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Int. J. Mol. Sci. 2016, 17(9), 1491; doi:10.3390/ijms17091491

BL-038, a Benzofuran Derivative, Induces Cell Apoptosis in Human Chondrosarcoma Cells through Reactive Oxygen Species/Mitochondrial Dysfunction and the Caspases Dependent Pathway

1
Central Laboratory, Shin-Kong Wu Ho-Su Memorial Hospital, Taipei 111, Taiwan
2
School of Pharmacy, College of Pharmacy, China Medical University, Taichung 404, Taiwan
3
Department of Orthopedic Surgery, China Medical University Hospital, Taichung 404, Taiwan
4
School of Chinese Medicine, China Medical University, Taichung 404, Taiwan
5
Graduate Institute of Basic Medical Science, China Medical University, Taichung 404, Taiwan
6
Department of Pharmacology, School of Medicine, China Medical University, Taichung 404, Taiwan
7
Department of Biotechnology, College of Health Science, Asia University, Taichung 413, Taiwan
*
Authors to whom correspondence should be addressed.
Academic Editor: Ge Zhang
Received: 4 June 2016 / Revised: 4 August 2016 / Accepted: 31 August 2016 / Published: 7 September 2016
(This article belongs to the Special Issue Translational Molecular Medicine & Molecular Drug Discovery)
View Full-Text   |   Download PDF [7150 KB, uploaded 7 September 2016]   |  

Abstract

Chondrosarcoma is a highly malignant cartilage-forming bone tumor that has the capacity to invade locally and cause distant metastasis. Moreover, chondrosarcoma is intrinsically resistant to conventional chemotherapy or radiotherapy. The novel benzofuran derivative, BL-038 (2-amino-3-(2,6-dichlorophenyl)-6-(4-methoxyphenyl)benzofuran-4-yl acetate), has been evaluated for its anticancer effects in human chondrosarcoma cells. BL-038 caused cell apoptosis in two human chondrosarcoma cell lines, JJ012 and SW1353, but not in primary chondrocytes. Treatment of chondrosarcoma with BL-038 also induced reactive oxygen species (ROS) production. Furthermore, BL-038 decreased mitochondrial membrane potential (MMP) and changed mitochondrial-related apoptosis, by downregulating the anti-apoptotic activity members (Bcl-2, Bcl-xL) and upregulating pro-apoptotic members (Bax, Bak) of the B-cell lymphoma 2 (Bcl-2) family of proteins, key regulators of the apoptotic machinery in cells. These results demonstrate that in human chondrosarcoma cells, the apoptotic and cytotoxic effects of BL-038 are mediated by the intrinsic mitochondria-mediated apoptotic pathway, which in turn causes the release of cytochrome c, the activation of caspase-9 and caspase-3, and the cleavage of poly (ADP-ribose) polymerase (PARP), to elicit apoptosis response. Our results show that the benzofuran derivative BL-038 induces apoptosis in chondrosarcoma cells. View Full-Text
Keywords: chondrosarcoma; benzofuran derivative; ROS; apoptosis chondrosarcoma; benzofuran derivative; ROS; apoptosis
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MDPI and ACS Style

Liu, J.-F.; Chen, C.-Y.; Chen, H.-T.; Chang, C.-S.; Tang, C.-H. BL-038, a Benzofuran Derivative, Induces Cell Apoptosis in Human Chondrosarcoma Cells through Reactive Oxygen Species/Mitochondrial Dysfunction and the Caspases Dependent Pathway. Int. J. Mol. Sci. 2016, 17, 1491.

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