Curcumin-like compounds designed to modify amyloid beta peptide aggregation patterns

Antonella Battisti; Antonio Palumbo Piccionello; Antonella Sgarbossa; Silvia Vilasi; Caterina Ricci; Francesco Ghetti; Francesco Spinozzi; Antonella Marino Gammazza; Valentina Giacalone; Annamaria Martorana; Antonino Lauria; Claudio Ferrero; Donatella Bulone; Maria Rosalia Mangione; Pier Luigi San Biagio; Maria Grazia Ortore

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Curcumin-like compounds designed to modify amyloid beta peptide aggregation patterns

机译：姜黄素样化合物旨在修饰淀粉样β肽聚集模式

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Curcumin is a natural polyphenol able to bind the amyloid beta peptide, which is related to Alzheimer’s disease, and modify its self-assembly pathway. This paper focuses on a multi-disciplinary study that starts from the design of curcumin-like compounds with the key chemical features required for inhibiting amyloid beta aggregation, and reports the effects of these compounds on the in vitro aggregation of amyloid beta peptides. Chemoinformatic screening was performed through the calculation of molecular descriptors that were able to highlight the drug-like profile, followed by docking studies with an amyloid beta peptide fibril. The computational design underlined two different scaffolds that were easily synthesized in good yields. In vitro experiments, ranging from fluorescence spectroscopy and confocal microscopy up to small angle X-ray scattering, provided evidence that the synthesized compounds are able to modify the aggregation pattern of amyloid beta peptides both in the secondary structures, and in terms of the overall structure dimensions. The cytotoxic potential of the synthesized compounds was finally tested in vitro with a model neuronal cell line (LAN5). The overall view of this study suggests new concepts and potential difficulties in the design of novel drugs against diverse amyloidoses, including Alzheimer’s disease.

机译：姜黄素是一种天然多酚，能够结合与阿尔茨海默氏病有关的淀粉样β肽，并改变其自组装途径。本文着重于一项多学科研究，从设计具有抑制淀粉样蛋白β聚集所需关键化学特性的姜黄素样化合物开始，并报道这些化合物对体外聚集的作用淀粉样β肽。化学信息学筛选是通过计算能够突出药物样特征的分子描述子进行的，然后与淀粉样β肽原纤维进行对接研究。计算设计强调了两种不同的支架，它们很容易以高收率合成。从荧光光谱和共聚焦显微镜到小角度X射线散射的体外实验提供了证据，表明合成的化合物能够修饰二级结构中β淀粉样肽的聚集模式，以及整体结构尺寸。最后，使用模型神经元细胞系（LAN5）在体外测试了合成化合物的细胞毒性潜力。这项研究的总体观点表明，针对包括阿尔茨海默氏病在内的各种淀粉样蛋白的新型药物的设计存在着新的概念和潜在的困难。 展开▼

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《RSC Advances》 |2017年第50期|共11页

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Antonella Battisti; Antonio Palumbo Piccionello; Antonella Sgarbossa; Silvia Vilasi; Caterina Ricci; Francesco Ghetti; Francesco Spinozzi; Antonella Marino Gammazza; Valentina Giacalone; Annamaria Martorana; Antonino Lauria; Claudio Ferrero; Donatella Bulone; Maria Rosalia Mangione; Pier Luigi San Biagio; Maria Grazia Ortore;
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1. Curcumin-like compounds designed to modify amyloid beta peptide aggregation patterns [J] . Antonella Battisti, Antonio Palumbo Piccionello, Antonella Sgarbossa, RSC Advances . 2017,第50期

机译：姜黄素样化合物旨在修饰淀粉样β肽聚集模式

2. Rationally Designed Dehydroalanine (Delta Ala)-Containing Peptides Inhibit Amyloid-beta (A beta) Peptide Aggregation [J] . Rangachari V, Davey ZS, Healy B, Biopolymers: Original Research on Biomolecules and Biomolecular Assemblies . 2009,第6期

