Chigurupati Sridevi, Shaikh Sohrab Akhtar, Mohammad Jahidul Islam, Selvarajan Kesavanarayanan Krishnan, Nemala Appala Raju, Khaw Chu How, Teoh Chun Foo, Kee Ting Hei
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, AIMST University, Semeling, 08100 Bedong, Kedah, Malaysia.
Department of Pharmacology, Faculty of Pharmacy, AIMST University, Semeling, 08100 Bedong, Kedah, Malaysia.
Indian J Pharmacol. 2017 May-Jun;49(3):229-235. doi: 10.4103/ijp.IJP_293_16.
In this study, three (CS-1 to CS-3) azomethine derivatives of cinnamaldehyde were green synthesized, characterized, and their antioxidant and antidepressant activities were explored.
The antioxidant effect of these compounds was initially performed using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay methods before subjecting them to experiments. Compounds showing potent antioxidant activity (CS-1 and CS-2) were investigated further for their antidepressant activity using the forced swim test (FST) and tail suspension test (TST). Ascorbic acid (AA) and fluoxetine (20 mg/kg, p.o) were used as reference drugs for comparison in the antioxidant and antidepressant experiments, respectively.
It was observed that CS-2 and CS-3 exhibited highest DPPH (half maximal inhibitory concentration [IC]: 16.22 and 25.18 μg/mL) and ABTS (IC: 17.2 and 28.86 μg/mL) radical scavenging activity, respectively, compared to AA (IC: 15.73 and 16.79 μg/mL) and therefore, both CS-2 and CS-3 were tested for their antidepressant effect using FST and TST as experimental models. Pretreatment of CS-2 and CS-3 (20 mg/kg) for 10 days considerably decreased the immobility time in both the FST and TST models.
The antioxidant and antidepressant effect of CS-2 and CS-3 may be attributed to the presence of azomethine linkage in the molecule.
本研究绿色合成并表征了三种肉桂醛甲亚胺衍生物（CS-1至CS-3），并探究了它们的抗氧化和抗抑郁活性。
在对这些化合物进行实验之前，首先使用1,1-二苯基-2-苦基肼（DPPH）和2,2'-联氮双（3-乙基苯并噻唑啉-6-磺酸）（ABTS）测定方法检测它们的抗氧化作用。对显示出强效抗氧化活性的化合物（CS-1和CS-2），使用强迫游泳试验（FST）和悬尾试验（TST）进一步研究其抗抑郁活性。在抗氧化和抗抑郁实验中，分别使用抗坏血酸（AA）和氟西汀（20 mg/kg，口服）作为参比药物进行比较。
观察到，与AA（IC：15.73和16.79 μg/mL）相比，CS-2和CS-3分别表现出最高的DPPH（半数最大抑制浓度[IC]：16.22和25.18 μg/mL）和ABTS（IC：17.2和28.86 μg/mL）自由基清除活性，因此，使用FST和TST作为实验模型对CS-2和CS-3的抗抑郁作用进行了测试。CS-2和CS-3（20 mg/kg）预处理10天，在FST和TST模型中均显著缩短了不动时间。
CS-2和CS-3的抗氧化和抗抑郁作用可能归因于分子中存在甲亚胺键。
