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负载齐墩果酸/熊果酸的聚乳酸-羟基乙酸共聚物纳米粒在不同细胞系中的体外细胞毒性

In Vitro Cytotoxicity of Oleanolic/Ursolic Acids-Loaded in PLGA Nanoparticles in Different Cell Lines.

作者信息

Silva Amélia M, Alvarado Helen L, Abrego Guadalupe, Martins-Gomes Carlos, Garduño-Ramirez Maria L, García María L, Calpena Ana C, Souto Eliana B

机构信息

Centre for Research and Technology of Agro-Environmental and Biological Sciences (CITAB), University of Trás-os Montes e Alto Douro (UTAD), Quinta de Prados, 5001-801 Vila Real, Portugal.

Department of Biology and Environment, UTAD, Quinta de Prados, 5001-801 Vila Real, Portugal.

出版信息

Pharmaceutics. 2019 Jul 24;11(8):362. doi: 10.3390/pharmaceutics11080362.

Abstract

Oleanolic (OA) and ursolic (UA) acids are recognized triterpenoids with anti-cancer properties, showing cell-specific activity that can be enhanced when loaded into polymeric nanoparticles. The cytotoxic activity of OA and UA was assessed by Alamar Blue assay in three different cell lines, i.e., HepG2 (Human hepatoma cell line), Caco-2 (Human epithelial colorectal adenocarcinoma cell line) and Y-79 (Human retinoblastoma cell line). The natural and synthetic mixtures of these compounds were tested as free and loaded in polymeric nanoparticles in a concentration range from 2 to 32 µmol/L. The highest tested concentrations of the free triterpene mixtures produced statistically significant cell viability reduction in HepG2 and Caco-2 cells, compared to the control (untreated cells). When loaded in the developed PLGA nanoparticles, no differences were recorded for the tested concentrations in the same cell lines. However, in the Y-79 cell line, a decrease on cell viability was observed when testing the lowest concentration of both free triterpene mixtures, and after their loading into PLGA nanoparticles.

摘要

齐墩果酸(OA)和熊果酸(UA)是公认的具有抗癌特性的三萜类化合物,表现出细胞特异性活性,当负载于聚合物纳米颗粒中时其活性可增强。通过alamar蓝法在三种不同的细胞系中评估了OA和UA的细胞毒性活性,即HepG2(人肝癌细胞系)、Caco-2(人结肠直肠腺癌上皮细胞系)和Y-79(人视网膜母细胞瘤细胞系)。这些化合物的天然和合成混合物以游离形式以及负载于聚合物纳米颗粒中的形式进行测试,浓度范围为2至32 μmol/L。与对照(未处理细胞)相比,游离三萜混合物的最高测试浓度在HepG2和Caco-2细胞中产生了具有统计学意义的细胞活力降低。当负载于所制备的聚乳酸-羟基乙酸共聚物(PLGA)纳米颗粒中时,在相同细胞系中对测试浓度未记录到差异。然而,在Y-79细胞系中,当测试两种游离三萜混合物的最低浓度以及将它们负载于PLGA纳米颗粒后,观察到细胞活力有所下降。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/75f0/6723971/01d2617fbb79/pharmaceutics-11-00362-g001.jpg

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