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Exploring the potential of chitin and chitosan in nanobiocomposites for fungal immunological detection and antifungal action 探索甲壳素和壳聚糖纳米生物复合材料在真菌免疫学检测和抗真菌作用方面的潜力
IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2024-07-19 DOI: 10.1016/j.carres.2024.109220
Manuela Gómez-Gaviria, Héctor M. Mora-Montes

Chitin is a polymer of N-acetylglucosamine and an essential component of the fungal cell wall. Chitosan is the deacetylated form of chitin and is also important for maintaining the integrity of this structure. Both polysaccharides are widely distributed in nature and have been shown to have a variety of applications in biomedicine, including their potential in immune sensing and as potential antifungal agents. In addition, chitin has been reported to play an important role in the pathogen-host interaction, involving innate and adaptive immune responses. This paper will explore the role of chitin and chitosan when incorporated into nanobiocomposites to improve their efficacy in detecting fungi of medical interest and inhibiting their growth. Potential applications in diagnostic and therapeutic medicine will be discussed, highlighting their promise in the development of more sensitive and effective tools for the early diagnosis of fungal infections. This review aims to highlight the importance of the convergence of nanotechnology and biology in addressing public health challenges.

甲壳素是一种 N-乙酰葡糖胺聚合物,是真菌细胞壁的重要组成部分。壳聚糖是甲壳素的脱乙酰形式,对于保持这种结构的完整性也很重要。这两种多糖在自然界中分布广泛,已被证明在生物医学中具有多种用途,包括潜在的免疫传感和潜在的抗真菌剂。此外,有报道称几丁质在病原体与宿主的相互作用中扮演重要角色,涉及先天性免疫反应和适应性免疫反应。本文将探讨几丁质和壳聚糖在纳米生物复合材料中的作用,以提高其检测医学真菌和抑制真菌生长的功效。文章将讨论纳米生物复合材料在诊断和治疗医学中的潜在应用,强调它们在开发更灵敏、更有效的真菌感染早期诊断工具方面的前景。本综述旨在强调纳米技术与生物学融合在应对公共卫生挑战方面的重要性。
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引用次数: 0
Catalyst and base-free, direct oxidation of chitin to lactic acid with hydrogen peroxide 用过氧化氢将甲壳素直接氧化成乳酸的无催化剂和无碱工艺
IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2024-07-19 DOI: 10.1016/j.carres.2024.109218
Xiao Du, Tengfei Li, Lumei Wang, Dezhang Ren, Zhibao Huo

In recent years, the research on the conversion of chitin to high value-added chemicals has attracted more and more attention. At present, the method of preparing lactic acid from chitin mostly uses strong base or catalyst. The reaction system under alkaline condition not only corrodes the container but also easily harms the human body. Herein, a simple and effective method to convert chitin to organic acids in catalyst and base-free conditions is developed. The use of H2O2 only can efficiently convert chitin to organic acids in the absence of bases and catalysts. Under the optimal conditions of 30 mg chitin, 2.1 mL water, 0.9 mL H2O2 at 230 °C for 1.5 h, the lactic acid yield of chitin can reach 58.2 % and the total organic acid yield can reach 84.0 %. This work provides an efficient method for the resource utilization of chitin biomass.

近年来,甲壳素转化为高附加值化学品的研究越来越受到关注。目前,从甲壳素制备乳酸的方法大多使用强碱或催化剂。碱性条件下的反应体系不仅会腐蚀容器,还容易对人体造成伤害。在此,我们开发了一种在无催化剂和无碱条件下将甲壳素转化为有机酸的简单而有效的方法。在无碱和催化剂的条件下,仅使用 H2O2 就能有效地将甲壳素转化为有机酸。在 30 毫克甲壳素、2.1 毫升水、0.9 毫升 H2O2、230 °C、1.5 小时的最佳条件下,甲壳素的乳酸产率可达 58.2%,总有机酸产率可达 84.0%。这项工作为甲壳素生物质的资源化利用提供了一种有效的方法。
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引用次数: 0
Synthesis of hydrogels from biomaterials and their potential application in tissue engineering 利用生物材料合成水凝胶及其在组织工程中的潜在应用
IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2024-07-15 DOI: 10.1016/j.carres.2024.109216
Gabriela Martínez-Mejía , Ricardo Cuadras-Arconada , Nadia Adriana Vázquez-Torres , Rubén Caro-Briones , Andrés Castell-Rodríguez , José Manuel del Río , Mónica Corea , Rogelio Jiménez-Juárez

