Carbohydrate Research最新文献_第10页

Yam polysaccharide extraction, purification, structural features, and biological properties: A review 山药多糖的提取、纯化、结构特征及生物学特性综述。

IF 2.5 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research

Pub Date : 2026-01-01 Epub Date: 2025-11-19 DOI: 10.1016/j.carres.2025.109746

Chongbi Wei , Shaowa Lv , Lei Jiang , Fang Fang , Lei Liu , Shuang Sun , Yunjie Ma , Yuyan Guo

Yam (Dioscorea opposita Thunb.) is a widely used culinary and medicinal plant rhizome with a long application history. The polysaccharides in yam are important bioactive components. As a natural polysaccharide, yam polysaccharides exhibit strong advantages in terms of physicochemical properties, biological activity, and structural plasticity, making them a research hotspot in the fields of biomedicine and functional foods. However, systematic studies on the stable extraction, structural analysis, modification techniques, and structure-activity relationships of Chinese yam polysaccharide (CYP) remain limited. This review summarizes 124 research publications on CYP over the past 40 years, providing a comprehensive and systematic analysis of the extraction, separation, purification, characterization methods, structural modification, bioactivities, and applications of CYP. It is evident that CYP exhibits diverse biological activities due to its unique structural features, showing broad application potential in the fields of functional foods and pharmaceuticals. However, the structural complexity of CYP, including the variety of glycosidic bonds, differences in molecular weight, and branching structures, poses challenges for in-depth research. Future studies should focus on elucidating the structure-activity relationships, exploring the underlying mechanisms of action, and thereby fully leveraging the natural health benefits of CYP to promote innovation and industrial upgrading in related fields. In conclusion, this systematic review provides scientific guidance for further research and development of Chinese yam polysaccharide.

山药（Dioscorea opposita Thunb.）是一种应用广泛的药用植物根茎，具有悠久的应用历史。山药多糖是重要的生物活性成分。山药多糖作为一种天然多糖，在理化性质、生物活性、结构可塑性等方面具有很强的优势，是生物医学和功能食品领域的研究热点。然而，对山药多糖的稳定提取、结构分析、改性技术及构效关系等方面的系统研究仍然有限。本文综述了近40年来关于CYP的124篇研究论文，对CYP的提取、分离、纯化、表征方法、结构修饰、生物活性和应用等方面进行了系统的分析。由于其独特的结构特征，CYP具有多种生物活性，在功能食品和医药领域具有广阔的应用潜力。然而，CYP结构的复杂性，包括糖苷键的多样性、分子量的差异和分支结构的差异，给深入研究带来了挑战。未来的研究应重点阐明其构效关系，探索其作用机制，从而充分发挥CYP天然的健康效益，促进相关领域的创新和产业升级。本综述为山药多糖的进一步研究和开发提供了科学指导。

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引用次数: 0

A systematic review on polysaccharides from Ophiopogonis Radix and Liriopes Radix: Advances in the preparation, structural characterization and pharmacological activities 麦冬多糖和枳壳多糖的制备、结构表征和药理活性研究进展。

IF 2.5 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research

Pub Date : 2026-01-01 Epub Date: 2025-11-07 DOI: 10.1016/j.carres.2025.109744

Shuai Wang , Mingxuan Li , Xiaomeng Gong , Zhi Chen , Huagang Sheng , Fengxia Xu , Yanru Ren , Chao Zhang , Fei Guo , Zhiyuan Zhang

Ophiopogonis Radix and Liriopes Radix (Maidong), a traditional Chinese medicine esteemed for its yin-nourishing and lung-moistening properties, is a rich source of bioactive polysaccharides (Maidong polysaccharides, MDPs). This review systematically consolidates recent advances (from 2018 to October 2025) in the extraction, purification, structural characterization, and diverse bioactivities of MDPs. Modern research reveals that MDPs exhibit a broad spectrum of pharmacological activities, including antioxidant, anti-inflammatory, immunomodulatory, and gut microbiota-regulating effects. These properties underpin their potential therapeutic applications in managing conditions like diabetes, cardiovascular disorders, and inflammatory diseases. Despite promising findings, a clear understanding of the precise structural information and structure-activity relationships of MDPs remains limited. This comprehensive summary aims to lay a foundation for future research, highlighting the therapeutic potential of MDPs while identifying key areas requiring further investigation to fully exploit their health-promoting functions.

