distyrylbenzene and Alzheimer-Disease

distyrylbenzene has been researched along with Alzheimer-Disease* in 2 studies

Other Studies

2 other study(ies) available for distyrylbenzene and Alzheimer-Disease

Article	Year
Amphiphilic Distyrylbenzene Derivatives as Potential Therapeutic and Imaging Agents for Soluble and Insoluble Amyloid β Aggregates in Alzheimer's Disease. Journal of the American Chemical Society, 2021, 07-14, Volume: 143, Issue:27 Alzheimer's Disease (AD) is the most common neurodegenerative disease, and efficient therapeutic and early diagnostic agents for AD are still lacking. Herein, we report the development of a novel amphiphilic compound, LS-4, generated by linking a hydrophobic amyloid-binding distyrylbenzene fragment with a hydrophilic triazamacrocycle, which dramatically increases the binding affinity toward various amyloid β (Aβ) peptide aggregates, especially for soluble Aβ oligomers. Moreover, upon the administration of LS-4 to 5xFAD mice, fluorescence imaging of LS-4-treated brain sections reveals that LS-4 can penetrate the blood-brain barrier and bind to the Aβ oligomers Topics: Alzheimer Disease; Amyloid; Amyloid beta-Peptides; Animals; Drug Design; Mice; Mice, Transgenic; Molecular Structure; Neuroprotective Agents; Peptide Fragments; Plaque, Amyloid; Positron-Emission Tomography; Protein Binding; Styrenes	2021
Development of a new distyrylbenzene-derivative amyloid-β-aggregation and fibril formation inhibitor. Chemical & pharmaceutical bulletin, 2012, Volume: 60, Issue:9 Several new amyloid-β (Aβ) aggregation inhibitors were synthesized according to our theory that a hydrophilic moiety could be attached to the Aβ-recognition unit for the purpose of preventing amyloid plaque formation. A distyrylbenzene-derivative, DSB(EEX)(3), which consider the Aβ recognition unit (DSB, 1,4-distyrylbenzene) and expected to bind to amyloid fibrils (β-sheet structure), was combined with the hydrophilic aggregation disrupting element (EEX) (E, Glu; X, 2-(2-(2-aminoethoxy)ethoxy)acetic acid). This DSB(EEX)(3) compound, compared to several others synthesized similarly, was found to be the most active for reducing Aβ toxicity toward IMR-32 human neuroblastoma cells. Moreover, its inhibition of Aβ-aggregation or fibril formation was directly confirmed by transmission electron microscopy and atomic force microscopy. These results suggest that the Aβ aggregation inhibitor DSB(EEX)(3) disrupts clumps of Aβ protein and is a likely candidate for drug development to treat Alzheimer's disease. Topics: Alzheimer Disease; Amyloid; Amyloid beta-Peptides; Cell Line, Tumor; Humans; Styrenes	2012

Article

Year

Amphiphilic Distyrylbenzene Derivatives as Potential Therapeutic and Imaging Agents for Soluble and Insoluble Amyloid β Aggregates in Alzheimer's Disease.

Journal of the American Chemical Society, 2021, 07-14, Volume: 143, Issue:27

Alzheimer's Disease (AD) is the most common neurodegenerative disease, and efficient therapeutic and early diagnostic agents for AD are still lacking. Herein, we report the development of a novel amphiphilic compound, LS-4, generated by linking a hydrophobic amyloid-binding distyrylbenzene fragment with a hydrophilic triazamacrocycle, which dramatically increases the binding affinity toward various amyloid β (Aβ) peptide aggregates, especially for soluble Aβ oligomers. Moreover, upon the administration of LS-4 to 5xFAD mice, fluorescence imaging of LS-4-treated brain sections reveals that LS-4 can penetrate the blood-brain barrier and bind to the Aβ oligomers

Topics: Alzheimer Disease; Amyloid; Amyloid beta-Peptides; Animals; Drug Design; Mice; Mice, Transgenic; Molecular Structure; Neuroprotective Agents; Peptide Fragments; Plaque, Amyloid; Positron-Emission Tomography; Protein Binding; Styrenes

2021

Development of a new distyrylbenzene-derivative amyloid-β-aggregation and fibril formation inhibitor.

Chemical & pharmaceutical bulletin, 2012, Volume: 60, Issue:9

Several new amyloid-β (Aβ) aggregation inhibitors were synthesized according to our theory that a hydrophilic moiety could be attached to the Aβ-recognition unit for the purpose of preventing amyloid plaque formation. A distyrylbenzene-derivative, DSB(EEX)(3), which consider the Aβ recognition unit (DSB, 1,4-distyrylbenzene) and expected to bind to amyloid fibrils (β-sheet structure), was combined with the hydrophilic aggregation disrupting element (EEX) (E, Glu; X, 2-(2-(2-aminoethoxy)ethoxy)acetic acid). This DSB(EEX)(3) compound, compared to several others synthesized similarly, was found to be the most active for reducing Aβ toxicity toward IMR-32 human neuroblastoma cells. Moreover, its inhibition of Aβ-aggregation or fibril formation was directly confirmed by transmission electron microscopy and atomic force microscopy. These results suggest that the Aβ aggregation inhibitor DSB(EEX)(3) disrupts clumps of Aβ protein and is a likely candidate for drug development to treat Alzheimer's disease.

Topics: Alzheimer Disease; Amyloid; Amyloid beta-Peptides; Cell Line, Tumor; Humans; Styrenes

2012