Abstract
The epithelial–mesenchymal transition (EMT) of cancer cells is a crucial process in cancer cell metastasis. An Aquimarina sp. MC085 extract was found to inhibit A549 human lung cancer cell invasion, and caprolactin C (1), a new natural product, α-amino-ε-caprolactam linked to 3-methyl butanoic acid, was purified through bioactivity-guided isolation of the extract. Furthermore, its enantiomeric compound, ent-caprolactin C (2), was synthesized. Both 1 and 2 inhibited the invasion and γ-irradiation-induced migration of A549 cells. In transforming growth factor-β (TGF-β)-treated A549 cells, 2 inhibited the phosphorylation of Smad2/3 and suppressed the EMT cell marker proteins (N-cadherin, β-catenin, and vimentin), as well as the related messenger ribonucleic acid expression (N-cadherin, matrix metalloproteinase-9, Snail, and vimentin), while compound 1 did not suppress Smad2/3 phosphorylation and the expression of EMT cell markers. Therefore, compound 2 could be a potential candidate for antimetastatic agent development, because it suppresses TGF-β-induced EMT.
Highlights
College of Pharmacy, Yeungnam University, Gyeongsan-si 38541, Gyeongsangbuk-do, Korea; College of Korean Medicine, Gachon University, Seongnam 13120, Gyeonggi-do, Korea; Research Institute of Cell Culture, Yeungnam University, Gyeongsan-si 38541, Gyeongsangbuk-do, Korea
The process of epithelial cells transforming into cells with metastatic and invasive capacities is referred to as epithelial–mesenchymal transition (EMT), and it is considered a basic phenomenon of tissue and organ formation during embryonic development in vertebrates and invertebrates
transforming growth factor-β (TGF-β)-induced program has beenofrecognized as a anticancer agents
Summary
Its enantiomeric compound, ent-caprolactin C (2), was synthesized Both 1 and 2 inhibited the invasion and γ-irradiation-induced migration of A549 cells. The process of epithelial cells transforming into cells with metastatic and invasive capacities is referred to as epithelial–mesenchymal transition (EMT), and it is considered a basic phenomenon of tissue and organ formation during embryonic development in vertebrates and invertebrates. This phenomenon has been observed in the human wound-healing process, and EMT is closely related to the formation and progression of cancer cells [6,7]. The strong expression of EMT-induced transcription factors, such as Snail and β-catenin, in cancer cells is generally published maps and institutional affiliations
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