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Preparation and use of double branching polysialic acid active derivative

A technology of polysialic acid and its derivatives, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc. It can solve the problems of reduced biological activity, difficulty in realizing advantages, and loss of conjugates, etc. Achieve high biological activity, improve selectivity, and high retention

Inactive Publication Date: 2009-07-08
WENZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, single-chain polysialic acid is used in the polysialylation of proteins or other drugs. Several problems make it difficult to realize the advantages of the prepared polysialic acid and protein or drug conjugates.
One is that the binding of PSA reduces the biological activity of protein or drug conjugates
In addition, PSA can undergo partial hydrolytic cleavage during the formation of conjugates, so that the conjugates lose the advantages brought by the combination of PSA

Method used

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  • Preparation and use of double branching polysialic acid active derivative
  • Preparation and use of double branching polysialic acid active derivative
  • Preparation and use of double branching polysialic acid active derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 Different double-chain polyacetylneuraminic acid CA 2 -Lys-NHS preparation

[0047] Dissolve lysine (439 mg, 3 mmol) in 20 ml of water with a pH value of 8.0-8.3, and then add the freshly prepared active single-chain polyacetylneuraminic acid CA- DSG (1mmol) (prepared according to CN 101160326 method), while using 0.2mol / L NaOH to maintain the pH value of the system at 8.3. After stirring at room temperature overnight, the reaction was cooled to 0 °C. Now use diethyl ether to extract impurities from water, and then use chloroform to continuously extract three times. After the extract is concentrated, it is added dropwise into anhydrous diethyl ether to obtain a white precipitate. CA-Lys-COOH), the terminal functional group is carboxyl.

[0048] To the above product (0.9 mmol) dissolved in anhydrous dichloromethane (30 mL), triethylamine (TEA) was added until the pH value reached 8. Add reducing end activated derivatized single-chain polysialic acid CA-BS i...

Embodiment 2

[0050] Example 2 The same double-chain polyacetylneuraminic acid CA derived from non-reducing end activation 2 -Lys-NHS preparation

[0051] Lysine (0.2mmol) was dissolved in 40ml of borate buffer with a pH value of 8.0-8.3, and then the newly prepared active single-chain polyacetylneuraminic acid CA-DSG (0.6 mmol) (prepared by CN 101160326 method), while using 0.2mol / Lr NaOH to maintain the pH value of the system at 8.3. After stirring at room temperature overnight, the reaction was cooled to 0 °C. Now use diethyl ether to extract impurities from water, and then use chloroform to continuously extract three times. After the extract is concentrated, it is added dropwise into anhydrous diethyl ether to obtain a white precipitate. CA 2 -Lys-COOH), the terminal functional group is carboxyl.

[0052] At 0°C, the above-mentioned CA is dissolved in 2 -Lys-COOH (0.2mmol) in anhydrous dichloromethane (20mL) was added N-hydroxysuccinimide (0.6mmol) and DCC (0.6mmol), stirred at roo...

Embodiment 3

[0053] Example 3 The same double-chain polyacetylneuraminic acid CA derived from reducing end activation 2 -Lys-NHS preparation

[0054] Change the active single-chain polyacetylneuraminic acid CA-DSG (prepared according to the CN 101160326 method) derived from non-reducing end activation in the above example 2 into an equivalent amount of active single-chain polyacetylneuraminic acid derived from reducing end activation Acid CA-BS 3 That's it.

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Abstract

The invention belongs to the technical field of high molecular materials, and in particular relates to a new polysialic acid active derivative with a double bond structure and a preparation method thereof and application of the derivative to the medicine preparation. The derivative can be widely applied to the modification of amino-contained biological functional molecules, in particular to macromolecules such as proteins and polypeptides, and the improvement of medicinal solubility, stability and immunogenicity, thereby prolonging the half life of the medicines and improving the efficacy.

Description

Technical field: [0001] The invention belongs to the technical field of polymer materials, and in particular relates to a polysialic acid active derivative with a double-chain structure, a preparation method thereof and an application in medicine preparation. Said other molecules are especially macromolecules such as proteins and polypeptides, and the present invention also relates to pharmaceutical compositions comprising said conjugates. Background technique: [0002] At present, there are many kinds of drugs, which can be generally divided into two categories according to their molecular weight: one class has a lower molecular weight, usually below 1000, and most of them are commonly used chemically synthesized drugs and some natural drugs, such as nitrogen mustard. , cisplatin, 5-fluorouracil, paclitaxel, etc. all belong to this category; the other category has a larger molecular weight, most of which are protein and polypeptide drugs produced by genetic engineering. Ho...

Claims

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Application Information

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IPC IPC(8): C08B37/00A61K47/48A61K45/08A61P35/00
Inventor 林绍强赵承光李校堃赵应征梁广田吉来张卫星闫欣欣付小兵
Owner WENZHOU MEDICAL UNIV
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