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Amino-alcohol Bio-conjugate of Naproxen Exhibits Anti-inflammatory Activity through NF-κB Signaling Pathway

By Mahua Rani Das, Anindyajit Banerjee, Sourav Sarkar, Joydeb Majumder, Saikat Chakrabarti, Siddhartha Sankar Jana

Posted 10 Jan 2020
bioRxiv DOI: 10.1101/2020.01.10.901223

Naproxen sodium (Ns) is a well-known synthetic compound used vastly as a nonsteroidal anti-inflammatory drug (NSAID). Previously, we demonstrated that the hydrogels, made of Ns bio-conjugate (NBC), either with amino alcohol (NBC-1 and 2) or amino acid (NBC-3 and 4), displayed anti-inflammatory properties better than Ns, but the effectiveness was not well explored. Here, we investigated that NBC-2, conjugated with γ-amino alcohol, significantly reduces the expression of pro-inflammatory proteins; such as inducible nitric oxide synthase (iNOS) and cyclooxygenase isoform-2 (COX-2), and the production of pro-inflammatory mediator nitric oxide (NO) in lipopolysaccharide and interferon-γ (LPS/IFN-γ) treated mouse macrophage RAW 264.7 cells, compared with bio-conjugation of β-amino alcohol (NBC-1) or β-amino acid (NBC-3) or α-amino acid NBC (NBC-4). NBC-2 decreases the nuclear localization of transcription factors NF-κB by stabilizing its cytoplasmic functional inhibitor IκBα. Moreover, NBC-2 also displays selective inhibitory effect towards COX-1 enzyme activity as determined by enzymatic assay and in silico molecular docking analysis. Thus, we suggest that NBC-2 may be used as a self-delivery anti-inflammatory drug as compared with other NBCs.

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