Current pharmaceutical design最新文献

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The Association between Albumin, Globulin, Albumin-to-globulin Ratio, and Frailty in Middle-aged and Older Adults: Evidence from NHANES 2013-2014. 中老年人白蛋白、球蛋白、白蛋白/球蛋白比值与虚弱之间的关系:来自NHANES 2013-2014的证据
IF 2.6 4区 医学
Current pharmaceutical design Pub Date : 2025-05-15 DOI: 10.2174/0113816128362350250423113437
Lixin Sun, Cuie Li, Bin-Bin Feng, Yong-Yong Liu, Ruo-Wei Ma, Yu-Xuan Zhang, Guo-Cui Wu
{"title":"The Association between Albumin, Globulin, Albumin-to-globulin Ratio, and Frailty in Middle-aged and Older Adults: Evidence from NHANES 2013-2014.","authors":"Lixin Sun, Cuie Li, Bin-Bin Feng, Yong-Yong Liu, Ruo-Wei Ma, Yu-Xuan Zhang, Guo-Cui Wu","doi":"10.2174/0113816128362350250423113437","DOIUrl":"https://doi.org/10.2174/0113816128362350250423113437","url":null,"abstract":"<p><strong>Aim: </strong>Inflammation and nutritional status have significant roles in frailty. While albumin and the albumin-to-globulin ratio (AGR) are recognized as inflammatory and nutritional biomarkers, and globulin is associated with inflammation, their relationships with frailty remain underexplored. This study explored the relationships between albumin, globulin, AGR, and frailty among middle-aged and older adults, utilizing data from the National Health and Nutrition Examination Survey (NHANES) database.</p><p><strong>Methods: </strong>The study was a cross-sectional study with participants aged ≥45 years from the 2013-2014 NHANES database. The frailty assessment was based on a 36-item index of frailty constructed in NHANES, excluding nutritional indicators. The relationships between albumin, globulin, AGR, and frailty were analyzed using weighted multivariate regression analyses, smooth curve fitting, two-segment linear regression models, subgroup analyses, and interaction tests.</p><p><strong>Results: </strong>This study involved 1,506 middle-aged and older participants, with a frailty rate of 42.23%. Nonlinear relationships were identified between albumin, AGR, and frailty, while a linear relationship was observed between globulin and frailty. Two-segment linear regression models demonstrated that the inflection points for albumin and AGR were 3.90 and 1.91, respectively. On the left side of these inflection points, albumin and AGR were negatively associated with the prevalence of frailty. On the right side of these inflection points, albumin and AGR were not significantly associated with the prevalence of frailty.</p><p><strong>Conclusion: </strong>This study reveals two threshold effects on frailty in middle-aged and older adults: albumin and AGR. Below specific thresholds, both are linked to reduced frailty risk, but above these levels, neither shows a significant association. Globulin, however, consistently correlates with increased frailty. These findings highlight nonlinear relationships between albumin, AGR, and frailty, suggesting that maintaining optimal levels of these biomarkers may help prevent frailty.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144076584","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}
引用次数: 0
Mendelian Randomization Study on Serum Metabolites and Diabetic Nephropathy Risk: Identifying Potential Biomarkers for Early Intervention. 血清代谢物与糖尿病肾病风险的孟德尔随机研究:确定早期干预的潜在生物标志物。
IF 2.6 4区 医学
Current pharmaceutical design Pub Date : 2025-05-12 DOI: 10.2174/0113816128377862250429045226
Siyuan Song, Jiangyi Yu
{"title":"Mendelian Randomization Study on Serum Metabolites and Diabetic Nephropathy Risk: Identifying Potential Biomarkers for Early Intervention.","authors":"Siyuan Song, Jiangyi Yu","doi":"10.2174/0113816128377862250429045226","DOIUrl":"https://doi.org/10.2174/0113816128377862250429045226","url":null,"abstract":"<p><strong>Objective: </strong>In this study, the causation between serum metabolites and the risk of Diabetic Nephropathy (DN) was investigated by means of a Mendelian Randomization (MR) analysis.</p><p><strong>Method: </strong>Our data on diabetic nephropathy were obtained from the IEU OpenGWAS Project database, while serum metabolite data originated came from the GWAS summary statistics by Chen et al. The Inverse Variance Weighted (IVW) method was the main analysis approach, with Weighted Median (WME) and MREgger regression serving as supplementary approaches to construing the causalities between serum metabolites and the DN risk. In addition to the MR-Egger regression intercept, Cochran's Q test was utilized for sensitivity analysis, with P values used as the metric to assess the results.