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Bioactive Phytocompounds: Anti-amyloidogenic Effects Against Hen Egg-White Lysozyme Aggregation
The Protein Journal ( IF 1.9 ) Pub Date : 2021-01-03 , DOI: 10.1007/s10930-020-09946-5
Suman Chowdhury 1 , Suresh Kumar 1
Affiliation  

Amyloidosis is the process of fibril formation responsible for causing several diseases in the human being that involve protein aggregation such as Alzheimer’s, Parkinson’s, Huntington’s disease, and type II diabetes. Natural phytocompounds such as curcumin shown promising anti-amyloidogenic activity. In the present study, selective phytocompounds such as piperine, cinnamaldehyde, eugenol, and cuminaldehyde present in Piper nigrum L, Cinnamomum zeylanicum Blume, Eugenia caryophyllus Thumb, and Cuminum cyminum L, respectively were analyzed for anti-amyloidogenic activity using hen egg white-lysozyme (HEWL) as a model system. Out of the selected phytocompounds, piperine showed the most significant anti-amyloidogenic activity, as evident from in vitro assays that were validated by in silico molecular docking study. Piperine showed 64.7 ± 3.74% inhibition of amyloid formation at 50 μM concentration, as observed by Thioflavin T assay. Subsequently, the anti-amyloidogenic activity of piperine was further validated by congo red, intrinsic fluorescence assay, and transmission electron microscopy analysis. The in silico molecular binding interaction showed piperine with the highest docking score and glide energy. Piperine was found to be interacting with amyloidogenic region residues and Trp62, the most important residue involved in the amyloidogenesis process. In conclusion, piperine can be used as a positive lead for a potential therapeutic role in targeting diseases involved amyloidogenesis.



中文翻译:

生物活性植物化合物:抗母鸡卵白溶菌酶聚集的淀粉样蛋白生成作用。

淀粉样变性是原纤维形成的过程,其引起人类中涉及蛋白质聚集的多种疾病,例如阿尔茨海默氏病,帕金森氏病,亨廷顿氏病和II型糖尿病。天然植物化合物(如姜黄素)显示出有希望的抗淀粉样生成活性。在本研究中,选择性phytocompounds如胡椒碱,肉桂醛,丁子香酚,和枯茗醛存在于胡椒L,锡兰肉桂布鲁姆,尤金尼亚石竹Thumb和孜然芹使用鸡蛋白溶菌酶(HEWL)作为模型系统分别分析L的抗淀粉样蛋白生成活性。在所选的植物化合物中,胡椒碱显示出最显着的抗淀粉样蛋白生成活性,这是通过计算机分子对接研究验证的体外试验所证实的。如硫黄素T分析所观察到的,胡椒碱在50μM浓度下显示64.7±3.74%的淀粉样蛋白形成抑制。随后,通过刚果红,内在荧光分析和透射电子显微镜分析进一步验证了胡椒碱的抗淀粉样蛋白活性。在计算机上的分子结合相互作用显示胡椒碱具有最高的对接分数和滑移能。发现胡椒碱与淀粉样蛋白生成区残基和Trp62(参与淀粉样蛋白生成过程的最重要的残基)相互作用。

更新日期:2021-01-03
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