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Iodine (I)-23-hydroxyl betulinic acid, rpeparation method and application thereof

A betulinic acid and hydroxyl technology, applied in the fields of oncology, pharmaceutical preparations, and nuclear medicine, can solve problems such as no foreign reports, unclear molecular mechanism, etc., and achieve a simple preparation process, good stability, and strong anti-tumor pharmacological effects. Effect

Inactive Publication Date: 2007-06-13
JIANGSU INST OF NUCLEAR MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] 23-HBA is an innovative technological achievement in my country, and there is no foreign report
In addition, betulinic acid is an effective anti-inflammatory agent, but its molecular mechanism of action is still unclear.

Method used

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  • Iodine (I)-23-hydroxyl betulinic acid, rpeparation method and application thereof
  • Iodine (I)-23-hydroxyl betulinic acid, rpeparation method and application thereof
  • Iodine (I)-23-hydroxyl betulinic acid, rpeparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1: * Preparation of I-23-Hydroxybetulinic Acid

[0037]

[0038] A: Dissolve 20 μg of 23-hydroxybetulinic acid in 20 μL of ethanol, add 20 μL of 4mol / L hydrochloric acid solution, add 20 μL of 3% hydrogen peroxide, and add 1 mCiNaI * , vortexed for 1min to mix well, and placed at 40°C for 15min; adding 0.01mol / L sodium metabisulfite to terminate the reaction. Adjust the pH to 7 with ammonia water.

[0039] B: Add 2 mL of water to A, extract with ethyl acetate (5 mL x 3 times), collect the organic phase, and dry it with nitrogen in a water bath at 60°C.

Embodiment 2

[0040] Example 2: * Identification of I-23-hydroxybetulinic acid

[0041] Determination by thin layer chromatography and high performance liquid chromatography.

[0042] A: Thin-layer chromatography: silica gel paper as support, developing solvent as dichloromethane / methanol=9 / 1, Rf=0.5-0.7. After sample application, when the development is completed, the markers are detected as yellow spots at Rf=0.5-0.7 under ultraviolet light; the silica gel paper is cut into ten sections, and the radioactive count is measured by a gamma counter, and the radioactivity is concentrated at Rf=0.5-0.7. Free iodine is at Rf = 0-0.1.

[0043] B: HPLC: BIORAD HPLC, YWG C18 reverse phase column, acetonitrile / water=6 / 4 (containing 0.1% glacial acetic acid), flow rate 1mL / min, detect with ultraviolet detector (wavelength 254nm) and radioactive detector simultaneously, The retention time of free iodine is about 1.3min, * The retention time of I-23-hydroxy betulinic acid is about 5min.

Embodiment 3

[0044] Example 3: 131 Stability of I-23-hydroxybetulinic acid

[0045] Get the obtained by blowing dry under the item of embodiment 1 131 I-23-Hydroxybetulinic acid was dissolved in physiological saline and placed in a 4°C refrigerator at 37°C. After standing for 8 days, the radiochemical purity is still greater than 90%. It shows that the marker is stable at 4°C and 37°C, which can meet the requirements of routine clinical use.

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Abstract

The present invention relates to an iodo (*I)-23-hydroxybetulic acid, its preparation method and application, belonging to the field of nuclear medicine, oncology and pharmaceutical preparation technology. Said compound iodo (*I)-23-hydroxybetulic acid is a product by using iodine to label the anti-tumor Chinese medicine active component 23-hydroxybetulic acid, and its preparation method is characterized by making 23-hydroxybetulic acid undergo the process of structure reformation and introducing radiative nuclide iodine into its double bond position. Said invention also provides medicine or medicine composition formed from iodo (*I)-23-hydroxybetulic acid as active component and pharmaceutically-acceptable carrier, said medicine or medicine composition can be used for diagnosing and curing several tumors and cancers.

Description

technical field [0001] The invention relates to a tumor diagnosis (single photon emission computed tomography / SPECT, positron emission computed tomography / PET), a therapeutic reagent iodine ( * 1) -23-hydroxy betulinic acid and its medicine or pharmaceutical composition, preparation method and application. It involves the technical fields of nuclear medicine, oncology, and pharmaceutical preparations. Background technique [0002] Tumor is one of the diseases that seriously endanger human health. Although the level of modern medical diagnosis is continuously improved, such as the application of medical imaging examination, tumor marker detection and molecular biological gene chip technology, the improvement of the five-year survival rate and quality of life of cancer patients is still not ideal, one of the reasons It is the lack of detection technology and effective treatment that can obtain information on the pathophysiology and biochemical metabolism of early tumor tissu...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00C07J9/00A61K51/04A61P35/00A61P31/18A61K101/02
Inventor 杨敏王广基曹国宪俞惠新徐宇平蒋孟军张荣军项景德潘栋辉叶文才
Owner JIANGSU INST OF NUCLEAR MEDICINE
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