polymerase 12 (PARP12) plays a crucial role in DNA damage response (DDR) through DNA repair, maintaining genomic stability. Mutations in PARP12 contribute to genomic instability, leading to cancer progression. Targeting PARP12 mutants with small molecule inhibitors offers a promising therapeutic strategy.</p><p><strong>Objective: </strong>This study aims to identify potent inhibitors for PARP12 mutants using molecular docking-based virtual screening from the National Cancer Institute (NCI) compound library, followed by molecular dynamics (MD) simulations to validate binding stability.</p><p><strong>Methods: </strong>Homology models of human PARP12 mutants were developed for virtual screening. The topscoring compounds were refined through molecular docking, and their stability was analyzed using allatomistic MD simulations. Binding free energy (MMGBSA) calculations and structural dynamics assessments, including RMSD, RMSF, RoG, and SASA, were conducted to evaluate the drug-receptor interactions.</p><p><strong>Results: </strong>Three promising inhibitors, NCI-32743, NCI-32982, and NCI-659779, demonstrated high binding affinity and stability with PARP12 mutants. These compounds showed significant inhibitory potential, maintaining strong interactions with the target protein throughout the simulation period. ADMET and pharmacokinetic analyses confirmed their drug likeness and potential for further development.</p><p><strong>Conclusion: </strong>The identified inhibitors exhibit strong potential for targeting PARP12 mutants in cancer therapy. Further in vitro and in vivo studies are required to confirm their efficacy and therapeutic viability for clinical applications.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143983344","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":"In Vitro Study on the Antitumor Bioactivity of Anderson-Type Polyoxometalates.","authors":"Chenguang Yao, Ting Tan, Jiangning Yan, Zijia Zhao, Romina Onintsoa Diarimalala, Junjie Wang, William Wang, Hanluo Li, Jingbiao Liu, Yanhong Wei, Kanghong Hu","doi":"10.2174/0113816128367617250323075703","DOIUrl":"https://doi.org/10.2174/0113816128367617250323075703","url":null,"abstract":"<p><strong>Objective: </strong>To develop new Anderson-type polyoxometalates (POMs) with high efficiency and low cytotoxicity, and investigate the effects and mechanisms against lung (A549), cervical (Hela), and breast cancer (MCF7) cell lines.</p><p><strong>Methods: </strong>Cytotoxicity assessments on Hela, A549, and MCF-7 tumor cells were tested by MTT assay. Antitumor activities of B1 (vanadium-centered, methyl-modified) and B7 (vanadium-centered, hydroxylmodified) were detected by apoptosis, scratch, and colony formation assay. The antitumor molecular mechanisms were explored by western blotting.</p><p><strong>Results: </strong>This study synthesized and evaluated twelve Anderson-type compounds which were centered with vanadium, chromium, iron, cobalt, nickel, and copper heteroatoms, modified with methyl and hydroxyl at the side chains. Cytotoxicity assessments revealed that compounds B1 and B7 exhibited superior efficacy, with IC50 values of approximately 7 μmol/L of three cell lines. B1 and B7 inhibited proliferation and migration in these cell lines and induced apoptosis in MCF7 and A549 cells. Mechanistic investigations indicated that B1 induces apoptosis in MCF7 cells by inhibiting the AKT signaling pathway and downregulating the expression of apoptosis-related proteins Bcl-2 and Caspase-9.</p><p><strong>Conclusion: </strong>Novel Anderson-type POMs B1 (vanadium-centered, methyl-modified) and B7 (vanadiumcentered, hydroxyl-modified) exhibited superior efficacy against tumor cells and induced apoptosis via PI3K/ AKT pathway, which provides new theoretical avenues for developing POM-mediated antitumor chemotherapeutic medications.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-04-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143957487","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}