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Article

A Flavone Constituent from Myoporum bontioides Induces M-Phase Cell Cycle Arrest of MCF-7 Breast Cancer Cells

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Department of Marine Technology and Resources, National Sun-Yat-sen University, Kaohisung 804, Taiwan
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Division of Hematology and Oncology, Department of Internal Medicine, China Medical University Hospital, Taichung 404, Taiwan
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College of Medicine, China Medical University, Taichung 404, Taiwan
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Department of Pharmacy, Kinmen Hospital, Kinmen 891, Taiwan
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Cancer Center, China Medical University Hospital, Taichung 404, Taiwan
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School of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan
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School of Pharmacy, Taipei Medical University, Taipei 110, Taiwan
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Department of Fragrance and Cosmetic Science, College of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Molecules 2017, 22(3), 472; https://doi.org/10.3390/molecules22030472
Received: 29 December 2016 / Revised: 4 March 2017 / Accepted: 13 March 2017 / Published: 15 March 2017
(This article belongs to the Section Natural Products Chemistry)
Abstract: Myoporum bontioides is a traditional medicinal plant in Asia with various biological activities, including anti-inflammatory and anti-bacterial characteristics. To identify the bioactive constituents from M. bontioides, a newly-identified flavone, 3,4′-dimethoxy-3′,5,7-trihydroxyflavone (compound 1), along with eight known compounds, were investigated in human MCF-7 breast cancer, SCC4 oral cancer, and THP-1 monocytic leukemia cells. Among these compounds, compound 1 exhibited the strongest antiproliferative activity with half-maximal inhibitory concentration (IC50) values ranging from 3.3 μM (MCF-7) to 8.6 μM (SCC4). Flow cytometric analysis indicated that compound 1 induced G2/M cell cycle arrest in MCF-7 cells. Mechanistic evidence suggests that the G2/M arrest could be attributable to compound 1’s modulatory effects on the phosphorylation and expression of numerous key signaling effectors, including cell division cycle 2 (CDC2), CDC25C, and p53. Notably, compound 1 downregulated the expression of histone deacetylase 2 (HDAC2) and HDAC4, leading to increased histone H3 acetylation and p21 upregulation. Together, these findings suggest the translational potential of compound 1 as a breast cancer treatment. View Full-Text
Keywords: Myoporum bontioides; Myoporaceae; flavone; cell cycle arrest; breast cancer Myoporum bontioides; Myoporaceae; flavone; cell cycle arrest; breast cancer
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    Description: The 1H and 13C-NMR, HMQC, HMBC, and NOESY plots of compound 1.
MDPI and ACS Style

Weng, J.-R.; Bai, L.-Y.; Lin, W.-Y.; Chiu, C.-F.; Chen, Y.-C.; Chao, S.-W.; Feng, C.-H. A Flavone Constituent from Myoporum bontioides Induces M-Phase Cell Cycle Arrest of MCF-7 Breast Cancer Cells. Molecules 2017, 22, 472. https://doi.org/10.3390/molecules22030472

AMA Style

Weng J-R, Bai L-Y, Lin W-Y, Chiu C-F, Chen Y-C, Chao S-W, Feng C-H. A Flavone Constituent from Myoporum bontioides Induces M-Phase Cell Cycle Arrest of MCF-7 Breast Cancer Cells. Molecules. 2017; 22(3):472. https://doi.org/10.3390/molecules22030472

Chicago/Turabian Style

Weng, Jing-Ru, Li-Yuan Bai, Wei-Yu Lin, Chang-Fang Chiu, Yu-Chang Chen, Shi-Wei Chao, and Chia-Hsien Feng. 2017. "A Flavone Constituent from Myoporum bontioides Induces M-Phase Cell Cycle Arrest of MCF-7 Breast Cancer Cells" Molecules 22, no. 3: 472. https://doi.org/10.3390/molecules22030472

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