</p><p><strong>Results: </strong>In total, 14 SNPs regarding serum metabolites were chosen as Instrumental Variables (IVs). The IVW results indicated that levels of Behenoylcarnitine (C22), Arachidoylcarnitine (C20), and the ratio of 5-methylthioadenosine (MTA) to phosphate exerted a positive causal effect on the DN risk. Conversely, levels of 5-hydroxylysine, Butyrylglycine, 1-stearoyl-glycerophosphocholine (18:0), Isobutyrylglycine, 1-stearoyl-2- oleoyl-GPE (18:0/18:1), N2,N5-diacetylornithine, 2-butenoylglycine, 3-hydroxybutyroylglycine, N-acetylisoputreanine, the ratio of Arginine to Ornithine, and the ratio of Aspartate to Mannose exerted a negative impact of causality on the DN risk. By identifying these serum metabolites, high-risk patients can be recognized in the early stages of diabetic nephropathy, enabling preventive measures or delaying its progression. These findings also provide a solid foundation for further research into the underlying etiology of diabetic nephropathy.</p><p><strong>Conclusion: </strong>The translation of serum metabolites into clinical applications for DN aims to utilize changes in serum metabolites as biomarkers for early diagnosis, thereby monitoring the progression of DN and providing a foundation for personalized treatment. For instance, the development of serum metabolite diagnostic kits could be used for early detection and prevention of DN. Changes in metabolites can help identify different stages of DN.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143961696","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}
引用次数: 0
Expanding the Potential of Gene Therapy for Duchenne Muscular Dystrophy. 拓展杜氏肌营养不良症基因治疗的潜力。
IF 2.6 4区 医学
Current pharmaceutical design Pub Date : 2025-05-12 DOI: 10.2174/0113816128386290250507101412
Gyas Khan, Md Sadique Hussain
{"title":"Expanding the Potential of Gene Therapy for Duchenne Muscular Dystrophy.","authors":"Gyas Khan, Md Sadique Hussain","doi":"10.2174/0113816128386290250507101412","DOIUrl":"https://doi.org/10.2174/0113816128386290250507101412","url":null,"abstract":"<p><p>Duchenne muscular dystrophy (DMD) is a severe X-linked neuromuscular disorder caused by mutations in the DMD gene, leading to progressive muscle degeneration, loss of ambulation, cardiomyopathy, and early mortality. While advances in multidisciplinary care and pharmacological interventions, including corticosteroids and exon-skipping therapies, have improved patient outcomes, current treatments primarily provide symptomatic relief without addressing the underlying genetic defect. Gene therapy has emerged as a promising approach to modify disease progression, particularly through the use of adeno-associated virus (AAV)-mediated delivery of micro-dystrophin constructs. These truncated genes retain essential functional domains, enabling the restoration of dystrophin expression within the packaging limits of AAV vectors. Early-phase clinical trials have demonstrated encouraging safety profiles and transgene expression; however, challenges such as immune responses, variability in functional improvement, and long-term durability remain. Recent innovations, including optimized AAV capsids, immunomodulatory strategies, and genome editing technologies like CRISPR-Cas9, are actively being explored to overcome these barriers. Additionally, scalable vector manufacturing and the integration of real-world data are essential for broader clinical translation. This review synthesizes current advancements, clinical milestones, and future directions in gene therapy for DMD, emphasizing the need for precise dosing, long-term efficacy, and equitable access to fully realize the therapeutic potential of these evolving strategies.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144062589","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}
引用次数: 0
Analysis of Factors Influencing Cardiovascular Events and Mortality in Patients on Dialysis after Parathyroidectomy. 甲状旁腺切除术后透析患者心血管事件及死亡率的影响因素分析。
IF 2.6 4区 医学
Current pharmaceutical design Pub Date : 2025-05-12 DOI: 10.2174/0113816128390373250507062606
Taohong Yang, Yang Xue, Jianping Ren, XinYu Li, Wenting Xu, Guangyang Nie, Deguang Wang, Xuerong Wang
