PMID- 35697364
OWN - NLM
STAT- MEDLINE
DCOM- 20221115
LR  - 20221115
IS  - 1472-8206 (Electronic)
IS  - 0767-3981 (Linking)
VI  - 36
IP  - 6
DP  - 2022 Dec
TI  - Evidence that the anti-inflammatory effect of 4-aryl-4H-chromenes is linked to 
      macrophage repolarization.
PG  - 1020-1030
LID - 10.1111/fcp.12809 [doi]
AB  - The inflammatory response is a common feature of many pathological conditions, 
      and there is urgent necessity for new substances that minimize the harmful 
      effects of inflammation. Chromenes represent a class of compounds with multiple 
      pharmacological actions that have already been described and may be potential 
      candidates for studies of therapeutic action. This study aimed to test novel 
      4-aryl-4H-chromene-derived molecules in an in vitro model of inflammation using 
      lipopolysaccharide (LPS)-induced Raw 264.7 cells. Seven compounds derived from 
      4-aryl-4H-chromene were tested on Raw 264.7 cells to evaluate their cytotoxic 
      effects. Next, the effect of the selected compounds on the pro-inflammatory 
      mediators (tumor necrosis factor-alpha [TNF-alpha], monocyte chemoattractant 
      protein-1 [MCP-1], interleukin [IL]-6) and on the anti-inflammatory mediators 
      (IL-10 and IL-13) was analyzed, and finally, the effect of the compounds on 
      macrophage apoptosis and expression of surface receptors (toll-like receptor 4 
      [TLR-4] and mannose) was evaluated. The results of this study demonstrated that 
      changes in the molecular structure of 4-aryl-4H-chromene altered its cytotoxic 
      profile. Therefore, derivatives that showed safe results were selected for 
      further analyses (named compounds: 4-6). In these experiments, the compounds were 
      able to decrease nitric oxide (NO) levels and production of MCP-1, IL-6, IL-10, 
      and IL-13. Furthermore, these derivatives were effective in reducing macrophage 
      apoptosis and the expression of surface receptors, as TLR-4/CD284. Moreover, 
      compounds 5 and 6 also were effective in increasing mannose receptor (CD206) 
      expression. The results indicate, for the first time to our knowledge, that the 
      anti-inflammatory effect produced by chromenes is linked to macrophage 
      repolarization (M1 to M2).
CI  - (c) 2022 Societe Francaise de Pharmacologie et de Therapeutique. Published by John 
      Wiley & Sons Ltd.
FAU - Dos Reis, Gustavo O
AU  - Dos Reis GO
AD  - Postgraduation Program in Pharmacy, Federal University of Santa Catarina, 
      Florianopolis, Brazil.
FAU - da Rosa, Julia S
AU  - da Rosa JS
AD  - Postgraduation Program in Pharmacy, Federal University of Santa Catarina, 
      Florianopolis, Brazil.
FAU - Lubschinksi, Taina L
AU  - Lubschinksi TL
AD  - Postgraduation Program in Pharmacy, Federal University of Santa Catarina, 
      Florianopolis, Brazil.
FAU - Martin, Erlon F
AU  - Martin EF
AUID- ORCID: 0000-0002-7844-0757
AD  - Postgraduation Program in Pharmacy, Federal University of Santa Catarina, 
      Florianopolis, Brazil.
FAU - Sandjo, Louis P
AU  - Sandjo LP
AD  - Department of Pharmaceutical Sciences, Federal University of Santa Catarina, 
      Florianopolis, Santa Catarina, Brazil.
FAU - Dalmarco, Eduardo M
AU  - Dalmarco EM
AUID- ORCID: 0000-0002-5220-5396
AD  - Postgraduation Program in Pharmacy, Federal University of Santa Catarina, 
      Florianopolis, Brazil.
AD  - Department of Clinical Analysis, Centre of Health Sciences, Federal University of 
      Santa Catarina, University Campus, Trindade, Florianopolis, Santa Catarina, 
      Brazil.
LA  - eng
PT  - Journal Article
DEP - 20220617
PL  - England
TA  - Fundam Clin Pharmacol
JT  - Fundamental & clinical pharmacology
JID - 8710411
RN  - 0 (Anti-Inflammatory Agents)
RN  - 0 (Benzopyrans)
RN  - 130068-27-8 (Interleukin-10)
RN  - 0 (Interleukin-13)
RN  - 0 (Interleukin-6)
RN  - 0 (Lipopolysaccharides)
RN  - 0 (Toll-Like Receptor 4)
SB  - IM
MH  - *Anti-Inflammatory Agents/pharmacology
MH  - *Benzopyrans/pharmacology
MH  - Inflammation/metabolism
MH  - Interleukin-10/metabolism
MH  - Interleukin-13/metabolism
MH  - Interleukin-6/metabolism
MH  - Lipopolysaccharides
MH  - *Macrophages/drug effects
MH  - Toll-Like Receptor 4
MH  - Animals
MH  - Mice
MH  - RAW 264.7 Cells
OTO - NOTNLM
OT  - LPS
OT  - Raw 264.7
OT  - chromenes
OT  - inflammation
OT  - macrophage polarization
EDAT- 2022/06/14 06:00
MHDA- 2022/11/15 06:00
CRDT- 2022/06/13 20:43
PHST- 2022/03/15 00:00 [received]
PHST- 2022/06/10 00:00 [accepted]
PHST- 2022/06/14 06:00 [pubmed]
PHST- 2022/11/15 06:00 [medline]
PHST- 2022/06/13 20:43 [entrez]
AID - 10.1111/fcp.12809 [doi]
PST - ppublish
SO  - Fundam Clin Pharmacol. 2022 Dec;36(6):1020-1030. doi: 10.1111/fcp.12809. Epub 
      2022 Jun 17.