Lepr agonists / cxcr4 antagonists and their use in the preparation of medicaments for the treatment or prevention of insomnia

By regulating the leptin receptor and chemokine receptor signaling pathways through the LEPR agonist and CXCR4 antagonist in Suanzaoren Decoction, mitochondrial dysfunction was corrected, solving the problem of poor efficacy of existing insomnia treatments and achieving significant sleep improvement and cognitive recovery.

CN122398842APending Publication Date: 2026-07-17INSTITUTE OF CHINESE MATERIA MEDICA CHINA ACADEMY OF CHINESE MEDICAL SCIENCES
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-05-14
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing treatments for insomnia have failed to effectively target mitochondrial function, resulting in limited therapeutic effects and unclear underlying molecular mechanisms.

Method used

The Ziziphus jujuba seed decoction, composed of LEPR agonist and CXCR4 antagonist, corrects mitochondrial fission-fusion imbalance, enhances tricarboxylic acid cycle enzyme activity, and restores brain energy homeostasis by regulating the leptin receptor (LEPR) and chemokine receptor 4 (CXCR4) signaling pathways.

Benefits of technology

It significantly shortens the sleep latency, prolongs sleep time, restores cognitive function, reduces neuronal damage, improves mitochondrial energy metabolism, and alleviates insomnia symptoms.

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Abstract

本发明提供了一种LEPR激动剂 / CXCR4拮抗剂及其在制备治疗或预防失眠的药物中的应用，属于生物医药技术领域。本发明酸枣仁汤（SZRD）通过JAK2‑STAT信号通路调节LEPR和CXCR4的表达。分子对接和表面等离子体共振（SPR）证实，LEPR与5种SZRD衍生化合物具有高结合亲和力，这些化合物分别是：知母皂苷A2、酸枣仁皂苷B、绿原酸、甘草苷和异甘草苷。SZRD通过靶向LEPR / CXCR4介导的线粒体调控并恢复脑能量稳态来缓解失眠。将LEPR / CXCR4确定为先前未被识别的失眠治疗靶点，并为SZRD的多成分、多靶点作用提供了多方面的见解。
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