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Molecules 2017, 22(7), 1157;

2,5-Dihydroxyacetophenone Induces Apoptosis of Multiple Myeloma Cells by Regulating the MAPK Activation Pathway

College of Korean Medicine, Kyung Hee University, 24 Kyungheedae-ro, Dongdaemun-gu, Seoul 02447, Korea
Natural Products Research Institute, Korean Institute of Science and Technology, 679 Saimdang-ro, Gangneung, Gangwon-do 25451, Korea
Department of Botany and Microbiology, College of Science, King Saud University, Riyadh 11451, Saudi Arabia
School of Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth, WA 6009, Australia
Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117600, Singapore
Authors to whom correspondence should be addressed.
Academic Editors: Nancy D. Turner and Isabel C.F.R. Ferreira
Received: 16 June 2017 / Revised: 3 July 2017 / Accepted: 7 July 2017 / Published: 11 July 2017
(This article belongs to the Collection Bioactive Compounds)
Full-Text   |   PDF [3415 KB, uploaded 11 July 2017]   |  


2,5-Dihydroxyacetophenone (DHAP) is an active compound obtained from Radix rehmanniae preparata, which is widely used as a herbal medicine in many Asian countries. DHAP has been found to possess anti-inflammatory, anti-anxiety, and neuroprotective qualities. For the present study, we evaluated the anti-cancer effects of DHAP on multiple myeloma cells. It was discovered that DHAP downregulated the expression of oncogenic gene products like Bcl-xl, Bcl-2, Mcl-1, Survivin, Cyclin D1, IAP-1, Cyclin E, COX-2, and MMP-9, and upregulated the expression of Bax and p21 proteins, consistent with the induction of G2/M phase cell cycle arrest and apoptosis in U266 cells. DHAP inhibited cell proliferation and induced apoptosis, as characterized by the cleavage of PARP and the activation of caspase-3, caspase-8, and caspase-9. Mitogen-activated protein kinase (MAPK) pathways have been linked to the modulation of the angiogenesis, proliferation, metastasis, and invasion of tumors. We therefore attempted to determine the effect of DHAP on MAPK signaling pathways, and discovered that DHAP treatment induced a sustained activation of JNK, ERK1/2, and p38 MAPKs. DHAP also potentiated the pro-apoptotic and anti-proliferative effects of bortezomib in U266 cells. Our results suggest that DHAP can be an effective therapeutic agent to target multiple myeloma. View Full-Text
Keywords: 2,5-dihydroxyacetophenone; multiple myeloma; MAPK; apoptosis 2,5-dihydroxyacetophenone; multiple myeloma; MAPK; apoptosis

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Ko, J.-H.; Lee, J.H.; Jung, S.H.; Lee, S.-G.; Chinnathambi, A.; Alharbi, S.A.; Yang, W.M.; Um, J.-Y.; Sethi, G.; Ahn, K.S. 2,5-Dihydroxyacetophenone Induces Apoptosis of Multiple Myeloma Cells by Regulating the MAPK Activation Pathway. Molecules 2017, 22, 1157.

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