期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 22, 期 2, 页码 -出版社
MDPI
DOI: 10.3390/ijms22020973
关键词
curcuminoids; tetrahydrocurcuminoids; α 7 nicotinic receptors; positive allosteric modulation
资金
- Spanish Ministerio de Ciencia, Innovacion y Universidades (MICIU-FEDER) [RTI2018-097189-B-C22]
- CSIC [2019E030, BFU2008-02160, SAF2011-22802]
This study evaluated a range of natural products and synthetic compounds, finding that phloretin, demethoxycurcumin, and bis-demethoxicurcuming act as positive allosteric modulators (PAMs) of α7 nAChR; and some new curcumin derivatives have the ability to enhance ACh-evoked signal, with tetrahydrocurcuminoid analog 23 showing particularly promising activity values.
The alpha 7 nicotinic acetylcholine receptor (alpha 7 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 alpha 7 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 alpha 7 nAChR. Biological evaluation showed that phloretin, demethoxycurcumin, and bis-demethoxicurcuming behave as PAMs of alpha 7 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.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据