scholarly journals Spatholobus suberectusColumn Extract Inhibits Estrogen Receptor Positive Breast Cancer via Suppressing ER MAPK PI3K/AKT Pathway

2016 ◽  
Vol 2016 ◽  
pp. 1-13 ◽  
Author(s):  
Jia-Qi Sun ◽  
Gan-Lin Zhang ◽  
Yi Zhang ◽  
Nan Nan ◽  
Xu Sun ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Chinese Herb ◽  
Luciferase Reporter ◽  
Akt Pathway ◽  
G1 Phase ◽  
Reporter System ◽  
Estrogen Receptor Positive ◽  
Spatholobus Suberectus ◽  
Mcf 7

Although Chinese herbal compounds have long been alternatively applied for cancer treatment in China, their treatment effects have not been sufficiently investigated. The Chinese herbSpatholobus suberectusis commonly prescribed to cancer patients. HPLC analysis has shown that the main components ofSpatholobus suberectusare flavonoids that can be classified as phytoestrogens, having a structure similar to estrogen. This study was designed to investigate the effects ofSpatholobus suberectuscolumn extract (SSCE) on the estrogen receptor-positive (ER+) breast cancer cell line MCF-7 and its possible molecular mechanism. In our study, MTT assay was performed to evaluate cell viability. The results show that SSCE (80, 160, and 320 μg/ml) significantly decreased the viability of MCF-7 cells. SSCE also triggered apoptosis, arrested the cell cycle at the G0/G1 phase, and inhibited cell migration. A dual-luciferase reporter system showed that SSCE suppressed intranuclear p-ER activity; Western blot analysis confirmed the repressed expression of phosphorylated-ER alpha (p-ERα), ERK1/2, p-ERK1/2, AKT, p-AKT, p-mTOR, PI3K, and p-PI3K, indicating that SSCE suppressed the MAPK PI3K/AKT signaling pathway. Collectively, our results suggest that SSCE causes apoptosis, an arrest in the G0/G1 phase, and a decrease in migration in ER+ MCF-7 cells via hypoactivity of the ER and suppression of the MAPK PI3K/AKT pathway.

A potential estrogen mimetic effect of a bis(ethyl)polyamine analogue on estrogen receptor positive MCF-7 breast cancer cells

Amino Acids ◽  
2011 ◽  
Vol 42 (2-3) ◽  
pp. 899-911 ◽  
Author(s):  
Irina Nayvelt ◽  
Shali John ◽  
Hui-Chen Hsu ◽  
PingAr Yang ◽  
Wensheng Liu ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Cancer Cells ◽  
Breast Cancer Cells ◽  
Estrogen Receptor Positive ◽  
Polyamine Analogue ◽  
Mcf 7

scholarly journals Coenzyme Q0 Enhances Ultraviolet B–Induced Apoptosis in Human Estrogen Receptor–Positive Breast (MCF-7) Cancer Cells

2016 ◽  
Vol 16 (3) ◽  
pp. 385-396 ◽  
Author(s):  
Hui-Min Wang ◽  
Hsin-Ling Yang ◽  
Varadharajan Thiyagarajan ◽  
Tzu-Hsiang Huang ◽  
Pei-Jane Huang ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Reactive Oxygen Species ◽  
Dna Damage ◽  
Estrogen Receptor ◽  
Ultraviolet B ◽  
Oxygen Species ◽  
Estrogen Receptor Positive ◽  
Human Estrogen Receptor ◽  
Induced Apoptosis ◽  
Mcf 7

Coenzyme Q0 (CoQ0; 2,3-dimethoxy-5-methyl-1,4-benzoquinone), a major active constituent of Antrodia camphorata, has been shown to inhibit human triple-negative breast cancer (MDA-MB-231) cells through induction of apoptosis and cell-cycle arrest. Ecological studies have suggested a possible association between ultraviolet B (UVB) radiation and reduction in the risk of breast cancer. However, the underlying mechanism of the combination of CoQ0 and UVB in human estrogen receptor–positive breast cancer (MCF-7) remains unclear. In this study, the possible effect of CoQ0 on inducing apoptosis in MCF-7 cells under exposure to low-dose UVB (0.05 J/cm2) has been investigated. CoQ0 treatment (0-35 µM, for 24-72 hours) inhibits moderately the growth of breast cancer MCF-7 cells, and the cell viability was significantly decreased when the cells were pretreated with UVB irradiation. It was noted that there was a remarkable accumulation of subploid cells, the so-called sub-G1 peak, in CoQ0-treated cells by using flow cytometric analysis, which suggests that the viability reduction observed after treatment may result from apoptosis induction in MCF-7 cells. CoQ0 caused an elevation of reactive oxygen species, as indicated by dichlorofluorescein fluorescence, and UVB pretreatment significantly increased CoQ0-induced reactive oxygen species generation in MCF-7 cells. In addition, cells were exposed to CoQ0, and the induction of DNA damage was evaluated by single-cell gel electrophoresis (comet assay). CoQ0-induced DNA damage was remarkably enhanced by UVB pretreatment. Furthermore, CoQ0 induced apoptosis in MCF-7 cells, which was associated with PARP degradation, Bcl-2/Bax dysregulation, and p53 expression as shown by western blot. Collectively, these findings suggest that CoQ0 might be an important supplemental agent for treating patients with breast cancer.

