Cinnamyl Sulfonamide Hydroxamate Derivatives Inhibited LPS-Stimulated NF-kB Expression in RAW 264.7 Cells In Vitro and Mitigated Experimental Colitis in Wistar Rats In Vivo

Joshi, Mit and Reddy, Neetinkumar D and Kumar, Nitesh and Sumalatha, Suhani and Rao, Mallikarjuna C (2020) Cinnamyl Sulfonamide Hydroxamate Derivatives Inhibited LPS-Stimulated NF-kB Expression in RAW 264.7 Cells In Vitro and Mitigated Experimental Colitis in Wistar Rats In Vivo. Current Pharmaceutical Design, 26. pp. 1-10. ISSN 1381-6128

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Abstract

Background: Histone deacetylase (HDAC) inhibition has been found to be effective in the treatment of inflammatory bowel disease. Previous studies have reported that Cinnamyl sulfonamide hydroxamate derivatives possess non-selective HDAC inhibition.Objective: The present study was designed to screen three selected Cinnamyl sulfonamide hydroxamate derivatives,NMJ-1, NMJ-2, and NMJ3, for in vitro anti-inflammatory response by assessing the expression of pNF-κB in lipopolysaccharide (LPS)-induced inflammatory changes on RAW 264.7 cells, and in vivo anti-inflammatory response in acetic acid (AA) and 2.4-dinitrochlorobenzene (DNCB)-induced colitis models in Wistar rats.Method: AA-induced colitis was produced in Wistar rats by intra-colonic administration of 1 ml AA. DNCBinduced colitis was produced by spraying 250 μL DNCB in acetone (20g/L) on the nape of the rats for 14 days,followed by the intracolonic administration on day 15. Drugs were administered for three days after the induction of colitis. Results: In vitro anti-inflammatory effect was observed by NMJ1 and NMJ2 through a significant decrease in pNF-κB overexpression-induced by LPS. Similar effect was observed in anti-colitis response by NMJ2 in both models by reversing the colitis-induced changes in length, weight, anti-oxidant profile and histopathology of the colon.Conclusion: NMJ2 was found to be most effective among the tested compounds as an anti-inflammatory agent in both in vitro and in vivo inflammatory studies

Item Type: Article
Uncontrolled Keywords: Inflammatory bowel disease; Cinnamyl sulfonamide hydroxamate derivatives; Sulphasalazine; 2,4-Dinitrochlorobenzene- nduced colitis; Acetic acid-induced colitis; HDAC inhibitors; Anti-oxidant, NF-κB
Subjects: Medicine > KMC Manipal > Anatomy
Pharmacy > MCOPS Manipal > Pharmacology
Depositing User: KMC Library
Date Deposited: 21 Oct 2020 10:27
Last Modified: 21 Oct 2020 10:27
URI: http://eprints.manipal.edu/id/eprint/155915

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