[目的]制备β-谷甾醇修饰的人参皂苷Rb1脂质体(β-Rb1-Lip),减少Rb1降解并增强人参皂苷Rb1降脂效果.[方法]采用薄膜水和法制备了β-谷甾醇修饰的人参皂苷Rb1脂质体,利用MTT法评估脂质体的生物安全性,借助油红O染色试验和酶标仪测量TG含量,考察了脂质体β-Rb1-Lip对脂肪细胞3T3-L1的脂滴积聚抑制作用.[结果]制备的β-Rb1-Lip脂质体的包封率为83.74％,平均粒径为 198 nm,β-Rb1-Lip 在 12 h 内 Rb1 释放率约为80％,表现出良好的缓释效果.对于降脂活性,50 µmol/L的β-Rb1-Lip表现出显著的细胞内脂滴抑制率,与同浓度Rb1单体相比,β-Rb1-Lip对3T3-L1细胞内脂滴的抑制效果更为显著,且对细胞没有毒副作用.[结论]β-Rb1-Lip具有包封率高、粒径小和缓释效果明显的特征,能够持续释放活性成分人参皂苷Rb1,增强其降脂功效并减少用量.
Investigating the inhibitory effect of β-Rb1-Lip on lipid droplet accumulation in 3T3-L1 adipocytes
[Objective]β-Sitosterol-modified ginsenoside Rb1 liposomes(β-Rb1-Lip)were prepared to reduce the degradation of Rb1 and enhance the lipid-lowering effects of ginsenoside Rb1.[Methods]β-sitosterol-modified ginsenoside Rb1 liposomes were prepared by the thin-film hydration method.The biosafety of the liposomes was assessed using the MTT assay.The inhibition of lipid droplet accumulation in 3T3-L1 adipocytes by β-Rb1-Lip was investigated using Oil Red O staining and triglyceride(TG)content measurement with an enzyme-linked immunosorbent assay.[Results]The prepared β-Rb1-Lip liposomes had an encapsulation efficiency of 83.74％and an average particle size of 198 nm.The release rate of Rb1 from β-Rb1-Lip was about 80％within 12 hours,demonstrating a good sustained-release effect.Regarding lipid-lowering activity,β-Rb1-Lip at 50 μmol/L showed a significant inhibitory rate of intracellular lipid droplets.Compared to the same concentration of Rb1 monomer,β-Rb1-Lip had a more significant inhibitory effect on the accumulation of lipid droplets in 3T3-L1 cells and did not exhibit cytotoxicity.[Conclusion]β-Rb1-Lip has high encapsulation efficiency,small particle size,and obvious sustained-release characteristics.It can continuously release the active component ginsenoside Rb1,enhance its lipid-lowering efficacy,and reduce the dosage,providing support for the development of Rb1 lipid-lowering products.
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