Synthesis and Anti-Inflammatory Activity of Ferulic Acid-Sesquiterpene Lactone Hybrids

Acute lung injury (ALI) is a respiratory failure disease associated with high mortality rates in patients. The primary pathological damage is attributed to the excessive release of pro-inflammatory mediators in pulmonary tissue. However, specific therapy for ALI has not been developed. In this study...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2024-02, Vol.29 (5), p.936
Main Authors: Duan, Xiyan, Liu, Ning, Lv, Ke, Wang, Junqi, Li, Mingyue, Zhang, Yanwei, Huo, Xiaoguang, Bao, Shiqi, Shen, Zhuo, Zhang, Xuemei
Format: Article
Language:English
Subjects:
Acids
acute lung injury
Acute Lung Injury - drug therapy
Animals
anti-inflammatory activity
Anti-Inflammatory Agents - pharmacology
Anti-inflammatory drugs
Bioavailability
Brain cancer
Coumaric Acids
Cytokines
Cytokines - metabolism
Drug dosages
ferulic acid
Fibroblasts
Health aspects
Humans
Inflammation
Lactones - pharmacology
Lipopolysaccharides - adverse effects
Lung - metabolism
Lung diseases
Mice
micheliolide
Microbiota
Mortality
parthenolide
Sepsis
Sesquiterpenes - pharmacology
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Summary:Acute lung injury (ALI) is a respiratory failure disease associated with high mortality rates in patients. The primary pathological damage is attributed to the excessive release of pro-inflammatory mediators in pulmonary tissue. However, specific therapy for ALI has not been developed. In this study, a series of novel ferulic acid-parthenolide (FA-PTL) and ferulic acid-micheliolide (FA-MCL) hybrid derivatives were designed, synthesized, and evaluated for their anti-inflammatory activities in vitro. Compounds , , and showed pronounced anti-inflammatory activity against LPS-induced expression of pro-inflammatory cytokines in vitro. Importantly, compound displayed good water solubility, and treatment of mice with compound (10 mg/kg) significantly prevented weight loss and ameliorated inflammatory cell infiltration and edema in lung tissue, as well as improving the alveolar structure. These results suggest that compound (((1a ,7a ,8 ,10a ,10b , )-8-((dimethylamino)methyl)-1a-methyl-9-oxo-1a,2,3,6,7,7a,8,9,10a,10b-decahydrooxireno[2',3':9,10]cyclodeca[1,2-b]furan-5-yl)methyl ( )-3-(4-hydroxy-3-methoxyphenyl)acrylate 2-hydroxypropane-1,2,3-tricarboxylate) might be considered as a lead compound for further evaluation as a potential anti-ALI agent.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules29050936