期刊
APPLIED SCIENCES-BASEL
卷 12, 期 13, 页码 -出版社
MDPI
DOI: 10.3390/app12136531
关键词
resveratrol derivative; tubulin; actin; migration; invasion; breast cancer; spheroids; docking studies
类别
资金
- Italian Ministry of Research and University (MIUR)
- MIUR
- AIRC (Associazione Italiana per la Ricerca sul Cancro) [IG20122]
- PAC (Progetto Strategico Regionale Calabria Alta Formazione) Calabria 2014/2020-Asse Prioritario 12, Linea B, Azione 10.5.12
- Italian Minister of University and Research [MIUR] [D.M. 1062, 1062_R13_GREEN]
- PON R&I 2014-2020-project from Area di Specializzazione Salute [ARS01_00568]
- Italian Ministry of Health
Chemotherapy is widely used for cancer treatment but it lacks selectivity on healthy cells and can lead to the development of drug resistance. However, a better understanding of cancer genetics has led to the development of new targeted anticancer treatments that show high specificity and reduced toxicity. Multi-target drug design is also becoming a key focus in drug research and development. In this study, a resveratrol derivative showed interesting anti-inflammatory and anti-proliferative properties against breast cancer cells, as well as the ability to disrupt cytoskeleton dynamics and interfere with migration and metastasis. This compound could be a promising starting point for the development of safer and more effective multi-targeted agents.
Chemotherapy is commonly used for cancer treatment, however the lack of selectivity on healthy cells and the development of resistance phenomena are the major issues. A better understanding of cancer genetics helped the development of new targeted anticancer treatments, which permit drug delivery with high specificity and lower toxicity. Moreover, the multi-target drug design concept represents the current trend for future drug research and development. Starting from good results previously obtained by our research group on the resveratrol (RSV) phenylacetamide derivative 2, which displayed an interesting anti-inflammatory and anti-proliferative activity towards the breast cancer cells MCF-7 and MDA-MB-231, we identified other features, as the ability to perturb the cytoskeleton dynamics and interfere with the migration and metastatic processes. In vitro and in silico studies demonstrate that the derivative 2 is a tubulin and actin polymerization inhibitor and an actin depolymerization promotor. In addition, it interferes with the metastatic potential in both the breast cancer cells, inhibiting the in vitro cell migration and decreasing the spheroids number. These promising results demonstrate that the RSV phenylacetamide derivative 2 could be an important starting point in the discovery and development of safer and more efficacy multi-targeted agents.
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