{"title":"Analysis of Factors Influencing Cardiovascular Events and Mortality in Patients on Dialysis after Parathyroidectomy.","authors":"Taohong Yang, Yang Xue, Jianping Ren, XinYu Li, Wenting Xu, Guangyang Nie, Deguang Wang, Xuerong Wang","doi":"10.2174/0113816128390373250507062606","DOIUrl":"https://doi.org/10.2174/0113816128390373250507062606","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Background: &lt;/strong&gt;Renal secondary hyperparathyroidism (SHPT) represents a prevalent complication among dialysis patients, significantly impacting long-term prognosis. Parathyroidectomy (PTX) serves as a clinically effective therapeutic option for patients diagnosed with refractory secondary hyperparathyroidism.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Objective: &lt;/strong&gt;This study aims to assess the impact of PTX on cardiovascular events (CVEs) and all-cause mortality in dialysis patients, as well as to analyze the incidence and potential determinants of postoperative cardiovascular events and all-cause mortality.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Methods: &lt;/strong&gt;We collected data on 710 patients with renal secondary hyperparathyroidism who were treated with PTX between February 2011 and April 2019. A total of 633 patients who underwent PTX were finally included and matched with 462 patients who did not undergo PTX on a 1:1 basis according to age and follow-up duration. Ultimately, 179 pairs were successfully matched to investigate the differences in all-cause mortality and CVEs. The Logistic/Cox regression analyses were employed to identify independent factors associated with adverse CVEs and all-cause mortality among patients receiving PTX. Nomogram prediction models were constructed based on independent influencing factors.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;Among 633 patients who underwent PTX, 117 (18.5%) died and 192 (30.3%) experienced CVEs during median 5-year follow-up. No significant differences in cardiovascular/death events were observed between matched groups. In patients who underwent PTX, the logistic regression analysis revealed that age and history of diabetes mellitus were independent risk factors for CVEs. The pre-operative use of cinacalcet and/or calcitriol was associated with a reduced risk of CVEs. With respect to preoperative and postoperative calcium levels, the highest tertile was identified as a risk factor when compared with the lowest tertile. Cox regression showed age, diabetes history, and highest preoperative phosphorus tertile negatively correlated with survival, while albumin (ALB) was positively correlated. The predictive nomogram model had an area under the receiver operating characteristic (ROC) curve of 0.649 for CVE prediction. The areas under the ROC curve for predicting 3-, 5-, and 10-year mortality prediction were 0.865, 0.865, and 0.953, respectively.&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Conclusion: &lt;/strong&gt;PTX does not reduce the incidence of cardiovascular events and mortality in patients on maintenance dialysis. In patients who underwent PTX, older age, a history of diabetes mellitus, and higher preoperative calcium/postoperative calcium levels were independent risk factors for adverse CVEs; preoperative use of cinacalcet and/or calcitriol was a protective risk for CVEs. Older age, a history of diabetes mellitus, lower ALB levels, and hyperphosphatemia were independent risk factors for all-cause mortality following PTX. These predictive models may assist ","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143984816","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}
引用次数: 0
Artificial Intelligence in Medicine and Imaging Applications. 人工智能在医学和成像中的应用。
IF 2.6 4区 医学
Current pharmaceutical design Pub Date : 2025-05-09 DOI: 10.2174/0113816128381171250415171256
Kuldeep Rajpoot
{"title":"Artificial Intelligence in Medicine and Imaging Applications.","authors":"Kuldeep Rajpoot","doi":"10.2174/0113816128381171250415171256","DOIUrl":"https://doi.org/10.2174/0113816128381171250415171256","url":null,"abstract":"<p><p>Artificial intelligence (AI) can completely transform drug development methods by delivering faster, more accurate, efficient results. However, the effective use of AI requires the accessibility of data of excellent quality, the resolution of ethical dilemmas, and an awareness of the drawbacks of AI-based techniques. Moreover, the application of AI in drug discovery is gaining popularity as an alternative to both the complex and time-consuming process of