Artificial Cells, Nanomedicine, and Biotechnology最新文献

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Epidemiology and potential mechanisms of structural progression in osteoarthritis. 骨关节炎的流行病学和潜在的结构进展机制。
IF 5.6 3区 生物学
Artificial Cells, Nanomedicine, and Biotechnology Pub Date : 2026-12-01 Epub Date: 2026-09-19 DOI: 10.1080/21691401.2026.2724794
Sunita Das, Priyabrata Swain, Subhasmita Swain, R D K Misra, Tapash R Rautray
{"title":"Epidemiology and potential mechanisms of structural progression in osteoarthritis.","authors":"Sunita Das, Priyabrata Swain, Subhasmita Swain, R D K Misra, Tapash R Rautray","doi":"10.1080/21691401.2026.2724794","DOIUrl":"https://doi.org/10.1080/21691401.2026.2724794","url":null,"abstract":"<p><p>There is a critical need to understand the mechanisms that govern structural progression in osteoarthritis. While epidemiological studies have largely identified obesity and joint injury as the dominant factors that contribute to osteoarthritis, recent findings suggest that cellular, molecular and biomechanical factors are responsible for the progression of osteoarthritis. At the tissue level, osteoarthritis involves progressive cartilage degeneration, synovial inflammation, disruption of the extracellular matrix and subchondral bone remodelling. The key pathogenic processes include chondrocyte apoptosis, aberrant autophagy, cellular senescence and functional dysregulation, together with synovial hyperplasia and fibrosis. Genomic studies and Mendelian randomization have identified genetic loci that contribute to osteoarthritis susceptibility and might explain some of the observed heterogeneity in disease phenotypes and progression. Given that there are presently no standard therapies or guidelines to arrest structural progression in osteoarthritis, there is an immediate need to categorize robust biomarkers for initial detection of osteoarthritis and develop rehabilitations that target primary pathogenic pathways. To accomplish this, it is important to integrate epidemiological, genetic and mechanistic data to define osteoarthritis phenotypes, stratifying risk, with the ultimate objective of translating fundamental insights into effective prevention and treatment strategies. The present overview aims to address this aspect of osteoarthritis.</p>","PeriodicalId":8736,"journal":{"name":"Artificial Cells, Nanomedicine, and Biotechnology","volume":"54 1","pages":"781-818"},"PeriodicalIF":5.6,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"149007786","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Engineering nanobodies for drug delivery systems in Alzheimer's disease. 用于阿尔茨海默病药物输送系统的工程纳米体。
IF 5.6 3区 生物学
Artificial Cells, Nanomedicine, and Biotechnology Pub Date : 2026-12-01 Epub Date: 2026-01-22 DOI: 10.1080/21691401.2026.2617707
Thee Jootar, Suradej Hongeng, Wararat Chiangjong
{"title":"Engineering nanobodies for drug delivery systems in Alzheimer's disease.","authors":"Thee Jootar, Suradej Hongeng, Wararat Chiangjong","doi":"10.1080/21691401.2026.2617707","DOIUrl":"10.1080/21691401.2026.2617707","url":null,"abstract":"<p><p>Alzheimer's disease (AD) remains a major global health challenge, with current therapies offering only symptomatic relief. A significant constraint in the development of effective treatments is the blood-brain barrier (BBB), as it greatly limits the access of therapeutic drugs targeting amyloid-β (Aβ) aggregation, tau hyperphosphorylation and neuroinflammation. Nanobodies, single-domain antibody fragments derived from camelids, have emerged as versatile tools with unique properties such as small size, high stability and the ability to penetrate the BBB. Engineered formats allow for specific targeting of Aβ and tau, receptor-mediated transcytosis, and conjugation with therapeutic or diagnostic substances. Preclinical studies show that nanobody-based strategies can reduce pathological burden, attenuate neuroinflammation and improve cognitive outcomes in AD models. Manufacturing scale-up, long-term safety and regulatory validation are among the remaining challenges, yet nanobody engineering represents a viable path to disease-modifying medicines. Innovative approaches, including artificial intelligence-driven design, i.e. 4-1BB agonist nanobodies, and clustered regularly interspaced short palindromic repeat-facilitated diversification of nanobody libraries - such as targeted complementarity-determining region 3 mutagenesis followed by functional screening against disease-relevant tau or Aβ conformers - alongside half-life extension strategies, are commencing to surmount these obstacles and enhance the potential of nanobody platforms to develop into clinically viable disease-modifying therapies.