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Folate-IgG conjugate as well as preparation method and application thereof

A technology of conjugates and folic acid, which is applied in the field of folic acid-IgG conjugates and its preparation and application, can solve the problems of no improvement in erythrocyte sedimentation rate and anemia, large side effects of treatment, difficult treatment, etc., and achieve fast blood clearance and reduce toxicity. Side effects, strong penetrating effects

Active Publication Date: 2011-03-16
ZHEJIANG JIANFENG HANSHENG BIOSCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no improvement in RF, erythrocyte sedimentation rate and anemia, and long-term application will cause serious side effects
[0037] These two diseases have treatment difficulties and side effects, and more targeted targeted therapy technologies are needed to treat these diseases

Method used

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  • Folate-IgG conjugate as well as preparation method and application thereof
  • Folate-IgG conjugate as well as preparation method and application thereof
  • Folate-IgG conjugate as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Folic acid-IgG conjugates are composed of folic acid and human IgG. The molecular formula of folic acid is: C 19 h 19 N 7 o 6 . Its preparation method is as follows:

[0056] React 0.1 folic acid (F) with 0.1 dicyclohexylcarbodiimide (DCC) and 0.1 hydroxysuccinimide ester (NHS) in DMSO at room temperature for 2 hours, centrifuge to collect the precipitate, and mix with 0.01 times the amount of human After the IgG was reacted at room temperature for 2 hours, the reactant was passed through PD-10 molecular sieves, and the collected product was the folic acid-IgG conjugate.

Embodiment 2

[0058] Folic acid-IgG conjugates are composed of folic acid and recombinant IgG. The molecular formula of folic acid is: C 19 h 19 N 7 o 6 . Its preparation method is as follows:

[0059] React 30 mol of folic acid with 40 mol of dicyclohexylcarbodiimide (DCC) and 30 mol of hydroxysuccinimide ester (NHS) in DMSO at room temperature for 5 hours, centrifuge to collect the precipitate, and react with 2.0 times the amount of recombinant IgG at room temperature for 5 Hours later, the reactant was passed through PD-10 molecular sieves, and the collected product was the folic acid-IgG conjugate.

Embodiment 3

[0061] Folic acid-IgG conjugates are composed of folic acid and the Fc segment of recombinant IgG. The molecular formula of folic acid is: C 19 h 19 N 7 o 6 . Its preparation method is as follows:

[0062] React 10 mol of folic acid with 20 mol of dicyclohexylcarbodiimide (DCC) and 10 mol of hydroxysuccinimide ester (NHS) in DMSO at room temperature for 3 hours, centrifuge to collect the precipitate, and mix with 1.0 times the amount of Fc segment of recombinant IgG After reacting at room temperature for 4 hours, the reactant was passed through PD-10 molecular sieves, and the collected product was the folic acid-IgG conjugate.

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Abstract

The invention provides a folate-IgG conjugate as well as a preparation method and application thereof. The folate-IgG conjugate is composed of folate and human souce IgG or recombinant IgG or the Fc section of IgG. The method for preparing the folate-IgG conjugate comprises the following steps: leading 0.1 to 30mol of the folate to react with 0.1 to 40mol of dicyclohexylcarbodiimide and 0.1 to 30mol of hydroxysuccinimide eater in dimethylsulfoxide (DMSO) at room temperature; centrifuging to extract precipitate; leading the precipitate to react with 0.01 to 2.0 times of the human source IgG or the recombinant IgG or the Fc section of the IgG at room temperature for 2 to 5 hours; and filtering the reactant through a molecular screen, and collecting the product, namely the folate-IgG conjugate. The folate-IgG conjugate can be used as a medicament for treating cancer and a medicament for treating autoimmune diseases. The folate-IgG conjugate can be specifically combined to cancer cells and macrophages activated in a patient body with the autoimmune diseases, but cannot be combined to normal cells, so that the problem of damaging the normal cells by the cancer treatment medicament and autoimmune disease medicament in the prior art can be solved.

Description

technical field [0001] The present invention relates to folic acid-IgG conjugate, its preparation method and its application. Background technique [0002] Folic acid was extracted and purified from spinach by H.K. Mitchell in 1941. It is a water-soluble B vitamin composed of pteridine, p-aminobenzoic acid and glutamic acid residues. It is an essential substance for the human body. , has the effect of promoting the maturation of young cells in the bone marrow. If the lack of folic acid can lead to the increase of abnormal immature cells of red blood cells and the decrease of white blood cells. The latest research shows that folic acid may trigger the apoptosis of cancer cells, have a certain impact on the gene expression of cancer cells, and have a certain anti-cancer effect. The most important reason is that folic acid can bind to folic acid receptors in the body. Folate receptors (FR) are divided into α and β subtypes. Studies have shown that in 90% of ovarian cancer, adv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K16/00C07K1/113A61K31/519A61K47/48A61P35/00A61P35/02A61P37/02A61P19/04A61P1/00A61P17/06A61P11/00A61K47/68
Inventor 丁虹刘颖
Owner ZHEJIANG JIANFENG HANSHENG BIOSCI
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