PMID- 25767679
OWN - NLM
STAT- PubMed-not-MEDLINE
DCOM- 20150313
LR  - 20201001
IS  - 1976-9148 (Print)
IS  - 2005-4483 (Electronic)
IS  - 1976-9148 (Linking)
VI  - 23
IP  - 2
DP  - 2015 Mar
TI  - Inhibitory Effect of 3-(4-Hydroxyphenyl)-1-(thiophen-2-yl) prop-2-en-1-one, a 
      Chalcone Derivative on MCP-1 Expression in Macrophages via Inhibition of ROS and 
      Akt Signaling.
PG  - 119-27
LID - 10.4062/biomolther.2014.127 [doi]
AB  - Chalcones (1,3-diaryl-2-propen-1-ones), a subfamily of flavonoid, are widely 
      known to possess potent anti-inflammatory and anti-oxidant properties. In this 
      study, we investigated the effect of 
      3-(4-Hydroxyphenyl)-1-(thio3-(4-Hydroxyphenyl phen-2-yl)prop-2-en-1-one 
      (TI-I-175), a synthetic chalcone derivative, on endotoxin-induced expression of 
      monocyte chemoattractant protein-1 (MCP-1), one of the key chemokines that 
      regulates migration and infiltration of immune cells, and its potential 
      mechanisms. TII-175 potently inhibited MCP-1 mRNA expression stimulated by 
      lipopolysaccharide (LPS) in RAW 264.7 macrophages without significant effect on 
      cell viability. Treatment of cells with TI-I-175 markedly prevented LPS-induced 
      transcriptional activation of activator protein-1 (AP-1) as measured by 
      luciferase reporter assay, while nuclear factor-kappaB (NF-kappaB) activity was not 
      inhibited by TI-I-175, implying that TI-I-175 suppressed MCP-1 expression 
      probably via regulation of AP-1. In addition, TI-I-175 treatment significantly 
      inhibited LPS-induced Akt phosphorylation and led to a significant decrease in 
      reactive oxygen species (ROS) production by LPS, which act as up-stream signaling 
      events required for AP-1 activation in RAW 264.7 macrophages. Taken together, 
      these results indicate that TI-I-175 suppresses MCP-1 gene expression in 
      LPS-stimulated RAW 264.7 macrophages via suppression of ROS production and Akt 
      activation.
FAU - Kim, Mi Jin
AU  - Kim MJ
AD  - College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
FAU - Kadayat, Taraman
AU  - Kadayat T
AD  - College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
FAU - Um, Yeon Ji
AU  - Um YJ
AD  - College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
FAU - Jeong, Tae Cheon
AU  - Jeong TC
AD  - College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
FAU - Lee, Eung-Seok
AU  - Lee ES
AD  - College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
FAU - Park, Pil-Hoon
AU  - Park PH
AD  - College of Pharmacy, Yeungnam University, Gyeongsan 712-749, Republic of Korea.
LA  - eng
PT  - Journal Article
DEP - 20150301
PL  - Korea (South)
TA  - Biomol Ther (Seoul)
JT  - Biomolecules & therapeutics
JID - 101472832
PMC - PMC4354312
OTO - NOTNLM
OT  - Chalcone
OT  - Inflammation
OT  - Lipopolysaccharide
OT  - MCP-1
OT  - Reactive oxygen species
EDAT- 2015/03/15 06:00
MHDA- 2015/03/15 06:01
PMCR- 2015/03/01
CRDT- 2015/03/14 06:00
PHST- 2014/11/19 00:00 [received]
PHST- 2014/12/17 00:00 [revised]
PHST- 2014/12/18 00:00 [accepted]
PHST- 2015/03/14 06:00 [entrez]
PHST- 2015/03/15 06:00 [pubmed]
PHST- 2015/03/15 06:01 [medline]
PHST- 2015/03/01 00:00 [pmc-release]
AID - bt-23-119 [pii]
AID - 10.4062/biomolther.2014.127 [doi]
PST - ppublish
SO  - Biomol Ther (Seoul). 2015 Mar;23(2):119-27. doi: 10.4062/biomolther.2014.127. 
      Epub 2015 Mar 1.