</p>","PeriodicalId":8736,"journal":{"name":"Artificial Cells, Nanomedicine, and Biotechnology","volume":"54 1","pages":"104-118"},"PeriodicalIF":5.6,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146017334","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Gut microbiota-nanoparticle interactions in Parkinson's disease: mechanistic insights and therapeutic perspective. 肠道微生物-纳米颗粒在帕金森病中的相互作用:机制见解和治疗观点。
IF 5.6 3区 生物学
Artificial Cells, Nanomedicine, and Biotechnology Pub Date : 2026-12-01 Epub Date: 2026-07-17 DOI: 10.1080/21691401.2026.2694921
Leila Kafshdooz, Reza Safaralizadeh
{"title":"Gut microbiota-nanoparticle interactions in Parkinson's disease: mechanistic insights and therapeutic perspective.","authors":"Leila Kafshdooz, Reza Safaralizadeh","doi":"10.1080/21691401.2026.2694921","DOIUrl":"https://doi.org/10.1080/21691401.2026.2694921","url":null,"abstract":"<p><strong>Objective: </strong>This review introduces the 'nanomaterial-microbiome-brain interface' as a conceptual framework uniting three systems: gut microbiota, nanoparticles, and neurodegeneration.</p><p><strong>Main findings: </strong>We synthesize evidence showing that titanium dioxide, silver, and zinc oxide nanoparticles differentially alter microbial composition. These microbial shifts intersect with established gut-brain mechanisms, including short-chain fatty acid production and immune modulation, providing plausible pathways linking nanomaterial exposure to neurological outcomes.</p><p><strong>Conclusion: </strong>We propose the 'nanomaterial-microbiome-brain interface' as a novel conceptual framework with twofold relevance-serving both as a potential contributor to Parkinson's disease pathogenesis through unintentional environmental exposure, and as an underexplored avenue for therapeutic intervention. Critical knowledge gaps persist. Addressing these gaps will require integrated approaches that bridge nanomaterial research, microbiome science, and neurodegeneration studies.</p>","PeriodicalId":8736,"journal":{"name":"Artificial Cells, Nanomedicine, and Biotechnology","volume":"54 1","pages":"321-336"},"PeriodicalIF":5.6,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148468539","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Green synthesis of ZnO nanoparticles using pomegranate husk extract: comparative evaluation of antioxidant, enzyme inhibition, and cytotoxic properties. 用石榴皮提取物绿色合成氧化锌纳米粒子:抗氧化、酶抑制和细胞毒性的比较评价。
IF 5.6 3区 生物学
Artificial Cells, Nanomedicine, and Biotechnology Pub Date : 2026-12-01 Epub Date: 2026-05-16 DOI: 10.1080/21691401.2026.2668258
Shi-Yan Cheah, You-Kang Phang, Sharon Chia-Yen Lim, Ming-Xiu Koh, Sinouvassane Djearamane, Hemaroopini Subramaniam, Boon-Hoe Lim, Fang Li, Mohammod Aminuzzaman, Ling-Shing Wong, Lai-Hock Tey
{"title":"Green synthesis of ZnO nanoparticles using pomegranate husk extract: comparative evaluation of antioxidant, enzyme inhibition, and cytotoxic properties.","authors":"Shi-Yan Cheah, You-Kang Phang, Sharon Chia-Yen Lim, Ming-Xiu Koh, Sinouvassane Djearamane, Hemaroopini Subramaniam, Boon-Hoe Lim, Fang Li, Mohammod Aminuzzaman, Ling-Shing Wong, Lai-Hock Tey","doi":"10.1080/21691401.2026.2668258","DOIUrl":"10.1080/21691401.2026.2668258","url":null,"abstract":"<p><p>The prevalence of obesity has risen sharply in recent years, prompting the need for safer and more biocompatible therapeutic alternatives to conventional anti-obesity drugs. In this study, zinc oxide nanoparticles (ZnO NPs) were synthesized using pomegranate husk extract <i>via</i> two