1. N -(2-Hydroxyphenyl)-2-Propylpentanamide (HO-AAVPA) Induces Apoptosis and Cell Cycle Arrest in Breast Cancer Cells, Decreasing GPER Expression.
- Author
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Prestegui Martel B, Chávez-Blanco AD, Domínguez-Gómez G, Dueñas González A, Gaona-Aguas P, Flores-Mejía R, Somilleda-Ventura SA, Rodríguez-Cortes O, Morales-Bárcena R, Martínez Muñoz A, Mejia Barradas CM, Mendieta Wejebe JE, and Correa Basurto J
- Subjects
- Humans, Female, MCF-7 Cells, Cell Line, Tumor, Cell Proliferation drug effects, Gene Expression Regulation, Neoplastic drug effects, Antineoplastic Agents pharmacology, Antineoplastic Agents chemistry, Amides pharmacology, Amides chemistry, Apoptosis drug effects, Receptors, G-Protein-Coupled metabolism, Receptors, G-Protein-Coupled genetics, Receptors, Estrogen metabolism, Breast Neoplasms metabolism, Breast Neoplasms pathology, Breast Neoplasms drug therapy, Breast Neoplasms genetics, Cell Cycle Checkpoints drug effects
- Abstract
In this work, we performed anti-proliferative assays for the compound N -(2-hydroxyphenyl)-2-propylpentanamide (HO-AAVPA) on breast cancer (BC) cells (MCF-7, SKBR3, and triple-negative BC (TNBC) MDA-MB-231 cells) to explore its pharmacological mechanism regarding the type of cell death associated with G protein-coupled estrogen receptor (GPER) expression. The results show that HO-AAVPA induces cell apoptosis at 5 h or 48 h in either estrogen-dependent (MCF-7) or -independent BC cells (SKBR3 and MDA-MB-231). At 5 h, the apoptosis rate for MCF-7 cells was 68.4% and that for MDA-MB-231 cells was 56.1%; at 48 h, that for SKBR3 was 61.6%, that for MCF-7 cells was 54.9%, and that for MDA-MB-231 (TNBC) was 43.1%. HO-AAVPA increased the S phase in MCF-7 cells and reduced the G2/M phase in MCF-7 and MDA-MB-231 cells. GPER expression decreased more than VPA in the presence of HO-AAVPA. In conclusion, the effects of HO-AAVPA on cell apoptosis could be modulated by epigenetic effects through a decrease in GPER expression.
- Published
- 2024
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