木脂素衍生物、其制备方法及用途
By structurally modifying arctigenin, lignan derivatives were developed, solving the problem of poor oral efficacy of existing inhibitors. This resulted in effective inhibition of mitochondrial respiratory chain complex I and improved oral pharmacokinetic properties, making it suitable for the treatment of tumors and age-related diseases.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES
- Filing Date
- 2022-03-25
- Publication Date
- 2026-07-17
AI Technical Summary
Existing mitochondrial respiratory chain complex I inhibitors, such as arctigenin, are easily metabolized after oral administration, have poor pharmacokinetic properties, and low bioavailability, which limits their application as oral drugs. At the same time, tumors and senescent cells rely on the OXPHOS process for energy, and there is a lack of effective means of inhibition.
By structurally modifying arctigenin, a lignan derivative was developed, which improved the inhibitory activity against mitochondrial respiratory chain complex I and enhanced its oral pharmacokinetic properties.
It achieves effective inhibition of mitochondrial respiratory chain complex I, improves oral efficacy, has better drug-like properties, and is suitable for the prevention or treatment of diseases related to OXPHOS and age-related diseases.
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Figure CN117440947B_ABST