discovering as well as developing novel medications. Importantly, machine learning (ML) as well as natural language processing, for example, may boost both productivity as well as accuracy by analyzing vast volumes of data. This review article discusses in detail the promise of AI in drug discovery as well as offers insights into various topics such as societal issues related to the application of AI in medicine (e.g., legislation, interpretability and explainability, privacy and anonymity, and ethics and fairness), the importance of AI in the development of drug delivery systems, causability and explainability of AI in medicine, and opportunities and challenges for AI in clinical adoption, threat or opportunity of AI in medical imaging, the missing pieces of AI in medicine, approval of AI and ML-based medical devices.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143961620","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}
引用次数: 0
Binding Interaction and Stability Analysis of Quercetin and its Derivatives as Potential Inhibitors of Triple Negative Breast Cancer (TNBC) against PARP1 Protein: An in-silico Study. 槲皮素及其衍生物作为三阴性乳腺癌(TNBC)对PARP1蛋白的潜在抑制剂的结合相互作用和稳定性分析:一项硅研究。
IF 2.6 4区 医学
Current pharmaceutical design Pub Date : 2025-05-09 DOI: 10.2174/0113816128373506250414160220
Md Alfaz Hossain, Fahmida Mariam Fariha, Md Arju Hossain, Md Reduanul Haque Kavey, Md Shamim, Md Mobinul Hoque, Ali Mohamod Wasaf Hasan, Md Ataur Rahman, Abdel Halim Harrath, Md Habibur Rahman
{"title":"Binding Interaction and Stability Analysis of Quercetin and its Derivatives as Potential Inhibitors of Triple Negative Breast Cancer (TNBC) against PARP1 Protein: An in-silico Study.","authors":"Md Alfaz Hossain, Fahmida Mariam Fariha, Md Arju Hossain, Md Reduanul Haque Kavey, Md Shamim, Md Mobinul Hoque, Ali Mohamod Wasaf Hasan, Md Ataur Rahman, Abdel Halim Harrath, Md Habibur Rahman","doi":"10.2174/0113816128373506250414160220","DOIUrl":"https://doi.org/10.2174/0113816128373506250414160220","url":null,"abstract":"<p><strong>Background: </strong>Triple-negative breast cancer (TNBC) is an aggressive subtype characterized by the absence of estrogen and progesterone receptors (ER, PR) and low or absent HER2 expression, limiting treatment options. Quercetin, a flavonoid with anti-cancer properties, has the potential to be a therapeutic intervention.</p><p><strong>Objectives: </strong>The study aimed to explore the potential of Quercetin derivatives as therapeutic agents for TNBC using several computational methods.</p><p><strong>Methods: </strong>The study utilized PASS prediction, molecular docking, ADMET prediction, QSAR models, MD simulations, binding free energy, and DFT calculations to evaluate the efficacy of quercetin derivatives.</p><p><strong>Results: </strong>ADMET analysis confirmed the solubility, non-carcinogenicity, and low toxicity of four quercetin derivatives: LM01, LM02, LM05, and LM10. These derivatives exhibited strong binding affinity against TNBC protein PPAR1, with binding energies of -10.6, -10.7, -11.4, and -10 kcal/mol, respectively. MD simulations confirmed their stability, with consistent RMSD values and favorable RMSF values. Post-simulation calculations and reduced HOMO-LUMO energy gaps further supported their potential as promising candidates.</p><p><strong>Conclusion: </strong>Our computational findings suggest that quercetin derivatives, particularly LM01, LM02, and LM10, exhibit strong stability and binding affinity, positioning them as promising candidates for TNBC treatment. Further experimental validation is required to confirm their therapeutic potential.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144062586","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}
引用次数: 0
Emerging Trends in the Pharmacological and Therapeutic Potential of Ginger: From Traditional Medicine to Nanotechnological Innovations. 生姜药理和治疗潜力的新趋势:从传统医学到纳米技术创新。
IF 2.6 4区 医学
Current pharmaceutical design Pub Date : 2025-05-08 DOI: 10.2174/0113816128372023250324050304
Jitendra Gupta, Devesh Kumar, Reena Gupta, Sumant Kumar, Mohit Kumar