green approaches: conventional heating and microwave-assisted synthesis. Structural and morphological characterizations confirmed successful nanoparticle formation. Microwave-assisted ZnO nanoparticles (MA-ZnO NPs) exhibited smaller particle dimensions and narrower polydispersity compared with conventionally synthesized ZnO NPs. Both types of ZnO NPs demonstrated notable antioxidant activity (>62% scavenging in DPPH and ABTS assays) and strong inhibitory effects against pancreatic lipase and α-amylase (>70%), comparable to standard drugs such as orlistat and acarbose. Cytotoxicity assays using Vero cells confirmed high biocompatibility, with >60% cell viability. This work presents a comparative evaluation of two green synthesis methods and highlights the potential of biogenic ZnO NPs as multifunctional agents for oxidative stress reduction and enzyme inhibition in obesity management.</p>","PeriodicalId":8736,"journal":{"name":"Artificial Cells, Nanomedicine, and Biotechnology","volume":"54 1","pages":"120-136"},"PeriodicalIF":5.6,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147959372","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Molecular mechanisms of phytochemicals from Zanthoxylum nitidum (Roxb.) DC. against hepatocellular carcinoma: insights from network pharmacology, molecular docking, and bioinformatics. 花椒植物化学物质的分子机制直流。抗肝癌:来自网络药理学、分子对接和生物信息学的见解。
IF 5.6 3区 生物学
Artificial Cells, Nanomedicine, and Biotechnology Pub Date : 2026-12-01 Epub Date: 2026-07-24 DOI: 10.1080/21691401.2026.2700918
Rongjie Zhang, Ge Zhou, Jinhai Luo, Yingzi Wu, Yingjuan Huang
{"title":"Molecular mechanisms of phytochemicals from <i>Zanthoxylum nitidum</i> (Roxb.) DC. against hepatocellular carcinoma: insights from network pharmacology, molecular docking, and bioinformatics.","authors":"Rongjie Zhang, Ge Zhou, Jinhai Luo, Yingzi Wu, Yingjuan Huang","doi":"10.1080/21691401.2026.2700918","DOIUrl":"https://doi.org/10.1080/21691401.2026.2700918","url":null,"abstract":"<p><p>Hepatocellular carcinoma (HCC) is an aggressive malignancy with limited therapies. We explored the anti-HCC mechanisms of <i>Zanthoxylum nitidum</i> (Roxb.) DC. via network pharmacology, bioinformatics and molecular docking. We identified its active components, targets and HCC-related key genes by differential expression analysis. Enrichment analysis showed these targets act in HCC-related pathways like alcoholic liver disease and the PPAR signalling pathway. Machine learning screened 5 characteristic genes (<i>ESR1, CCNA2, CYP2B6, CHRM2, IL10</i>), among which <i>ESR1</i> and <i>CCNA2</i> correlate with patient prognosis. These genes regulate tumour microenvironment and show epigenetic variations in methylation and copy number. Molecular docking confirmed stable binding between plant components and core targets. This study first reveals the multi-target anti-HCC mechanisms of <i>Z. nitidum</i>, offering evidence for its clinical use. Follow-up experiments are needed to validate our findings.</p>","PeriodicalId":8736,"journal":{"name":"Artificial Cells, Nanomedicine, and Biotechnology","volume":"54 1","pages":"395-414"},"PeriodicalIF":5.6,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148583400","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Folate receptor-targeted PEGylated PLGA nanoparticles for the site-specific delivery of hesperidin in epithelial ovarian cancer. 叶酸受体靶向聚乙二醇化PLGA纳米颗粒用于上皮性卵巢癌橙皮苷的位点特异性递送。
IF 4.5 3区 生物学
Artificial Cells, Nanomedicine, and Biotechnology Pub Date : 2026-12-01 Epub Date: 2026-06-08 DOI: 10.1080/21691401.2026.2668273
Rohini Kharwade, Nilesh M Mahajan, Darshan R Telange, Priyanka N Yadav, Sachin R More
