Transferrin-polyethylene glycol medicine molecular compound and its use

A technology of transferrin and polyethylene glycol, which can be used in drug combinations, peptide/protein components, medical preparations of inactive ingredients, etc., can solve the problem of insignificant tumor targeting, increase drug stability, and weaken immunogens To achieve the effect of prolonging plasma half-life, enhancing anti-tumor effect and improving distribution

Inactive Publication Date: 2007-02-14
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The combination of PEG and biomacromolecular drugs can increase the stability of the drug; weaken or eliminate immunogenicity; prolong the half-life of the drug in vivo; although, after the anti-tumor drug is modified by PEG, it can increase the effect of the drug on the tumor through passive targeting. However, since it has no specific recognition effect on tumor cells, its distribution in tumor tissue and normal tissue is not significantly different, and the tumor targeting effect is not significant

Method used

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  • Transferrin-polyethylene glycol medicine molecular compound and its use
  • Transferrin-polyethylene glycol medicine molecular compound and its use
  • Transferrin-polyethylene glycol medicine molecular compound and its use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1 Preparation of Tf-PEG-tumor necrosis factor-alpha molecular complex (I)

[0059] Take 20nmol tumor necrosis factor-α (TNF-α) and 100nmol MAL-PEG-NHS (average molecular weight 3400), react in 1mL HEPES buffer (15mM, pH8.0) at 4°C for 1 hour, add 5 6-amino-n-hexanoic acid of twice the molar amount of PEG terminates the reaction. Load 0.5mL once on a cation exchange column (POROS 20HS, diameter 4.6mm, column bed volume 1.66mL), BioCAD workstation, UV detector (wavelength 280nm) for separation and purification, and collect the MAL-PEG-TNF-α fraction. Measure the contents of TNF-α and PEG in the MAL-PEG-TNF-α component respectively, and the molar ratio of TNF-α and PEG is 1: 1.9, and the yield (compared with the amount of TNF-α participating in the reaction) is 18.90% .

[0060] Dissolve 0.5 μmol of Tf in 1 mL of 30 mM HEPES buffer (containing 1 mM EDTA, pH 8.5), add 4 μmol of thiol reagent 2-iminothiophene hydrochloride, and react for 3 h at room temperature und...

Embodiment 2

[0062] Example 2 Preparation of Tf-PEG-tumor necrosis factor-alpha molecule complex (II)

[0063]Take 20nmol TNF-α and 400nmol MAL-PEG-NHS (average molecular weight 3400), in 1mL of HEPES buffer (15mM, pH8.0), react at 4°C for 1 hour, add 6- Aminocaproic acid terminates the reaction. Load 0.5mL once on a cation exchange column (POROS 20HS, diameter 4.6mm, column bed volume 1.66mL), BioCAD workstation, UV detector (wavelength 280nm) for separation and purification, and collect the MAL-PEG-TNF-α fraction. Measure the contents of TNF-α and PEG in the MAL-PEG-TNF-α component respectively, the molar ratio of TNF-α and PEG is 1: 2.6, and the yield (compared with the amount of TNF-α participating in the reaction) is 50.44% .

[0064] Dissolve 0.5 μmol of Tf in 1 mL of 30 mM HEPES buffer (containing 1 mM EDTA, pH 8.5), add 4 μmol of thiol reagent 2-iminothiophene hydrochloride, and react for 3 h at room temperature under argon. The reaction product is passed through a gel desalting...

Embodiment 3

[0065] Example 3 Preparation of Tf-PEG-tumor necrosis factor-alpha molecule complex (III)

[0066] Take 20nmol TNF-α and 800nmol MAL-PEG-NHS (average molecular weight 3400), in 1mL of HEPES buffer (15mM, pH8.0), react at 4°C for 1 hour, add 6- Aminocaproic acid terminates the reaction. Load 0.5mL once on a cation exchange column (POROS 20HS, diameter 4.6mm, column bed volume 1.66mL), BioCAD workstation, UV detector (wavelength 280nm) for separation and purification, and collect the MAL-PEG-TNF-α fraction. Measure the contents of TNF-α and PEG in the MAL-PEG-TNF-α component respectively, and the molar ratio of TNF-α and PEG is 1: 3.7, and the yield (compared with the amount of TNF-α participating in the reaction) is 60.81%. .

[0067] Dissolve 0.5 μmol of Tf in 1 mL of 30 mM HEPES buffer (containing 1 mM EDTA, pH 8.5), add 4 μmol of thiol reagent 2-iminothiophene hydrochloride, and react for 3 h at room temperature under argon. The reaction product is passed through the gel ...

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Abstract

A transferring-polyethanediol-medicine molecule composition for the target therapy of tumor is disclosed. It features the combination of transferring and polyethanediol to make it has both active and passive target functions. Its advantages are long semi-life and high accumulation degree in tumor tissue. It can be used to prepare the antineoplastic medicines.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and in particular relates to a transferrin-polyethylene glycol-drug molecule complex and its application in tumor targeting therapy. technical background [0002] Protein polypeptide anti-tumor drugs are a class of drugs that use cell biology and molecular biology to regulate the body's immune system or the growth of tumors, thereby inhibiting tumor growth, especially for the recovery of blood cell groups after chemotherapy and radiotherapy. Works great. At present, this type of drug has been paid attention to in clinical tumor treatment, but there are still some problems in its application, such as: not stable enough in vivo, and the half-life is very short; due to lack of selectivity, it leads to relatively even tissue distribution. Normal tissue and cytotoxic side effects are large; often produce a certain amount of antigenicity, leading to the occurrence of immune reactions and so on. There...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K38/40C07K17/08A61K47/34A61P35/00A61K47/60A61K47/66
Inventor 姜嫣嫣裴元英柳晨洪鸣凰朱赛杰孔淑仪
Owner FUDAN UNIV
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