Related Experiment Video
Updated: May 23, 2026

Screening Bioactive Nanoparticles in Phagocytic Immune Cells for Inhibitors of Toll-like Receptor Signaling
Published on: July 26, 2017
Design and synthesis of trolline derivatives with Nrf2 pathway-associated anti-inflammatory activity
Bill Zhereng Liao1, Qi-Mei Tan1, Ya-Lin Li1
1Jiangsu Key Laboratory of Bioactive Natural Product Research, State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, People's Republic of China.
Abstract:
Activation of nuclear factor erythroid-2-related factor 2 (NRF2) has been proven to be an effective means to prevent the development of inflammatory diseases. In this study, series of trolline derivatives (4 -25) were designed and synthesized as potential anti-inflammatory agents. Among them, compound 5 showed the best activity, with an IC₅₀ value of 7.86 μM, by evaluation of the inhibition of NO production in LPS-stimulated RAW264.7 macrophages. Chiral separation of compound 5 further gave 5-S and 5-R, and 5-S proved to be the more active enantiomer in the NO assay (IC₅₀ = 5.89 μM), while 5-R was less active (IC₅₀ = 13.71 μM). Moreover, 5-S significantly reduced the production of TNF-α, IL-1β, and IL-6 in LPS-stimulated RAW264.7 cells. Western blot analysis showed that 5-S increased Nrf2 expression and promoted its nuclear translocation, accompanied by upregulation of the downstream target proteins HO-1 and NQO1. These results suggest that the anti-inflammatory effect of 5-S is associated with activation of the Nrf2 pathway. Overall, 5-S may serve as a potential lead for further development of trolline-based anti-inflammatory agents.
Related Concept Videos
NF-κB-dependent Signaling Pathway
NF-κB-dependent Signaling Mechanism
The heterodimer of NF-κB...
TGF - β Signaling Pathway
NF-kB-dependent Signaling Pathway
NF-κB-dependent Signaling Mechanism
The heterodimer of NF-κB...
Inhibitors of Viral Protein Synthesis
Inflammatory Response
Inflammation can be triggered by various stimuli, such as impact, abrasion, chemical irritation, infections, and extreme hot or cold temperatures. These can damage cells and connective tissue fibers,...
Nitric Oxide Signaling Pathway