麦冬、麦冬是一种具有滋阴润肺功效的中药，富含生物活性多糖（麦冬多糖，MDPs）。本文系统地总结了从2018年到2025年10月在MDPs的提取、纯化、结构表征和多种生物活性方面的最新进展。现代研究表明，MDPs具有广泛的药理活性，包括抗氧化、抗炎、免疫调节和肠道微生物调节作用。这些特性支持了它们在管理糖尿病、心血管疾病和炎症性疾病等疾病方面的潜在治疗应用。尽管有很好的发现，但对MDPs的精确结构信息和结构-活性关系的清晰理解仍然有限。本文的综合总结旨在为未来的研究奠定基础，突出mdp的治疗潜力，同时确定需要进一步研究的关键领域，以充分利用其促进健康的功能。

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引用次数: 0

Synthesis and in vitro studies of doxorubicin-Cu2+ prodrug and glucose oxidase co-encapsulated oxidized hyaluronic acid/carboxymethyl chitosan hydrogels on breast cancer cell line 4T1 阿霉素- cu2 +前药与葡萄糖氧化酶共包封氧化透明质酸/羧甲基壳聚糖水凝胶在乳腺癌细胞株4T1上的合成及体外研究

IF 2.5 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research

Pub Date : 2026-01-01 Epub Date: 2025-11-25 DOI: 10.1016/j.carres.2025.109769

Shuhan Li , Huwei Bian , Yuting Tan , Yan Li , Dan Shou , Tao Jiang , Yong Kong

Breast cancer is one of the most life-threatening malignancies worldwide, and the chemotherapy of breast cancer is often hindered by drug resistance and systemic toxicity. Developing safer and more efficient multi-therapy strategies is therefore urgently needed. Doxorubicin (DOX) is first combined with Cu²⁺ through coordination bonds, and the resulting DOX-Cu²⁺ prodrug is then co-encapsulated with glucose oxidase (GOx) in the oxidized hyaluronic acid (OHA)/carboxymethyl chitosan (CMCS) hydrogels cross-linked through the Schiff base reaction. The weakly acidic environment of tumor cells can cause the degradation of the hydrogels and the dissociation of the DOX-Cu²⁺ complex, resulting in the release of DOX for chemotherapy. The released Cu²⁺ can be reduced to Cu ⁺ by glutathione (GSH), and the Cu⁺ can participate in the Fenton-like reaction with the overexpressed H₂O₂ in tumor cells to produce hydroxyl radicals (·OH) for chemodynamic therapy (CDT). During the degradation of the hydrogels, the GOx is also released, which can deplete the glucose in tumor cells for starvation therapy; meanwhile, the H₂O₂ generated during the GOx-catalyzed oxidation of glucose can in turn participate in the Fenton-like reaction with Cu⁺ to enhance CDT. The results of cytotoxicity assay indicate that the OHA/CMCS hydrogels have good biocompatibility, while the DOX-Cu²⁺ and GOx co-encapsulated hydrogels (OHA/CMCS/DOX-Cu²⁺/GOx) display significant cytotoxicity due to the multi-therapy synergies of chemotherapy, enhanced CDT and starvation therapy.

乳腺癌是世界上最危及生命的恶性肿瘤之一，乳腺癌的化疗常常受到耐药性和全身毒性的阻碍。因此，迫切需要开发更安全、更有效的综合治疗策略。多柔比星（DOX）首先通过配位键与Cu2+结合，生成的DOX-Cu2+前药通过席夫碱反应与葡萄糖氧化酶（GOx）在氧化透明质酸(OHA)/羧甲基壳聚糖（CMCS）水凝胶中共包被。肿瘤细胞的弱酸性环境可使水凝胶降解，DOX- cu2 +复合物解离，释放DOX用于化疗。释放的Cu2+可被谷胱甘肽（GSH）还原为Cu+， Cu+可与肿瘤细胞中过表达的H2O2参与fenton样反应，产生羟基自由基（·OH），用于化学动力治疗（CDT）。在水凝胶降解的过程中，GOx也被释放出来，它可以消耗肿瘤细胞中的葡萄糖，用于饥饿治疗；同时，gox催化葡萄糖氧化过程中产生的H2O2又能与Cu+参与类fenton反应，增强CDT。细胞毒性实验结果表明，OHA/CMCS水凝胶具有良好的生物相容性，而DOX-Cu2+/GOx共包被水凝胶（OHA/CMCS/DOX-Cu2+/GOx）由于化疗、增强CDT和饥饿治疗的多疗法协同作用而表现出显著的细胞毒性。

