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Geraniin inhibits TGF-β1-induced epithelial-mesenchymal transition and suppresses A549 lung cancer migration, invasion and anoikis resistance.
Bioorg Med Chem Lett. 2015 Sep 01; 25(17):3529-34.BM

Abstract

The epithelial-mesenchymal transition (EMT) is an important cellular process during which epithelial polarized cells become motile mesenchymal-appeared cells, which, in turn, induces the metastatic of cancer. Geraniin is a polyphenolic component isolated from Phyllanthus amarus, which exhibits a wide range of pharmacological and physiological activities, such as antitumor, anti-hyperglycemic, anti-hypertensive, antimicrobial, and antiviral activities. However, the possible role of geraniin in the EMT is unclear. We investigated the effect of geraniin on the EMT. Transforming growth factor-beta 1 (TGF-β1) induces the EMT to promote lung adenocarcinoma migration, invasion, and anoikis resistance. To understand the suppressive role of geraniin in lung cancer migration, invasion, and anoikis resistance, we investigated the use of geraniin as inhibitors of TGF-β1-induced EMT in A549 lung cancer cells in vitro. Here, we show that geraniin remarkably increased expression of the epithelial marker E-cadherin and repressed Snail upregulation and expression of the mesenchymal marker N-cadherin and vimentin during the TGF-β1-induced EMT. Geraniin also inhibited the TGF-β1-induced increase in cell migration, invasion, and anoikis resistance of A549 lung cancer cells. Additionally, geraniin markedly inhibited TGF-β1-regulated activation of Smad2. Taken together, our findings provide new evidence that geraniin suppresses lung cancer migration, invasion, and anoikis resistance in vitro by inhibiting the TGF-β1-induced EMT.

Authors+Show Affiliations

Laboratory of Molecular Oncology, Cheil General Hospital & Women's Healthcare Center, Dankook University College of Medicine, Seoul, South Korea. Electronic address: drug9054@naver.com.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

26169124

Citation

Ko, Hyeonseok. "Geraniin Inhibits TGF-β1-induced Epithelial-mesenchymal Transition and Suppresses A549 Lung Cancer Migration, Invasion and Anoikis Resistance." Bioorganic & Medicinal Chemistry Letters, vol. 25, no. 17, 2015, pp. 3529-34.
Ko H. Geraniin inhibits TGF-β1-induced epithelial-mesenchymal transition and suppresses A549 lung cancer migration, invasion and anoikis resistance. Bioorg Med Chem Lett. 2015;25(17):3529-34.
Ko, H. (2015). Geraniin inhibits TGF-β1-induced epithelial-mesenchymal transition and suppresses A549 lung cancer migration, invasion and anoikis resistance. Bioorganic & Medicinal Chemistry Letters, 25(17), 3529-34. https://doi.org/10.1016/j.bmcl.2015.06.093
Ko H. Geraniin Inhibits TGF-β1-induced Epithelial-mesenchymal Transition and Suppresses A549 Lung Cancer Migration, Invasion and Anoikis Resistance. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3529-34. PubMed PMID: 26169124.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Geraniin inhibits TGF-β1-induced epithelial-mesenchymal transition and suppresses A549 lung cancer migration, invasion and anoikis resistance. A1 - Ko,Hyeonseok, Y1 - 2015/07/04/ PY - 2015/03/13/received PY - 2015/06/02/revised PY - 2015/06/25/accepted PY - 2015/7/15/entrez PY - 2015/7/15/pubmed PY - 2016/5/18/medline KW - Anoikis resistance KW - Epithelial–mesenchymal transition (EMT) KW - Geraniin KW - Invasion KW - Lung cancer KW - Migration KW - Transforming growth factor-beta 1 (TGF-β1) SP - 3529 EP - 34 JF - Bioorganic & medicinal chemistry letters JO - Bioorg Med Chem Lett VL - 25 IS - 17 N2 - The epithelial-mesenchymal transition (EMT) is an important cellular process during which epithelial polarized cells become motile mesenchymal-appeared cells, which, in turn, induces the metastatic of cancer. Geraniin is a polyphenolic component isolated from Phyllanthus amarus, which exhibits a wide range of pharmacological and physiological activities, such as antitumor, anti-hyperglycemic, anti-hypertensive, antimicrobial, and antiviral activities. However, the possible role of geraniin in the EMT is unclear. We investigated the effect of geraniin on the EMT. Transforming growth factor-beta 1 (TGF-β1) induces the EMT to promote lung adenocarcinoma migration, invasion, and anoikis resistance. To understand the suppressive role of geraniin in lung cancer migration, invasion, and anoikis resistance, we investigated the use of geraniin as inhibitors of TGF-β1-induced EMT in A549 lung cancer cells in vitro. Here, we show that geraniin remarkably increased expression of the epithelial marker E-cadherin and repressed Snail upregulation and expression of the mesenchymal marker N-cadherin and vimentin during the TGF-β1-induced EMT. Geraniin also inhibited the TGF-β1-induced increase in cell migration, invasion, and anoikis resistance of A549 lung cancer cells. Additionally, geraniin markedly inhibited TGF-β1-regulated activation of Smad2. Taken together, our findings provide new evidence that geraniin suppresses lung cancer migration, invasion, and anoikis resistance in vitro by inhibiting the TGF-β1-induced EMT. SN - 1464-3405 UR - https://www.unboundmedicine.com/medline/citation/26169124/Geraniin_inhibits_TGF_β1_induced_epithelial_mesenchymal_transition_and_suppresses_A549_lung_cancer_migration_invasion_and_anoikis_resistance_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0960-894X(15)00698-8 DB - PRIME DP - Unbound Medicine ER -