{"title":"Folate receptor-targeted PEGylated PLGA nanoparticles for the site-specific delivery of hesperidin in epithelial ovarian cancer.","authors":"Rohini Kharwade, Nilesh M Mahajan, Darshan R Telange, Priyanka N Yadav, Sachin R More","doi":"10.1080/21691401.2026.2668273","DOIUrl":"10.1080/21691401.2026.2668273","url":null,"abstract":"<p><p>Hesperidin (HSP) is a polyphenolic compound employed widely in the therapy of epithelial ovarian cancer (EOC). However, the low bioavailability, attributed to first-pass metabolism, low dissolution and poor tumour specificity, hampered its clinical effectiveness. Therefore, HSP-loaded folic acid-PEGylated poly(lactic-co-glycolic acid) (PLGA) nanoparticles (HSP-PEGylated PLGA FA NPs) were synthesized to improve dissolution and target specificity of HSP for the management of EOC. The NPs were synthesized by nanoprecipitation and assessed for entrapment efficiency, particle size, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD) and in vitro dissolution. Additionally, antioxidant assay, cytotoxicity, cellular uptake and flow cytometric were performed on folate receptor overexpressing SKOV3 cell line. Physico-chemical characterization supported the formation of HSP-PEGylated PLGA FA NPs with entrapment efficiency ∼89.34%, particle size ∼205 nm, and a zeta potential of ∼ -25 mV, demonstrating their physical stability. The NPs enhanced HSP release at pH 5.5 compared to pH 7.4. The NPs showed greater cytotoxicity at an IC50 value of ∼29 µM/mL and enhanced early apoptosis ∼44% as compared to HSP-PEGylated PLGA NPs ∼32% towards the FA receptor overexpressed EOC cell line. The developed formulation shows promising potential as a targeted NP system for the management of EOC.</p>","PeriodicalId":8736,"journal":{"name":"Artificial Cells, Nanomedicine, and Biotechnology","volume":"54 1","pages":"180-205"},"PeriodicalIF":4.5,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148203894","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Engineering a synthetic niche for hADSC preconditioning with PRP, Lp-SN, and resveratrol nanoparticles. 利用PRP, Lp-SN和白藜芦醇纳米颗粒设计hADSC预处理的合成生态位。
IF 5.6 3区 生物学
Artificial Cells, Nanomedicine, and Biotechnology Pub Date : 2026-12-01 Epub Date: 2026-06-26 DOI: 10.1080/21691401.2026.2691659
Shima Abbasi, Neda Akbari, Mojtaba Yazdani, Hassan Dianat-Moghadam, Mostafa Khalili
{"title":"Engineering a synthetic niche for hADSC preconditioning with PRP, Lp-SN, and resveratrol nanoparticles.","authors":"Shima Abbasi, Neda Akbari, Mojtaba Yazdani, Hassan Dianat-Moghadam, Mostafa Khalili","doi":"10.1080/21691401.2026.2691659","DOIUrl":"https://doi.org/10.1080/21691401.2026.2691659","url":null,"abstract":"<p><p><i>Ex vivo</i> expansion of human adipose-derived stem cells (hADSCs) remains challenging because reduced-serum culture conditions can compromise short-term cell function. Here, we evaluated a microenvironment-inspired tri-component preconditioning regimen composed of platelet-rich plasma (PRP), Lactobacillus plantarum cell-free supernatant (Lp-SN), and resveratrol-loaded PLGA nanoparticles (RSV-PLGA-NPs) as a reduced-serum culture support strategy. Using a Box-Behnken design, we identified a formulation space in which PRP, Lp-SN, and RSV-PLGA-NPs were associated with improved hADSC viability and increased expression of selected stemness-associated genes in vitro. Omission-control experiments comparing the full formulation with partial combinations and blank PLGA NPs showed attenuated responses when individual components were removed, whereas the NP carrier alone had no significant effect. These findings support the utility of this tri-component system as a preliminary <i>ex vivo</i> preconditioning approach for short-term hADSC culture support. However, the results should be interpreted within the limits of the present <i>in vitro</i> study, as long-term expansion, post-treatment differentiation capacity, and <i>in vivo</i> performance were not evaluated.</p>","PeriodicalId":8736,"journal":{"name":"Artificial Cells, Nanomedicine, and Biotechnology","volume":"54 1","pages":"276-289"},"PeriodicalIF":5.6,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148337502","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Bio-Inspired lipid nanovesicles (iNVs) incorporating membrane proteins from healthy tendon stem cells for targeted protein restoration in tendinopathic in vitro model. 结合健康肌腱干细胞膜蛋白的仿生脂质纳米囊泡(iNVs)用于肌腱病体外模型的靶向蛋白修复。
IF 5.6 3区 生物学
Artificial Cells, Nanomedicine, and Biotechnology Pub Date : 2026-12-01 Epub Date: 2026-01-28 DOI: 10.1080/21691401.2025.2599071