In this study, a series of hydrogels were synthesized from chitosan(s) that was crosslinking with glutaraldehyde at different concentrations. Ascorbic acid in an acidic medium was used to facilitate non-covalent interactions. The chitosan(s) was obtained from shrimp cytoskeleton; while ascorbic acid was extracted from xoconostle juice. The hydrogel reaction was monitored by UV–vis spectroscopy (550 nm) to determine the reaction kinetics and reaction order at 60 °C. The hydrogels structures were characterized by NMR, FT-IR, HR-MS and SEM, while the degree of cross-linking was examined with TGA-DA. The extracellular matrices were obtained as stable hydrogels where reached maximum crosslinking was of 7 %, independent of glutaraldehyde quantity added. The rheological properties showed a behavior of weak gels and a dependence of crosslinking agent concentration on strength at different temperatures. The cytotoxicity assay showed that the gels had no adverse effects on cellular growth for all concentrations of glutaraldehyde.

本研究用不同浓度的戊二醛交联壳聚糖,合成了一系列水凝胶。酸性介质中的抗坏血酸可促进非共价相互作用。壳聚糖是从虾的细胞骨架中提取的,而抗坏血酸是从牛肝菌汁中提取的。通过紫外-可见光谱(550 nm)监测水凝胶反应,以确定在 60 °C 下的反应动力学和反应顺序。核磁共振、傅立叶变换红外光谱、HR-MS 和扫描电镜对水凝胶结构进行了表征,TGA-DA 对交联程度进行了检测。获得的细胞外基质是稳定的水凝胶,最大交联度为 7%,与戊二醛的添加量无关。流变特性显示,在不同温度下,交联剂浓度对强度的影响与弱凝胶的行为有关。细胞毒性试验表明,在所有浓度的戊二醛中,凝胶都不会对细胞生长产生不利影响。
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引用次数: 0
Enzyme immobilization with nanomaterials for hydrolysis of lignocellulosic biomass: Challenges and future Perspectives 利用纳米材料固定酶以水解木质纤维素生物质:挑战与未来展望
IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2024-07-14 DOI: 10.1016/j.carres.2024.109208
Neha Kotwal , Deepak Pathania , Anita Singh , Zaheer Ud Din Sheikh , Richa Kothari

Enzyme immobilization has emerged as a prodigious strategy in the enzymatic hydrolysis of lignocellulosic biomass (LCB) promising enhanced efficacy and stability of the enzymes. Further, enzyme immobilization on magnetic nanoparticles (MNPs) facilitates the easy recovery and reuse of biocatalysts. This results in the development of a nanobiocatalytic system, that serves as an eco-friendly and inexpensive LCB deconstruction approach. This review provides an overview of nanomaterials used for immobilization with special emphasis on the nanomaterial-enzyme interactions and strategies of immobilization. After the succinct outline of the immobilization procedures and supporting materials, a comprehensive assessment of the catalysis enabled by nanomaterial-immobilized biocatalysts for the conversion and degradation of lignocellulosic biomasses is provided by gathering state-of-the-art examples. The challenges and future directions associated with this technique providing a potential solution in the present article. Insight on the recent advancements in the process of nanomaterial-based immobilization for the hydrolysis of lignocellulosic biomass has also been highlighted in the article.

酶固定化已成为木质纤维素生物质(LCB)酶水解过程中的一项重要策略,有望提高酶的功效和稳定性。此外,将酶固定在磁性纳米颗粒(MNPs)上有利于生物催化剂的轻松回收和重复使用。这样就开发出了一种纳米生物催化系统,可作为一种生态友好、成本低廉的低浓溴酸解构方法。本综述概述了用于固定化的纳米材料,特别强调了纳米材料与酶的相互作用以及固定化策略。在简要概述了固定化程序和辅助材料之后,通过收集最先进的实例,对纳米材料固定化生物催化剂在木质纤维素生物质转化和降解中的催化作用进行了全面评估。本文还探讨了与该技术相关的挑战和未来发展方向,并提供了潜在的解决方案。文章还重点介绍了基于纳米材料的固定化技术在水解木质纤维素生物质过程中的最新进展。
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引用次数: 0
GSH-responsive and folate receptor-targeted pyridine bisfolate-encapsulated chitosan nanoparticles for enhanced intracellular drug delivery in MCF−7 cells GSH 响应型和叶酸受体靶向吡啶双酯包封壳聚糖纳米粒子用于增强 MCF-7 细胞的胞内给药能力
IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2024-07-14 DOI: 10.1016/j.carres.2024.109207
Fawzya I. Elshami , Gehad Elrefaei , Mohamed M. Ibrahim , Ibrahim Elmehasseb , Shaban Y. Shaban

