Newly Modified Nanoformulation of Quercetin as Promising Chemotherapeutic Anticancer Agent

Q3 Biochemistry, Genetics and Molecular Biology

Biointerface Research in Applied Chemistry Pub Date : 2022-10-31 DOI:10.33263/briac134.387

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引用次数: 1

Abstract

Previous studies have demonstrated the potential anticancer effect of quercetin (QUR). However, water insolubility and less bioavailability of QUR reduce its efficiency in cancer therapy. So, this study aims to develop a nanoformulation of quercetin (QURnp) and evaluate its anticancer effect against Ehrlich ascites carcinoma (EAC)-bearing mice compared with native QUR. QUR- loaded pluronic nanoparticles (QURnp) were prepared and characterized. To investigate the anticancer effect of QUR and QURnp, histopathological, ultrastructural, immunohistochemical, cell cycle analysis, western blot, and qRT-PCR studies were performed on EAC tumor cells, as well as antioxidant biomarkers. The results showed that QURnp destroyed tumor cells and significantly elevated antioxidant status with the reduction in MDA and NO levels. QURnp caused mitochondrial degeneration in tumor cells. Furthermore, QURnp completely reduced tumor growth by inhibiting the IL-6/STAT3 signaling pathway, inducing cell cycle arrest at the G1/S phase via overexpression of p27 and suppression of angiogenesis via downregulation in VEGF gene expression. Moreover, immunohistochemical studies indicated that QURnp showed significant inhibition of proliferation marker Ki-67 and anti-apoptotic marker Bcl-2. This study demonstrated that QURnp is a promising anticancer agent superior to native QUR.

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新改性槲皮素纳米制剂作为抗癌化疗药物的研究进展

先前的研究已经证明槲皮素（QUR）具有潜在的抗癌作用。然而，QUR的水不溶性和生物利用度较低，降低了其在癌症治疗中的效率。因此，本研究旨在开发槲皮素（QURnp）的纳米制剂，并与天然槲皮素进行比较，评价其对埃立克腹水癌（EAC）荷瘤小鼠的抗癌作用。制备并表征了负载QUR的pluronic纳米粒子（QURnp）。为了研究QUR和QURnp的抗癌作用，对EAC肿瘤细胞以及抗氧化生物标志物进行了组织病理学、超微结构、免疫组织化学、细胞周期分析、蛋白质印迹和qRT-PCR研究。结果表明，QURnp破坏肿瘤细胞，并显著提高抗氧化状态，降低MDA和NO水平。QURnp引起肿瘤细胞线粒体变性。此外，QURnp通过抑制IL-6/STAT3信号通路，通过p27的过表达诱导细胞周期停滞在G1/S期，并通过下调VEGF基因表达抑制血管生成，从而完全减少肿瘤生长。此外，免疫组织化学研究表明，QURnp对增殖标志物Ki-67和抗凋亡标志物Bcl-2表现出显著的抑制作用。该研究表明，QURnp是一种有前景的抗癌剂，优于天然QUR。

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来源期刊

Biointerface Research in Applied Chemistry CHEMISTRY, APPLIED-

CiteScore

4.80

自引率

0.00%

发文量

256

期刊介绍： Biointerface Research in Applied Chemistry is an international and interdisciplinary research journal that focuses on all aspects of nanoscience, bioscience and applied chemistry. Submissions are solicited in all topical areas, ranging from basic aspects of the science materials to practical applications of such materials. With 6 issues per year, the first one published on the 15th of February of 2011, Biointerface Research in Applied Chemistry is an open-access journal, making all research results freely available online. The aim is to publish original papers, short communications as well as review papers highlighting interdisciplinary research, the potential applications of the molecules and materials in the bio-field. Our aim is to encourage scientists to publish their experimental and theoretical results in as much detail as possible.