M C Ciardulli, E P Lamparelli, S Brongo, N Maffulli, G Della Porta
{"title":"Bio-Inspired lipid nanovesicles (iNVs) incorporating membrane proteins from healthy tendon stem cells for targeted protein restoration in tendinopathic <i>in vitro</i> model.","authors":"M C Ciardulli, E P Lamparelli, S Brongo, N Maffulli, G Della Porta","doi":"10.1080/21691401.2025.2599071","DOIUrl":"10.1080/21691401.2025.2599071","url":null,"abstract":"<p><p>The potential of human tendon-stem-cell-inspired nanovesicles (hTSC-iNVs) to act as a delivery platform for Tenomodulin (TNMD), a membrane glycoprotein essential for restoring function in pathological tendon stem cells, was investigated. Membrane proteins extracted from healthy TSCs were incorporated into Single Unilamellar Vesicles (SUVs) generated through microfluidic technology. Two formulations, iNVs-20 and iNVs-300, were produced using distinct protein-to-lipid ratios. These conditions resulted in protein loadings of 23 µg/mg for iNVs-20 and 2.5 µg/mg for iNVs-300, expressed as protein per milligram of total lipid. Physicochemical characterization showed that iNVs-20 had a larger mean diameter (188 ± 59.4 nm; PDI 0.10) and moderate ζ- potential (-11.3 mV), whereas iNVs-300 were smaller (149 ± 58 nm; PDI 0.15) with a more negative ζ-potential (-58.6 mV), potentially reflecting differences in the amount of loaded proteins. Approximately 90% of vesicles in both formulations successfully incorporated TNMD. Both types exhibited minimal cytotoxicity and were efficiently internalized by tendinopathic TSCs, leading to increased TNMD expression. iNVs-300 delivered the highest protein amount to pathological cells. Western blot and immunofluorescence analyses confirmed a time-dependent rise in higher-glycosylated form of TNMD after 48 h, demonstrating effective delivery that preserves functional post-translational modifications.</p>","PeriodicalId":8736,"journal":{"name":"Artificial Cells, Nanomedicine, and Biotechnology","volume":"54 1","pages":"37-52"},"PeriodicalIF":5.6,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"148148309","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Lipidation of a nuclear localization sequence enhances broad-spectrum antimicrobial activity: synthesis, characterization, and in silico analysis. 核定位序列的脂化增强了广谱抗菌活性:合成、表征和硅分析。
IF 5.6 3区 生物学
Artificial Cells, Nanomedicine, and Biotechnology Pub Date : 2026-12-01 Epub Date: 2026-03-31 DOI: 10.1080/21691401.2026.2649071
Rani Maharani, Taufik Muhammad Fakih, Muhamad Imam Muhajir, Anggun Fuji Rizqiyani, Ace Tatang Hidayat, Reza Aditama, Retno Lestari, Doddy Irawan Setyo Utomo, Tarwadi Tarwadi
{"title":"Lipidation of a nuclear localization sequence enhances broad-spectrum antimicrobial activity: synthesis, characterization, and in silico analysis.","authors":"Rani Maharani, Taufik Muhammad Fakih, Muhamad Imam Muhajir, Anggun Fuji Rizqiyani, Ace Tatang Hidayat, Reza Aditama, Retno Lestari, Doddy Irawan Setyo Utomo, Tarwadi Tarwadi","doi":"10.1080/21691401.2026.2649071","DOIUrl":"10.1080/21691401.2026.2649071","url":null,"abstract":"<p><p>Lipidation enhances the antimicrobial potential of cationic peptides by increasing amphiphilicity. The nuclear localization signal peptide PKKKRKV, although cell-penetrating, has weak intrinsic antimicrobial activity. This study evaluates whether conjugation with fatty acids of varying chain lengths (C16-C18) and saturation can improve its antimicrobial properties and elucidate the associated structure-activity relationships. Five PKKKRKV-based lipopeptides (LP-1-LP-5) were synthesized using Fmoc solid-phase peptide synthesis and conjugated with different fatty acids. The compounds were purified by RP-HPLC and characterized by mass spectrometry and NMR. Antimicrobial activity was assessed against Gram-positive bacteria (<i>Staphylococcus epidermidis, Staphylococcus aureus</i>), Gram-negative bacteria <i>(Escherichia coli, Salmonella typhimurium</i>), and the fungus <i>Candida albicans</i> using broth microdilution assays. In silico studies, including molecular docking, molecular dynamics simulations, and DFT calculations, were