TY - JOUR
T1 - Anti-tumor activity of benzylideneacetophenone derivatives via proteasomal inhibition in prostate cancer cells
AU - Lee, Yun Hee
AU - Yun, Jaesuk
AU - Jung, Jae Chul
AU - Oh, Seikwan
AU - Jung, Young Suk
N1 - Funding Information:
This research was supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP) (No. 2009-0083538 and MRC 2010-0029355).
PY - 2016/5
Y1 - 2016/5
N2 - A number of some chalcone derivatives possess promising biological properties including anti-inflammation, anti-oxidant, and anti-tumor activity. Although it has been shown that some derivatives of chalcone induce apoptosis in different kinds of cancer cells, the involved mechanism of action is not well defined. The purpose of this study is to investigate the primary target of a benzylideneacetophenone derivative (JC3), which is a synthetic compound derived from the chalcone family, in human cancer, using prostate cancer cells as a working model. Herein, we show that JC3 inhibits proteasomal activity as indicated by both in vitro and in cell-based assays. Especially, the JC3-dimer was more potent than monomer in the aspect of proteasome inhibition, which induced apoptosis significantly in the prostate cancer cells. Owing to the critical roles of the proteasome in the biology of human tumor progression, invasion, and metastasis, these findings give an important clue for the development of novel anti-tumor agents.
AB - A number of some chalcone derivatives possess promising biological properties including anti-inflammation, anti-oxidant, and anti-tumor activity. Although it has been shown that some derivatives of chalcone induce apoptosis in different kinds of cancer cells, the involved mechanism of action is not well defined. The purpose of this study is to investigate the primary target of a benzylideneacetophenone derivative (JC3), which is a synthetic compound derived from the chalcone family, in human cancer, using prostate cancer cells as a working model. Herein, we show that JC3 inhibits proteasomal activity as indicated by both in vitro and in cell-based assays. Especially, the JC3-dimer was more potent than monomer in the aspect of proteasome inhibition, which induced apoptosis significantly in the prostate cancer cells. Owing to the critical roles of the proteasome in the biology of human tumor progression, invasion, and metastasis, these findings give an important clue for the development of novel anti-tumor agents.
UR - http://www.scopus.com/inward/record.url?scp=84973326483&partnerID=8YFLogxK
U2 - 10.1691/ph.2016.5845
DO - 10.1691/ph.2016.5845
M3 - Article
C2 - 27348972
AN - SCOPUS:84973326483
SN - 0031-7144
VL - 71
SP - 274
EP - 279
JO - Pharmazie
JF - Pharmazie
IS - 5
ER -