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Pyridocarbazole alkaloids from Ochrosia borbonica: lipid-lowering agents inhibit the cell proliferation and adipogenesis of 3T3-L1 adipocyte via intercalating into supercoiled DNA / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.) ; (6): 663-671, 2019.
Artigo em Inglês | WPRIM | ID: wpr-776842
ABSTRACT
Bioassay-guided fractionation of an ethanolic extract of Ochrosia borbonica led to the isolation of two known pyridocarbazole alkaloids, ellipticine (1) and 9-methoxyellipticine (2), and six known monoterpenoid indole alkaloids (3-8). Lipid-lowering assay in 3T3-L1 cell model revealed that 1 and 2 could significantly inhibit the lipid droplet formation (EC = 0.41 and 0.92 μmol·L, respectively) and lower triglyceride levels by 50%-60% at the concentration of 1 μmol·L, being more potent than the positive drug luteolin (EC = 2.63 μmol·L). A mechanistic study indicated that 1 and 2 could intercalate into supercoiled DNA, which consequently inhibited the mitotic clonal expansion of 3T3-L1 cells at the early differentiation phase, leading to the retardance of following adipogenesis and lipogenesis. These findings suggest that 1 and 2 may serve as promising leads for further development of anti-obesity drugs.

Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Tipo de estudo: Estudo prognóstico Idioma: Inglês Revista: Chinese Journal of Natural Medicines (English Ed.) Ano de publicação: 2019 Tipo de documento: Artigo

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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Tipo de estudo: Estudo prognóstico Idioma: Inglês Revista: Chinese Journal of Natural Medicines (English Ed.) Ano de publicação: 2019 Tipo de documento: Artigo