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Int J Mol Sci
2021 Jan 19;222:. doi: 10.3390/ijms22020973.
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Natural Polyhydroxy Flavonoids, Curcuminoids, and Synthetic Curcumin Analogs as α7 nAChRs Positive Allosteric Modulators.
Ximenis M
,
Mulet J
,
Sala S
,
Sala F
,
Criado M
,
González-Muñiz R
,
Pérez de Vega MJ
.
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The α7 nicotinic acetylcholine receptor (α7 nAChR) is a ligand-gated ion channel that is involved in cognition disorders, schizophrenia, pain, and inflammation. Allosteric modulation of this receptor might be advantageous to reduce the toxicity in comparison with full agonists. Our previous results obtained with some hydroxy-chalcones, which were identified as positive allosteric modulators (PAMs) of α7 nAChR, prompted us to evaluate the potential of some structurally related naturally occurring flavonoids and curcuminoids and some synthetic curcumin analogues, with the aim of identifying new allosteric modulators of the α7 nAChR. Biological evaluation showed that phloretin, demethoxycurcumin, and bis-demethoxicurcuming behave as PAMs of α7 nAChR. In addition, some new curcumin derivatives were able to enhance the signal evoked by ACh; the activity values found for the tetrahydrocurcuminoid analog 23 were especially promising.
RTI2018-097189-B-C22 Spanish Ministerio de Ciencia, Innovación y Universidades (MICIU-FEDER), 2019E030 CSIC, BFU2008-02160 Spanish Ministerio de Ciencia, Innovación y Universidades (MICIU-FEDER), SAF2011-22802 to SS Spanish Ministerio de Ciencia e Innovación
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