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首页> 外文期刊>Drug Design, Development and Therapy >Pharmacological Evaluation of Aldehydic-Pyrrolidinedione Against HCT-116, MDA-MB231, NIH/3T3, MCF-7 Cancer Cell Lines, Antioxidant and Enzyme Inhibition Studies
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Pharmacological Evaluation of Aldehydic-Pyrrolidinedione Against HCT-116, MDA-MB231, NIH/3T3, MCF-7 Cancer Cell Lines, Antioxidant and Enzyme Inhibition Studies

机译：醛-PyrolidoIche对HCT-116，MDA-MB231，NIH / 3T3，MCF-7癌细胞系，抗氧化剂和酶抑制研究的药理评价

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Purpose: The current work was designed to synthesize a bioactive derivative of succinimide and evaluate it for anti-Alzheimer, anticancer and anti-diabetic potentials. Methods: The compound was synthesized by Michael addition of butyraldehyde with N -phenylmaleimide. The synthesized compound was screened for biological potentials including anti-cholinesterase, in-vitro anti-diabetic, antioxidant and anthelmintic potentials. The anti-cholinesterase potential was evaluated against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), anti-diabetic potential against α-glucosidase, antioxidant potential against ABTS, DPPH and Hsub2/subOsub2/sub and anthelmintic potential against Perethima posthuma and Ascaridia galli respectively. Results: The compound demonstrated significant AChE and BChE inhibition i.e., 71.34±1.92 and 73.42 ±1.92 at the concentration of 1000 μg/mL respectively. Other dilutions exhibited concentration-dependent inhibitory activity against both enzymes. In the MTT assay, the newly synthesized compound was found active against all of the cell lines viz, HCT-116, MDA-MB231, NIH/3T3 and MCF-7 and the highest cytotoxicity potential was observed against the colon cancer cell line (HCT-116) with an ICsub50/sub value of 78 μg/mL exhibiting its highest potential. Moreover, the compound exhibited prominent α-glucosidase inhibitory potentials (79.86±2.54% at 1000 μg/mL) with ICsub50/sub value of 156.23 μg/mL. Further, our test compound exhibited considerable scavenging activity against DPPH, ABTS and Hsub2/subOsub2/sub free radicals with percent inhibitions of 75.84±1.58, 72.85±1.17 and 54.82±1.82 and ICsub50/sub values of 84.36, 139.74 and 752.21 μg/mL respectively. Our test sample exhibited significant anthelmintic potentials. It demonstrated significant paralysis and death of the test worms in an unbelievably short time in comparison with albendazole. Conclusion: Going into the detail of all observations, it may be deduced that the newly synthesized succinimide derivative could be an important drug candidate against neurodegenerative disorders like Alzheimer’s disease, cancer, diabetes mellitus and worms. Further detailed studies in animal models are required for in-vivo analysis of the compound.
机译：目的：目前的工作旨在合成琥珀酰亚胺的生物活性衍生物，并评估抗阿尔茨海默，抗癌和抗糖尿病势。方法：用N-苯基马来酰亚胺的丁烯醛加入丁醛合成该化合物。筛选合成的化合物，用于生物潜力，包括抗胆碱酯酶，体外抗糖尿病，抗氧化剂和抗氧化势。对乙酰胆碱酯酶（ACHE）和丁酰基胆碱酯酶（BCHE），抗糖尿病势抵抗α-葡糖苷酶，抗氧化剂潜力，对抗ABTS，DPPH和H 2 O 2的抗糖尿病势势来评价抗胆管酶酶的潜力。分别对患有Perethima posthuma和蛔虫病的潜力和胰岛素潜力。结果：该化合物分别以浓度为1000μg/ mL的71.34±1.92和73.42±1.92显着疼痛和BCHE抑制。其他稀释液表现出对两种酶的浓度依赖性抑制活性。在MTT测定中，发现新合成的化合物对所有细胞系VIZ，HCT-116，MDA-MB231，NIH / 3T3和MCF-7以及对结肠癌细胞系（HCT）观察到最高细胞毒性电位（HCT -116）具有78μg/ ml的IC 50 值，其最高潜力。此外，该化合物具有突出的α-葡萄糖苷酶抑制电位（79.86±2.54％，1000μg/ ml），IC 50 值为156.23μg/ ml。此外，我们的测试化合物对DPPH，ABTS和H 2 O 2 自由基具有相当大的清除活性，其抑制百分比为75.84±1.58,72.85±1.17和54.82±1.82和IC 50 值分别为84.36,139.74和752.21μg/ mL。我们的测试样品表现出显着的一个明显的潜在潜力。与阿伦唑相比，它在令人难以置信的短时间内表现出考试蠕虫的显着瘫痪和死亡。结论：进入所有观察的细节，可能推断出新合成的琥珀酰亚胺衍生物可能是针对阿尔茨海默病，癌症，糖尿病和蠕虫等神经变性障碍的重要药物候选者。化合物的体内分析需要进一步详细的动物模型研究。

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