Design, biological evaluation, and molecular modelling insights of cupressic acid derivatives as promising anti-inflammatory agents

The major labdanes in the oleogum resin of Araucaria heterophylla (Salisb.) Franco, 13-epi-cupressic acid (1) and acetyl-13-epi-cupressic acid (2) were used to prepare seven new (3-9), along with one known (10) derivatives. RAW264.7 cells were used to evaluate the anti-inflammatory activity of the d...

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Bibliographic Details
Published in:Journal of enzyme inhibition and medicinal chemistry 2023-12, Vol.38 (1), p.2187327-2187327
Main Authors: Soliman, Amal F., Elimam, Diaaeldin M., El-Senduny, Fardous F., Alossaimi, Manal A., Alamri, Mubarak, Abdel Bar, Fatma M.
Format: Article
Language:English
Subjects:
Acids
Anti-inflammatory agents
Anti-Inflammatory Agents - pharmacology
anti-inflammatory leads
COX-2 gene expression
Cupressic acid derivatives
Cyclooxygenase 2 - metabolism
Diterpenes
Enzymes
Hydrophobicity
Inflammation
Interleukin 6
labdane diterpenoids
Lipopolysaccharides
Lipopolysaccharides - pharmacology
Molecular modelling
NMR
Nuclear magnetic resonance
Pharmacy
Phospholipase A2
Phospholipases A2
RAW264.7 cell line
Research Paper
Tumor necrosis factor-TNF
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Summary:The major labdanes in the oleogum resin of Araucaria heterophylla (Salisb.) Franco, 13-epi-cupressic acid (1) and acetyl-13-epi-cupressic acid (2) were used to prepare seven new (3-9), along with one known (10) derivatives. RAW264.7 cells were used to evaluate the anti-inflammatory activity of the derivatives (1-10) via measuring the level of COX-2 expression and IL-6. Pre-treated RAW264.7 cells with 1-10 (except for derivative 7) at 25 µM for 24h exhibited downregulation of COX-2 expression in response to LPS stimulation. Moreover, pre-treatment with compounds 1, 2, or 3 significantly attenuated the LPS-stimulated IL-6 level in RAW264.7 cells (p 
ISSN:1475-6366
1475-6374
DOI:10.1080/14756366.2023.2187327