title: Anti-Inflammatory Effects of Protein Kinase Inhibitor Pyrrol Derivate.
abstract: In our previous studies we showed antitumor and anti-inflammatory activities of protein kinases inhibitor pyrrol derivate 1-(4-Cl-benzyl)-3-Cl-4-(CF3-fenylamino)-1H-pyrrol-2,5-dione (MI-1) on rat colon cancer model. Therefore anti-inflammatory effect of MI-1 on rat acetic acid induced ulcerative colitis (UC) model was aimed to be discovered. The anti-inflammatory effects of MI-1 (2.7 mg/kg daily) compared to reference drug Prednisolone (0.7 mg/kg daily) after 14-day usage were evaluated on macro- and light microscopy levels and expressed in 21-grade scale. Redox status of bowel mucosa was also estimated. It was shown that in UC group the grade of total injury (GTI) was equal to 9.6 (GTIcontrol= 0). Increase of malonic dialdehyde (MDA) by 89% and protein carbonyl groups (PCG) by 60% and decrease of superoxide dismutase (SOD) by 40% were also observed. Prednisolone decreased GTI to 3 and leveled SOD activity, but MDA and PCG remained higher than control ones by 52% and 42%, respectively. MI-1 restored colon mucosa integrity and decreased mucosa inflammation down to GTI = 0.5 and leveled PCG and SOD. Thus, MI-1 possessed anti-inflammatory properties, which were more expressed that Prednisolone ones, as well as normalized mucosa redox balance, and so has a prospect for correction of inflammatory processes.
authors.affiliation: Institute of Biology, Taras Shevchenko National University, Volodymyrska 64/13, Kyiv 01601, Ukraine.
authors.forename: Halyna M
authors.identifier: 0000-0002-1296-1007
authors.initials: HM
authors.lastname: Kuznietsova
authors.affiliation: Institute of Biology, Taras Shevchenko National University, Volodymyrska 64/13, Kyiv 01601, Ukraine.
authors.forename: Maryna S
authors.initials: MS
authors.lastname: Yena
authors.affiliation: Institute of Biology, Taras Shevchenko National University, Volodymyrska 64/13, Kyiv 01601, Ukraine.
authors.forename: Iryna P
authors.initials: IP
authors.lastname: Kotlyar
authors.affiliation: Institute of Biology, Taras Shevchenko National University, Volodymyrska 64/13, Kyiv 01601, Ukraine.
authors.forename: Olexandr V
authors.initials: OV
authors.lastname: Ogloblya
authors.affiliation: Institute of Biology, Taras Shevchenko National University, Volodymyrska 64/13, Kyiv 01601, Ukraine.
authors.forename: Volodymyr K
authors.initials: VK
authors.lastname: Rybalchenko
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D003093:Colitis, Ulcerative / Q000139:chemically induced / Q000188:drug therapy*; D003106:Colon / Q000187:drug effects; D007413:Intestinal Mucosa / Q000187:drug effects; D011239:Prednisolone / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D051381:Rats
chemical_list: D000893:Anti-Inflammatory Agents; D047428:Protein Kinase Inhibitors; D011239:Prednisolone