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Molecules 2016, 21(5), 574; doi:10.3390/molecules21050574

Celastrol Induces Cell Apoptosis and Inhibits the Expression of the AML1-ETO/C-KIT Oncoprotein in t(8;21) Leukemia

1
School of Basic Medical Sciences, Hubei University of Medicine, Shiyan 442000, China
2
Key Laboratory of Nutrition and Metabolism, Institute for Nutritional Sciences, Shanghai Institutes for Biological Sciences, Graduate School of the Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 200031, China
3
Laboratory of Chinese Herbal Pharmacology, Oncology Center, Renmin Hospital, Hubei University of Medicine, Shiyan 442000, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 24 February 2016 / Revised: 22 April 2016 / Accepted: 25 April 2016 / Published: 30 April 2016
(This article belongs to the Section Natural Products)
View Full-Text   |   Download PDF [1792 KB, uploaded 30 April 2016]   |  

Abstract

Resistance to chemotherapy is a major challenge to improving overall survival in Acute Myeloid Leukemia (AML). Therefore, the development of innovative therapies and the identification of more novel agents for AML are urgently needed. Celastrol, a compound extracted from the Chinese herb Tripterygium wilfordii Hook, exerts anticancer activity. We investigated the effect of celastrol in the t(8;21) AML cell lines Kasumi-1 and SKNO-1. We demonstrated that inhibition of cell proliferation activated caspases and disrupted mitochondrial function. In addition, we found that celastrol downregulated the AML1-ETO fusion protein, therefore downregulating C-KIT kinases and inhibiting AKT, STAT3 and Erk1/2. These findings provide clear evidence that celastrol might provide clinical benefits to patients with t(8;21) leukemia. View Full-Text
Keywords: celastrol; t(8;21) leukemia; apoptosis; mitochondrial dysfunction; C-KIT celastrol; t(8;21) leukemia; apoptosis; mitochondrial dysfunction; C-KIT
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Yu, X.; Ruan, X.; Zhang, J.; Zhao, Q. Celastrol Induces Cell Apoptosis and Inhibits the Expression of the AML1-ETO/C-KIT Oncoprotein in t(8;21) Leukemia. Molecules 2016, 21, 574.

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