8-oxocoptisine and Acute-Disease
8-oxocoptisine has been researched along with Acute-Disease* in 1 studies
Other Studies
1 other study(ies) available for 8-oxocoptisine and Acute-Disease
Article | Year |
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Synthesis and Structure-Activity Relationships of Quaternary Coptisine Derivatives as Potential Anti-ulcerative Colitis Agents.
Thirty quaternary coptisine derivatives from a synthesized library were found to activate the in vitro transcription of x-box-binding protein 1 (XBP1). Among these, the dihydrocoptisines were demonstrated by in vitro XBP1 transcriptional activity assays and animal experiments to be much more active anti-ulcerative colitis (UC) agents than quaternary coptisines, tetrahydrocoptisines, and the positive control. Unsubstituted dihydrocoptisine exhibited more significant anti-UC efficacy than dihydrocoptisines substituted at the C-8 or C-13 position. The EC50 value of dihydrocoptisine for XBP1 transcriptional activation was 2.25 nM. Dihydrocoptisine exhibited a significant dose-effect relationship, as indicated by biomarkers in in vitro and in vivo experiments. According to this study, the starting material's reductive states and the substitution patterns of the dihydrocoptisines were determined to be the critical parameters for modulating their anti-UC efficacy, and the dihydrocoptisine skeleton was designated as the key pharmacophore. The synthesized dihydrocoptisine is a promising lead for developing anti-UC drugs. Topics: Acute Disease; Animals; Anti-Inflammatory Agents; Berberine; Cell Line; Colitis, Ulcerative; Colon; Dextran Sulfate; DNA-Binding Proteins; Mice, Inbred C57BL; Muscle Contraction; Muscle, Smooth; Rats; Regulatory Factor X Transcription Factors; Stereoisomerism; Structure-Activity Relationship; Transcription Factors; Transcriptional Activation; X-Box Binding Protein 1 | 2015 |