| Full text | |
| Author(s): |
Zanesco-Fontes, Ideli
;
Lopes Silva, Ana Carolina
;
da Silva, Patricia Bento
;
Duarte, Jonatas Lobato
;
Di Filippo, Leonardo Delello
;
Chorilli, Marlus
;
Cominetti, Marcia Regina
;
Baptista Moreno Martin, Ana Carolina
Total Authors: 8
|
| Document type: | Journal article |
| Source: | AAPS PHARMSCITECH; v. 22, n. 5, p. 8-pg., 2021-05-18. |
| Abstract | |
The apoptotic, cytotoxic, and cytostatic activities for [10]-gingerol in triple-negative breast cancer cells (TNBCs) were already reported. However, despite these important antitumor activities, the compound has the disadvantage to have a hydrophobic characteristic, hindering in vivo administration. To surpass this issue, in this study we have created a [10]-gingerol-loaded nanoemulsion (10GNE) in order to increase the stability and solubility of the compound. The nanoemulsion was characterized and tested for its cytotoxic, cytostatic, and apoptotic effects on a panel of murine and human TNBC cell lines, as well as non-tumor cells, and compared with a [10]-gingerol-free nanoemulsion (NE) and with [10]-gingerol itself. Except for the murine 4T1.13 cell line, the IC50 of the free 10G molecule, after 72 h of incubation, was higher in all cell lines tested, both murine and human, demonstrating therefore the efficacy of the 10GNE regarding cytotoxicity. In murine tumor cells, 60 mu M 10GNE was able to arrest cell cycle at sub-G0 phase and induce apoptosis, leading to 48% and 78% of total cell death in 4T1.13 and 4T1Br4 murine tumor cells, respectively. This represents an improvement compared to 10G-free molecule that only induced 74% of total apoptosis at 100 mu M in 4T1Br4 cells. Taken together, our results show that nanoformulation preserved the [10]-gingerol cytotoxic and cytostatic properties and improved its apoptotic function on murine TNBC cell lines. These data open new perspectives to a more suitable drug-delivery approach for [10]-gingerol for TNBC treatment that should be further demonstrated using in vivo assays. (AU) | |
| FAPESP's process: | 18/17756-4 - [10]-gingerol formulation: in vitro studies in triple-negative breast cancer cells |
| Grantee: | Ideli Zanesco Fontes Baptista |
| Support Opportunities: | Scholarships in Brazil - Scientific Initiation |
| FAPESP's process: | 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery |
| Grantee: | Glaucius Oliva |
| Support Opportunities: | Research Grants - Research, Innovation and Dissemination Centers - RIDC |
| FAPESP's process: | 16/23202-6 - SENSITIZER EFFECTS AND MECHANISMS OF ACTION OF [10]-GINGEROL IN COMBINATION WITH DOXORUBICIN FOR BREAST CANCER TREATMENT: IN VITRO AND IN VIVO STUDIES |
| Grantee: | Ana Carolina Baptista Moreno Martin |
| Support Opportunities: | Scholarships in Brazil - Post-Doctoral |