Mixture solution containing conjugate of transferrin and quercetin and use thereof

A technology of transferrin and mixed solution, which is applied in the direction of medical preparations containing active ingredients, medical preparations with non-active ingredients, drug combinations, etc., can solve the problems of cell toxicity, etc. Mild, less toxic effect

Inactive Publication Date: 2012-11-21
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 use thereof
  • Mixture solution containing conjugate of transferrin and quercetin and use thereof
  • Mixture solution containing conjugate of transferrin and quercetin and use thereof

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 (pH 7.4), then add 0.4ml 1.25×10 -4 M human transferrin (purchased from Sigma-Aldrich, T3309) in phosphate buffer solution (pH 7.4), the molar concentration ratio of human transferrin and quercetin in the mixed solution is 1:4; The solution was diluted to a quercetin concentration of 40 μM; the mixed solution was shaken evenly and left to stand for 12 hours, and the transferrin reacted with the quercetin to obtain a mixed solution containing a conjugate of the transferrin and quercetin. After UV-Vis absorption spectroscopy analysis, the results are as follows: figure 1 As shown in A, a new absorption peak appeared at 323nm, indicating that quercetin and transferrin interacted to form a conjugate, resulting in characteristic absorption.

[0026] Similarly, after preparing quercetin and human transferrin with pH 4.8 phosphate buffer solution respectively, and then mixing them, the m...

Embodiment 2

[0030] Add 0.2ml 10×10 to a 5.00ml volumetric flask -4 M quercetin in phosphate buffer solution (pH 6.8), then add 0.4ml 1.25×10 -4Phosphate buffer solution (pH 6.8) 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; The solution was diluted to a quercetin concentration of 40 μM; the mixed solution was shaken evenly and left to stand for 12 hours, and the transferrin reacted with the quercetin to obtain a mixed solution containing a conjugate of the transferrin and quercetin. The same results as in Example 1 were obtained by UV-visible absorption spectrum, fluorescence spectrum and circular dichroism analysis, that is, the combination of the two under neutral conditions.

Embodiment 3

[0032] Add 0.2ml 10×10 to a 5.00ml volumetric flask -4 M quercetin in phosphate buffer solution (pH 7.8), then add 0.4ml 1.25×10 -4 Phosphate buffer solution (pH 7.8) 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; The solution was diluted to a quercetin concentration of 40 μM; the mixed solution was shaken evenly and left to stand for 12 hours, and the transferrin reacted with the quercetin to obtain a mixed solution containing a conjugate of the 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, the combination of the two under neutral conditions.

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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] Formula I [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. Howeve...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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