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叶酸受体介导的靶向作用增强了叶提取物的细胞毒性、疗效和选择性:及证据。

Folic Acid Receptor-Mediated Targeting Enhances the Cytotoxicity, Efficacy, and Selectivity of Leaf Extract: and Evidence.

作者信息

Yu Yue, Wang Jia, Kaul Sunil C, Wadhwa Renu, Miyako Eijiro

机构信息

Department of Materials and Chemistry, Nanomaterials Research Institute, National Institute of Advanced Industrial Science and Technology, Tsukuba, Japan.

DAILAB, DBT-AIST International Center for Translational and Environmental Research (DAICENTER), AIST, Tsukuba, Japan.

出版信息

Front Oncol. 2019 Jul 4;9:602. doi: 10.3389/fonc.2019.00602. eCollection 2019.

Abstract

Nanomedicine holds great potential for drug delivery to achieve more effective and safer cancer treatment. Earlier, we reported that the alcoholic extract of leaves (i-Extract) has selective cancer cell killing activity. Herein, we developed a folate receptor-targeting i-Extract nanocomplex (FRi-ExNC) that suspends well in water and possesses enhanced selective anticancer activity in both and assays. Comparative analyses of folate receptor (FR)-positive and -negative cells revealed that FRi-ExNC caused a stronger decrease in Cyclin D/Cdk4 and anti-apoptotic protein Bcl-2, as well as a higher increase in the growth arrest regulating protein p21 and pro-apoptotic protein PARP-1, in FR-enriched cancer cells. Our results demonstrate that FRi-ExNC could be a natural source-based nanomedicine for targeted cancer therapy.

摘要

纳米医学在药物递送方面具有巨大潜力,可实现更有效、更安全的癌症治疗。此前,我们报道过树叶的乙醇提取物(i-Extract)具有选择性癌细胞杀伤活性。在此,我们开发了一种叶酸受体靶向的i-Extract纳米复合物(FRi-ExNC),它在水中具有良好的悬浮性,并且在体外和体内实验中均具有增强的选择性抗癌活性。对叶酸受体(FR)阳性和阴性细胞的比较分析表明,在富含FR的癌细胞中,FRi-ExNC导致细胞周期蛋白D/细胞周期蛋白依赖性激酶4(Cyclin D/Cdk4)和抗凋亡蛋白Bcl-2的下降更为明显,同时生长停滞调节蛋白p21和促凋亡蛋白PARP-1的增加幅度更高。我们的结果表明,FRi-ExNC可能是一种基于天然来源的纳米药物,用于靶向癌症治疗。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4b7/6621239/9352f192d6d4/fonc-09-00602-g0001.jpg

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