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The Wedelolactone Derivative Inhibits Estrogen Receptor-Mediated Breast, Endometrial, and Ovarian Cancer Cells Growth
- Source :
- BioMed Research International, Vol 2014 (2014), BioMed Research International
- Publication Year :
- 2014
- Publisher :
- Hindawi Limited, 2014.
-
Abstract
- Estrogen and estrogen receptor (ER)-mediated signaling pathways play important roles in the etiology and progression of human breast, endometrial, and ovarian cancers. Attenuating ER activities by natural products and their derivatives is a relatively practical strategy to control and reduce breast, endometrial, and ovarian cancer risk. Here, we found 3-butoxy-1,8,9-trihydroxy-6H-benzofuro[3,2-c]benzopyran-6-one (BTB), a new derivative of wedelolactone, could effectively inhibit the 17-estradiol (E2)-induced ER transactivation and suppress the growth of breast cancer as well as endometrial and ovarian cancer cells. Our results indicate that 2.5 μM BTB effectively suppresses ER-positive, but not ER-negative, breast, endometrial, and ovarian cancer cells. Furthermore, our data indicate that BTB can modulate ER transactivation and suppress the expression of E2-mediated ER target genes (Cyclin D1, E2F1, and TERT) in the ER-positive MCF-7, Ishikawa, and SKOV-3 cells. Importantly, this BTB mediated inhibition of ER activity is selective since BTB does not suppress the activities of other nuclear receptors, including glucocorticoid receptor and progesterone receptor, suggesting that BTB functions as a selective ER signaling inhibitor with the potential to treat breast, endometrial, and ovarian cancers.
- Subjects :
- medicine.medical_specialty
Article Subject
medicine.drug_class
Estrogen receptor
lcsh:Medicine
Breast Neoplasms
General Biochemistry, Genetics and Molecular Biology
Transactivation
Breast cancer
Coumarins
Internal medicine
Progesterone receptor
medicine
Humans
Cyclin D1
Cell Proliferation
Ovarian Neoplasms
General Immunology and Microbiology
Estradiol
business.industry
lcsh:R
Estrogen Receptor alpha
General Medicine
medicine.disease
Endometrial Neoplasms
Gene Expression Regulation, Neoplastic
Endocrinology
Nuclear receptor
Estrogen
Cancer research
MCF-7 Cells
Female
Ovarian cancer
business
Estrogen receptor alpha
Signal Transduction
Research Article
Subjects
Details
- Language :
- English
- ISSN :
- 23146141 and 23146133
- Volume :
- 2014
- Database :
- OpenAIRE
- Journal :
- BioMed Research International
- Accession number :
- edsair.doi.dedup.....5996d6e7fbc768e0b9953b64aa3a450b