{"title":"Design, synthesis, and inhibition of novel ferulic acid derivatives on free fatty acid induced cellular lipid accumulation.","authors":"Ying-Ying Liu, Yi-Fan Xu, Xin-Ru Li, Qi-Pan Fan, Jia-Hao Liu, Si-Yu Zhou, Yu-Qing Qian, Ming-Dong Li","doi":"10.1080/10286020.2025.2459600","DOIUrl":null,"url":null,"abstract":"<p><p>Abnormal accumulation of hepatocyte lipids is a hallmark feature of NAFLD. Ferulic acid (FA), an ingredient with antioxidant activity in Chinese herbs, can be used to treat NAFLD by activating AMPK phosphorylation. In this study, we synthesized ten acrylic acid derivatives <b>A1-A10</b>. The inhibition of lipid accumulation showed that most target compounds could inhibit lipid accumulation at 400 μM; compound <b>A3</b> showed a better inhibitory effect than other compounds. Molecular docking results proved that <b>A3</b> could bind to PPARγ, and multiple binding sites existed in both the ferulic acid cohort and the substituted benzene cohort.</p>","PeriodicalId":15180,"journal":{"name":"Journal of Asian Natural Products Research","volume":" ","pages":"1-16"},"PeriodicalIF":1.3000,"publicationDate":"2025-02-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Asian Natural Products Research","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/10286020.2025.2459600","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, APPLIED","Score":null,"Total":0}
引用次数: 0
Abstract
Abnormal accumulation of hepatocyte lipids is a hallmark feature of NAFLD. Ferulic acid (FA), an ingredient with antioxidant activity in Chinese herbs, can be used to treat NAFLD by activating AMPK phosphorylation. In this study, we synthesized ten acrylic acid derivatives A1-A10. The inhibition of lipid accumulation showed that most target compounds could inhibit lipid accumulation at 400 μM; compound A3 showed a better inhibitory effect than other compounds. Molecular docking results proved that A3 could bind to PPARγ, and multiple binding sites existed in both the ferulic acid cohort and the substituted benzene cohort.
期刊介绍:
The Journal of Asian Natural Products Research (JANPR) publishes chemical and pharmaceutical studies in the English language in the field of natural product research on Asian ethnic medicine. The journal publishes work from scientists in Asian countries, e.g. China, Japan, Korea and India, including contributions from other countries concerning natural products of Asia. The journal is chemistry-orientated. Major fields covered are: isolation and structural elucidation of natural constituents (including those for non-medical uses), synthesis and transformation (including biosynthesis and biotransformation) of natural products, pharmacognosy, and allied topics. Biological evaluation of crude extracts are acceptable only as supporting data for pure isolates with well-characterized structures.
All published research articles in this journal have undergone rigorous peer review, based on initial editor screening and anonymized refereeing by at least two expert referees.