Nervonic acid derivative as well as preparation method and application thereof

By chemically modifying nervonic acid, a white solid nervonic acid derivative was prepared, which solved the problems of low extraction rate, high cost and complicated preparation. It achieved efficient penetration of the blood-brain barrier, exerted a dual mechanism to treat Alzheimer's disease and significantly improved cognitive function.

CN122444631APending Publication Date: 2026-07-24NORTHWEST A & F UNIV
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Patent Information

Application Number
CN202610644178.2
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-05-11
Publication Date
2026-07-24

AI Technical Summary

Technical Problem

The current nervonic acid has a low extraction rate, high cost, poor stability, and complex preparation process and low purity of derivatives, resulting in limited efficacy and significant side effects in the treatment of Alzheimer's disease, as well as low blood-brain barrier penetration.

Method used

A nervonic acid derivative was prepared by modifying its chemical structure using specific methods, including activating the carboxyl group with 1-hydroxybenzotriazole (HOBT) and 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDCI), adding 4-(2-aminoethyl)phenyl-1,2-diol hydrochloride and N,N-diisopropylethylamine, and quenching the reaction with distilled water, extraction and purification by column chromatography to obtain a white solid product.

Benefits of technology

It significantly improves the stability and targeting of nervonic acid, enabling it to penetrate the blood-brain barrier and accumulate in the hippocampus. By inhibiting neuroinflammation and hippocampal neuronal ferroptosis, it significantly improves cognitive impairment caused by Alzheimer's disease, providing a novel treatment option.

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Abstract

The invention provides a nervonic acid derivative as well as a preparation method and application thereof. The nervonic acid derivative is a sixth derivative, and the chemical structure of the sixth derivative is shown in the specification. The nervonic acid derivative and the corresponding medicine thereof disclosed by the invention break through the bottleneck of the blood brain barrier, accurately remove amyloid protein plaques in the brain, repair damaged neural pathways and remarkably improve cognitive impairment.
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