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用于三阴性乳腺癌中芹菜素治疗的仿生纳米颗粒平台的开发。

Development of a biomimetic nanoparticle platform for apigenin therapy in triple-negative breast cancer.

作者信息

Wang Chenyang, Ren Xiaojing, Han Yanmei, Nan Ding, Zhang Yajing, Gao Zairong

机构信息

Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.

Hubei Province Key Laboratory of Molecular Imaging, Wuhan, China.

出版信息

Front Oncol. 2025 May 16;15:1521529. doi: 10.3389/fonc.2025.1521529. eCollection 2025.

DOI:10.3389/fonc.2025.1521529
PMID:40452850
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12122512/
Abstract

BACKGROUND

This study investigates the therapeutic potential and mechanisms of Apigenin (AGN) in treating triple-negative breast cancer (TNBC). Although AGN is recognized for its anti-tumor properties, its specific mechanisms in TNBC remain unclear.

METHODS

To identify key genes associated with AGN's effects on breast cancer, we utilized network pharmacology, conducting Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses. We developed a macrophage membrane-coated nanomicelle system (m@peg-AGN) to enhance drug delivery and facilitate immune evasion.

RESULTS

Our analyses identified 21 overlapping genes between AGN and breast cancer, including CDH1, TP53, and CCND1, critical in cancer progression. The m@peg-AGN system demonstrated superior immune evasion and effective tumor targeting, resulting in good tumor suppression without detected toxicity in major organs.

CONCLUSIONS

This study demonstrated the targeted tumor genes to TNBC for AGN, then innovatively integrates network pharmacology with biomimetic nanotechnology, developing a novel m@peg-AGN delivery system for TNBC treatment. This system enhanced the AGN's water solubility and increased the accumulation to the tumor site. This compound has exhibited good anti-tumor effects , thereby could advance the treatment for TNBC.

摘要

背景

本研究探讨芹菜素（AGN）治疗三阴性乳腺癌（TNBC）的治疗潜力及其机制。尽管AGN因其抗肿瘤特性而受到认可，但其在TNBC中的具体机制仍不清楚。

方法

为了确定与AGN对乳腺癌作用相关的关键基因，我们利用网络药理学进行基因本体（GO）和京都基因与基因组百科全书（KEGG）通路富集分析。我们开发了一种巨噬细胞膜包被的纳米胶束系统（m@peg-AGN），以增强药物递送并促进免疫逃逸。

结果

我们的分析确定了AGN与乳腺癌之间的21个重叠基因，包括CDH1、TP53和CCND1，这些基因在癌症进展中至关重要。m@peg-AGN系统表现出卓越的免疫逃逸和有效的肿瘤靶向性，在主要器官未检测到毒性的情况下实现了良好的肿瘤抑制效果。

结论

本研究确定了AGN针对TNBC的靶向肿瘤基因，然后创新性地将网络药理学与仿生纳米技术相结合，开发了一种用于TNBC治疗 的新型m@peg-AGN递送系统。该系统提高了AGN的水溶性并增加了在肿瘤部位的蓄积。该化合物已表现出良好的抗肿瘤效果，从而可能推动TNBC的治疗进展。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/7caf2e87ef1f/fonc-15-1521529-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/df36c451110e/fonc-15-1521529-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/12cb6b55c266/fonc-15-1521529-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/61c35730e1a6/fonc-15-1521529-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/e5a922b405b0/fonc-15-1521529-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/74344cd99953/fonc-15-1521529-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/227532005b7b/fonc-15-1521529-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/7caf2e87ef1f/fonc-15-1521529-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/df36c451110e/fonc-15-1521529-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/12cb6b55c266/fonc-15-1521529-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/61c35730e1a6/fonc-15-1521529-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/e5a922b405b0/fonc-15-1521529-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/74344cd99953/fonc-15-1521529-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/227532005b7b/fonc-15-1521529-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5b26/12122512/7caf2e87ef1f/fonc-15-1521529-g007.jpg

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本文引用的文献

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Apigenin: Molecular Mechanisms and Therapeutic Potential against Cancer Spreading.芹菜素：抗癌转移的分子机制与治疗潜力。
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Macrophage-derived biomimetic nanoparticles enhanced SDT combined with immunotherapy inhibited tumor growth and metastasis.巨噬细胞衍生的仿生纳米颗粒增强的 SDT 联合免疫疗法抑制肿瘤生长和转移。
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Impact of TP53 mutations in Triple Negative Breast Cancer.TP53突变在三阴性乳腺癌中的影响。
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Network Pharmacology and Molecular Docking-Based Mechanism Study to Reveal the Protective Effect of Salvianolic Acid C in a Rat Model of Ischemic Stroke.基于网络药理学和分子对接的机制研究揭示丹酚酸C在大鼠缺血性脑卒中模型中的保护作用
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Luteolin and its derivative apigenin suppress the inducible PD-L1 expression to improve anti-tumor immunity in KRAS-mutant lung cancer.木犀草素及其衍生物芹菜素可抑制诱导型程序性死亡配体1（PD-L1）的表达，以增强KRAS突变型肺癌的抗肿瘤免疫力。
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