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