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1.
Bioorg Med Chem Lett ; 107: 129788, 2024 Jul 15.
Article in English | MEDLINE | ID: mdl-38740144

ABSTRACT

Effectively inhibition of amyloid ß (Aß) aggregation is considered an important method for treatment of the Alzheimer's disease. Herein, inspired by the ability of trans-clovamide to effectively inhibit Aß aggregation, we synthesized a series of structurally related catecholamine derivatives and tested them as Aß aggregation inhibitors using the Thioflavin T assay. The results show that they demonstrated a higher inhibitory rate against Aß aggregation. Furthermore, these compounds exhibited high water solubilities and low cytotoxicities. Additionally, transmission electron microscopy images and dynamic light scattering of their Aß aggregations were observed. Docking simulations revealed that the catechol moiety of the synthesized compounds can form hydrogen bonds with the key regions of Aß and thereby inhibit Aß aggregation.


Subject(s)
Amyloid beta-Peptides , Catecholamines , Molecular Docking Simulation , Protein Aggregates , Amyloid beta-Peptides/antagonists & inhibitors , Amyloid beta-Peptides/metabolism , Catecholamines/metabolism , Humans , Protein Aggregates/drug effects , Structure-Activity Relationship , Molecular Structure , Alzheimer Disease/drug therapy , Alzheimer Disease/metabolism , Dose-Response Relationship, Drug
2.
Article in English | MEDLINE | ID: mdl-27429636

ABSTRACT

Fatty liver disease is a condition in which abnormally large numbers of lipid droplets accumulate in liver cells. Fatty liver disease induces inflammation under conditions of oxidative stress and may result in cancer. To identify plants that protect against fatty liver disease, we examined the inhibitory effects of plant extracts on lipid droplet formation in mouse hepatoma cells. A screen of 98 water extracts of plants revealed 4 extracts with inhibitory effects. One of these extracts, Rubus suavissimus S. Lee (Tien-cha or Chinese sweet tea) leaf extract, which showed strong inhibitory effects, was tested in a mouse fatty liver model. In these mouse experiments, intake of the plant extract significantly protected mice against fatty liver disease without affecting body weight gain. Our results suggest that RSE directly affects liver cells and protects them from fatty liver disease.

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