Folic acid receptor-targeted drug delivery system is a promising candidate for tumor-targeted delivery because its elevated expression specifically on tumor cells enables the selective delivery of cytotoxic cargo to cancerous tissue, thereby minimizing toxic side effects and increasing the therapeutic index. Pyridine bisfolate-chitosan (PyBFA@CS NPs) and folate-chitosan nanocomposite (FA@CS NPs) were synthesized with suitable particle size (256.0 ± 15.0 and 161.0 ± 5.0 nm), high stability (ζ = −27.0 ± 0.1 and −30.0 ± 0.2 mV), respectively, and satisfactory biocompatibility to target cells expressing folate receptors and try to answer the question: Is the metal center always important for activity? Since almost all pharmaceuticals work by binding to specific proteins or DNA, the in vitro binding of human serum albumin (HSA) to PyBFA@CS NPs and FA@CS NPs has been investigated and compared with PyBFA. Strong affinity to HSA is shown by quenching and binding constants in the range of 105 and 104 M−1, respectively with PyBFA@CS NPs showing the strongest. The compounds-HSA kinetic stability, affinity, and association constants were investigated using a stopped-flow method. The findings showed that all formulations bind by a static quenching mechanism that consists of two reversible steps: rapid second-order binding and a more slowly first-order isomerization reaction. The overall coordination affinity of HSA to PyBFA@CS NPs (6.6 × 106 M−1), PyBFA (4.4 × 106 M−1), and FA@CS NPs (1.3 × 106 M−1) was measured and The relative reactivity is roughly (PyBFA@CS NPs)/(PyBFA)/(FA@CS NPs) = 5/3/1. Additionally, in vitro cytotoxicity revealed that, consistent with the binding constants and coordination affinity, active-targeting formulations greatly inhibited FR-positive MCF-7 cells in compared to FRs-negative A549 cells in the following trend: PyBFA@CS NPs > PyBFA > FA@CS NPs. Furthermore, in vitro drug release of PyBFA@CS NPs was found to be stable in PBS at pH 7.4, however, the in pH 5.4 and in pH 5.4 containing 10 mM glutathione (GSH) (mimicking the tumor microenvironment) reached 43 % and 73 %, respectively indicating that the PyBFA@CS NPs system is sensitive to GSH. Folate-modified nanoparticles, PyBFA@CS NPs, are a promising therapeutic for MCF-7 therapy because they not only showed a greater affinity for HSA, but also showed higher cleavage efficiency toward the minor groove of pBR322 DNA via the hydrolytic way, as well as effective antibacterial activity that avoids the usage of extra antibiotics.‬‬‬‬‬‬‬‬‬‬‬‬ ‬‬‬‬‬‬‬‬‬‬‬‬‬‬

