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1.
Bioorg Med Chem Lett ; 107: 129788, 2024 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-38740144

RESUMO

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.


Assuntos
Peptídeos beta-Amiloides , Catecolaminas , Simulação de Acoplamento Molecular , Agregados Proteicos , Peptídeos beta-Amiloides/antagonistas & inibidores , Peptídeos beta-Amiloides/metabolismo , Catecolaminas/metabolismo , Humanos , Agregados Proteicos/efeitos dos fármacos , Relação Estrutura-Atividade , Estrutura Molecular , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/metabolismo , Relação Dose-Resposta a Droga
2.
Artigo em Inglês | MEDLINE | ID: mdl-27429636

RESUMO

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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