Design, synthesis, and inhibition of novel ferulic acid derivatives on free fatty acid induced cellular lipid accumulation.

IF 1.3 3区医学 Q3 CHEMISTRY, APPLIED

Journal of Asian Natural Products Research Pub Date : 2025-02-23 DOI:10.1080/10286020.2025.2459600

Ying-Ying Liu, Yi-Fan Xu, Xin-Ru Li, Qi-Pan Fan, Jia-Hao Liu, Si-Yu Zhou, Yu-Qing Qian, Ming-Dong Li

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.

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新型阿魏酸衍生物对游离脂肪酸诱导的细胞脂质积累的设计、合成和抑制作用。

肝细胞脂质异常积聚是NAFLD的一个显著特征。阿魏酸（FA）是一种具有抗氧化活性的中草药成分，可通过激活AMPK磷酸化来治疗NAFLD。在这项研究中，我们合成了十个丙烯酸衍生物A1-A10。对脂质积累的抑制表明，大多数靶化合物在400 μM范围内对脂质积累具有抑制作用；化合物A3表现出较好的抑制作用。分子对接结果证明A3可以与PPARγ结合，并且在阿魏酸基团和取代苯基团中都存在多个结合位点。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Asian Natural Products Research 医学-药学

CiteScore

3.20

自引率

5.90%

发文量

审稿时长

2.3 months

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.