叶酸受体靶向给药系统是一种很有前景的肿瘤靶向给药系统,因为叶酸受体在肿瘤细胞中的特异性表达升高,可以将细胞毒性物质选择性地输送到肿瘤组织,从而最大限度地减少毒副作用,提高治疗指数。我们合成了吡啶双酚壳聚糖(PyBFA@CS NPs)和叶酸壳聚糖纳米复合材料(FA@CS NPs),它们具有合适的粒径(256.0 ± 15.0 nm 和 161.0 ± 5.0 nm)、高稳定性(ζ = -27.0 ± 0.1 mV 和 -30.0 ± 0.2 mV)和令人满意的生物相容性,可用于靶向表达叶酸受体的细胞,并尝试回答这个问题:金属中心对活性是否总是很重要?由于几乎所有药物都是通过与特定蛋白质或 DNA 结合来发挥作用的,因此研究了人血清白蛋白(HSA)与 PyBFA@CS NPs 和 FA@CS NPs 的体外结合情况,并与 PyBFA 进行了比较。研究结果表明,PyBFA@CS NPs 与人血清白蛋白(HSA)的淬灭度和结合常数分别在 105 和 104 M-1 之间,与 HSA 的亲和力最强。采用停流法研究了化合物与 HSA 的动力学稳定性、亲和力和结合常数。研究结果表明,所有配方都是通过静态淬火机制结合的,该机制包括两个可逆步骤:快速的二阶结合和较缓慢的一阶异构化反应。测定了 HSA 与 PyBFA@CS NPs(6.6 × 106 M-1)、PyBFA(4.4 × 106 M-1)和 FA@CS NPs(1.3 × 106 M-1)的总体配位亲和力,其相对反应活性大致为(PyBFA@CS NPs)/(PyBFA)/(FA@CS NPs)=5/3/1。此外,体外细胞毒性显示,与结合常数和配位亲和力一致,活性靶向制剂对 FR 阳性的 MCF-7 细胞和 FR 阴性的 A549 细胞的抑制作用呈以下趋势:PyBFA@CS NPs > PyBFA > FA@CS NPs。此外,在 pH 7.4 的 PBS 中,PyBFA@CS NPs 的体外药物释放稳定,但在 pH 5.4 和含有 10 mM 谷胱甘肽(GSH)(模拟肿瘤微环境)的 pH 5.4 中,药物释放分别达到 43% 和 73%,表明 PyBFA@CS NPs 系统对 GSH 敏感。叶酸修饰的纳米粒子--PyBFA@CS NPs--是一种用于 MCF-7 治疗的有前途的疗法,因为它们不仅对 HSA 有更大的亲和力,而且通过水解方式对 pBR322 DNA 小沟的裂解效率更高,同时还具有有效的抗菌活性,可避免使用额外的抗生素。
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引用次数: 0
pH-responsive chitosan-mediated spherical mesoporous silica microspheres for high loading and controlled delivery of 5-Fluorouracil pH 响应壳聚糖介导的球形介孔二氧化硅微球,用于 5-氟尿嘧啶的高负载和可控给药。
IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2024-07-09 DOI: 10.1016/j.carres.2024.109206
Qianqian Zhang , Tong Wan , Guocheng Jin , Shiai Xu

The objective of this study is to develop a drug carrier to overcome the inherent drawbacks of 5-Fluorouracil (5-Fu), including low bioavailability, short half-life, and systemic toxicity. In the present work, mesoporous silica nanoparticles (MSNs) capped by chitosan (CS) to encapsulate 5-Fu (5-Fu MSNs/CS) were fabricated by the sol-gel process, ultrasonic impregnation, and emulsion cross-linking. The 5-Fu MSNs/CS microspheres exhibit pH-responsive drug release and remarkable drug encapsulation capacity, as well as perfect sphericity, high specific surface area (680.62 cm2/g), and uniform particle size (2.64 ± 0.05 μm). The drug-loading content and encapsulation efficiency are 14.12 ± 0.53 % and 82.21 ± 2.13 %, respectively. The cumulative release of 5-Fu from MSNs/CS microspheres is fast and sustained at pH 5.0 (89.56 ± 0.97 %) compared to that at pH 7.4 (57.88 ± 0.91 %) in 96 h, and it is Fickian diffusion controlled. In conclusion, the MSNs/CS microspheres prepared in this study could be potential carriers for 5-Fu delivery.

本研究旨在开发一种药物载体,以克服 5-氟尿嘧啶(5-Fu)固有的缺点,包括生物利用度低、半衰期短和全身毒性。本研究采用溶胶-凝胶法、超声浸渍法和乳液交联法制备了壳聚糖(CS)包裹的介孔二氧化硅纳米颗粒(MSNs)来封装 5-Fu(5-Fu MSNs/CS)。所制备的 5-Fu MSNs/CS 微球具有良好的球形度、高比表面积(680.62 cm2/g)和均匀的粒径(2.64 ± 0.05 μm),并具有 pH 值响应性药物释放和显著的药物包封能力。载药量和包封效率分别为 14.12 ± 0.53 % 和 82.21 ± 2.13 %。与 pH 值为 7.4 时(57.88 ± 0.91 %)相比,MSNs/CS 微球在 pH 值为 5.0 时(89.56 ± 0.97 %),5-Fu 在 96 小时内的累积释放速度快且持续,并且是费克扩散控制的。总之,本研究制备的 MSNs/CS 微球可作为潜在的 5-Fu 递送载体。
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引用次数: 0
In silico approaches for better understanding cysteine cathepsin-glycosaminoglycan interactions 更好地理解半胱氨酸螯合蛋白-氨基糖相互作用的硅学方法
IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2024-07-06 DOI: 10.1016/j.carres.2024.109201
Krzysztof K. Bojarski , Alexis David , Fabien Lecaille , Sergey A. Samsonov

