Medical application of gamma- and delta-tocopherol and derivatives thereof serving as novel radioprotectants

A technology of tocopherol and its derivatives, which is applied in the field of medical application of γ- and δ-tocopherol and its derivatives as a new type of radiation protection agent, which can solve the problem of large dosage

Active Publication Date: 2014-01-22
INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, in the irradiated mouse model, the doses of these three compounds that produced radioprotective effects were all relatively large

Method used

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  • Medical application of gamma- and delta-tocopherol and derivatives thereof serving as novel radioprotectants
  • Medical application of gamma- and delta-tocopherol and derivatives thereof serving as novel radioprotectants
  • Medical application of gamma- and delta-tocopherol and derivatives thereof serving as novel radioprotectants

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Embodiment

[0033] The present invention can be further illustrated by the following examples, but these examples are not meant to limit the present invention in any way.

[0034] Method for preparing compound of general formula I

[0035]

[0036] That is, it is prepared by reacting the raw material phenol I'with the corresponding acid anhydride (R1CO) 20 under the catalysis of 4-dimethylaminopyridine and the presence of a base such as triethylamine; and the acid anhydride is prepared by reacting the corresponding acid with excess acetic anhydride .

[0037] General method: Weigh 10mmol of raw phenol, dissolve it in 50mL of dichloromethane, add 11mmol of triethylamine and 1mmol of 4-dimethylaminopyridine, add 10.5mmol of acid anhydride under stirring and cooling with ice water, add 10.5mmol of acid anhydride, after addition, heat up naturally, TLC tracking During the reaction process, until the phenol point of the raw material disappears, add dilute hydrochloric acid to acidify, split, wash wi...

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Abstract

The invention discloses a medical application of gamma- and delta-tocopherol and derivatives thereof serving as novel radioprotectants. The invention relates to an application of a compound shown in a general formula I in the specification with the anti-radiation damage activity, an isomer of the compound and a medicine composition containing the compound and the isomer of the compound in the alleviation of hematopoietic function damage caused by radiation or / and chemotherapy drugs, the rising of blood leukocyte level and / or resistance of radiation damage, or tumor adjuvant therapy and the like or serving as tool drugs for researching radiation damage.

Description

Technical field: [0001] The present invention relates to γ- and δ-tocopherols, their derivatives, isomers, and possible stereoisomers having anti-radiation activity as shown in general formula I, and pharmaceutical compositions containing them are effective in reducing radiation or / And the application of hematopoietic function damage caused by chemotherapeutic drugs, increased blood white blood cell level and / or resistance to radiation damage, or tumor adjuvant therapy, or as a tool for research on radiation damage. technical background: [0002] Radioprotectants are compounds that can reduce the biological effects of radiation (reference: Hall, Radiobiology for the Radiobiologist, Lippincott Williams & Wilkins, Philadelphia, Pa. [1994]). Through pre- and / or post-radiation administration, the lethality of animals induced by radiation can be reduced. Radioprotectors work through different mechanisms (reference: Bump and Malaker (eds.), Radioprotectors: Chemical, Biological, and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/355A61P39/00
Inventor 从玉文余祖胤杨日芳丛悦柳晓兰善亚君张刘珍
Owner INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA
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