Size-Dependent Biological Effects of Quercetin Nanocrystals

被引：19

作者：

Liu, Qian ^{[1
]}

Yang, Xi ^{[1
]}

Sun, Jianxu ^{[1
]}

Yu, Fanglin ^{[1
]}

Zhang, Hui ^{[1
]}

Gao, Jing ^{[1
]}

Zheng, Aiping ^{[1
]}

机构：

[1] Beijing Inst Pharmacol & Toxicol, State Key Lab Toxicol & Med Countermeasures, 27th Taiping Rd, Beijing 100850, Peoples R China

来源：

MOLECULES | 2019年 / 24卷 / 07期

基金：

中国国家自然科学基金;

关键词：

quercetin; nanocrystals; anti-tumor; invasion; signal transducer and activator of transcription 3 signal pathway; PROSTATE-CANCER; PROTEIN CORONA; IN-VITRO; PACLITAXEL NANOSUSPENSIONS; LUNG-CANCER; CELL-LINE; FORMULATION; MIGRATION; DELIVERY; GROWTH;

D O I：

10.3390/molecules24071438

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Quercetin (QE) is an attractive natural compound for cancer prevention due to its beneficial anti-oxidative and anti-proliferative effects. However, QE is poorly soluble in water and slightly soluble in oil, which results in its low oral bioavailability and limits its application in the clinic. The aim of this study was to prepare QE nanocrystals (QE-NCs) with improved solubility and high drug loading, furthermore, the size-dependent anti-cancer effects of QE-NCs were studied. We prepared QE-NCs with three different particle sizes by wet milling, then, cell proliferation, migration and invasion were studied in A549 cells. The QE-NCs had antitumor effects in a dose- and size-dependent manner. Compared with the large particles, the small particles had a strong inhibitory impact on cell biological effects (p < 0.05 or p < 0.01). Moreover, Western blot assay indicated that QE-NCs may inhibit the migration and invasion of A549 cells by inhibiting the STAT3 signaling pathway, and the particle size may have an effect on this process. In this study, it was proven that NCs could dramatically enhance the anticancer efficacy of QE at the cellular level. In addition, particle size had a considerable influence on the dissolution behavior and antitumor effects of NCs.

引用

页数：14

共 55 条

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