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引用次数: 0

Preparation and characterization of chitosan/citric acid composite film and its application in blueberry preservation 壳聚糖/柠檬酸复合膜的制备、表征及其在蓝莓保鲜中的应用

IF 2.5 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research

Pub Date : 2026-01-01 Epub Date: 2025-10-24 DOI: 10.1016/j.carres.2025.109714

Lan Wang, Jiaxin Ma, Xuya Zhang, Shenghui He, Yiheng Duan

Chitosan (CS) is widely utilized as a natural preservative for fruits and vegetables; however, its practical application is constrained by inferior mechanical properties and low water resistance. In this study, citric acid (CA) was incorporated into the chitosan matrix to leverage its multifunctional carboxyl groups and inherent antibacterial properties, aiming to enhance both the mechanical and antibacterial performance of the resulting composite films. The structure of the CS/CA composite films was characterized using Fourier transform infrared spectroscopy (FT-IR), ¹H nuclear magnetic resonance (¹H NMR) spectroscopy, X-ray diffraction (XRD), and scanning electron microscopy (SEM). The physicochemical properties, antimicrobial activity, and potential for blueberry preservation of CS/CA films with varying CA content were systematically evaluated. Results indicated that the incorporation of CA induced cross-linking of CS chains via hydrogen bonding and amidation, leading to significant improvements in optical transparency, thermal stability, and hydrophilicity. The mechanical properties of the composite films were remarkably enhanced, with the maximum tensile strength increasing by up to fourfold compared to that of pure CS films. Composite films, particularly CS/CA4–CS/CA6, exhibited strong antibacterial effects against S. aureus and E. coli. Preservation tests on blueberries demonstrated the superior efficacy of the CS/CA composite films, especially CS/CA7, which showed optimal performance with only 5.6 % weight loss, maintained firmness at 228.3 g, the highest anthocyanin retention, and a 46.75 % reduction in decay rate compared to the control. These findings indicate that CS/CA composite films are promising environmentally friendly materials for active food packaging applications.

壳聚糖（CS）是一种广泛应用于果蔬的天然防腐剂；然而，其实际应用受到较差的力学性能和较低的耐水性的限制。本研究将柠檬酸（CA）加入到壳聚糖基质中，利用其多功能羧基和固有的抗菌性能，旨在提高复合膜的机械性能和抗菌性能。采用傅里叶变换红外光谱（FT-IR）、1H核磁共振（1H NMR）、x射线衍射（XRD）和扫描电镜（SEM）对CS/CA复合膜的结构进行了表征。系统评价了不同CA含量CS/CA膜的理化性质、抑菌活性和保存蓝莓的潜力。结果表明，CA的掺入诱导CS链通过氢键和酰胺化发生交联，从而显著改善了CS链的光学透明度、热稳定性和亲水性。复合膜的力学性能得到了显著提高，最大抗拉强度比纯CS膜提高了4倍。复合膜，特别是CS/ CA4-CS /CA6对金黄色葡萄球菌和大肠杆菌具有较强的抗菌作用。对蓝莓的保鲜试验表明，CS/CA复合膜的保鲜效果较好，其中CS/CA7的保鲜效果最佳，其蓝莓质量仅下降5.6%，硬度保持在228.3 g，花青素保有量最高，腐烂率比对照降低46.75%。这些研究结果表明，CS/CA复合薄膜是一种很有前途的环保材料，可用于活性食品包装。

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引用次数: 0

Structural characterization, in vitro antioxidant and lipid-lowering activities of purified polysaccharides from hawthorn leaf 山楂叶纯化多糖的结构表征、体外抗氧化和降脂活性。

