Antiproliferative Activity and Cellular Uptake of Evodiamine and Rutaecarpine based on 3D Tumour Models

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Guo , H , Liu , D , Gao , B , Zhang , X , You , M , Ren , H , Zhang , H , Almeida Santos , H & Xu , F 2016 , ' Antiproliferative Activity and Cellular Uptake of Evodiamine and Rutaecarpine based on 3D Tumour Models ' , Molecules , vol. 21 , no. 7 , 954 , pp. 954 . https://doi.org/10.3390/molecules21070954

Title: Antiproliferative Activity and Cellular Uptake of Evodiamine and Rutaecarpine based on 3D Tumour Models
Author: Guo, Hui; Liu, Dongmei; Gao, Bin; Zhang, Xiaohui; You, Minli; Ren, Hui; Zhang, Hongbo; Almeida Santos, Helder; Xu, Feng
Contributor: University of Helsinki, Faculty of Pharmacy
University of Helsinki, Faculty of Pharmacy
Date: 2016-07-21
Language: eng
Number of pages: 13
Belongs to series: Molecules
ISSN: 1420-3049
URI: http://hdl.handle.net/10138/166523
Abstract: Evodiamine (EVO) and rutaecarpine (RUT) are promising anti-tumor drug candidates. The evaluation of the anti-proliferative activity and cellular uptake of EVO and RUT in 3D multicellular spheroids of cancer cells would better recapitulate the native situation and thus better reflect an in vivo response to the treatment. Herein, we employed the 3D culture of MCF-7 and SMMC-7721 cells based on hanging drop method and evaluated the anti-proliferative activity and cellular uptake of EVO and RUT in 3D multicellular spheroids, and compared the results with those obtained from 2D monolayers. The drugs’ IC50 values were significantly increased from the range of 6.4–44.1 μM in 2D monolayers to 21.8–138.0 μM in 3D multicellular spheroids, which may be due to enhanced mass barrier and reduced drug penetration in 3D models. The fluorescence of EVO and RUT was measured via fluorescence spectroscopy and the cellular uptake of both drugs was characterized in 2D tumor models. The results showed that the cellular uptake concentrations of RUT increased with increasing drug concentrations. However, the EVO concentrations uptaken by the cells showed only a small change with increasing drug concentrations, which may be due to the different solubility of EVO and Rut in solvents. Overall, this study provided a new vision of the anti-tumor activity of EVO and RUT via 3D multicellular spheroids and cellular uptake through the fluorescence of compounds.
Subject: 317 Pharmacy
116 Chemical sciences
cellular uptake
auto-fluorescence
3D multicellular spheroids
hanging drop method
IN-VITRO
BREAST-CANCER
DRUG DISCOVERY
CELLS
CAMPTOTHECIN
DERIVATIVES
APOPTOSIS
LINES
TRANSFORMATION
MECHANISM
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