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Preparation of icaritin and derivatives thereof and application of icaritin and derivatives of icaritin in radiotherapy

A technology of icariin and its derivatives, which is applied in the preparation of icariin or its derivatives and its new medical application, and the preparation of drugs that increase the effect of radiation therapy and reduce the side effects of radiation therapy. Icaritin or its derivatives In the field of drug preparation, it can solve the problems of reducing the side effects of radiotherapy and increasing the effect of radiotherapy with icariin

Active Publication Date: 2014-02-12
XIAMEN LUJIA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] So far, there are no reports about icariin increasing the effect of radiotherapy or reducing the side effects of radiotherapy

Method used

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  • Preparation of icaritin and derivatives thereof and application of icaritin and derivatives of icaritin in radiotherapy
  • Preparation of icaritin and derivatives thereof and application of icaritin and derivatives of icaritin in radiotherapy
  • Preparation of icaritin and derivatives thereof and application of icaritin and derivatives of icaritin in radiotherapy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0183] Embodiment 1, the preparation of icariin derivative ICT-5-Fu condensate:

[0184]

[0185] 30 ml of tetrahydrofuran, 1 mmol of raw material ICT, 1 mmol of 5-fluorouracil (5-Fu), 1.3 mmol of DEAD and 1.3 mmol of triphenylphosphine were sequentially added into a 100 ml three-neck flask. The reaction was stirred overnight at room temperature. After the reaction was completed, 20 ml of water was added to the reaction system, extracted with ethyl acetate, the organic phases were combined, dried, filtered, concentrated to obtain a crude product, and purified by silica gel column chromatography to obtain pure ICT-5-Fu with a yield of 67%.

Embodiment 2

[0186] Embodiment 2, icariin derivative ICDE-01~ICDE-03 (when R 1 is methyl, R 2 for time) preparation:

[0187] 2.1 Preparation of intermediate IC-02:

[0188] Among them, R 1 For -Me:

[0189] Add 50 ml of acetone to a 100 ml three-necked flask, then, under stirring conditions, add 1 mmol of raw material IC-01, 1.2 mmol of allyl bromide and 1.5mmolK 2 CO 3 , the reaction solution was heated to reflux and stirred for 10 hours. After the reaction was completed, the solvent was evaporated to dryness under reduced pressure and recrystallized from ethanol to obtain the product IC-02 as a yellow solid with a yield of 70%.

[0190] 2.2 Preparation of intermediate IC-03:

[0191] Among them, R 1 For-Me, R 2 for Time:

[0192]In the there-necked flask of 100 milliliters, add 50 milliliters of methanol, then, under stirring condition, add 1mmol raw material IC-02 successively, 1.2mmol aldehyde (R 2 CHO) and 1.5mmol sodium ethylate, the reaction solution was heated...

Embodiment 3

[0205] Embodiment 3, icariin derivative ICDE-01 (when R 1 is benzyl, R 2 for time) preparation:

[0206] Among them, R 1 is benzyl, R 2 for Time:

[0207] Add 50 ml of methanol into a 100 ml three-neck flask, then exchange the reaction system with nitrogen three times, add 1 mmol of raw material IC-04, 10 mg of 10% Pd / C in sequence, and stir for 10 hours under hydrogen atmosphere. After the reaction was completed, the solvent was evaporated to dryness under reduced pressure, and recrystallized from ethanol / ethyl acetate to obtain the product ICDE-01 as a yellow solid with a yield of 60%.

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Abstract

The invention relates to preparation of icaritin and derivatives thereof and application of icaritin and derivatives of icaritin in radiotherapy. Specifically, the invention discloses derivatives of icaritin, shown in a formula I and a preparation method thereof and also discloses application of icaritin and derivatives of icaritin in radiotherapy. The icaritin and derivatives of icaritin can simultaneously serve as radiosensitizers and radioprotectants.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy. Specifically, the present invention relates to the preparation of icariin or its derivatives and its new medical application; use in medicines. Background technique [0002] Malignant tumors have become one of the diseases with the highest morbidity and mortality in my country. Radiation therapy is one of the main means of treating malignant tumors. The ideal goal of radiotherapy is to radically cure malignant tumors while minimizing damage to normal tissues, so as to ensure the long-term survival and quality of life of patients. However, due to the heterogeneity of tumors and the existence of individual differences, it is inevitable to bring different degrees of side effects to patients during radiotherapy, which has also become a bottleneck restricting the application of radiotherapy technology. [0003] Radiosensitizers refer to chemical substances that can increase the...

Claims

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Application Information

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IPC IPC(8): C07D405/04C07D407/04C07D311/30C07D405/12C07D471/04A61K31/4433A61K31/352A61K31/453A61K31/5377A61K31/496A61K31/506A61K31/41A61K31/437A61K41/00A61P35/00A61P39/00
CPCY02P20/55C07D405/04A61K41/0038C07D311/30C07D405/12C07D407/04C07D471/04
Inventor 张震寰董环文张美洪金省张世民张鲁榕
Owner XIAMEN LUJIA BIOTECH
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