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Molecules 2013, 18(3), 2924-2933; doi:10.3390/molecules18032924
Article

5-Episinuleptolide Acetate, a Norcembranoidal Diterpene from the Formosan Soft Coral Sinularia sp., Induces Leukemia Cell Apoptosis through Hsp90 Inhibition

1,†, 2,†, 3,4, 3, 2,5, 2, 2, 5,6, 2,6, 7 and 1,2,*
Received: 23 January 2013; in revised form: 22 February 2013 / Accepted: 25 February 2013 / Published: 4 March 2013
(This article belongs to the collection Bioactive Compounds)
Download PDF [457 KB, uploaded 18 June 2014]
Abstract: 5-Episinuleptolide acetate (5EPA), a cytotoxic norcembranoidal diterpene recently identified from the Formosan soft coral Sinularia sp., exhibited potent activity against the K562, Molt 4 and HL 60 cancer cell lines. The antiproliferative assay, as well as the annexin V-FITC/propidium iodide (PI) apoptotic assay, indicated that the HL 60 cell line is the most sensitive one towards 5EPA. This diterpenoid led to caspases -3, -8, and -9 activation as well as PARP cleavage. It also induced ROS generation, calcium accumulation and disruption of mitochondrial membrane potential. Additionally, the expression levels of Hsp90 protein and several client proteins were downregulated in response to 5EPA treatment. These results suggest that 5EPA’s cytotoxic effect on HL 60 cells may be attributed to the inhibition of Hsp90 as well as the induction of mitochondrial stress which finally results in apoptotic cell death.
Keywords: 5-episinuleptolide acetate; apoptosis; soft coral; Hsp90; mitochondria; ROS; Sinularia sp. 5-episinuleptolide acetate; apoptosis; soft coral; Hsp90; mitochondria; ROS; Sinularia sp.
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.

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MDPI and ACS Style

Huang, K.-J.; Chen, Y.-C.; El-Shazly, M.; Du, Y.-C.; Su, J.-H.; Tsao, C.-W.; Yen, W.-H.; Chang, W.-B.; Su, Y.-D.; Yeh, Y.-T.; Lu, M.-C. 5-Episinuleptolide Acetate, a Norcembranoidal Diterpene from the Formosan Soft Coral Sinularia sp., Induces Leukemia Cell Apoptosis through Hsp90 Inhibition. Molecules 2013, 18, 2924-2933.

AMA Style

Huang K-J, Chen Y-C, El-Shazly M, Du Y-C, Su J-H, Tsao C-W, Yen W-H, Chang W-B, Su Y-D, Yeh Y-T, Lu M-C. 5-Episinuleptolide Acetate, a Norcembranoidal Diterpene from the Formosan Soft Coral Sinularia sp., Induces Leukemia Cell Apoptosis through Hsp90 Inhibition. Molecules. 2013; 18(3):2924-2933.

Chicago/Turabian Style

Huang, Kao-Jean; Chen, Yu-Cheng; El-Shazly, Mohamed; Du, Ying-Chi; Su, Jui-Hsin; Tsao, Chia-Wei; Yen, Wei-Hsuan; Chang, Wen-Been; Su, Yin-Di; Yeh, Yao-Tsung; Lu, Mei-Chin. 2013. "5-Episinuleptolide Acetate, a Norcembranoidal Diterpene from the Formosan Soft Coral Sinularia sp., Induces Leukemia Cell Apoptosis through Hsp90 Inhibition." Molecules 18, no. 3: 2924-2933.


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