scholarly journals Synergistic Cytotoxicity between Elephantopus scaber and Tamoxifen on MCF-7-Derived Multicellular Tumor Spheroid

2021 ◽  
Vol 2021 ◽  
pp. 1-15
Author(s):  
Wan Yong Ho ◽  
Sok Sian Liew ◽  
Swee Keong Yeap ◽  
Noorjahan Banu Alitheen
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Tumor Spheroid ◽  
Multicellular Tumor Spheroid ◽  
Synergistic Cytotoxicity ◽  
Estrogen Receptor Positive ◽  
Elephantopus Scaber ◽  
Combinatorial Treatment ◽  
Mcf 7 ◽  
Positive Breast Cancer

Elephantopus scaber Linn, a traditional herb, exhibited anticancer properties, and it was cytotoxic against the monolayer estrogen receptor-positive breast cancer cell line, MCF-7, in the previous study. In order to determine the potential of E. scaber as a complementary medicine for breast cancer, this study aimed to evaluate the synergism between E. scaber and tamoxifen in cytotoxicity using MCF-7 in the form of 3-dimensional multicellular tumor spheroid (MCTS) cultures. MCTS represents a more reliable model for studying drug penetration as compared to monolayer cells due to its greater resemblance to solid tumor. Combination of E. scaber ethanol extract and tamoxifen, which were used in concentrations lower than their respective IC50 values, had successfully induced apoptosis on MCTS in this study. The combinatorial treatment showed >58% increase of lactate dehydrogenase release in cell media, cell cycle arrest at the S phase, and 1.3 fold increase in depolarization of mitochondrial membrane potential. The treated MCTS also experienced DNA fragmentation; this had been quantified by TUNEL-positive assay, which showed >64% increase in DNA damaged cells. Higher externalization of phospatidylserine and distorted and disintegrated spheroids stained by acridine orange/propidium iodide showed that the cell death was mainly due to apoptosis. Further exploration showed that the combinatorial treatment elevated caspases-8 and 9 activities involving both extrinsic and intrinsic pathways of apoptosis. The treatment also upregulated the expression of proapoptotic gene HSP 105 and downregulated the expression of prosurvival genes such as c-Jun, ICAM1, and VEGF. In conclusion, these results suggested that the coupling of E. scaber to low concentration of tamoxifen showed synergism in cytotoxicity and reducing drug resistance in estrogen receptor-positive breast cancer.

Synthesis, Biological Investigation and Docking Study of Novel Chromen Derivatives as Anti-Cancer Agents

2019 ◽  
Vol 19 (9) ◽  
pp. 1150-1160 ◽  
Author(s):  
Pritam N. Dube ◽  
Nikhil S. Sakle ◽  
Sachin A. Dhawale ◽  
Shweta A. More ◽  
Santosh N. Mokale
Keyword(s):  
Breast Cancer ◽  
Estrogen Receptor ◽  
Docking Study ◽  
Compound C ◽  
Anti Cancer ◽  
Estrogen Receptor Positive ◽  
Cytotoxic Compounds ◽  
Cancer Activity ◽  
Mcf 7

Background: According to the latest global cancer data, cancer burden rises to 18.1 million new cases and 9.6 million cancer deaths in 2018. Among that female breast cancer ranks as the fifth leading cause of death (627000 deaths, 6.6%). The main causative factor involved in breast cancer development and progression is the Estrogen Receptor (ER) which is the essential target for anti-cancer drug discovery. Since millennia ER-α has been considered as an oncology mark for the treatment of breast cancer. Methods: A series of novel 6-methyl-3-(3-oxo-1-phenyl-3-(4-(2-(piperidin-1-yl)ethoxy)phenyl)propyl)-2Hchromen- 2-one was designed, synthesized and screened for their anti-breast cancer activity against estrogen receptor-positive MCF-7, ZR-75-1 and negative MDA-MB-435 human breast cancer cell lines. Estrogen level of all the potent cytotoxic compounds were measured on day 30 of intoxication was compared with the control and N-methyl-N-nitrosourea (MNU) group. The docking study was performed to predict binding orientation towards the estrogen receptor-α. Results: Among the synthesized compounds C-3, C-5 and C-15 were showing potent cytotoxicity against estrogen receptor-positive MCF-7. The potent cytotoxic compounds C-3, C-5 and C-15 were further evaluated for in vivo anti-cancer activity by MNU induced mammary carcinoma in female sprague-dawley rats. The in vivo anticancer activity result shows that the compound C-5 has protuberant affinity towards estrogen receptor as standard TAM (Tamoxifen). The docking of the synthesized chromen derivatives showed interaction modes comparable to that of the co-crystallized ligands. Conclusion: The designed class has very promising starting point for the development and further improvement in anti-breast cancer class of drugs.

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