Cytotoxic effects of tamoxifen in breast cancer cells

Abstract

Aim: To investigate the cytotoxic effects of tamoxifen on the breast cancer cell line (MCF7). Methods:The cytotoxic effects of tamoxifen on MCF7 cells were investigated using caspase-9 activity and high content screening assays. Apoptosis mechanisms following tamoxifen treatment were also investigated. Results:The most significant cytotoxic effect of tamoxifen in MCF7 cells was a half-maximal inhibitory concentration (IC 50 ) of 4.506 µg/mL. A significant increase in caspase-9 activity was also observed when MCF7 cells were treated with tamoxifen (5 µg/mL). Furthermore, increased cell membrane permeability, cytochrome c level, and nuclear intensity were observed with tamoxifen (100 µg/mL) compared with doxorubicin (20 µg/mL) treatment. However, a noticeable decrease in cell viability and mitochondrial membrane permeability was observed with tamoxifen (100 µg/mL) treatment compared with doxorubicin (20 µg/mL) as a positive control. Conclusion:Tamoxifen showed in vitro cytotoxic effects in MCF7 cells as demonstrated by high-content screening and caspase-9 activity assays. Tamoxifen inhibits estrogen mechanisms, although toxic effect was observed.

Synthesis, Anti-proliferative Activity, and Molecular Docking Study of New Series of 1,3-5-Triazine Schiff Base Derivatives

“…In addition, the substituent on the benzylidene ring showed great impact on the anti-proliferative activity, where the chloro derivatives showed better anti-cancer activities compared to other unsubstituted and bromo substituent analogs. The obtained results are consistent with the previously reported results, where the presence of piperidine on the s -triazine ring and the presence of an electronegative atom on the benzylidene increased the compounds activity against the cancer cells [ 32 , 33 , 34 , 35 ].…”

“…s -Triazine-hydrazone derivatives 4a-r were screened for their anti-proliferative activity against two representative human cancer cell lines; breast cancer MCF-7 and colon cancer HCT-116 and compared with tamoxifen [ 35 ] as a reference compound using (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Based on the data illustrated in Table 1 ( Supporting information, Method S1 ), the s -triazine-hydrazone derivatives displayed varied anti-proliferative activity, with better efficacy on MCF-7 than HCT-116 cells.…”

The Proteomics and Metabolomics Analysis for Screening the Molecular Targets of Action of β-Eudesmol in Cholangiocarcinoma

“…Cytc, the hemoprotein located in cell mitochondria, plays role in mitochondrial electron transport, cardiolipin peroxidation (Kagan et al, 2005), ROS formation, and cell apoptosis (Cai et al, 1998). Regarding cell apoptosis, several compounds such as tamoxifen (an anticancer drug for breast cancer) and botulin (triterpene from plants, e.g., birch trees) induce the release of Cytc from mitochondria in a dose-dependent manner (Hassan et al, 2018;Zhou et al, 2018). BAG3, the protein belonged to the member of BAG family, plays a role in the protection of cells from the apoptosis process by stabilizing antiapoptotic Bcl-2 family proteins as bcl-2 and bcl-XL (Kim et al, 2013).…”

Evaluation the effect of several anticancer drugs on Vietnamese breast cancer cells

“…The primary mechanism in the response of cancer cells with chemotherapy is the activation of apoptotic pathways. The cell viability is an important parameter and is directly associated with the cytotoxic effects of a drug 19 . In this research, DOX and MMC caused apoptosis both in MCF-7 and VNBRCA cells, the IC50 values of DOX and MMC on VNBRCA cells were higher than on MCF-7 cells ( Table 1).…”