Cysteine cathepsins constitute the largest cathepsin family, with 11 proteases in human that are present primarily within acidic endosomal and lysosomal compartments. They are involved in the turnover of intracellular and extracellular proteins. They are synthesized as inactive procathepsins that are converted to mature active forms. Cathepsins play important roles in physiological and pathological processes and, therefore, receive increasing attention as potential therapeutic targets. Their maturation and activity can be regulated by glycosaminoglycans (GAGs), long linear negatively charged polysaccharides composed of recurring dimeric units. In this review, we summarize recent computational progress in the field of (pro)cathepsin-GAG complexes analyses.

半胱氨酸酪蛋白构成了最大的酪蛋白家族,在人类中有 11 种蛋白酶,主要存在于酸性内体和溶酶体内。它们参与细胞内和细胞外蛋白质的周转。它们合成为无活性的前胰蛋白酶,然后转化为成熟的活性形式。胰凝乳蛋白在生理和病理过程中发挥着重要作用,因此作为潜在的治疗靶点受到越来越多的关注。它们的成熟和活性可受糖胺聚糖(GAGs)的调节,糖胺聚糖是由重复出现的二聚单位组成的带负电荷的长线性多糖。在这篇综述中,我们总结了(原)胰蛋白酶-GAG 复合物分析领域的最新计算进展。
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引用次数: 0
Anti-virus activity and mechanisms of natural polysaccharides from medicinal herbs 药材中天然多糖的抗病毒活性和机制。
IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2024-07-06 DOI: 10.1016/j.carres.2024.109205
Xiaoyan Huang, Xingyin Chen, Yuanhua Xian, Faming Jiang

There has been a sudden increase in viral diseases, such as coronavirus disease 2019 (COVID-19), causing significant harm to human and animal well-being, as well as economic development. Medicinal herbs, with a history of thousands of years in clinical use, contain versatile polysaccharides as one of their primary compounds. This review offers an overview of the antiviral effects of polysaccharides from medicinal herbs on viruses in humans, poultry, swine and aquaculture in recent years. The mechanism of these antiviral polysaccharides, involved in hindering various stages of the viral life cycle thereby blocking virus infection, is summarized. The review also explores other underlying mechanisms of antiviral effects, such as enhancing the immune response, regulating inflammatory reactions, balancing gut flora, reducing oxidative stress, and suppressing apoptosis through various corresponding signaling pathways. The structure-function relationships discussed in this article also aid in understanding the antiviral mechanism of natural polysaccharides, indicating the need for more in-depth research and analysis. Natural polysaccharides from medicinal herbs have emerged as valuable resources in the fight against viral infections, exhibiting high effectiveness. This review emphasizes the promising role of polysaccharides from medicinal herbs as potential candidates for blocking viral infections in humans and animals.

病毒性疾病突然增多,如 2019 年冠状病毒病(COVID-19),对人类和动物的福祉以及经济发展造成了重大危害。具有数千年临床应用历史的药用草本植物,其主要化合物之一含有多功能多糖。本综述概述了近年来药材多糖对人类、家禽、猪和水产养殖中病毒的抗病毒作用。综述了这些抗病毒多糖阻碍病毒生命周期各个阶段从而阻断病毒感染的机制。综述还探讨了抗病毒作用的其他潜在机制,如通过各种相应的信号通路增强免疫反应、调节炎症反应、平衡肠道菌群、减少氧化应激和抑制细胞凋亡。本文所讨论的结构-功能关系也有助于理解天然多糖的抗病毒机制,表明有必要进行更深入的研究和分析。药材中的天然多糖已成为抗病毒感染的宝贵资源,表现出很高的有效性。本综述强调了药材多糖作为阻断人类和动物病毒感染的潜在候选物质所具有的广阔前景。
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引用次数: 0
Total synthesis of the hexasaccharide arabinan domain of mycobacterial arabinogalactan 分枝杆菌阿拉伯半乳聚糖六糖阿拉伯聚糖结构域的全合成。
IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2024-07-04 DOI: 10.1016/j.carres.2024.109204
Sixian Fang , Cai Huang , Jiaming Ao , Qian Xiao, Siai Zhou, Wenbin Deng, Hui Cai, Feiqing Ding