IF 2.5 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research

Pub Date : 2025-12-01 Epub Date: 2025-10-03 DOI: 10.1016/j.carres.2025.109695

Ting Yang , Yang Yang , Rong Chen , Pinyi Gao , Danqi Li , Xuegui Liu

This study investigates the structural features and lipid-regulating mechanisms of hawthorn leaf polysaccharides (HLPs). Three acidic polysaccharides (HLP-1, HLP-2, and HLP-3) were isolated from hawthorn leaves and characterized via high-performance gel permeation chromatography (HPGPC), ion chromatography (IC), methylation analysis, and nuclear magnetic resonance (NMR) spectroscopy. Structural analyses revealed their molecular weights were 10.19 kDa, 400.38 kDa, and 435.52 kDa, respectively, with primary composition of galacturonic acid, galactose, and rhamnose. The Congo red assay indicated potential ordered aggregation with molecular weight-dependent thermal stability. Among the three, HLP-1 demonstrated the most potent in vitro bioactivity, including superior antioxidant capacity; in HepG2 cells, it most effectively reduced TG, TC, and LDL-c levels and increased HDL-c, outperforming HLP-2 and HLP-3. Mechanistically, HLP-1's hypolipidemic effect was linked to suppression of the SREBP-1c pathway. Furthermore, this study establishes the structure-activity relationship between HLPs' structural properties and lipid-lowering effects, laying a foundation for future HLP-based therapeutic interventions in metabolic diseases.

本研究探讨了山楂叶多糖（hlp）的结构特征和脂质调节机制。从山楂叶中分离得到三种酸性多糖（HLP-1、HLP-2和HLP-3），并通过高效凝胶渗透色谱（HPGPC）、离子色谱（IC）、甲基化分析和核磁共振（NMR）光谱对其进行了表征。结构分析表明，它们的分子量分别为10.19 kDa、400.38 kDa和435.52 kDa，主要成分为半乳糖醛酸、半乳糖和鼠李糖。刚果红分析表明潜在的有序聚集具有分子量依赖的热稳定性。其中，HLP-1表现出最强的体外生物活性，包括较强的抗氧化能力；在HepG2细胞中，它最有效地降低TG、TC和LDL-c水平，并增加HDL-c水平，优于HLP-2和HLP-3。从机制上讲，HLP-1的降血脂作用与抑制SREBP-1c途径有关。进一步，本研究建立了hlp结构特性与降脂作用的构效关系，为今后基于hlp的代谢性疾病治疗干预奠定基础。

{"title":"Structural characterization, in vitro antioxidant and lipid-lowering activities of purified polysaccharides from hawthorn leaf","authors":"Ting Yang , Yang Yang , Rong Chen , Pinyi Gao , Danqi Li , Xuegui Liu","doi":"10.1016/j.carres.2025.109695","DOIUrl":"10.1016/j.carres.2025.109695","url":null,"abstract":"<div><div>This study investigates the structural features and lipid-regulating mechanisms of hawthorn leaf polysaccharides (HLPs). Three acidic polysaccharides (HLP-1, HLP-2, and HLP-3) were isolated from hawthorn leaves and characterized via high-performance gel permeation chromatography (HPGPC), ion chromatography (IC), methylation analysis, and nuclear magnetic resonance (NMR) spectroscopy. Structural analyses revealed their molecular weights were 10.19 kDa, 400.38 kDa, and 435.52 kDa, respectively, with primary composition of galacturonic acid, galactose, and rhamnose. The Congo red assay indicated potential ordered aggregation with molecular weight-dependent thermal stability. Among the three, HLP-1 demonstrated the most potent <em>in vitro</em> bioactivity, including superior antioxidant capacity; in HepG2 cells, it most effectively reduced TG, TC, and LDL-c levels and increased HDL-c, outperforming HLP-2 and HLP-3. Mechanistically, HLP-1's hypolipidemic effect was linked to suppression of the <em>SREBP-1c</em> pathway. Furthermore, this study establishes the structure-activity relationship between HLPs' structural properties and lipid-lowering effects, laying a foundation for future HLP-based therapeutic interventions in metabolic diseases.</div></div>","PeriodicalId":9415,"journal":{"name":"Carbohydrate Research","volume":"558 ","pages":"Article 109695"},"PeriodicalIF":2.5,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145238056","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Structures of W77F/W212F and W77F/W212F Toxascaris leonine galectin complex with glucose W77F/W212F和W77F/W212F狮子座弓形虫凝集素与葡萄糖复合物的结构

IF 2.5 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research

Pub Date : 2025-12-01 Epub Date: 2025-09-02 DOI: 10.1016/j.carres.2025.109657

Min Seon Ha , Chang Woo Han , Mi Suk Jeong , Se Bok Jang

Galectins are glycan-binding proteins (GBPs) characterized by conserved carbohydrate recognition domains (CRDs). Galectin-9, which contains two CRDs, regulates immune responses through interactions with glycoproteins. However, the full-length structure of galectin-9 remains unresolved. Toxascaris leonina galectin (Tl-gal), a homolog of human galectin-9 with ∼35 % sequence identity, shares a similar overall structure, including conserved residues like tryptophan. In Tl-gal, the W77 and W212 residues are directly involved in carbohydrate binding. Here, we present the crystal structures of the Tl-gal W77F/W212F mutant in apo form or complexed with glucose. Comparative structural analysis revealed that mutation of these tryptophan residues induces conformational changes in the overall structure of Tl-gal. These findings underscore the critical role played by conserved tryptophan residues in maintaining galectin structure and glycan-binding function.

