Downregulation of inflammatory responses by novel caffeic acid ester derivative by inhibiting NF-kappa B.
BACKGROUND
Considering anti-tumorigenic activity of caffeic acid phenyl ester, synthesis of several esterified form of caffeic acid is a novel approach in designing for potent drugs.


RESULTS
Our study demonstrates that esterified caffeic acid with methyl vanillate, termed as caffeic acid methyl vanillate ester (CAMVE), blocked inflammatory stimuli-induced inflammatory responses. It decreased amounts of iNOS, Cox-2, and ICAM1 by inhibiting NF-kappaB through inhibition of IKK activity, I kappaB alpha degradation, and p65 nuclear translocation.


CONCLUSIONS
Overall, our data suggest that novel caffeic acid ester down-regulates inflammatory responses through inhibition of NF-kappaB and dependent several gene expressions, further suggesting its efficacy as a promising therapeutic agent.
Bose
Julie S
JS
Reliance Life Sciences Pvt. Ltd., Mumbai, India.
Gangan
Vijay
V
Jain
Swatantra Kumar
SK
Manna
Sunil K
SK
D021581:Active Transport, Cell Nucleus / Q000187:drug effects; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002109:Caffeic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D045744:Cell Line, Tumor; D051546:Cyclooxygenase 2 / Q000187:drug effects / Q000276:immunology / Q000378:metabolism; D015536:Down-Regulation; D006801:Humans; D051550:I-kappa B Kinase / Q000037:antagonists & inhibitors / Q000276:immunology / Q000378:metabolism*; D007249:Inflammation / Q000276:immunology / Q000378:metabolism; D018799:Intercellular Adhesion Molecule-1 / Q000187:drug effects / Q000276:immunology / Q000378:metabolism; D051379:Mice; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009569:Nitric Oxide / Q000037:antagonists & inhibitors / Q000276:immunology / Q000378:metabolism*; D051996:Transcription Factor RelA / Q000037:antagonists & inhibitors / Q000378:metabolism
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002109:Caffeic Acids; D016328:NF-kappa B; D051996:Transcription Factor RelA; C541004:caffeic acid methyl vanillate ester; D018799:Intercellular Adhesion Molecule-1; D009569:Nitric Oxide; D051546:Cyclooxygenase 2; D051550:I-kappa B Kinase
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