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Mixture solution containing conjugate of transferrin and quercetin and its use

A transferrin and mixed solution technology, which is applied to medical preparations containing active ingredients, medical preparations with non-active ingredients, and drug combinations, etc., can solve the problems of cell toxicity, etc., and the method is simple and easy, and the toxicity is reduced , the effect of mild experimental conditions

Inactive Publication Date: 2007-12-19
INST OF CHEM CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the existing research on drug targeting mainly focuses on the coupling of drug molecules and transferrin through conjugates, and transferrin is transported to tumor cells as a mediating system. Drugs can also be toxic to cells in the treatment of tumors

Method used

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  • Mixture solution containing conjugate of transferrin and quercetin and its use
  • Mixture solution containing conjugate of transferrin and quercetin and its use
  • Mixture solution containing conjugate of transferrin and quercetin and its use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Add 0.2ml 10×10 to a 5.00ml volumetric flask -4 M quercetin in phosphate buffer solution (pH7.4), then add 0.4ml 1.25×10 -4 Phosphate buffer solution (pH7.4) of human transferrin (purchased from Sigma-Aldrich Company, T3309), the molar concentration ratio of human transferrin and quercetin in the mixed solution is 1: 4; Solution Dilute the solution to a quercetin concentration of 40 μM; shake the mixed solution evenly and let it stand for 12 hours to react the transferrin and quercetin to obtain a mixed solution containing a combination of transferrin and quercetin. As shown in Figure 1A, a new absorption peak appeared at 323nm after UV-Vis absorption spectrum analysis, indicating that quercetin and transferrin interacted to form a conjugate, and thus characteristic absorption appeared.

[0026] Similarly, after preparing quercetin and human transferrin respectively with a phosphate buffer solution of pH 4.8, and then mixing them, the molar concentration ratio of human...

Embodiment 2

[0030] Add 0.2ml 10×10 to a 5.00ml volumetric flask -4 M quercetin in phosphate buffer solution (pH6.8), then add 0.4ml 1.25×10 -4 Phosphate buffer solution (pH6.8) of M human transferrin (purchased from Sigma-Aldrich Company, T3309), the molar concentration ratio of human transferrin and quercetin in the mixed solution is 1: 4; Solution Dilute the solution to a quercetin concentration of 40 μM; shake the mixed solution evenly and let it stand for 12 hours to react the transferrin and quercetin to obtain a mixed solution containing a combination of transferrin and quercetin. Through the analysis of ultraviolet-visible absorption spectrum, fluorescence spectrum and circular dichroism spectrum, the same result as in Example 1 was obtained, that is, under neutral conditions, the two were combined.

Embodiment 3

[0032] Add 0.2ml 10×10 to a 5.00ml volumetric flask -4M quercetin in phosphate buffer solution (pH7.8), then add 0.4ml 1.25×10 -4 Phosphate buffer solution (pH7.8) of M human transferrin (purchased from Sigma-Aldrich Company, T3309), the molar concentration ratio of human transferrin in the mixed solution and quercetin is 1: 4; Solution Dilute the solution to a quercetin concentration of 40 μM; shake the mixed solution evenly and let it stand for 12 hours to react the transferrin and quercetin to obtain a mixed solution containing a combination of transferrin and quercetin. Through the analysis of ultraviolet-visible absorption spectrum, fluorescence spectrum and circular dichroism spectrum, the same result as in Example 1 was obtained, that is, under neutral conditions, the two were combined.

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Abstract

The present invention relates to one kind of mixture solution containing conjugate of transferrin and quercetin. The mixture solution is prepared through dissolving transferrin and quercetin separately in pH 6.8-7.8 phosphate buffer solution, mixing transferrin solution and quercetin solution in the molar ratio between transferrin and quercetin of 1 to 4, diluting the mixture solution with phosphate buffer solution to quercetin concentration of 40 micromole, shaking and standing to obtain the mixture solution containing conjugate of transferrin and quercetin. The mixture solution has conjugated transferrin and quercetin in phosphate buffer solution of proper pH condition, raised cytotoxic effect on tumor of quercetin, and raised targeting effect of small medicine molecule on tumor cell, and may be used in preparing medicine for treating colonic adenocarcinoma.

Description

technical field [0001] The invention relates to a mixed solution containing a combination of transferrin and quercetin, in particular to the interaction between a biomacromolecule transferrin (Tf) and a drug small molecule quercetin, which is regulated by quercetin A conjugate produced by a conformational change of transferrin and its use in the preparation of a drug for treating colon adenocarcinoma cells (LoVo). Background technique [0002] Drug small molecule quercetin (3,5,7,3',4'-pentahydroxyflavone) is a widely distributed flavonoid compound, and its structural formula is shown in formula I, which is two benzene rings (in formula I A and B rings) are formed by linking (C ring) through an oxygen-containing heterocycle. [0003] [0004] Studies have shown that in food, most quercetin has the ability to resist oxidation and chelate metal ions, and also has many biological and biochemical effects, such as anti-inflammatory and anti-tumor activities. However, due to ...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K47/48A61P35/00A61K47/64
Inventor 杜鸿雁张亚周向俊峰唐亚林
Owner INST OF CHEM CHINESE ACAD OF SCI
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