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Eur J Pharmacol ; 892: 173689, 2021 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-33127360

RESUMO

Portulaca oleracea L. is used as a folk medicine in many countries because of its wide range of pharmacological effects. HM-chromanone, isolated from P. oleracea using bioassay-guided fractionation and HPLC, belongs to the homoisoflavonoid group and has been shown to exert several biological effects. In this study, we evaluated whether HM-chromanone inhibits adipogenesis by regulating adipogenic transcription factors in 3T3-L1 adipocytes. The results showed that HM-chromanone suppresses adipocyte differentiation and adipogenesis in a dose-dependent manner in 3T3-L1 adipocytes. The HM-chromanone-treated adipocytes exhibited lower triglyceride accumulation and leptin secretion, and higher glycerol and adiponectin secretion than the control adipocytes. Microscopic observation using oil red O staining revealed a dose-dependent reduction in the number of lipid droplets in the HM-chromanone-treated adipocytes compared to the control group. HM-chromanone significantly down-regulated the protein expression of major adipogenic transcription factors sterol regulatory element binding protein-1c (SREBP-1c), peroxisome proliferator-activated receptor γ (PPARγ), and CCAAT/enhancer binding protein α (C/EBPα) and markedly inhibited several key adipogenic enzymes including fatty acid synthase (FAS) and acetyl-CoA carboxylase (ACC). In addition, adipose triglyceride lipase (ATGL) and hormone-sensitive lipase (HSL) were both more activated in the HM-chromanone-treated adipocytes than in the control adipocytes. HM-chromanone also promoted the phosphorylation of 5' Adenosine monophosphate-activated protein kinase (AMPK), which inhibits adipogenesis through the regulation of adipogenic transcription factors. These results suggest that HM-chromanone may be an effective anti-adipogenesis agent that functions via the suppression of adipogenic transcription factors and the activation of AMPK.


Assuntos
Proteínas Quinases Ativadas por AMP/metabolismo , Adipócitos/efeitos dos fármacos , Adipogenia/efeitos dos fármacos , Fármacos Antiobesidade/farmacologia , Isoflavonas/farmacologia , Fatores de Transcrição/metabolismo , Células 3T3-L1 , Adipócitos/enzimologia , Adipócitos/patologia , Adipogenia/genética , Animais , Regulação da Expressão Gênica , Metabolismo dos Lipídeos/efeitos dos fármacos , Camundongos , Fosforilação , Transdução de Sinais , Fatores de Transcrição/genética
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