Tocotrienol ether derivative as well as preparation method and application thereof

By synthesizing and optimizing the administration method tocotrienol ether derivatives, the problem of low bioavailability of vitamin E nanoformula is solved, and effective protection and hematopoietic recovery of the hematopoietic system caused by ionizing radiation is achieved.

CN120271544APending Publication Date: 2025-07-08ACADEMY OF MILITARY MEDICAL SCIENCES
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Patent Information

Application Number
CN202410028593.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-01-08
Publication Date
2025-07-08

AI Technical Summary

Technical Problem

Existing vitamin E nanoformulations have limitations in improving bioavailability, and it is difficult to effectively protect or alleviate the damage to the hematopoietic system caused by ionizing radiation, especially the treatment of H-ARS is not effective.

Method used

A series of tocotrienol ether derivatives were designed and synthesized, and delta-T3H derivatives with higher G-CSF induction were prepared through esterification and reduction reactions, and the administration method was optimized to improve bioavailability, including subcutaneous injection.

Benefits of technology

δ-T3H derivatives significantly improve bioavailability, show stronger radiation protection, can significantly increase the production of G-CSF, promote hematopoietic recovery, improve the survival rate of mice and the regeneration of peripheral blood cells.

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Abstract

The invention provides a tocotrienol ether derivative as shown in a formula I, and an isomer, a prodrug, a pharmaceutically acceptable salt, a hydrate or a solvent compound of the tocotrienol ether derivative, r is selected from hydrogen, a substituted or unsubstituted alkyl group with 1 to 10 carbon atoms, a substituted or unsubstituted alkenyl group with 2 to 10 carbon atoms, a substituted or unsubstituted alkynyl group with 2 to 10 carbon atoms, a substituted or unsubstituted aryl group with 6 to 20 carbon atoms, or a substituted or unsubstituted heteroaryl group with 5 to 12 members, a substituted or unsubstituted cycloalkyl group with 3 to 8 carbon atoms or a heterocycloalkyl group with 3 to 8 carbon atoms. The derivative has a better effect on the whole, and is expected to actually become a potential and lasting radiation protective agent aiming at H-ARS.
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