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柚皮素载药固体脂质纳米粒对 RIN5F 胰腺β细胞的细胞毒性作用 自噬阻断。

Cytotoxic Impact of Naringenin-Loaded Solid Lipid Nanoparticles on RIN5F Pancreatic β Cells Autophagy Blockage.

机构信息

Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

Student Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran.

出版信息

Recent Adv Drug Deliv Formul. 2024;18(4):304-314. doi: 10.2174/0126673878297658240804192222.

DOI:10.2174/0126673878297658240804192222
PMID:39356101
Abstract

BACKGROUND

Autophagy plays a crucial role in modulating the proliferation of cancer diseases. However, the application of Naringenin (Nar), a compound with potential benefits against these diseases, has been limited due to its poor solubility and bioavailability.

OBJECTIVE

This study aimed to develop solid lipid nanoparticles (Nar-SLNs) loaded with Nar to enhance their therapeutic impact.

METHODS

experiments using Rin-5F cells exposed to Nar and Nar-SLNs were carried out to investigate the protective effects of Nar and its nanoformulation against the pancreatic cancer cell line of Rin-5F.

RESULTS

Treatment with Nar and Nar-SLN led to an increase in autophagic markers (Akt, LC3, Beclin1, and ATG genes) and a decrease in the level of miR-21. Both Nar and Nar-SLN treatments inhibited cell proliferation and reduced the expression of autophagic markers. Notably, Nar-SLNs exhibited greater efficacy compared to free Nar.

CONCLUSION

These findings suggest that SLNs effectively enhance the cytotoxic impact of Nar, making Nar-SLNs a promising candidate for suppressing or preventing Rin-5F cell growth.

摘要

背景

自噬在调节癌症疾病的增殖方面起着至关重要的作用。然而,由于其溶解度和生物利用度差,具有潜在益处的柚皮素(Nar)化合物的应用受到限制。

目的

本研究旨在开发负载柚皮素的固体脂质纳米粒(Nar-SLNs),以增强其治疗效果。

方法

用柚皮素和 Nar-SLNs 处理 Rin-5F 细胞,研究柚皮素及其纳米制剂对 Rin-5F 胰腺癌细胞系的保护作用。

结果

柚皮素和 Nar-SLN 处理导致自噬标志物(Akt、LC3、Beclin1 和 ATG 基因)增加,miR-21 水平降低。柚皮素和 Nar-SLN 处理均抑制细胞增殖并降低自噬标志物的表达。值得注意的是,Nar-SLNs 的效果优于游离柚皮素。

结论

这些发现表明 SLNs 可有效增强 Nar 的细胞毒性作用,使 Nar-SLNs 成为抑制或预防 Rin-5F 细胞生长的有前途的候选物。

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Front Endocrinol (Lausanne). 2023 Mar 29;14:1141516. doi: 10.3389/fendo.2023.1141516. eCollection 2023.
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Pre-clinical and clinical importance of miR-21 in human cancers: Tumorigenesis, therapy response, delivery approaches and targeting agents.miR-21 在人类癌症中的临床前和临床重要性:肿瘤发生、治疗反应、递药途径和靶向制剂。
Pharmacol Res. 2023 Jan;187:106568. doi: 10.1016/j.phrs.2022.106568. Epub 2022 Nov 21.
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