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Application of two-to-one zinc complex of deferiprone in preparation of anti-cancer drugs

An anti-cancer drug and complex technology, applied in the medical field, can solve the problems of losing chelated iron and losing efficacy.

Inactive Publication Date: 2015-10-28
孔小乐
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The biggest problem with deferiprone at present is that its main part loses its efficacy through glucuronidation in the liver; the enzyme β-glucuronidase covalently bonds the 3-hydroxyl group of deferiprone to glucose, causing it to lose its chelation iron capacity

Method used

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  • Application of two-to-one zinc complex of deferiprone in preparation of anti-cancer drugs
  • Application of two-to-one zinc complex of deferiprone in preparation of anti-cancer drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0007] Prepared with zinc gluconate: take 0.5 g of zinc gluconate (D-gluconic acid-zinc molecular weight 454) (with zinc atom 70mg) and 0.31 g deferiprone (molecular weight 139), dissolve in 0.1L deionized water, use 125mg hydrogen Potassium oxide (2.3mmol) adjusts the pH to about 8 to determine the formation of a 2 to 1 zinc complex of deferiprone, where the concentration of zinc is 11mM and the concentration of deferiprone is 22mM. The solution can be administered orally or rectally via a titration pump to treat cancer patients. Use other zinc salt preparation (zinc target 1.1mmol): take zinc chloride 147.5mg (molecular weight 134) or anhydrous zinc sulfate 178mg (molecular weight 161) or zinc sulfate heptahydrate 316mg (hao alum, molecular weight 287) and 0.31g iron Ketone (molecular weight 139), dissolved in 0.1L of water, adjust the pH to about 8 with 125mg potassium hydroxide (2.3mmol) to determine the formation of a 2-to-1 zinc complex of deferiprone, including 11mM zinc...

Embodiment 2

[0009] The inhibitory effect of a 2:1 zinc complex of 1,2-dimethylpyridinone (with a zinc concentration of 115μM and deferiprone at 230μM) on lung cancer cell line A549.

[0010] The method for preparing the zinc deferiprone complex solution is obtained by diluting the solution prepared in Example 1 zinc gluconate with PBS 10 times (the concentration of deferiprone is 0.00022M).

[0011] MTT solution preparation method: Weigh 0.5 g of MTT, dissolve it in 100ml of phosphate buffered saline (PBS), filter with a 0.22μm filter to remove bacteria in the solution, and store at 4°C away from light.

[0012] (1) Cell culture: A549 cell line. Culture condition: PRMI-1640 medium with 10% calf serum, relative humidity 94%, 5% CO 2 , 37℃, cell concentration is 2×10 6 Passage 5mL. (2) Cell treatment: Lung cancer cell line A549 is cultured by conventional methods. During the experiment, cells in logarithmic growth phase are collected, the cell suspension concentration is adjusted, 100 μL is added...

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Abstract

The invention discloses an application of a two-to-one zinc complex of deferiprone in preparation of anti-cancer drugs, and belongs to the field of medicine. The drug molecular structure, namely the two-to-one zinc complex of 1,2-dimethyl-3-hydroxy-4-pyridone, can restrain absorption of cancer cell iron, and accordingly cancer can be cured.

Description

Technical field [0001] The invention relates to the medical field, and discloses the application of a zinc complex of deferiprone as a medicine for treating cancer. Background technique [0002] Iron chelating agents have been used to treat iron overload caused by long-term blood transfusion, with the purpose of expelling the iron accumulated in the body. Typical iron chelating agents include deferoxamine (DFO), the trade name of deferiprone (Obeianco), and deferoxino (Exjade). The deferiprone involved in the present invention was marketed in India as early as 1996 (US patent US20030158234), and the current patent for hemochromatosis and iron overload caused by long-term blood transfusion has expired. Its patentee's new patent (the production method of new use of deferiprone CN201010272148) emphasizes the use of deferiprone to remove iron from the heart. The claims and specifications of these two patents are silent on the therapeutic use of cancer. The biggest problem with def...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4412A61K31/555A61P35/00A61P35/02
Inventor 孔小乐
Owner 孔小乐