机译：合理设计的含脱氢丙氨酸（Δtala）的肽抑制淀粉样β（A beta）肽的聚集。

3. Copper enhances amyloid-beta peptide neurotoxicity and non beta-aggregation: a series of experiments conducted upon copper-bound and copper-free amyloid-beta peptide. [J] . Dai X, Sun Y, Gao Z, Journal of Molecular Neuroscience: MN . 2010,第1期

机译：铜增强淀粉样β肽的神经毒性和非β聚集性：对铜结合的和无铜的淀粉样β肽进行的一系列实验。

4. Aggregation studies of beta-amyloid 25-35 fragment in interaction with other modified beta-amyloid peptide fragments [C] . Lukasz P.Frankiewicz, Wiktor Banachewicz, Aleksandra Misicka International Peptide Symposium;European Peptide Symposium . 2005

机译：与其他改性β-淀粉样蛋白肽片段相互作用β-淀粉样蛋白25-35片段的聚集研究

5. Molecular Dynamics Studies of Amyloid-beta Peptides monomers and Design of Fluorescent Bioprobes for Aggregation-Induced Emission Fluorogens on DNA Surfaces. [D] . Xiong, Hao. 2011

机译：淀粉样β肽单体的分子动力学研究和用于聚集诱导DNA表面发射荧光的荧光生物探针的设计。

6. Structure-Based Peptide Design to Modulate Amyloid Beta Aggregation and Reduce Cytotoxicity [O] . Jitendra Kumar, Risa Namsechi, Valerie L. Sim -1

机译：基于结构的肽设计可调节淀粉样β聚集并降低细胞毒性

7. Curcumin-like compounds designed to modify amyloid beta peptide aggregation patterns [O] . Battisti, A., PALUMBO PICCIONELLO, A., Sgarbossa, A., 2017

机译：姜黄素样化合物旨在修饰淀粉样β肽聚集模式

1. 电化学活性的二茂铁-肽的合成及其对β-淀粉样肽聚集的抑制作用 [J] . 李学强 ,魏传晚 ,刘晓芳 . 有机化学 . 2010,第010期

2. 响应面法优化姜黄素提取工艺及其对类淀粉样蛋白聚集形成的抑制 [J] . 张良 ,杨松 ,何剑为 . 食品科学 . 2013,第020期

3. 姜黄素对β-淀粉样肽(25-35)诱导去血清培养PC12细胞周期异常与细胞凋亡的影响 [J] . 谢朝阳 ,祝其锋 ,吴斌华 . 中国新药杂志 . 2007,第001期

4. 聚乙烯亚胺修饰的氧化石墨烯对人胰岛淀粉样蛋白聚集的抑制作用 [J] . 陆通 ,王春洋 ,朱智慧 . 高等学校化学学报 . 2018,第006期

5. 跟踪β-淀粉样肽聚集体的探针—1,4-二苯基三氮唑衍生物的合成 [J] . 孙斌 ,王江淋 . 化学研究与应用 . 2021,第003期

6. 表面等离子共振技术运用于抗淀粉样蛋白聚集化合物的实验研究 [C] . 曾瑾 ,鄢良春 ,赵军宁 . 四川省药理学学会首届学术年会暨四川省药学会第八届药理学与临床药理学专委会第一次学术年会 . 2016