半乳糖凝集素是一种以保守的碳水化合物识别结构域（CRDs）为特征的聚糖结合蛋白（GBPs）。半乳糖凝集素-9含有两种crd，通过与糖蛋白的相互作用调节免疫反应。然而，半乳糖凝集素-9的全长结构尚不清楚。狮子座弓形虫的半乳糖凝集素（Tl-gal）是人类半乳糖凝集素-9的同源物，具有~ 35%的序列同源性，具有相似的整体结构，包括色氨酸等保守残基。在Tl-gal中，W77和W212残基直接参与碳水化合物的结合。在这里，我们展示了Tl-gal W77F/W212F突变体载子形式或与葡萄糖络合的晶体结构。比较结构分析表明，这些色氨酸残基的突变引起了Tl-gal整体结构的构象变化。这些发现强调了保守的色氨酸残基在维持凝集素结构和聚糖结合功能中所起的关键作用。

引用次数: 0

Identification, purification and functional characterization of a thermostable marine chitinase for potential fungal control via chitin degradation mechanism 一种耐热性海洋几丁质酶的鉴定、纯化及功能表征

IF 2.5 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research

Pub Date : 2025-12-01 Epub Date: 2025-09-03 DOI: 10.1016/j.carres.2025.109654

Atheena P.V. , Keyur Raval , Ritu Raval

The growing prevalence of treatment-resistant Candida species highlights an urgent need for innovative antifungal therapies. The current range of antifungals, limited to polyenes, azoles, and echinocandins, are becoming insufficient due to the rise of resistance, including cross-resistance among fungal strains. Marine environment is an underexplored reservoir of unique enzymes which can be extremophilic. This study presents the cloning and expression of a chitinase gene from the bacterium Bacillus thuringiensis (BtChi), expressed in an E. coli system, yielding a protein with a molecular weight of approximately 71 kDa. Disc diffusion and MIC experiments indicated that 5 μg/mL chitinase efficiently suppressed the growth of Candida albicans. Initial characterization identified the optimal activity at 40 °C and pH 7.0. The enzyme retained over 75 % activity across a pH range of 4–8 and a temperature range of 30–70 °C after 120 min. Activity was further enhanced by 24 % with 100 mM Na⁺. Kinetic parameters with colloidal chitin revealed K_m and V_max values to be 0.05 mg/mL and 1.37 U/mL respectively. This study holds the potential of developing a potent natural anti-fungal against the present day chemical counterparts.

耐药念珠菌种类的日益流行突出了迫切需要创新的抗真菌治疗。目前的抗真菌药物范围仅限于多烯类、唑类和棘白菌素，由于耐药性的上升，包括真菌菌株之间的交叉耐药性，这些抗真菌药物正变得不足。海洋环境是一个尚未开发的独特酶的储存库，这些酶可能是极端嗜酸性的。本研究从苏云金芽孢杆菌（Bacillus thuringiensis, BtChi）中克隆并表达了一个几丁质酶基因，该基因在大肠杆菌系统中表达，产生一个分子量约为71 kDa的蛋白。圆盘扩散和MIC实验表明，5 μg/mL几丁质酶能有效抑制白色念珠菌的生长。初步鉴定在40°C和pH 7.0条件下活性最佳。在pH为4-8、温度为30-70°C的条件下，酶在120分钟后仍保持75%以上的活性。100 mM Na+使活性进一步增强24%。胶体甲壳素的动力学参数显示Km和Vmax分别为0.05 mg/mL和1.37 U/mL。这项研究有潜力开发一种有效的天然抗真菌药物，对抗目前的化学对应物。

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引用次数: 0

Editorial – VSI: Chitosan and its derivatives: biomedicine and beyond 编辑- VSI：壳聚糖及其衍生物：生物医学及其应用。

