Promising Technologies

Pharmaceutical Compound for Treating Neurodegenerative Disease

  • Inventor
    Prof. Eosu Kim
    MD, Ph.D
    Dept of Psychiatry
  • Category
    Alzheimer's Disease, Dementia
  • Keywords
    Alzheimer’s disease, Dementia, Cognitive aging, AMPK, neuroprotection, cognitive enhancer, anti-dementic drug
  • Current development stage
  • Patent Status
    PCT/KR2017/005061
    EPO,US patent application
  • Brief Description
    AMP-activated kinase (AMPK) is a pivotal enzyme regulating metabolism. Activating AMPK has been shown to enhance cognitive function. AMPK activity has been also related to various actions suppressing Alzheimer’s pathophysiology by modulating autophagy, beta-amyloid clearance, mitochondrial biogenesis, neurogenesis, and cell protection. YE-06 is a novel compound and a novel AMPK activator, screened from a chemical library and structurally modified. YE-06 enhances cognitive function in a mouse model of Alzheimer’s disease, which was identified by Water Morris Maze Test and Passive Avoidance Test. YE-06 suppresses acetylcholinesterase activity and increases acetylcholine content in the brain and inhibits apoptotic neuronal death against beta-amyloid toxicity, and such cell protection ability of YE-06 is superior than that of donepezil, which was identified by TUNEL assay. Half-life (T1/2) of YE-06 upon 2mg/kg peroral treatment was 3.73±0.54 hrs and bioavailability was 76.06% and Permeability of YE-06 was – 4.4±0.15 (medium degree), measured by PAMPA assay. Cardiotoxicity assessed by hERG K+ Channel Binding Assay was also ‘negative’ and Acute in vivo toxicity was as 0% lethality at 1000mg/kg (n = 6).
  • Representative figure

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