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Size-Dependent Biological Effects of Quercetin Nanocrystals

State Key Laboratory of Toxicology and Medical Countermeasures, Beijing Institute of Pharmacology and Toxicology, 27th Taiping Road, Haidian District, Beijing 100850, China
Authors to whom correspondence should be addressed.
Academic Editors: Alejandro Baeza, Fernando Novio and Juan Luis Paris
Molecules 2019, 24(7), 1438;
Received: 25 February 2019 / Revised: 10 April 2019 / Accepted: 11 April 2019 / Published: 11 April 2019
(This article belongs to the Special Issue Nanomaterials for Cancer Diagnosis and Therapy)
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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. View Full-Text
Keywords: quercetin; nanocrystals; anti-tumor; invasion; signal transducer and activator of transcription 3 signal pathway quercetin; nanocrystals; anti-tumor; invasion; signal transducer and activator of transcription 3 signal pathway

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Liu, Q.; Yang, X.; Sun, J.; Yu, F.; Zhang, H.; Gao, J.; Zheng, A. Size-Dependent Biological Effects of Quercetin Nanocrystals. Molecules 2019, 24, 1438.

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