Virtual screening and evaluation of bioactive peptides from Haliotis discus hannai as potential HMGCR inhibitors for hyperlipidemia treatment

皱纹盘鲍活性肽作为高脂血症治疗潜在 HMGCR 抑制剂的虚拟筛选与评估

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作者:Kun Qiao, Lina Liu, Yihui Chen, Qiongmei Huang, Bei Chen, Jingna Wu, Wenmei Huang, Zhiyu Liu

Conclusion

This study provides novel insights into developing natural drugs for hyperlipidemia; moreover, the results will facilitate the functional application of marine bioactive peptides.

Results

In this study, the most suitable protease for preparing HMGCR inhibitory peptides was screened using the evaluation indexes of peptide yield and HMGCR inhibition rate. Peptide sequences with molecular weights <1 kDa were identified, and peptide fragments were docked with HMGCR for virtual screening. The inhibitory effects of these peptides on HMGCR activity were evaluated in vitro using a high-fat Hep-G2 cell model. The screened peptides possessed significant HMGCR inhibitory activity and reduced cholesterol micelle solubility and total cholesterol and triglyceride levels in hyperlipidemic Hep-G2 cells.

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