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Thymopeptide-5 active esters, medicinal composition containing same and application thereof

A technology of peptide active ester and thymus, which is applied in the field of esterified derivatives of thymopentin, can solve the problems of direct modification of thymopentin into ester and other problems, and achieve the half-life extension, high biological activity and good application prospect Effect

Inactive Publication Date: 2013-02-20
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although the research on thymopentin is relatively extensive, there is no report on the direct modification of thymopentin into an ester

Method used

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  • Thymopeptide-5 active esters, medicinal composition containing same and application thereof
  • Thymopeptide-5 active esters, medicinal composition containing same and application thereof
  • Thymopeptide-5 active esters, medicinal composition containing same and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1. thymopentin diethyl ester

[0032]

[0033] Put 20ml of absolute ethanol in the reaction bottle, add 2ml of thionyl chloride in ice bath, add 200mg of thymopentin, and stir until the reaction is complete. Excess ethanol and thionyl chloride were removed by rotary evaporation under reduced pressure to obtain a white product. After methanol was dissolved, it was determined by HPLC-MS, m / z 736.4, 368.8 (base peak).

Embodiment 2

[0034] Embodiment 2. thymopentin dihexyl ester

[0035]

[0036] Put 20ml of anhydrous ethanol in a reaction bottle, add 2ml of thionyl chloride under ice-bath conditions, add 200mg of thymopentin, and react under stirring conditions until equilibrium is reached. Hexanol was removed under reduced pressure by rotary evaporation, separated and purified to obtain a white product. m / z 848.6, 424.9, determined by HPLC-MS.

Embodiment 3

[0037] Embodiment 3. thymopentin dilauryl ester

[0038]

[0039] 50ml of lauryl alcohol (lauryl alcohol) was mixed with 50ml of tetrahydrofuran, 2ml of thionyl chloride was added under ice-bath conditions, 500mg of thymopentin was added, and the reaction was continued until equilibrium was reached. After the reaction was completed, thionyl chloride and tetrahydrofuran were removed under reduced pressure by rotary evaporation. Acetic acid solution was added to the residual reaction solution, and after the layers were separated, the aqueous layer was freeze-dried, separated and purified, and the product was analyzed by HPLC-MS, with m / z of 508.7 and 1016.4.

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PUM

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Abstract

The invention relates to thymopeptide-5 active esters, medicinal composition containing the same and application thereof. The thymopeptide-5 active esters are esters generated by combining thymopeptide-5 C-end carboxyl and / or aspartic acid lateral chain carboxyl with alcoholic hydroxyl. Experimental results show that the thymopeptide-5 active esters have the functions of significant immune potentiation and oxidation resistance, enhanced stability and prolonged half-life.

Description

technical field [0001] The present invention relates to the esterified derivatives of thymopentin and the pharmaceutical composition containing one or more of them and the application. Background technique [0002] Thymopoietin (thymopoietin) is a polypeptide hormone containing 49 amino acid residues secreted by thymus epithelial cells. Thymopentin (TP-5) is the 32-36 amino acid fragment of thymopoietin. Its amino acid sequence is: Arg-Lys-Asp-Val-Tyr. TP-5 is the active site of thymopoietin, and its function is the same as that of thymopoietin. It is an immune enhancer for T lymphocytes, which can promote the maturation and differentiation of T cells, and promote mature T cells to secrete a variety of lymphocytes. Factors (such as interleukin 2 and γ-interferon, etc.), can also promote the production of interleukin-2 receptors and increase the activity of SOD in peripheral blood. In animal models with impaired immune balance, whether the immune response is too high or too...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06A61K38/08A61P35/00A61P31/12A61P37/00
Inventor 梅兴国迟强
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A