Recently I am researching about NF-KAPPA-B; TNF-ALPHA PRODUCTION; HEME OXYGENASE-1; INNATE IMMUNITY; INFLAMMATION; PATHWAY; NRF2; MACROPHAGES; ACTIVATION; INDUCTION, Saw an article supported by the National Natural Science Funding of ChinaNational Natural Science Foundation of China (NSFC) [21977001]. COA of Formula: C8H6O2. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Chen, LZ; Wu, J; Li, K; Wu, QQ; Chen, R; Liu, XH; Ruan, BF. The CAS is 87-41-2. Through research, I have a further understanding and discovery of Isobenzofuran-1(3H)-one
Phthalide is a promising chemical scaffold and has been proved to show potent anti-inflammatory efficacy. In this study, three series, total of 31 novel phthalide derivatives were designed and synthesized, their anti-inflammatory activities were screened in vitro and in vivo. The anti-inflammatory activity of all the compounds were screened on LPS induced NO production to evaluating their inhibitory effects. Structure-activity relationship has been concluded, and finally 3-((4-((4-ufluorobenzyl)oxy)phenyl)(-hydroxy)methyl)-5,7-dimethoxyisobenzofuran-1 (3H)-one (compound 9o) was found to be the active one with low toxicity, which showed 95.23% inhibitory rate at 10 mu M with IC50 value of 0.76 mu M against LPS-induced NO over expression. Preliminary mechanism studies indicated that compound 9o activated Nrf2/HO-1 signaling pathway via accumulation ROS and blocks the NF-kappa B/MAPK signaling pathway. The in vivo anti-inflammatory activity shown that compound 90 had obvious therapeutic effect against the adjuvant-induced rat arthritis model. (C) 2020 Elsevier Masson SAS. All rights reserved.
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Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem