科研之友
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摘要
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 3 T3-L1 cell model revealed that 1 and 2 could significantly inhibit the lipid droplet formation(EC50（28） 0.41 and 0.92 μ mol·L–1, respectively) and lower triglyceride levels by 50%-60% at the concentration of 1 μ mol·L–1, being more potent than the positive drug luteolin(EC50（28） 2.63 μmol·L–1). A mechanistic study indicated that 1 and 2 could intercalate into supercoiled DNA, which consequently inhibited the mitotic clonal expansion of 3 T3-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 d evelopment of anti-obesity drugs.
