1. Ethoxy mansonone G as an anticancer agent in estrogen receptor-positive and endocrine-resistant breast cancer.
- Author
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Chonsut P, Mahalapbutr P, Pradubyat N, Chavasiri W, Wonganan P, and Ketchart W
- Subjects
- Antineoplastic Agents, Hormonal administration & dosage, Antineoplastic Agents, Hormonal chemistry, Breast Neoplasms pathology, Drug Resistance, Neoplasm, Drug Synergism, Estrogen Receptor alpha metabolism, Ethyl Ethers administration & dosage, Ethyl Ethers chemistry, Ethyl Ethers pharmacology, Female, Gene Expression Regulation, Neoplastic, Humans, MCF-7 Cells, Molecular Docking Simulation, Naphthoquinones chemistry, Naphthoquinones pharmacology, Receptors, Estrogen metabolism, Tamoxifen administration & dosage, Tamoxifen pharmacology, Antineoplastic Agents, Hormonal pharmacology, Breast Neoplasms drug therapy, Cell Proliferation drug effects, Naphthoquinones administration & dosage
- Abstract
Objectives: To study anticancer effects, underlying mechanism and safety of ethoxy mansonone G (EMG) which is the potent derivative of mansonone G (MG) in breast cancer cells., Methods: Anticancer, antimigration, anti-invasion effects and anchorage-independent growth were investigated by MTT, scratch, matrigel invasion and soft agar assays. Estrogen receptor (ER)-targeted genes and endocrine-resistant genes were assessed by RT-PCR and Western blot., Key Findings: Ethoxy mansonone G is the most potent MG derivative and has anticancer effects in ER-positive, endocrine-resistant and ER-negative breast cancer cells. Our results demonstrated that EMG can significantly inhibit estrogen-induced cell proliferation and the expression of ER-targeted genes in ER-positive breast cancer cells, suggesting the anti-estrogenic property of EMG which is consisting with the virtual molecular docking that EMG could possibly bind to the ERα. Moreover, EMG has synergistic effect with tamoxifen in endocrine-resistant cells. EMG also inhibited cell proliferation, invasion and anchorage-independent growth by reducing expression of genes involved in endocrine resistance and invasive factors during the metastatic process., Conclusion: Ethoxy mansonone G has an anticancer effect in breast cancer cells and is possible to use as a therapeutic agent in patients with breast cancer., (© 2019 Royal Pharmaceutical Society.)
- Published
- 2019
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