Preparation, characterization, and anticancer activity evaluation of Ganoderma lucidum polysaccharide/5-fluorouracil conjugate

IF 2.3 4区化学 Q3 CHEMISTRY, PHYSICAL

Colloid and Polymer Science Pub Date : 2025-05-21 DOI:10.1007/s00396-025-05414-7

Ying Wang, YunXia Yang, Daliang Zhu, Hongmei Zhang, Yanqing Wang

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Abstract

Polysaccharide-based drug delivery systems have gained significant attention due to their biocompatibility and potential for targeted therapy. In this study, we utilized Ganoderma lucidum polysaccharides (GLP) as a macromolecular carrier to synthesize polysaccharide drug conjugates by forming ester bonds with 5-fluorouracil (5-FU) derivatives (5-FUAC). This not only improves the solubility and stability of 5-FU but also enhances its targeted delivery to tumor tissues, potentially reducing systemic toxicity. Utilizing Ganoderma lucidum polysaccharides (GLP) as a macromolecular carrier, we successfully synthesized GLP-5-FU conjugates by forming ester bonds with 5-fluorouracil derivatives (5-FUAC). These conjugates were then characterized using spectrum analysis technologies. The drug loading capacities of 5-FU in the GLP-5-FU conjugates were found to be approximately 4.7%. Morphological observations revealed that the GLP-5-FU conjugates had a regular spherical shape. In terms of drug release, 5-FU was found to be released faster at pH 6.8 compared to pH 7.4. To investigate the dynamic viscoelastic behavior of GLP and GLP-5-FU conjugates in water, dynamic rheology analysis was conducted. In terms of cytotoxicity, the GLP-5-FU conjugates exhibited greater inhibition of proliferation compared to 5-FU and GLP alone in HeLa, 786-O, and SKOV3 cells. Furthermore, the GLP-5-FU conjugates showed lower cytotoxicity to 293A cells.

Graphical Abstract

Abstract Image

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灵芝多糖/5-氟尿嘧啶偶联物的制备、表征及抗癌活性评价

基于多糖的药物传递系统由于其生物相容性和靶向治疗的潜力而受到了极大的关注。本研究以灵芝多糖（GLP）为大分子载体，与5-氟尿嘧啶（5-FU）衍生物（5-FUAC）形成酯键，合成多糖药物偶联物。这不仅提高了5-FU的溶解度和稳定性，而且增强了其对肿瘤组织的靶向递送，潜在地降低了全身毒性。以灵芝多糖（GLP）为大分子载体，通过与5-氟尿嘧啶衍生物（5-FUAC）形成酯键，成功合成了GLP-5- fu缀合物。然后使用光谱分析技术对这些共轭物进行了表征。GLP-5-FU偶联物中5-FU的载药量约为4.7%。形态学观察表明，GLP-5-FU共轭物呈规则的球形。在药物释放方面，5-FU在pH值为6.8时比pH值为7.4时释放更快。为了研究GLP和GLP-5- fu共轭物在水中的动态粘弹性行为，进行了动态流变学分析。在细胞毒性方面，在HeLa、786-O和SKOV3细胞中，GLP-5-FU缀合物比5-FU和GLP单独具有更大的增殖抑制作用。此外，GLP-5-FU偶联物对293A细胞具有较低的细胞毒性。图形抽象

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来源期刊

Colloid and Polymer Science 化学-高分子科学

CiteScore

4.60

自引率

4.20%

发文量

111

审稿时长

2.2 months

期刊介绍： Colloid and Polymer Science - a leading international journal of longstanding tradition - is devoted to colloid and polymer science and its interdisciplinary interactions. As such, it responds to a demand which has lost none of its actuality as revealed in the trends of contemporary materials science.