Cheng, Xiao-jing published the artcileTacrine-Hydrogen Sulfide Donor Hybrid Ameliorates Cognitive Impairment in the Aluminum Chloride Mouse Model of Alzheimer’s Disease, HPLC of Formula: 1885-29-6, the main research area is tacrine hydrogen sulfide Alzheimer antiAlzheimer acetylcholinesterase; AChE; HS donor; Tacrine; hepatotoxicity; neuroinflammation; synaptic plasticity.
Alzheimer’s disease (AD) is a neurodegenerative disorder, characterized by progressive loss of memory and cognitive function, and is associated with the deficiency of synaptic acetylcholine, as well as chronic neuroinflammation. Tacrine, a potent acetylcholinesterase (AChE) inhibitor, was previously a prescribed clin. therapeutic agent for AD, but was recently withdrawn because it caused widespread hepatotoxicity. Hydrogen sulfide (H2S) has neuroprotective, hepatoprotective and anti-inflammatory effects. In this study, we synthesized a new compound, a tacrine- H2S donor hybrid (THS) by introducing H2S-releasing moieties (ACS81) to tacrine. Subsequently, pharmacol. and biol. evaluations of THS were conducted in the aluminum trichloride (AlCl3)-induced AD mice model. We found that THS (15mmol/kg) improved cognitive and locomotor activity in AD mice in the step-through test and open field test resp. THS showed strong AChE inhibitory activity in the serum and hippocampus of AD mice and induced increased hippocampal H2S levels. Furthermore, THS reduced mRNA expression of the proinflammatory cytokines, TNF-α, IL-6, and IL-1β and increased synapse-associated proteins (synaptophysin and postsynaptic d. protein 95) in the hippocampus of AD mice. Importantly, THS, unlike tacrine, did not increase liver transaminases (alanine transaminase and aspartate transaminase) or proinflammatory cytokines, indicating THS is much safer than tacrine. Therefore, the multifunctional effects of this new hybrid compound of tacrine and H2S indicate it is a promising compound for further research into the treatment of AD.
ACS Chemical Neuroscience published new progress about Alzheimer disease. 1885-29-6 belongs to class nitriles-buliding-blocks, name is 2-Aminobenzonitrile(Flakes or Chunks), and the molecular formula is C7H6N2, HPLC of Formula: 1885-29-6.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts