Use of a compound targeting liver sinusoidal endothelial cells, isorhamnetin, in the preparation of a medicament for treating liver fibrosis

By targeting hepatic sinusoidal endothelial cells with isorhamnetin, regulating fenestration structure and mitochondrial autophagy flux, and inhibiting cellular senescence, the problem of lack of direct intervention in existing drug treatments for liver fibrosis has been solved, and effective treatment of liver fibrosis has been achieved.

CN122398780APending Publication Date: 2026-07-17SAINS NEW MEDICAL COLLEGE OF GUANGXI UNIV OF TRADITIONAL CHINESE MEDICINE
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SAINS NEW MEDICAL COLLEGE OF GUANGXI UNIV OF TRADITIONAL CHINESE MEDICINE
Filing Date
2026-05-20
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Current drug treatments for liver fibrosis lack effective drugs that directly intervene in the fibrosis process. Research on targeting hepatic sinusoidal endothelial cells has mostly focused on complex nanodelivery systems, and the regulatory effects of natural small molecule compounds on hepatic sinusoidal endothelial cell function have not been reported.

Method used

Isorhamnetin was used as a compound targeting hepatic sinusoidal endothelial cells. By regulating the fenestration structure of hepatic sinusoidal endothelial cells, mitochondrial autophagy flux, and inhibiting cell senescence, the liver microcirculation was restored and HSC activation signals were blocked, thus preparing a drug for the treatment of liver fibrosis.

Benefits of technology

Isorhamnetin significantly restores the number of fenestrations in hepatic sinusoidal endothelial cells, improves hepatic microcirculation, regulates metabolic disorders, inhibits cell senescence, enhances the vitality of hepatic sinusoidal endothelial cells, and achieves an anti-hepatic fibrosis effect.

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Abstract

本发明公开了一种靶向肝窦内皮细胞的化合物异鼠李素在制备治疗肝纤维化药物中的应用,属于生物医药技术领域。所述异鼠李素的化学式为C16H12O7,其可与药学上可接受的载体联合制备成药物或者其药学上可接受的盐作为药物活性组分制备成药物。异鼠李素作为药物活性组分的浓度为25μM‑100μM。具有靶向人肝窦内皮细胞HHSEC改善其生理功能的作用。本发明实验证实了异鼠李素能靶向肝窦内皮细胞,具有重建肝窦内皮细胞窗孔结构、改善细胞微循环;修复细胞线粒体自噬、恢复线粒体膜电位、降低线粒体ROS、上调Beclin1 / LC3Ⅱ / FUNDC1;抑制细胞衰老;调控SCD1 / ELOVL3代谢通路等作用。
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