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

Mit Joshi, Neetinkumar D. Reddy, Nitesh Kumara, Suhani Sumalatha, C. Mallikarjuna Rao

Research output: Contribution to journalArticle

Abstract

BACKGROUND: Histone deacetylase (HDAC) inhibition has been found to be effective in the treatment of inflammatory bowel disease. Previous studies reported that Cinnamyl sulfonamide hydroxamate derivatives possessed nonselective HDAC inhibition. OBJECTIVE: The present study was designed to screen three selected Cinnamyl sulfonamide hydroxamate derivatives, NMJ1, 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. DNCB-induced 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 observed by NMJ1 and NMJ2 by a significant decrease in pNF-κB overexpression-induced by LPS. Similar effect was observed in anti-colitis responses by NMJ2 in both models by reversing the colitis-induced changes in length, weight, antioxidant 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.

Original languageEnglish
JournalCurrent Pharmaceutical Design
DOIs
Publication statusAccepted/In press - 24-06-2020

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery

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