A novel targeted anticancer drug delivery strategy: Cnidium officinale polysaccharide conjugated with carboxymethyl-5-fluorouracil and folic acid for ovarian cancer therapy

文献类型: 外文期刊

第一作者: Zhang, Yutong

作者: Zhang, Yutong;Zhang, Yanjun;Zhang, Yutong;Palanisamy, Subramanian;Kwon, Mi-Hye;Kou, Fang;Uthamapriya, Rajavel Arumugam;Lee, Dongki;Lee, Dong-Jin;You, Sangguan;Palanisamy, Subramanian;Kwon, Mi-Hye;Uthamapriya, Rajavel Arumugam;You, Sangguan;Ge, Yunfei;Bao, Honghui;Bao, Honghui;Bao, Honghui

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关键词: Polysaccharide; 5-fluorouracil; Folic acid; Anticancer; Drug deliver

期刊名称:INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES ( 影响因子:8.5; 五年影响因子:8.7 )

ISSN: 0141-8130

年卷期: 2025 年 285 卷

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收录情况: SCI

摘要: To mitigate adverse reactions induced by 5-fluorouracil (5-FU), Cnidium officinale fraction 2 (F2) polysaccharides served as the macromolecular carrier, facilitating its reaction with carboxymethyl-5-fluorouracil (C-5-FU) for producing F2-C-5-FU. Subsequently, this compound could react with folic acid (FA) through the ester bond, forming F2-C-5-FU-FA, as verified through NMR analysis. The in vitro anticancer efficacy of F2-C-5-FU-FA was evaluated using SKOV-3 cells that expressed folate receptor (FR) and FR-deficient A549 cells, showing greater cytotoxicity in the SKOV-3 cell line due to the FRs on the cell membrane. In vivo experiments were conducted on SKOV-3-bearing xenograft mice using an in vivo imaging system (IVIS). Animals injected with F2-C-5-FU-FA exhibited significantly stronger targeting of tumor tissue compared to those injected with F2-C-5-FU. These findings highlighted enhanced drug delivery and accumulation in targeted tumor regions facilitated by folatetargeted conjugates. Moreover, F2-C-5FU-FA showed reduced cardiac toxicity in mice and minimal spleen accumulation, indicating a negligible effect on the immune system. Overall, this study introduced a novel strategy for achieving highly efficient anticancer drug delivery into tumor cells that express FR.

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