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Article

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

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Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang City 110016, China
2
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang City 110016, China
*
Authors to whom correspondence should be addressed.
Academic Editor: Lars Porskjær Christensen
Molecules 2022, 27(11), 3537; https://doi.org/10.3390/molecules27113537
Received: 28 April 2022 / Revised: 22 May 2022 / Accepted: 27 May 2022 / Published: 31 May 2022
A series of 1,7-diphenyl-1,4-heptadien-3-ones with various substituents (HO-, CH3O-, CH3-, 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 CU-19 and CU-21 reduced the level of NO, TNF-α, 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 CU-19 and CU-21 inhibited the nuclear translocation of NF-κB and phosphorylation of MAPKs (ERK, JNK, and p38). A preliminary pharmacokinetic study in rats revealed that the pharmacokinetic properties of CU-19 and CU-21 were dramatically ameliorated in comparison with the pharmacokinetic properties of curcumin. View Full-Text
Keywords: curcumin; 1,7-diphenyl-1,4-heptadien-3-one; neuroinflammation; anti-inflammation; BV2 cell; synthesis curcumin; 1,7-diphenyl-1,4-heptadien-3-one; neuroinflammation; anti-inflammation; BV2 cell; synthesis
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MDPI and ACS Style

Zhao, X.; Fang, J.; Jia, Y.; Wu, Z.; Zhang, M.; Xia, M.; Dong, J. Synthesis and Anti-Neuroinflammatory Activity of 1,7-diphenyl-1,4-heptadien-3-ones in LPS-Stimulated BV2 Microglia Via Inhibiting NF-κB/MAPK Signaling Pathways. Molecules 2022, 27, 3537. https://doi.org/10.3390/molecules27113537

AMA Style

Zhao X, Fang J, Jia Y, Wu Z, Zhang M, Xia M, Dong J. Synthesis and Anti-Neuroinflammatory Activity of 1,7-diphenyl-1,4-heptadien-3-ones in LPS-Stimulated BV2 Microglia Via Inhibiting NF-κB/MAPK Signaling Pathways. Molecules. 2022; 27(11):3537. https://doi.org/10.3390/molecules27113537

Chicago/Turabian Style

Zhao, Xuan, Jiqing Fang, Yu Jia, Zi Wu, Meihui Zhang, Mingyu Xia, and Jinhua Dong. 2022. "Synthesis and Anti-Neuroinflammatory Activity of 1,7-diphenyl-1,4-heptadien-3-ones in LPS-Stimulated BV2 Microglia Via Inhibiting NF-κB/MAPK Signaling Pathways" Molecules 27, no. 11: 3537. https://doi.org/10.3390/molecules27113537

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