conducted to investigate potential mechanisms and electronic properties. Lipidation significantly improved antimicrobial activity. LP-5 (C18:1, unsaturated) showed the broadest spectrum, with MIC values of 11.59-23.19 µM against both Gram-positive and Gram-negative bacteria. LP-2 (C16:0, saturated) exhibited selective potency against <i>E. coli</i> (MIC = 6.96 µM), while LP-3 and LP-4 demonstrated moderate, broad-spectrum activity. Computational analyses indicated favorable target interactions, though they did not fully correlate with experimental results. LP-4 and LP-5 showed the smallest HOMO-LUMO gaps (∼0.111-0.112 eV), suggesting higher electronic reactivity. Overall, lipidation of PKKKRKV is a promising strategy for developing antimicrobial agents. Chain length and saturation significantly influence activity, with LP-5 emerging as the most promising broad-spectrum candidate. Further studies are required to validate mechanisms and assess toxicity..</p>","PeriodicalId":8736,"journal":{"name":"Artificial Cells, Nanomedicine, and Biotechnology","volume":"54 1","pages":"264-288"},"PeriodicalIF":5.6,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147589593","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Formulation and characterization of ascorbic acid-based zinc oxide nanoparticles for assessing antidiabetic and neuroprotective effects in STZ-induced diabetic rats. 抗坏血酸氧化锌纳米颗粒的制备及表征对stz诱导的糖尿病大鼠的抗糖尿病和神经保护作用。
IF 5.6 3区 生物学
Artificial Cells, Nanomedicine, and Biotechnology Pub Date : 2026-12-01 Epub Date: 2026-04-28 DOI: 10.1080/21691401.2026.2662205
Sindu M B, Syed Sagheer Ahmed, Mohamed Rahamathulla, Bharathi D R, Mohammad Ali, Ali Alamri, Yahya Alhamhoom, Mohammed Muqtader Ahmed, Ismail Pasha
{"title":"Formulation and characterization of ascorbic acid-based zinc oxide nanoparticles for assessing antidiabetic and neuroprotective effects in STZ-induced diabetic rats.","authors":"Sindu M B, Syed Sagheer Ahmed, Mohamed Rahamathulla, Bharathi D R, Mohammad Ali, Ali Alamri, Yahya Alhamhoom, Mohammed Muqtader Ahmed, Ismail Pasha","doi":"10.1080/21691401.2026.2662205","DOIUrl":"10.1080/21691401.2026.2662205","url":null,"abstract":"<p><p>Ascorbic acid (AA) has strong antioxidant and anti-diabetic activities; nevertheless, its therapeutic value is restricted due to rapid degradation, low-bioavailability and short systemic retention. To address these constraints, this study describes the development of a green-synthesized zinc oxide nanoparticle (ZnO NP)-based delivery system functionalized with AA (ZnO-AA NPs) and assesses its antidiabetic and neuroprotective effects. AA-assisted precipitation method was used to develop ZnO-AA NPs, which were then characterized by dynamic light scattering (DLS), zeta potential (ZP), scanning electron microscopy (SEM), FTIR spectroscopy and X-ray diffraction (XRD). The nanoparticles had a homogeneous size (∼38 nm), good colloidal stability and a crystalline wurtzite structure. <i>In vitro</i>, ZnO-AA NPs showed dose-dependent inhibition of α-amylase and α-glucosidase. <i>In vivo</i>, oral ZnO-AA NPs (25 and 50 mg/kg) significantly improved glycaemic control, lipid profile and antioxidant enzyme levels compared to free AA (*<i>p</i>* < 0.01, *<i>p</i>* < 0.001; one-way/two-way ANOVA). ZnO-AA NPs dramatically reduced diabetes-related cognitive impairment, resulting in improved performance in the Morris water maze (MWM) and open field tests (OFTs) (*<i>p</i>* < 0.001), decreased hippocampal acetylcholinesterase (AChE) activity and preserved neuronal architecture. Overall, the ZnO-AA nanoformulation represents a multifunctional nanomedicine technique that improves the therapeutic efficacy of AA and has considerable promise for the treatment of diabetes and its associated neurodegenerative consequences.</p>","PeriodicalId":8736,"journal":{"name":"Artificial Cells, Nanomedicine, and Biotechnology","volume":"54 1","pages":"53-72"},"PeriodicalIF":5.6,"publicationDate":"2026-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147760263","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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