Baicalein, unlike 4-hydroxytamoxifen but similar to G15, suppresses 17β-estradiol-induced cell invasion, and matrix metalloproteinase-9 expression and activation in MCF-7 human breast cancer cells

  • Authors:
    • Yan Chen
    • Duan‑Yang Hong
    • Jing Wang
    • Jun Ling‑Hu
    • Yan‑Yan Zhang
    • Di Pan
    • Yi‑Ni Xu
    • Ling Tao
    • Hong Luo
    • Xiang‑Chun Shen
  • View Affiliations

  • Published online on: June 2, 2017     https://doi.org/10.3892/ol.2017.6298
  • Pages: 1823-1830
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Abstract

Estrogen performs an important role in the growth and development of breast cancer. There are at least three major receptors, including estrogen receptor (ER)α and β, and G protein‑coupled receptor 30 (GPR30), which mediate the actions of estrogen through using transcriptional and rapid non‑genomic signaling pathways. Flavonoids have been considered candidates for chemopreventive agents in breast cancer. Baicalein, the primary flavonoid derived from the root of Scutellaria baicalensis Georgi, has been reported to exert an anti‑estrogenic effect. In the present study, the effects of baicalein on 17β‑estradiol (E2)‑induced cell invasion, and matrix metalloproteinase‑9 (MMP‑9) expression and activation were investigated. Furthermore, its effects were compared with that of the active form of the ER modulator tamoxifen 4‑hydroxytamoxifen (OHT) and the GPR30 antagonist G15 in ERα‑ and GPR30‑positive MCF‑7 breast cancer cells. The results demonstrated that OHT failed to prevent E2‑induced cell invasion, upregulation and proteolytic activity of MMP‑9. However, baicalein was able to significantly suppress these E2‑induced effects. Furthermore, E2‑stimulated invasion, and MMP‑9 expression and activation were significantly attenuated following G15 treatment. In addition, baicalein significantly inhibited G‑1, a specific GPR30 agonist, induced invasion, and reduced G‑1 promoted expression and activity of MMP‑9, consistent with effects of G15. The results of the present study suggest that baicalein is a therapeutic candidate for GPR30‑positive breast cancer treatment, and besides ERα targeting the GPR30 receptor it may achieve additional therapeutic benefits in breast cancer.
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August-2017
Volume 14 Issue 2

Print ISSN: 1792-1074
Online ISSN:1792-1082

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Spandidos Publications style
Chen Y, Hong DY, Wang J, Ling‑Hu J, Zhang YY, Pan D, Xu YN, Tao L, Luo H, Shen XC, Shen XC, et al: Baicalein, unlike 4-hydroxytamoxifen but similar to G15, suppresses 17β-estradiol-induced cell invasion, and matrix metalloproteinase-9 expression and activation in MCF-7 human breast cancer cells. Oncol Lett 14: 1823-1830, 2017.
APA
Chen, Y., Hong, D., Wang, J., Ling‑Hu, J., Zhang, Y., Pan, D. ... Shen, X. (2017). Baicalein, unlike 4-hydroxytamoxifen but similar to G15, suppresses 17β-estradiol-induced cell invasion, and matrix metalloproteinase-9 expression and activation in MCF-7 human breast cancer cells. Oncology Letters, 14, 1823-1830. https://doi.org/10.3892/ol.2017.6298
MLA
Chen, Y., Hong, D., Wang, J., Ling‑Hu, J., Zhang, Y., Pan, D., Xu, Y., Tao, L., Luo, H., Shen, X."Baicalein, unlike 4-hydroxytamoxifen but similar to G15, suppresses 17β-estradiol-induced cell invasion, and matrix metalloproteinase-9 expression and activation in MCF-7 human breast cancer cells". Oncology Letters 14.2 (2017): 1823-1830.
Chicago
Chen, Y., Hong, D., Wang, J., Ling‑Hu, J., Zhang, Y., Pan, D., Xu, Y., Tao, L., Luo, H., Shen, X."Baicalein, unlike 4-hydroxytamoxifen but similar to G15, suppresses 17β-estradiol-induced cell invasion, and matrix metalloproteinase-9 expression and activation in MCF-7 human breast cancer cells". Oncology Letters 14, no. 2 (2017): 1823-1830. https://doi.org/10.3892/ol.2017.6298