EUK 134, a synthetic superoxide dismutase (SOD)/catalase mimetic, exhibits potent antioxidant activities, and inhibits the formation of β-amyloid and related amyloid fibril.

 EUK 134 shows potent catalase and SOD activities, and protects human fibroblasts against cytotoxicity by glucose and glucose oxidase. [1] EUK 134 (20 μM) prevents Aβ-induced microglial proliferation in vitro. [2] 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. [3] EUK 134 significantly inhibits amyloid formation at two molar ratios of 1:1 and 5:1 (drugs to protein). [4]

 EUK 134 (2.5 mg/kg), in a middle cerebral artery occlusion model, significantly reduces brain infarct size, and apparently prevents further infarct growth. [1] EUK-134 prevents oxidative stress and attenuates rat brain damage induced by systemic administration of systemic kainic acid (KA). [5]

 

References

[1] Baker K, et al. J Pharmacol Exp Ther. 1998, 284(1), 215-221.

[2] Jekabsone A, et al. J Neuroinflammation. 2006, 3, 24.

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