Potent Inhibition of Platelet-Derived Growth Factor-Stimulated Rat Aortic Vascular Smooth Muscle Cell Cycle and Proliferation by (2E)-3-(4-hydroxy-3-methoxyphenyl)phenylpro-2-en-1-one, a Newly Synthesized Benzylideneacetophenone Derivative

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概要

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• One of the principal regulators of mitogenesis in vascular smooth muscle cells (VSMCs) is platelet-derived growth factor-BB (PDGF-BB). An increase of PDGF-BB expression has been observed in atherosclerotic lesions. The aim of this study was to elucidate the effects and molecular mechanism of (2E)-3-(4-hydroxy-3-methoxyphenyl) phenylpro-2-en-1-one (KTJ2242), a newly synthesized benzylideneacetophenone derivative, on PDGF-BB-stimulated rat aortic VSMCs. KTJ2242 induced accumulation of cells in the G1 phase of the cell cycle of VSMCs. We observed that KTJ2242 inhibited PDGF-BB-stimulated [3H]-thymidine incorporation into the DNA of VSMCs, and the cell number was significantly reduced in a concentration-dependent manner. Also, we observed that KTJ2242 decreased PDGF-BB-stimulated extracellular-regulated kinase 1 and 2 (ERK1/2) and Akt phosphorylation. These results suggest the possibility that KTJ2242 may be a potential agent with which to control vascular disorders and its antiproliferative mechanism may be mediated through partial Akt and ERK1/2-dependent signaling pathways.

著者

• Kim Tack-Joong

  Division of Biological Science and Technology, College of Science and Technology, Institute of Bioma

• Han Hyeong-Jun

  Department of Pharmacy, College of Pharmacy, Seoul National University

• Jung Jae-Chul

  Department of Neuroscience and Medical Research Institute, School of Medicine, Ewha Womans Universit

• Oh Seikwan

  Department of Neuroscience and Medical Research Institute, School of Medicine, Ewha Womans Universit

• Yun Yeo-Pyo

  College of Pharmacy, Chungbuk National University

• Kim Tack-joong

  Div. Of Biological Sci. And Technol. Coll. Of Sci. And Technol. Inst. Of Biomaterials Yonsei Univ.

• Yun Yeo-pyo

  College Of Pharmacy Chungbuk National University

• Yun Yeo-pyo

  College Of Pharmacy Cbitrc College Of Pharmacy And Medical Research Center Chungbuk National Univers

• Kim Tack-joong

  Division Of Biological Science And Technology College Of Science And Technology Yonsei University

• Jung Jae-Chul

  Department of Medicinal Chemistry, School of Pharmacy, University of Mississippi

• Jung Jae-Chul

  Department of Neuroscience and Medical Research Institute, School of Medicine, Ewha Womans University

• Yun Yeo-Pyo

  College of Pharmacy and Medical Research Center, Chungbuk National University

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