title: Remedial effects of novel 2,3-disubstituted thiazolidin-4-ones in chemical mediated inflammation.
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.
authors.affiliation: Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, Karnataka, India.
authors.forename: Jayesh
authors.initials: J
authors.lastname: Mudgal
authors.affiliation: Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, Karnataka, India.
authors.forename: Vasantharaju S
authors.initials: VS
authors.lastname: Gowdra
authors.affiliation: Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, Karnataka, India.
authors.forename: Geetha
authors.initials: G
authors.lastname: Mathew
authors.affiliation: Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, Karnataka, India.
authors.forename: Pawan G
authors.initials: PG
authors.lastname: Nayak
authors.affiliation: Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, Karnataka, India.
authors.forename: Nitin D
authors.initials: ND
authors.lastname: Reddy
authors.affiliation: Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, Karnataka, India.
authors.forename: Neelesh
authors.initials: N
authors.lastname: Namdeo
authors.affiliation: Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, Karnataka, India.
authors.forename: Ravilla R
authors.initials: RR
authors.lastname: Kumar
authors.affiliation: Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, Karnataka, India.
authors.forename: Chaitanya
authors.initials: C
authors.lastname: Kantamaneni
authors.affiliation: Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, Karnataka, India.
authors.forename: Mallikarjuna R
authors.initials: MR
authors.lastname: Chamallamudi
authors.affiliation: Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576 104, Karnataka, India. Electronic address: ng.kutty@manipal.edu.
authors.forename: Gopalan K
authors.initials: GK
authors.lastname: Nampurath
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015153:Blotting, Western; D002351:Carrageenan; D002460:Cell Line; D051545:Cyclooxygenase 1 / Q000378:metabolism; D004797:Enzyme-Linked Immunosorbent Assay; D005260:Female; D007249:Inflammation / Q000097:blood / Q000139:chemically induced*; D008264:Macrophages / Q000187:drug effects* / Q000276:immunology; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D053778:Thiazolidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000893:Anti-Inflammatory Agents; D053778:Thiazolidines; D002351:Carrageenan; D051545:Cyclooxygenase 1; C496511:PTGS1 protein, human
keywords: Cyclo-oxygenase; Cytokines; Inflammation; Myeloperoxidase; Prostaglandins; Thiazolidin-4-one