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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

作者： Zhang, Yutong 1 ; Palanisamy, Subramanian 3 ; Kwon, Mi-Hye 3 ; Ge, Yunfei 5 ; Kou, Fang 3 ; Uthamapriya, Rajavel Arumugam 3 ; Lee, Dongki 3 ; Lee, Dong-Jin 3 ; Bao, Honghui 6 ; You, Sangguan 3 ; Zhang, Yanjun 1 ;

作者机构： 1.Chinese Acad Trop Agr Sci, Spice & Beverage Res Inst, Natl Ctr Important Trop Crops Engn & Technol Res, Key Lab Proc Suitabil & Qual Control Special Trop, Hainan 571533, Peoples R China

2.Chinese Acad Trop Agr Sci, Sanya Res Inst, Sanya 572025, Hainan, Peoples R China

3.Gangneung Wonju Natl Univ, Dept Marine Food Sci & Technol, 120 Gangneung, Gangwon 210702, South Korea

4.Gangneung Wonju Natl Univ, East Coast Life Sci Inst, 120 Gangneung, Kangnung 210702, South Korea

5.Yunnan Agr Univ, Coll Food Sci & Technol, Kunming 650201, Yunnan, Peoples R China

6.Hubei Univ Arts & Sci, Sch Food Sci & Technol, Xiangyang 441053, Peoples R China

7.Hubei Univ Arts & Sci, Sch Chem Engn, Xiangyang 441053, Hubei, Peoples R China

8.Hubei Univ Arts & Sci, Hubei Prov Engn & Technol Res Ctr Food Ingredients, Xiangyang, Hubei, Peoples R China

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

页码：

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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