{"title":"Emerging Trends in the Pharmacological and Therapeutic Potential of Ginger: From Traditional Medicine to Nanotechnological Innovations.","authors":"Jitendra Gupta, Devesh Kumar, Reena Gupta, Sumant Kumar, Mohit Kumar","doi":"10.2174/0113816128372023250324050304","DOIUrl":"https://doi.org/10.2174/0113816128372023250324050304","url":null,"abstract":"<p><strong>Introduction: </strong>Ginger (Zingiber officinale) has a long history as a culinary and medicinal plant, widely recognized in traditional medicine for the treatment of various diseases. In recent years, advances in nanotechnology have provided innovative delivery systems, enhancing ginger's bioavailability and efficacy in modern therapeutic applications. This study aims to explore ginger's pharmacological and therapeutic potential, tracing its evolution from traditional medicine to its integration into modern nanotechnological innovations. By analysing emerging trends, this study seeks to highlight ginger's diverse bioactivities and its potential to enhance therapeutic efficacy through advanced delivery systems.</p><p><strong>Methods: </strong>Literature was searched from various databases, mainly from 1984 to 2024, such as Scopus, Web of Science, Google Scholar, PubMed and Science Direct using keywords including \"Ginger\", \"Zingiber officinale\", \"Gingerols\", \"Shogaols\", \"Paradols\" and \"Nanocarriers\" and their combination. This study examines the therapeutic potential of ginger by reviewing its traditional applications and exploring nanotechnological innovations in ginger-based drug delivery systems. Nanoemulsions, liposomes, and nanoparticles were assessed for their ability to improve the stability, bioavailability, and targeted delivery of ginger's bioactive compounds.</p><p><strong>Results: </strong>Ginger's bioactive constituents, including gingerols, shogaols, and paradols, exhibited significant pharmacological activities, including anti-inflammatory, antioxidant, anticancer, antidiabetic, and gastroprotective effects. Nano-based delivery systems have shown improved stability, controlled release, and targeted delivery, thereby maximising therapeutic efficacy in treating various diseases.</p><p><strong>Conclusion: </strong>Ginger holds significant therapeutic promise in both traditional and modern medicine, mainly when used with nanotechnology for improved bioavailability and efficacy. These findings support the development of ginger-based treatments as complementary therapies in holistic healthcare. Further research and clinical trials are essential to validate these applications and optimize dosages for clinical use.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143967675","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}
引用次数: 0
Synthesis and Structural Characterization of Ferrocenyl Carboxylate Containing Benzaldoxime Moieties and Preliminary Cytotoxicity against Cancer Cell Lines. 含苯甲醛肟的二茂铁羧酸酯的合成、结构表征及对癌细胞的初步细胞毒性研究。
IF 2.6 4区 医学
Current pharmaceutical design Pub Date : 2025-05-08 DOI: 10.2174/0113816128391868250430081054
Zhipeng Ruan, Jianping Yong, Le Li, Canzhong Lu, Olagoke Zacchaeus Olatunde
{"title":"Synthesis and Structural Characterization of Ferrocenyl Carboxylate Containing Benzaldoxime Moieties and Preliminary Cytotoxicity against Cancer Cell Lines.","authors":"Zhipeng Ruan, Jianping Yong, Le Li, Canzhong Lu, Olagoke Zacchaeus Olatunde","doi":"10.2174/0113816128391868250430081054","DOIUrl":"https://doi.org/10.2174/0113816128391868250430081054","url":null,"abstract":"<p><strong>Aim: </strong>This study aimed to design and synthesize new ferrocene derivatives for the development of potent anticancer drugs.</p><p><strong>Background: </strong>Cancer is a major cause of death globally. Some small-molecule anticancer drugs have been used in clinics for the treatment of cancer, and several candidates are in different phases of clinical trials. However, cancer chemotherapy is still highly inadequate due to the side effects of the clinical drugs. Thus, developing novel anticancer drugs is essential.</p><p><strong>Methods: </strong>Firstly, we synthesized the R-substituted benzaldoxime intermediates (2a-2s) using R-substituted benzaldehyde (1a-1s) and hydroxylamine hydrochloride. Then, the target compounds (3a-3s) were synthesized using ferrocene carboxylic acid and R-substituted benzaldoxime intermediates (2a-2s) using DCC and DMAP as catalysts. The purity of the target compounds was determined by HPLC, and their structures were characterized using NMR, SC-XRD, and HR-ESIMS. Subsequently, the preliminary in vitro cytotoxicity against HeLa, A549, and A2780 cell lines was evaluated using MTT assay.