The hexasaccharide arabinan domain of Mycobacterial Arabinogalactan was provided with the versatile methodology toward β-selective arabinofuranosylation directed by B(C6F5)3, demonstrating the effectiveness of the β-arabinofuranosylation strategy. Derivatization of the amino moiety at the reducing end are essential prerequisites for elucidating the biosynthetic pathway and conjugating of this compound to a protein carrier for vaccine generation.

通过 B(C6F5)3 引导的多用途方法,对分枝杆菌阿拉伯半乳聚糖的阿拉伯呋喃六糖结构域进行了 β-选择性阿拉伯呋喃基化,证明了 β-阿拉伯呋喃基化策略的有效性。还原端氨基的衍生化是阐明该化合物的生物合成途径以及将其与蛋白质载体共轭以生成疫苗的必要前提。
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引用次数: 0
pH-responsive chitosan copolymer synthesized via click chemistry for design of polymeric nanoparticles for targeted drug delivery 通过点击化学合成的 pH 响应壳聚糖共聚物,用于设计靶向给药的聚合物纳米颗粒。
IF 2.4 3区 化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2024-07-02 DOI: 10.1016/j.carres.2024.109200
Mariya Gover Antoniraj, Henry Linda Jeeva Kumari, A. Shanmugarathinam, Ruckmani Kandasamy

The polymeric nanoparticles (PNPs) loaded with prednisolone were developed to exhibit pH-responsive properties owing to the attachment of a hydrazone linkage between the copolymer chitosan and mPEG. In the diseased cellular environment, the hydrazone bond tends to break due to reduced pH, leading to the release of the drug from the PNPs at the required site of action. The fabricated PNPs exhibit spherical morphology, optimum size (∼200 nm), negative surface charge, and monodispersed particle size distribution. The encapsulation efficiency of the PNPs was determined to be 71.1 ± 0.79 % and two experiments (polymer weight loss and drug release) confirmed the pH-responsive properties of the PNPs. The cellular study cytotoxicity assay showed biocompatibility of PNPs and drug molecule-mediated toxicity to A549 cells. The ligand atrial natriuretic peptide-attached PNPs internalized into A549 cells via natriuretic peptide receptor-A to achieve target specificity. The PNPs cytotoxicity and pH-response medicated inflammation reduction functionality was studied in inflammation-induced RAW264.7 cell lines. The study observed the PNPs effectively reduced the inflammatory mediators NO and ROS levels in RAW264.7. The results showed that pH-responsive properties of PNPs and this novel fabricated delivery system effectively treat inflammatory and cancer diseases.

由于共聚物壳聚糖和 mPEG 之间的腙连接具有 pH 响应特性,因此开发出了负载泼尼松龙的聚合物纳米粒子(PNPs)。在病变的细胞环境中,由于 pH 值降低,腙键容易断裂,导致药物从 PNPs 释放到所需的作用部位。制备的 PNPs 呈球形,具有最佳尺寸(200 nm)、负表面电荷和单分散粒度分布。经测定,PNPs 的封装效率为 71.1 ± 0.79 %,两项实验(聚合物失重和药物释放)证实了 PNPs 的 pH 响应特性。细胞研究细胞毒性测定显示了 PNPs 的生物相容性和药物分子介导的对 A549 细胞的毒性。配体心房钠尿肽附着的 PNPs 通过钠尿肽受体-A 内化到 A549 细胞中,实现了靶向特异性。在炎症诱导的 RAW264.7 细胞系中研究了 PNPs 的细胞毒性和 pH 响应药物消炎功能。研究发现,PNPs 能有效降低 RAW264.7 细胞中的炎症介质 NO 和 ROS 水平。研究结果表明,PNPs 的 pH 响应特性和这种新型制造的递送系统能有效治疗炎症和癌症疾病。
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Carbohydrate Research
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