7. 肽抑制剂修饰的聚羧基甜菜碱对淀粉样β蛋白聚集的影响 [A] . 齐凤娟 . 2018

1. β淀粉样肽的成像及β淀粉样肽的聚集的抑制 [P] . 中国专利： CN102743769B . 2016.11.02

2. β淀粉样肽的成像及β淀粉样肽的聚集的抑制 [P] . 中国专利： CN102743769A . 2012-10-24

3. AMYLOID BETA PEPTIDES, SOLUBLE OLIGOMERS COMPRISING AMYLOID BETA PEPTIDES, METHODS FOR IDENTIFYING COMPOUNDS SUITABLE FOR TREATMENT OF DISEASES UTILIZING AMYLOID BETA PEPTIDES OR SOLUBLE OLIGOMERS, METHODS FOR SELECTING BINDING PROTEINS REACTIVE WITH THE AMYLOID PEPTIDES OR SOLUBLE OLIGOMERS UTILIZING AMYLOID BETA PEPTIDES OR SOLUBLE OLIGOMERS, USE OF AMYLOID PEPTIDES OR SOLUBLE OLIGOMERS IN MANUFACTURE OF PHARMACEUTICAL COMPOSITIONS, PHARMACEUTICAL COMPOSITIONS COMPRISING THE AMYLOID PEPTIDES OR SOLUBLE OLIGOMERS, VACCINES COMPRISING THE AMYLOID PEPTIDES OR SOLUBLE OLIGOMERS, NUCLEOTIDES ENCODING THE AMYLOID PEPTIDES, EXPRESSION SYSTEMS COMPRISING THE NUCLEOTIDES ENCODING THE AMYLOID BETA PEPTIDES, AND NON-HUMAN TRANSGENIC ANIMALS EXPRESSING THE NUCLEOTIDES ENCODING THE AMYLOID BETA PEPTIDES [P] . 外国专利： JP2015145414A . 2015-08-13

机译：淀粉状贝他肽，包含淀粉状贝他肽的可溶性低聚体，利用淀粉状贝他肽或可溶性低聚体来鉴定适合用于疾病治疗的化合物的方法，用于选择与蛋白质或多肽的多聚体的类固醇制备药物组合物中的淀粉状肽或可溶性寡聚体，包含淀粉状肽或可溶性寡聚体的药物组合，包含淀粉状肽或肽的类固醇，包括肽和核酸的多肽人转基因动物表达编码淀粉样β肽的核苷酸

4. Polypeptide, non-peptide or not exclusively peptide compound, nucleotide sequence, process of preparing a polypeptide and demonstrating or isolating compounds capable of inhibiting, at least in part, the interaction between a preseniline and the precursor of the beta-amyloid peptide and / or the beta-amyloid peptide, host cell, tests for interaction between a presenilin and the precursor of the beta-amyloid peptide and / or the beta-amyloid peptide and for checking molecules capable of inhibiting the interaction between a presenilin and the precursor of the beta-amyloid peptide and / or beta-amyloid peptide, ligand, defective recombinant virus, vector, pharmaceutical composition, use of polypeptides and nucleotide sequence and expression cassette [P] . 外国专利： BR9813105A . 2000-08-15

机译：多肽，非肽或非排他性肽化合物，核苷酸序列，制备多肽的方法以及证明或分离出能够至少部分抑制早老碱与β-淀粉样肽前体之间相互作用的化合物和/或β-淀粉样肽，宿主细胞，检测早老素与β-淀粉样肽和/或β-淀粉样肽前体之间的相互作用，并检查能够抑制早老素与β-前体之间相互作用的分子-淀粉样肽和/或β-淀粉样肽，配体，缺陷重组病毒，载体，药物组合物，多肽的用途以及核苷酸序列和表达盒

5. Isolated polynucleotide, host cell, protein, oligonucleotide, antibody, processes to produce a protein encoded by the polynucleotide, to determine a polynucleotide that encodes a beta-amyloid peptide-binding protein (bbp) in a sample, to detect in a sample a polypeptide , to diagnose a disease comprising the aberrant expression of human beta-amyloid peptide (bap), to diagnose, to identify compounds that regulate the activity of a beta-amyloid peptide-binding protein and to treat a patient needing to inhibit the accumulation of beta-amyloid peptide in the brain, and, transgenic or chimeric animal. [P] . 外国专利： BR9808562A . 2000-05-23

机译：分离的多核苷酸，宿主细胞，蛋白质，寡核苷酸，抗体，产生该多核苷酸编码的蛋白质的过程，以确定样品中编码β-淀粉样肽结合蛋白（bbp）的多核苷酸，以在样品中检测多肽，诊断包含人β淀粉样肽（bap）异常表达的疾病，诊断，鉴定调节β淀粉样肽结合蛋白活性的化合物以及治疗需要抑制β积累的患者-淀粉样肽在脑中以及转基因或嵌合动物中。

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Curcumin-like compounds designed to modify amyloid beta peptide aggregation patterns

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