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1,7-二苯基-1,4-庚二烯-3-酮的合成及其通过抑制 NF-B/MAPK 信号通路在 LPS 刺激的 BV2 小胶质细胞中的抗神经炎症活性。

Synthesis and Anti-Neuroinflammatory Activity of 1,7-diphenyl-1,4-heptadien-3-ones in LPS-Stimulated BV2 Microglia Via Inhibiting NF-B/MAPK Signaling Pathways.

机构信息

Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang City 110016, China.

School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang City 110016, China.

出版信息

Molecules. 2022 May 31;27(11):3537. doi: 10.3390/molecules27113537.

DOI:10.3390/molecules27113537
PMID:35684477
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9181915/
Abstract

A series of 1,7-diphenyl-1,4-heptadien-3-ones with various substituents (HO-, CHO-, CH-, Cl-) on the phenyl rings were synthesized and evaluated for anti-neuroinflammatory effects in LPS-stimulated BV2 microglia. The pharmacological results showed that the target compounds bearing methoxy groups greatly inhibited LPS-induced NO release, and that the active compounds and reduced the level of NO, TNF-, IL-6 and PGE-2, downregulated the expression of COX-2 and iNOS in LPS-stimulated BV2 cells. A study of the mechanism of action revealed that and inhibited the nuclear translocation of NF-B and phosphorylation of MAPKs (ERK, JNK, and p38). A preliminary pharmacokinetic study in rats revealed that the pharmacokinetic properties of and were dramatically ameliorated in comparison with the pharmacokinetic properties of curcumin.

摘要

一系列 1,7-二苯基-1,4-庚二烯-3-酮，其苯环上带有各种取代基（HO-、CHO-、CH-、Cl-），被合成并评估了它们在 LPS 刺激的 BV2 小胶质细胞中的抗炎作用。药理结果表明，带有甲氧基的目标化合物能显著抑制 LPS 诱导的 NO 释放，而活性化合物 和 能降低 LPS 刺激的 BV2 细胞中 NO、TNF-α、IL-6 和 PGE-2 的水平，下调 COX-2 和 iNOS 的表达。作用机制的研究表明， 和 抑制 NF-B 的核转位和 MAPKs（ERK、JNK 和 p38）的磷酸化。在大鼠中的初步药代动力学研究表明，与姜黄素的药代动力学性质相比， 和 的药代动力学性质得到了显著改善。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/ff6b20037ad5/molecules-27-03537-g007.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/017ca65299d3/molecules-27-03537-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/d098f35e575d/molecules-27-03537-g002.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/465d58f52a5a/molecules-27-03537-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/9c2965450a06/molecules-27-03537-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/776a8003255d/molecules-27-03537-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/ff6b20037ad5/molecules-27-03537-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/d3caca13057c/molecules-27-03537-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/017ca65299d3/molecules-27-03537-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/d098f35e575d/molecules-27-03537-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/0798b68b1ff4/molecules-27-03537-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/465d58f52a5a/molecules-27-03537-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/9c2965450a06/molecules-27-03537-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/776a8003255d/molecules-27-03537-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a397/9181915/ff6b20037ad5/molecules-27-03537-g007.jpg

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2
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Neuropeptides. 2021 Dec;90:102196. doi: 10.1016/j.npep.2021.102196. Epub 2021 Sep 2.
3
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J Ethnopharmacol. 2022 Jan 10;282:114605. doi: 10.1016/j.jep.2021.114605. Epub 2021 Sep 8.
4
Nilotinib inhibits microglia-mediated neuroinflammation to protect against dopaminergic neuronal death in Parkinson's disease models.尼洛替尼抑制小胶质细胞介导的神经炎症，防止帕金森病模型中多巴胺能神经元死亡。
Int Immunopharmacol. 2021 Oct;99:108025. doi: 10.1016/j.intimp.2021.108025. Epub 2021 Aug 5.
5
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10
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Redox Biol. 2020 Sep;36:101644. doi: 10.1016/j.redox.2020.101644. Epub 2020 Jul 17.