</p><p><strong>Results: </strong>The results showed compound 3a to exhibit cytotoxicity against both HeLa and A549 cancer cell lines with IC50 values of 0.691 and 0.876 mM, respectively. Compound 3k showed potent cytotoxicity against HeLa cell lines with an IC50 value of 0.097 mM, compounds 3n and 3o exhibited potent cytotoxicity against three cancer cell lines, compound 3q showed potent cytotoxicity against HeLa cell lines with an IC50 value of 0.175 mM, while compound 3s exhibited potent cytotoxicity against HeLa and A549 cell lines with IC50 values of 0.470 and 0.298 mM, respectively.</p><p><strong>Conclusion: </strong>In this work, 19 new ferrocene derivatives containing R-substituted benzaldoxime moieties (3a- 3s) were synthesized and their structures were confirmed. Their cytotoxicity against HeLa, A549, and A2780 cell lines was tested, and the results showed that several compounds exhibited potent cytotoxicity against the tested cancer cell lines. This work developed a variety of ferrocene compounds, providing lead compounds based on ferrocene pharmacophore for the development of anticancer drugs.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143994020","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}
引用次数: 0
Development of Satranidazole HCl-Loaded Oral Nanoparticulate Formulation for Colon Targeting and Colon Cancer Therapy Associated with Inflammatory Bowel Disease. 用于结肠靶向和炎症性肠病相关结肠癌治疗的含盐酸沙硝唑口服纳米颗粒制剂的研制
IF 2.6 4区 医学
Current pharmaceutical design Pub Date : 2025-05-07 DOI: 10.2174/0113816128368738250414070421
Debgopal Ganguly, Ananta Choudhury, Subhabrota Majumdar
{"title":"Development of Satranidazole HCl-Loaded Oral Nanoparticulate Formulation for Colon Targeting and Colon Cancer Therapy Associated with Inflammatory Bowel Disease.","authors":"Debgopal Ganguly, Ananta Choudhury, Subhabrota Majumdar","doi":"10.2174/0113816128368738250414070421","DOIUrl":"https://doi.org/10.2174/0113816128368738250414070421","url":null,"abstract":"<p><strong>Background: </strong>Colon-targeted drug delivery is a crucial area of research aimed at treating local disorders like IBD, including ulcerative colitis and Crohn's disease. By delivering drugs directly to the colon, this approach enhances therapeutic efficacy and minimizes systemic toxicity. Nanoparticles are an effective vehicle for controlled drug delivery, improving treatment outcomes for colon-specific diseases.</p><p><strong>Objective: </strong>The study aimed to develop an oral nanoparticulate formulation of Satranidazole (STZ) using a solvent evaporation technique for colonic targeting and characterize its physicochemical properties, compatibility, and in vitro drug release profile.</p><p><strong>Methods: </strong>Using a modified solvent evaporation method, STZ-loaded nanoparticles (STZ-NPs) were formulated using Eudragit RS100 and RL100 polymers. Preformulation studies, including FT-IR and DSC, were performed to confirm the compatibility between the drug and polymers. The nanoparticles were evaluated in terms of entrapment efficiency, particle size, zeta potential, polydispersity index, and in-vitro drug release study.</p><p><strong>Results: </strong>The optimized formulation (F3) demonstrated the highest entrapment efficiency (83.55%) with particle sizes ranging from 107.9 nm to 302 nm and a zeta potential between -34.25 mV and +48.8 mV. In vitro drug release studies showed controlled release over 16 hours, with the optimized batch achieving 95.85% drug release, indicating effective accumulation in the inflamed colon.</p><p><strong>Conclusion: </strong>The Satranidazole-loaded nanoparticles, containing time- and pH-dependent polymers, successfully inhibited premature drug release in acidic environments and provided controlled release at colonic pH. Thus, this delivery system shows promise as an effective treatment for IBD, offering targeted drug release and reduced systemic toxicity.</p>","PeriodicalId":10845,"journal":{"name":"Current pharmaceutical design","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-05-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143978312","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}
引用次数: 0
The Impact of Probiotic Supplementation on the Sleep Quality of Humans: A Review of Results of Randomized, Blinded, Controlled Studies. 补充益生菌对人类睡眠质量的影响:随机、盲法、对照研究结果综述。
IF 2.6 4区 医学
Current pharmaceutical design Pub Date : 2025-05-07 DOI: 10.2174/0113816128370349250413163229
Bhagavathi Sundaram Sivamaruthi, Chaiyavat Chaiyasut, Natarajan Sisubalan, Periyanaina Kesika
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