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评价查尔酮 1203 在多种小鼠实验性抑郁模型中的潜在抗抑郁样活性。

Evaluation of potential antidepressant-like activity of chalcone-1203 in various murine experimental depressant models.

机构信息

Zhejiang Provincial Key Engineering Technology Research Center of Marine Biomedical Products, Food and Pharmacy College, Zhejiang Ocean University, Zhejiang, 316000, Zhoushan, People's Republic of China,

出版信息

Neurochem Res. 2014 Feb;39(2):313-20. doi: 10.1007/s11064-013-1224-8. Epub 2013 Dec 17.

Abstract

Two classic animal behavior despair tests-the forced swimming test (FST) and the tail suspension test (TST) were used to evaluate antidepressant-like activity of a new chalcone compound, chalcone-1203 in mice. It was observed that chalcone-1203 at dose of 1, 5, and 10 mg/kg significantly reduced the immobility time in the FST and TST in mice 30 min after treatment. In addition, chalcone-1203 was found to exhibit significant oral activity in the FST in mice. It also produced a reduction in the ambulation in the open-field test in mice not previously habituated to the arena, but no effect in the locomotor activity in mice previously habituated to the open-field. The main monoamine neurotransmitters and their metabolites in mouse brain regions were also simultaneously determined by HPLC-ECD. It was found that chalcone-1203 significantly increased the concentrations of the main neurotransmitters 5-HT and NE in the hippocampus, hypothalamus and cortex. Chalcone-1203 also significantly reduced the ratio of 5-HIAA/5-HT in the hippocampus and cortex, shown down 5-HT metabolism compared with mice treated with stress vehicle. In conclusion, chalcone-1203 produced significant antidepressant-like activity, and the mechanism of action may be due to increased 5-HT and NE in the mouse hippocampus and cortex.

摘要

两种经典的动物行为绝望测试——强迫游泳测试(FST)和悬尾测试(TST)被用于评估新型查尔酮化合物查尔酮-1203 在小鼠体内的抗抑郁样活性。结果观察到,查尔酮-1203 在 1、5 和 10mg/kg 剂量下可显著减少处理 30 分钟后 FST 和 TST 中小鼠的不动时间。此外,查尔酮-1203 还在 FST 中显示出显著的口服活性。它还减少了未适应竞技场的小鼠在旷场试验中的活动,但对已适应旷场的小鼠的运动活性没有影响。还通过 HPLC-ECD 同时测定了小鼠脑区的主要单胺神经递质及其代谢物。结果发现,查尔酮-1203 可显著增加海马体、下丘脑和皮质中主要神经递质 5-HT 和 NE 的浓度。查尔酮-1203 还显著降低了海马体和皮质中 5-HIAA/5-HT 的比值,表明与用应激载体处理的小鼠相比,5-HT 代谢减少。总之,查尔酮-1203 产生了显著的抗抑郁样活性,其作用机制可能是由于增加了小鼠海马体和皮质中的 5-HT 和 NE。

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