Effect of sulfonamide derivatives of phenylglycine on scopolamine-induced amnesia in rats

Ibrain Pub Date : 2023-02-14 DOI:10.1002/ibra.12092
Ankit Ganeshpurkar, Ravi Singh, Pratigya Tripathi, Qadir Alam, Sairam Krishnamurthy, Ashok Kumar, Sushil K. Singh
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Abstract

Alzheimer's disease is a neurodegenerative disease responsible for dementia and other neuropsychiatric symptoms. In the present study, compounds 30 and 33, developed earlier in our laboratory as selective butyrylcholinesterase inhibitors, were tested against scopolamine-induced amnesia to evaluate their pharmacodynamic effect. The efficacy of the compounds was determined by behavioral experiments using the Y-maze and the Barnes maze and neurochemical testing. Both compounds reduced the effect of scopolamine treatment in the behavioral tasks at a dose of 20 mg/kg. The results of the neurochemical experiment indicated a reduction in cholinesterase activity in the prefrontal cortex and the hippocampus. The levels of antioxidant enzymes superoxide dismutase and catalase were restored compared to the scopolamine-treated groups. The docking study on rat butyrylcholinesterase (BChE) indicated tight binding, with free energies of −9.66 and −10.23 kcal/mol for compounds 30 and 33, respectively. The two aromatic amide derivatives of 2-phenyl-2-(phenylsulfonamido) acetic acid produced stable complexes with rat BChE in the molecular dynamics investigation.

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苯甘氨酸磺酰胺衍生物对东莨菪碱所致大鼠健忘症的影响
阿尔茨海默病是一种神经退行性疾病,可导致痴呆和其他神经精神症状。在本研究中,我们实验室早期开发的化合物30和33作为选择性丁酰胆碱酯酶抑制剂,对东莨菪碱诱导的健忘症进行了测试,以评估其药效学效果。通过使用Y迷宫和Barnes迷宫的行为实验以及神经化学测试来确定化合物的功效。这两种化合物都降低了东莨菪碱治疗行为任务的效果,剂量为20 mg/kg。神经化学实验的结果表明,前额叶皮层和海马体的胆碱酯酶活性降低。与东莨菪碱处理组相比,抗氧化酶超氧化物歧化酶和过氧化氢酶的水平得到恢复。对大鼠丁酰胆碱酯酶(BChE)的对接研究表明,其结合紧密,自由能为−9.66和−10.23 对于化合物30和33分别为kcal/mol。在分子动力学研究中,2-苯基-2-(苯基磺酰胺基)乙酸的两种芳香酰胺衍生物与大鼠BChE产生了稳定的配合物。
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