Remedial effects of novel 2,3-disubstituted thiazolidin-4-ones in chemical mediated inflammation

Jayesh Mudgal, Vasantharaju S. Gowdra, Geetha Mathew, Pawan G. Nayak, Nitin D. Reddy, Neelesh Namdeo, Ravilla R. Kumar, Chaitanya Kantamaneni, Mallikarjuna R. Chamallamudi, Gopalan K. Nampurath

Research output: Contribution to journalArticle

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Abstract

Abstract Three thiazolidin-4-one derivatives were synthesized, purified and characterized by chromatographic and spectroscopic methods. In the in vitro assays, these compounds inhibited reactive oxygen species (ROS), nitrite and cytokine generation in RAW 264.7 murine macrophages and whole blood. These derivatives attenuated carrageenan-induced acute inflammation in rats. The most effective compound 4C possessed identical anti-inflammatory action at two doses (50 and 100 mg/kg). Further, the effect of compound 4C on locally induced inflammatory mediators was investigated in carrageenan-induced air pouch inflammation in rats. In this model, compound 4C inhibited the cytokines, tumor necrosis factor (TNF)-α and interleukin (IL)-6 (systemic and local). Additionally, compound 4C was able to reduce locally elevated prostaglandin-E2 (PGE2). Inhibition of leukocyte infiltration by compound 4C was correlated with reduced locally released myeloperoxidase (MPO). To conclude, compound 4C corrected the inflammatory condition by negative effect on cytokine (TNF-α, IL-6) network and prostaglandin-E2 generation.

Original languageEnglish
Pages (from-to)34-42
Number of pages9
JournalChemico-Biological Interactions
Volume210
Issue number1
DOIs
Publication statusPublished - 05-03-2014

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Carrageenan
Cytokines
Inflammation
Dinoprostone
Rats
Interleukin-6
Tumor Necrosis Factor-alpha
Derivatives
Macrophages
Nitrites
Infiltration
Peroxidase
Assays
Reactive Oxygen Species
Leukocytes
Blood
Anti-Inflammatory Agents
Air
In Vitro Techniques

All Science Journal Classification (ASJC) codes

  • Toxicology

Cite this

Mudgal, Jayesh ; Gowdra, Vasantharaju S. ; Mathew, Geetha ; Nayak, Pawan G. ; Reddy, Nitin D. ; Namdeo, Neelesh ; Kumar, Ravilla R. ; Kantamaneni, Chaitanya ; Chamallamudi, Mallikarjuna R. ; Nampurath, Gopalan K. / Remedial effects of novel 2,3-disubstituted thiazolidin-4-ones in chemical mediated inflammation. In: Chemico-Biological Interactions. 2014 ; Vol. 210, No. 1. pp. 34-42.
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Remedial effects of novel 2,3-disubstituted thiazolidin-4-ones in chemical mediated inflammation. / Mudgal, Jayesh; Gowdra, Vasantharaju S.; Mathew, Geetha; Nayak, Pawan G.; Reddy, Nitin D.; Namdeo, Neelesh; Kumar, Ravilla R.; Kantamaneni, Chaitanya; Chamallamudi, Mallikarjuna R.; Nampurath, Gopalan K.

In: Chemico-Biological Interactions, Vol. 210, No. 1, 05.03.2014, p. 34-42.

Research output: Contribution to journalArticle

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AU - Kumar, Ravilla R.

AU - Kantamaneni, Chaitanya

AU - Chamallamudi, Mallikarjuna R.

AU - Nampurath, Gopalan K.

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N2 - Abstract Three thiazolidin-4-one derivatives were synthesized, purified and characterized by chromatographic and spectroscopic methods. In the in vitro assays, these compounds inhibited reactive oxygen species (ROS), nitrite and cytokine generation in RAW 264.7 murine macrophages and whole blood. These derivatives attenuated carrageenan-induced acute inflammation in rats. The most effective compound 4C possessed identical anti-inflammatory action at two doses (50 and 100 mg/kg). Further, the effect of compound 4C on locally induced inflammatory mediators was investigated in carrageenan-induced air pouch inflammation in rats. In this model, compound 4C inhibited the cytokines, tumor necrosis factor (TNF)-α and interleukin (IL)-6 (systemic and local). Additionally, compound 4C was able to reduce locally elevated prostaglandin-E2 (PGE2). Inhibition of leukocyte infiltration by compound 4C was correlated with reduced locally released myeloperoxidase (MPO). To conclude, compound 4C corrected the inflammatory condition by negative effect on cytokine (TNF-α, IL-6) network and prostaglandin-E2 generation.

AB - Abstract Three thiazolidin-4-one derivatives were synthesized, purified and characterized by chromatographic and spectroscopic methods. In the in vitro assays, these compounds inhibited reactive oxygen species (ROS), nitrite and cytokine generation in RAW 264.7 murine macrophages and whole blood. These derivatives attenuated carrageenan-induced acute inflammation in rats. The most effective compound 4C possessed identical anti-inflammatory action at two doses (50 and 100 mg/kg). Further, the effect of compound 4C on locally induced inflammatory mediators was investigated in carrageenan-induced air pouch inflammation in rats. In this model, compound 4C inhibited the cytokines, tumor necrosis factor (TNF)-α and interleukin (IL)-6 (systemic and local). Additionally, compound 4C was able to reduce locally elevated prostaglandin-E2 (PGE2). Inhibition of leukocyte infiltration by compound 4C was correlated with reduced locally released myeloperoxidase (MPO). To conclude, compound 4C corrected the inflammatory condition by negative effect on cytokine (TNF-α, IL-6) network and prostaglandin-E2 generation.

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