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<p>This study was designed to synthesize a series of carvacrol-based fibrate derivatives based on a molecular hybridization strategy. In acute hyperlipidemic mice, the target compound T7 exhibited a noticeable effect on lowering lipid and demonstrated a dose-dependent characteristic. In the high-fat diet (HFD) mouse model, T7 notably decreased triglyceride (TG), total cholesterol (TC), and low-density lipoprotein cholesterol (LDL-C) levels, and elevated high-density lipoprotein cholesterol (HDL-C) levels in both serum and liver tissues. Additionally, T7 appreciably increased the aspartate aminotransferase (AST) and alanine aminotransferase (ALT) found in both serum and liver tissues. Liver histopathological examination indicated that it could inhibit hepatic lipid accumulation and alleviate liver injury. After administration, T7 exhibited anti-oxidative stress and anti-inflammatory effects. It could appreciably increase the activity of superoxide dismutase (SOD), decrease the activity of lipid peroxidation product malondialdehyde (MDA), and appreciably reduce the pro-inflammatory factors interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α) levels. Molecular docking experiments demonstrated that T7 exhibited a strong binding affinity with the peroxisome proliferator-activated receptor-α (PPAR-α) receptor. T7 enhanced the PPAR-α expression in liver tissues, indicating that T7 may regulate lipid metabolism by activating the PPAR-α receptor. The hepatoprotective effect of T7 may be closely linked to its capacity to reduce oxidative stress and inflammatory responses. In conclusion, T7 may be a potential novel lipid-lowering candidate compound with the potential to improve liver injury.</p><p></p>

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Molecular hybridization strategy: design and synthesize carvacrol-based fibrate derivatives as novel lipid-lowering agents

  • 期刊论文

  • 发表日期：

    2025年10月27日

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  • Yunbi Zhang,
  • Wenjing Li,
  • Kexin Xu,
  • Boling Zhou,
  • Huanxian Shi,
  • Ling Ding,
  • Huizi Shangguan,
  • Yongheng Shi,
  • Xinya Xu,
  • Jiping Liu,
  • Yundong Xie

摘要

This study was designed to synthesize a series of carvacrol-based fibrate derivatives based on a molecular hybridization strategy. In acute hyperlipidemic mice, the target compound T7 exhibited a noticeable effect on lowering lipid and demonstrated a dose-dependent characteristic. In the high-fat diet (HFD) mouse model, T7 notably decreased triglyceride (TG), total cholesterol (TC), and low-density lipoprotein cholesterol (LDL-C) levels, and elevated high-density lipoprotein cholesterol (HDL-C) levels in both serum and liver tissues. Additionally, T7 appreciably increased the aspartate aminotransferase (AST) and alanine aminotransferase (ALT) found in both serum and liver tissues. Liver histopathological examination indicated that it could inhibit hepatic lipid accumulation and alleviate liver injury. After administration, T7 exhibited anti-oxidative stress and anti-inflammatory effects. It could appreciably increase the activity of superoxide dismutase (SOD), decrease the activity of lipid peroxidation product malondialdehyde (MDA), and appreciably reduce the pro-inflammatory factors interleukin-6 (IL-6) and tumour necrosis factor-α (TNF-α) levels. Molecular docking experiments demonstrated that T7 exhibited a strong binding affinity with the peroxisome proliferator-activated receptor-α (PPAR-α) receptor. T7 enhanced the PPAR-α expression in liver tissues, indicating that T7 may regulate lipid metabolism by activating the PPAR-α receptor. The hepatoprotective effect of T7 may be closely linked to its capacity to reduce oxidative stress and inflammatory responses. In conclusion, T7 may be a potential novel lipid-lowering candidate compound with the potential to improve liver injury.