PMID- 31594421
OWN - NLM
STAT- MEDLINE
DCOM- 20200408
LR  - 20200408
IS  - 1532-2513 (Electronic)
IS  - 0892-3973 (Linking)
VI  - 41
IP  - 6
DP  - 2019 Dec
TI  - Anti-inflammatory effect of synthesized indole-based chalcone 
      (2E)-3-(4-bromophenyl)-1-(1H-indol-3-yl) prop-2-en-1-one: an in vitro and in vivo 
      studies.
PG  - 568-576
LID - 10.1080/08923973.2019.1672177 [doi]
AB  - Purpose: Chalcones are precursors of flavonoids with a wide range of 
      pharmacological activities. This study evaluates the anti-inflammatory effect of 
      indole based chalcone derivative (2E)-3-(4-bromophenyl)-1-(1H-indol-3-yl) 
      prop-2-en-1-one (IC9) on lipopolysaccharide (LPS) activated murine macrophages 
      RAW264.7 cells and carrageenan-induced acute model in rats.Materials and methods: 
      LPS-treated RAW264.7 cell lines and carrageenan-induced animal model were 
      employed to evaluate the anti-inflammatory activity of IC9. The cell cytotoxicity 
      studies were carried out by MTT assay. Reactive oxygen species (ROS) production 
      and other inflammatory markers such as prostaglandin E2 (PGE2), nitric oxide (NO) 
      as well as cyclooxygenase-2 (COX-2) activity were determined using ELISA. The 
      RT-PCR was performed to determine mRNA expressions in the case of inducible 
      nitric oxide synthase (iNOS), COX-2, Toll-like receptor-4 (TLR-4) and also 
      nuclear translocation of NF-kappaB activity.Results: LPS-activated RAW264.7 cells 
      showed an increased level of ROS generation and other inflammatory markers such 
      as PGE2, NO level and COX-2 activity. Expression of iNOS, COX- 2 and TLR-4 mRNA 
      expression were also up-regulated along with nuclear translocation of NF-kappaB. On 
      IC9 supplementation, all the above parameters of LPS-activated cells were found 
      to be reversed, resembling the control group. Moreover, IC9 significantly 
      inhibited paw swelling and exhibited maximum inhibition of 78.45% at low dose of 
      7.5 mg/kg.bwt.Conclusions: The targeting anti-inflammatory efficacy and profound 
      NF-kappaB sensitive transcriptional regulatory mechanism of IC9 accounts for its 
      effective anti-inflammatory action.
FAU - Sasidharan, Rani
AU  - Sasidharan R
AD  - Department of Chemistry, School of Advanced Sciences, VIT University, Vellore, 
      India.
FAU - Sreedharannair Leelabaiamma, Manju
AU  - Sreedharannair Leelabaiamma M
AD  - Department of Chemistry, School of Advanced Sciences, VIT University, Vellore, 
      India.
FAU - Mohanan, Ratheesh
AU  - Mohanan R
AD  - Departments of Biochemistry, St. Thomas College, Pala, Kottayam, India.
FAU - Jose, Svenia P
AU  - Jose SP
AD  - Departments of Biochemistry, St. Thomas College, Pala, Kottayam, India.
FAU - Mathew, Bijo
AU  - Mathew B
AD  - Division of Drug Design and Medicinal Chemistry Research Lab, Department of 
      Pharmaceutical Chemistry, Ahalia School of Pharmacy, Palakkad, India.
FAU - Sukumaran, Sandya
AU  - Sukumaran S
AD  - Department of Inorganic and Physical Chemistry, Indian Institute of Science, 
      Bangalore, India.
LA  - eng
PT  - Journal Article
DEP - 20191008
PL  - England
TA  - Immunopharmacol Immunotoxicol
JT  - Immunopharmacology and immunotoxicology
JID - 8800150
RN  - 0 (Anti-Inflammatory Agents)
RN  - 0 (Chalcones)
RN  - 0 (Lipopolysaccharides)
RN  - 9000-07-1 (Carrageenan)
SB  - IM
EIN - Immunopharmacol Immunotoxicol. 2019 Dec;41(6):I. PMID: 31615301
MH  - Animals
MH  - *Anti-Inflammatory Agents/chemical synthesis/chemistry/pharmacology
MH  - Carrageenan/toxicity
MH  - *Chalcones/chemical synthesis/chemistry/pharmacology
MH  - Inflammation/chemically induced/drug therapy/metabolism/pathology
MH  - Lipopolysaccharides/toxicity
MH  - Male
MH  - Mice
MH  - RAW 264.7 Cells
MH  - Rats
MH  - Rats, Wistar
OTO - NOTNLM
OT  - Chalcones
OT  - TLR 4
OT  - inflammation
OT  - nuclear factor-Kappa beta
OT  - oxidative stress
EDAT- 2019/10/09 06:00
MHDA- 2020/04/09 06:00
CRDT- 2019/10/10 06:00
PHST- 2019/10/09 06:00 [pubmed]
PHST- 2020/04/09 06:00 [medline]
PHST- 2019/10/10 06:00 [entrez]
AID - 10.1080/08923973.2019.1672177 [doi]
PST - ppublish
SO  - Immunopharmacol Immunotoxicol. 2019 Dec;41(6):568-576. doi: 
      10.1080/08923973.2019.1672177. Epub 2019 Oct 8.