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Title 

Artocarpus altilis (Parkinson) fosberg extracts and geranyl dihydrochalcone inhibit STAT3 activity in prostate cancer DU145 cells

Authors 

Yoon Jung JeonSeung-Nam JungHyeyoun ChangJi Eun YunChang Woo LeeJoongku LeeSangho ChoiO NashDong Cho HanByoung-Mog Kwon

Publisher 

Wiley-Blackwell

Issue Date 

2015

Citation 

Phytotherapy Research, vol. 29, no. 5, pp. 749-756

Keywords 

antitumor effectsapoptosisArtocarpus altilisprostate cancerSTAT3

Abstract 

Artocarpus altilis (Parkinson) Fosberg has traditionally been used in Indonesia for the treatment of liver cirrhosis, hypertension, and diabetes. In many other countries, it is used for the treatment of malaria, yellow fever, and dengue fever. It has been reported that A. altilis extracts have antiatherosclerotic and cytoprotective effects, but its molecular targets in tumor cells are not yet fully understood. The A. altilis extracts and the partially purified fraction have been shown to inhibit STAT3 activity and the phosphorylation of STAT3 in a dose-dependent manner. To identify the active components, a bioassay-guided isolation of the partially purified fraction resulted in the identification of a geranyl dihydrochalcone, CG901. Its chemical structure was established on the basis of spectroscopic evidence and comparison with published data. The partially purified fraction and the isolated a geranyl dihydrochalcone, CG901, down-regulated the expression of STAT3 target genes, induced apoptosis in DU145 prostate cancer cells via caspase-3 and PARP degradation, and inhibited tumor growth in human prostate tumor (DU145) xenograft initiation model. These results suggest that A. altilis could be a good natural source and that the isolated compound will be a potential lead molecule for developing novel therapeutics against STAT3-related diseases, including cancer and inflammation.

ISSN 

0951-418X

Link 

http://dx.doi.org/10.1002/ptr.5311

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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