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摘要来源:
pharmacol premacolRep。2021Jun28。Epub2021 Jun28。pmid:34181212
Abstract Author(s):Sudheer Moorkoth, N Sai Prathyusha, Suman Manandhar, Yuanxin Xue, Runali Sankhe, K S R Pai, Nitesh Kumar
Article Affiliation:Sudheer Moorkoth
Abstract:BACKGROUND: Dehydrozingerone (DHZ) is an active ingredient of Zingiber officinale and structural half analogue of curcumin.在本研究中,评估了DHz的单胺氧化酶(MAO)抑制活性在硅和V中的抗抑郁活性ivo.
METHOD: The binding affinity of DHZ with MAO-A (PDB ID: 2Z5Y) was assessed using Schrodingers Maestro followed by free energy calculation, pharmacokinetic property prediction using Qikprop and Molecular dynamics simulation using Desmond.使用Escilatopram作为标准抗抑郁药,在C57 BL/6恶质上评估了DHz的体内抗抑郁活性。使用开放式测试(FST),强制游泳测试(FST)和尾悬浮测试(TST)来评估药物在第1和第7天的抗抑郁作用。在行为研究之后,使用液体色谱学跨度量估计了行为研究,神经肾上腺素,多巴胺和血清素)。 class =“ sub_abstract_label”>结果: dhz与硅中的moclobemide相比,对MAO-A酶具有更大的结合亲和力。 TST和FST中的固定性显着(P <0.05),体内降低了100mg/kg DHz的体内降低与各自的对照相比。与车辆对照相比,治疗后1小时的DHz治疗更有效。 A significant increase in levels of neurotransmitters was observed in mice brain homogenate in response to DHZ treatment, reassuring its antidepressant-like potential.
CONCLUSION: DHZ demonstrated MAO-A inhibition in silico, and the increased neurotransmitter levels in the brain in vivo were与抗抑郁药样效果相关。