title: Baicalin and baicalein inhibit transforming growth factor-β1-mediated epithelial-mesenchymal transition in human breast epithelial cells.
abstract: Since the epithelial-mesenchymal transition (EMT) is involved in many crucial functions of cancer cells, we set out to identify a natural compound capable of inhibiting EMT processes. TGF-β1 treatment induces EMT among normal mammary epithelial cells (MCF10A cells), as reflected by characteristic morphological changes into the fibroblastic phenotype, reduced expression of E-cadherin. Interestingly, butanol extracts of Scutellaria baicalensis Georgi significantly reduced the TGF-β1-mediated EMT of MCF10A cells. Further analysis revealed that baicalin and baicalein, the major flavones of these butanol extracts, inhibited TGF-β1-mediated EMT by reducing the expression level of the EMT-related transcription factor, Slug via the NF-κB pathway, and subsequently increased migration in MCF10A cells. Finally, both compounds reduced the TGF-β1-mediated EMT, anchorage-independent growth and cell migration of human breast cancer cells (MDA-MB-231 cells). Taken together, these results suggest that baicalin and baicalein of Scutellaria baicalensis Georgi may suppress the EMT of breast epithelial cells and the tumorigenic activity of breast cancer cells. Thus, these compounds could have potential as therapeutic or supplementary agents for the treatment of breast cancer.
authors: Department of Life Sciences, The Research Center for Cellular Homeostasis, Ewha Womans University, Seoul 120-750, Republic of Korea.
authors: Heesung
authors: H
authors: Chung
authors: The Division of Nephrology, Department of Internal Medicine, Ewha Medical Research Center, Ewha Womans University School of Medicine, 911-1 Mok-Dong, Yangcheon-Ku, Seoul 158-710, Republic of Korea.
authors: Hack Sun
authors: HS
authors: Choi
authors: College of Pharmacy, Ewha Womans University, Seoul 120-750, Republic of Korea.
authors: Eun-Kyoung
authors: EK
authors: Seo
authors: The Division of Nephrology, Department of Internal Medicine, Ewha Medical Research Center, Ewha Womans University School of Medicine, 911-1 Mok-Dong, Yangcheon-Ku, Seoul 158-710, Republic of Korea. Electronic address: dhkang@ewha.ac.kr.
authors: Duk-Hee
authors: DH
authors: Kang
authors: Department of Life Sciences, The Research Center for Cellular Homeostasis, Ewha Womans University, Seoul 120-750, Republic of Korea. Electronic address: OhES@ewha.ac.kr.
authors: Eok-Soo
authors: ES
authors: Oh
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D001940:Breast / Q000187:drug effects / Q000276:immunology / Q000473:pathology; D001943:Breast Neoplasms / Q000276:immunology / Q000473:pathology / Q000517:prevention & control*; D045744:Cell Line, Tumor; D004847:Epithelial Cells / Q000187:drug effects / Q000276:immunology / Q000473:pathology; D058750:Epithelial-Mesenchymal Transition / Q000187:drug effects*; D005260:Female; D044950:Flavanones / Q000737:chemistry / Q000494:pharmacology*; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D016328:NF-kappa B / Q000276:immunology; D031364:Scutellaria baicalensis / Q000737:chemistry; D053773:Transforming Growth Factor beta1 / Q000037:antagonists & inhibitors / Q000276:immunology*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000972:Antineoplastic Agents, Phytogenic; D044950:Flavanones; D005419:Flavonoids; D016328:NF-kappa B; D053773:Transforming Growth Factor beta1; C038044:baicalin; C006680:baicalein
keywords: Baicalein; Baicalin; Breast cancer; Epithelial mesenchymal transition; NF-κB; Slug