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Folate coupling antibody drug and its preparation method and use

A conjugate, folic acid technology, applied in the field of biomedicine, can solve the problems of no specific treatment drugs, difficult recovery of patients, ineffective toxic and side effects of treatment, etc.

Active Publication Date: 2012-12-19
ZHEJIANG JIANFENG HANSHENG BIOSCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0034] Although many drugs and treatment methods have been developed together to treat cancer, the high cost of treatment, the ineffectiveness of treatment, or its dreadful side effects make patients miserable
On the other hand, immune diseases have a long and repeated course, and there is no specific treatment drug at this stage, and many patients have difficulty recovering from their illness for life

Method used

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  • Folate coupling antibody drug and its preparation method and use
  • Folate coupling antibody drug and its preparation method and use
  • Folate coupling antibody drug and its preparation method and use

Examples

Experimental program
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Embodiment 1

[0139] Folic acid-GSH-IgG conjugate is composed of folic acid, GSH and human IgG. The molecular formula of Folate is: C 19 h 19 N 7 o 6 ; IgG is a recombinant IgG; the molecular formula of GSH is: C 10 h 17 N 3 o 6 S. Folic acid, GSH, and SPDP were purchased from Sigma, and recombinant IgG was purchased from Leinco Technologies. Its preparation method is as follows:

[0140] Folate-GSH was prepared by reacting 0.1 mol of Folate with 0.1 mol of DCC and 0.1 mol of NHS in DMSO at room temperature for 2 hours, centrifuging to remove the precipitate, and reacting with 0.1 mol of GSH in the dark under Ar environment overnight. SPDP was prepared into a 20 mmol / L solution, and IgG was reacted with 10 times the amount (molar amount) of SPDP at room temperature for 0.5 hours, and the product was separated with molecular sieve PD-10 to obtain IgG activated by SPDP. Folate-GSH was reacted with 0.1 times the amount (molar amount) of activated IgG (thiolated IgG) at room temperatu...

Embodiment 2

[0142] Folic acid-GSH-IgG conjugate, composed of Folate, GSH and human IgG. The molecular formula of Folate is: C 19 h 19 N 7 o 6 ; IgG is the Fc segment of human IgG; the molecular formula of GSH is: C 10 h 17 N 3 o 6 S. Folic acid, GSH, and SMPB were purchased from Sigma, and the Fc fragment of human IgG was purchased from Sino Biological Company. Its preparation method is as follows:

[0143] Folate-GSH was prepared by reacting 30 mol of Folate with 40 mol of DCC and 30 mol of NHS in DMSO at room temperature for 5 hours, centrifuging to remove the precipitate, and reacting with 30 mol of GSH in the dark under Ar environment overnight. SMPB was prepared into a 20 mmol / L solution, and IgG was reacted with 30 times the amount (molar amount) of SMPB at room temperature for 1 hour, and the product was separated with molecular sieve PD-10 to obtain activated IgG. Folate-GSH was reacted with 20 times the amount (molar amount) of activated IgG (thiolated IgG) at 4°C for 2...

Embodiment 3

[0145] Folic acid-GSH-IgG conjugate, composed of Folate, GSH and human IgG. The molecular formula of Folate is: C 19 h 19 N 7 o 6 ; IgG is human IgG1; the molecular formula of GSH is: C 10 h 17 N 3 o 6 S. Folic acid, GSH, and SMCC were purchased from Sigma, and human IgG1 was purchased from AXXORA. Its preparation method is as follows:

[0146] Folate-GSH was prepared by reacting 10 mol of Folate with 20 mol of DCC and 10 mol of NHS in DMSO at room temperature for 3 hours, centrifuging to remove the precipitate, and reacting with 10 mol of GSH in the dark under Ar environment overnight. SMCC was formulated into a 20 mmol / L solution, IgG was reacted with 20 times the amount (molar amount) of SMCC at room temperature for 1 hour, and the product was separated with molecular sieve PD-10 to obtain activated IgG. Folate-GSH was reacted with 10 times the amount (molar amount) of activated IgG (thiolated IgG) at room temperature for 20 hours, the reactant was passed through ...

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Abstract

The invention relates to a folate coupling antibody drug which is a FOLATE-GSH-IgG conjugate and its preparation method and use in treatment on tumors and autoimmune diseases. FOLATE is folate or its analogue. FOLATE and glutathione (GSH) form FOLATE-GSH by amino bonds. An amino group at an IgG end is activated or IgG is reduced into an incomplete antibody or a heavy chain antibody. The activated IgG and FOLATE-GSH are coupled into the FOLATE-GSH-IgG conjugate. In folate receptor high-expression-type cancer patients or autoimmune disease patients, the FOLATE-GSH-IgG conjugate can bind specifically with high expressed folate receptors on the surface of a disease cell, can activate an antibody or complement system by IgG to mediate cytotoxicity, can improve biological response adjustment, and does not produce cytotoxicity in a normal cell without expressed folate receptors. The folate coupling antibody drug improves targeting of an antibody-drug and an immunopotentiator and solves the problem that the existing drugs for treating cancers and autoimmune diseases produce damage on normal cells.

Description

technical field [0001] The invention belongs to the field of biomedicine, and specifically relates to a folic acid conjugated antibody drug (FOLATE-GSH-IgG conjugate), its preparation method and its application in treating tumors and autoimmune diseases. Background technique [0002] Folate is a water-soluble B vitamin composed of pteridine, p-aminobenzoic acid and glutamic acid residues, which was extracted and purified from spinach by H.K. Mitchell in 1941. Molecular formula is C 19 h 19 N 7 o 6 , the chemical structure is as follows: [0003] [0004] Folic acid is an essential substance for the human body, which can promote 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 c...

Claims

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Application Information

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IPC IPC(8): C07K16/00A61K31/519A61K47/48A61P35/00A61P37/02
Inventor 刘颖其他发明人请求不公开姓名
Owner ZHEJIANG JIANFENG HANSHENG BIOSCI
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