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Schiff base ligand L synthesis and its evaluation as anticancer and antidepressant agent
Journal of King Saud University-Science ( IF 3.7 ) Pub Date : 2020-12-30 , DOI: 10.1016/j.jksus.2020.101331
Maria Sadia , Jehangir Khan , Robina Naz , Muhammad Zahoor , Syed Wadood Ali Shah , Riaz Ullah , Sumaira Naz , Ahmed Bari , Hafiz Majid Mahmood , Syed Saeed Ali , Siddique A. Ansari , Muhammad Sohaib

Objectives

The current study focuses on the synthesis of Schiff base ligand L [1(pyridine-2-ylimino) methyl) naphthalene-2-ol], and its applications as anticancer agent against human lung (H-460) and breast (MCF-7) cell lines, and as antidepressant agent.

Methods

The Schiff base ligand L was synthesized by aldol condensation reaction by reacting commercially available 2-hydroxy-1-napthaldehyde with 2-amino-pyridine. The synthesized ligand was characterized by different spectroscopic techniques and evaluated for its anticancer potential against H-460 and MCF-7 cell lines. The antidepressant activity was evaluated by means of elevated plus maze model using Diazepam as reference drug.

Results

A dose dependent inhibitory response was recorded against both the cell line used. For highest tested dose (500 µg/ml), 89.20% of anticancer activity with IC50 = 23.99 µg/ml against H-460 was observed while an IC50 of 31.68 µg/ml against MCF-7 indicated the potential of this compound to be used as anticancer agent. A dose dependent response was also recorded for the synthesized ligand when tested as antidepressant in elevated plus maze model.

Conclusion

The synthesized Schiff base ligand L exhibited good anticancer and antidepressant activities that could be used as alternative drug to treat the related health complications. However, further toxicological and clinical studies are needed to confirm the safe use of this compound.



中文翻译:

席夫碱配体L的合成及其作为抗癌和抗抑郁药的评价

目标

目前的研究集中于席夫碱配体L [1(吡啶-2-ylimino)甲基)萘-2-醇的合成及其作为抗人肺(H-460)和乳腺癌(MCF-7)的抗癌剂的应用。 )细胞系,并作为抗抑郁药。

方法

通过使市售的2-羟基-1-萘甲醛与2-氨基吡啶反应,通过醛醇缩合反应合成席夫碱配体L。合成的配体通过不同的光谱技术进行表征,并评估其对H-460和MCF-7细胞系的抗癌潜力。使用地西p作为参考药物,通过升高的迷宫模型评估抗抑郁活性。

结果

记录了针对所使用的两种细胞系的剂量依赖性抑制反应。对于最高测试剂量(500 µg / ml),观察到89.20%的抗癌活性,对H-460的IC 50 = 23.99 µg / ml,而对MCF-7的IC 50为31.68 µg / ml,表明该化合物具有潜在的抗癌作用。用作抗癌剂。当在高架迷宫模型中作为抗抑郁药进行测试时,还记录了合成配体的剂量依赖性反应。

结论

合成的席夫碱配体L具有良好的抗癌和抗抑郁活性,可作为治疗相关健康并发症的替代药物。但是,需要进一步的毒理学和临床研究以确认该化合物的安全使用。

更新日期:2021-01-22
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