IF 2.5 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research

Pub Date : 2025-12-01 Epub Date: 2025-09-11 DOI: 10.1016/j.carres.2025.109669

引用次数: 0

First total synthesis of cyanopterin, a pterin glycoside isolated from a cyanobacterium 首次合成了从一种蓝藻菌中分离出来的蝶呤苷

IF 2.5 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research

Pub Date : 2025-12-01 Epub Date: 2025-10-21 DOI: 10.1016/j.carres.2025.109710

Tadashi Hanaya, Yuta Maeda, Kazumasa Ejiri

The first total synthesis and structural identification of cyanopterin, a pterin glycoside isolated from the cyanobacterium Synechocystis sp. PCC 6803, has been accomplished. The synthesis was achieved by convergent coupling of three key derivatives: d-glucuronate, d-galactose, and 6-hydroxymethylpterin. An α-selective glycosylation enabled efficient construction of the glucuronate–galactose disaccharide, while subsequent β-exclusive glycosylation with the 6-hydroxymethylpterin derivative furnished the desired pterin–disaccharide glycoside. Final deprotection provided cyanopterin in its natural form, allowing confirmation of its precise structure.

本文首次合成并鉴定了从藻胞菌中分离得到的一种蝶呤苷类化合物蓝翅素。通过三个关键衍生物：d-葡萄糖醛酸盐、d-半乳糖和6-羟甲基蝶呤的聚合偶联实现了合成。α-选择性糖基化可以有效地构建葡萄糖醛酸-半乳糖双糖，而随后与6-羟甲基蝶呤衍生物进行β-特异性糖基化可以得到所需的蝶呤-双糖糖苷。最后的去保护提供了自然形态的蓝翅虫素，从而确认了其精确的结构。

引用次数: 0

Silicon-polysaccharide fluorescent nanocomposite for everolimus delivery and theranostic application in clear cell renal cell carcinoma 硅-多糖荧光纳米复合物在透明细胞肾细胞癌中依维莫司的递送和治疗应用

IF 2.5 3区化学 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY

Carbohydrate Research

Pub Date : 2025-12-01 Epub Date: 2025-09-25 DOI: 10.1016/j.carres.2025.109688

Zhihong Lv, Yuping Xu, Huiying Liu, Hui Li, Hongyan Zhai

Everolimus showed therapeutic promise in treating clear cell renal cell carcinoma (ccRCC), yet its efficacy was limited by poor bioavailability and weak tumor targeting. In this study, we developed a multifunctional Co(II)-based MOF (CP1) using H₄L and bpp ligands, forming a 3D (4,8)-connected framework. To enhance stability and functionality, CP1 was coated with sodium alginate (SA) and APTMS, and further modified with a fluorescent benzopyranone derivative (compound 1) via Ullmann-type coupling, yielding 1-SA-APTMS@CP1. The final nanocarrier, 1-SA-APTMS@CP1@EVE, exhibited a high surface area (98.3 m²/g), mesoporosity (2–6 nm), and strong structural integrity. It enabled dual-channel fluorescence detection of GSH and NAD(P)H, with detection limits of 233 pM and 65 nM, respectively. In vitro, the system effectively inhibited ccRCC cell proliferation and downregulated TNFRSF18, a key immunomodulatory gene. This study provides a redox-responsive, fluorescence-trackable delivery platform for everolimus, offering potential for targeted and immune-synergistic therapy in ccRCC.

依维莫司在治疗透明细胞肾细胞癌（ccRCC）方面显示出良好的治疗前景，但其生物利用度差，肿瘤靶向性弱，限制了其疗效。在这项研究中，我们利用H4L和bpp配体开发了一个多功能的Co（II）基MOF (CP1)，形成了一个3D（4,8）连接的框架。为了提高CP1的稳定性和功能性，我们用海藻酸钠（SA）和APTMS包被CP1，并通过ullmann型偶联进一步用荧光苯并吡喃酮衍生物（化合物1）修饰CP1，得到1-SA-APTMS@CP1。最终得到的纳米载体1-SA-APTMS@CP1@EVE具有较高的比表面积（98.3 m2/g）、介孔（2-6 nm）和较强的结构完整性。双通道荧光检测GSH和NAD(P)H，检测限分别为233pm和65nm。在体外实验中，该系统有效抑制了ccRCC细胞的增殖，下调了关键的免疫调节基因TNFRSF18。这项研究为依维莫司提供了一个氧化还原反应性的、荧光可追踪的给药平台，为ccRCC的靶向和免疫协同治疗提供了潜力。

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引用次数: 0