In Vitro | In vitro activity: EUK 134 shows potent catalase and SOD activities, and protects human fibroblasts against cytotoxicity by glucose and glucose oxidase. EUK 134 (20 μM) prevents Aβ-induced microglial proliferation in vitro. In SK-N-MC cells, EUK134 protects neuronal cells against H(2)O(2) toxicity by attenuating oxidative stress through inhibition of MAPK pathway, and also results in decreased expression of pro-apoptotic genes p53 and Bax as well as enhanced expression of anti-apoptotic Bcl-2 gene. EUK 134 significantly inhibits amyloid formation at two molar ratios of 1:1 and 5:1 (drugs to protein).
Cell Assay: in SK-N-MC cells, EUK134 protects neuronal cells against H2O2 toxicity by attenuating oxidative stress through inhibition of MAPK pathway, and also results in decreased expression of pro-apoptotic genes p53 and Bax as well as enhanced expression of anti-apoptotic Bcl-2 gene. Pretreatment with EUK-134 (10 μM) was effective in the prevention of hypertrophic changes in H9C2 cells, reduction of oxidative stress, and prevention of metabolic shift. EUK-134 treatment improved the oxidative status of mitochondria and reversed hypertrophy-induced reduction of mitochondrial membrane potential. |
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