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Polyethylene glycol-modified thymus peptide 1 derivatives

Inactive Publication Date: 2005-11-02
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the pharmacokinetic properties of thymosin 1 itself are poor, and the residence time in the body is relatively short, so it is excluded, and its half-life is 2 hours.
Animal experiments prove that it cannot fully exert its due efficacy
This requires frequent injections of thymosin 1, which leads to inconvenient treatment and increased treatment costs. At the same time, because the price is too high for ordinary patients to bear, the quality of treatment decreases.

Method used

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  • Polyethylene glycol-modified thymus peptide 1 derivatives
  • Polyethylene glycol-modified thymus peptide 1 derivatives
  • Polyethylene glycol-modified thymus peptide 1 derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Ac-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Lys-Asp-Leu-Lys-Glu-Lys-Lys-Glu-Val-Val-Glu- Preparation of Glu-Ala-Glu-Asn-Glu-Cys-PEG40K

[0099] Step 1: Precursor for polyethylene glycol modification—C-terminal cysteine ​​thymosin 1 derivative prepared by solid-phase chemical synthesis:

[0100] (1) Amino acid monomers used

[0101] Fmoc-Ala-OH Fmoc-Lys(Boc)-OH

[0102] Fmoc-Asn(Trt)-OH Fmoc-Ser(tBu)-OH

[0103] Fmoc-Asp(OtBu)-OH Fmoc-Thr(tBu)-OH

[0104] Fmoc-Cys(Trt)-OH Fmoc-Val-OH

[0105] Fmoc-Glu(OtBu)-OH Fmoc-Ile-OH

[0106] Fmoc-Leu-OH

[0107] The abbreviation in the above formula means:

[0108] Fmoc: 9-fluorenylmethoxycarbonyl (9-fluorenylmethoxycarbonyl)

[0109] Boc: tert-butyloxycarbonyl (tert-butyloxycarbonyl)

[0110] Trt: Trityl (trityl)

[0111] OtBu: tert-butyl

[0112] tBu: tert-butyl

[0113] (2) The equipment and reagents used in the synthesis

[0114] Instruments: The synthesis of peptide sequences is carried out manually, an...

Embodiment 2

[0142] Ac-Ser-Asp-Ala-Ala-Val-Asp-Thr-Ser-Ser-Glu-Ile-Thr-Thr-Arg-Asp-Leu-Arg-Glu-Arg-Arg-Glu-Val-Val-Glu- Glu-Ala-Glu-Asn-Lys-PEG40K

[0143] Step 1: Solid-phase chemical synthesis to prepare precursor C-terminal lysine 14, 17, 19, 20, arginine-substituted thymosin 1 derivatives for polyethylene glycol modification:

[0144] For the solid-phase chemical synthesis method, see Example 1 for the solid-phase chemical preparation of the C-terminal cysteine ​​thymosin 1 derivative. 10 g of Wang resin (0.6 mmol / g resin, 6 mmol) linked with Fmoc-Lys(Boc)-OH was used for synthesis. The synthesis follows the Fmoc amino acid and the synthesis cycle is repeated with the corresponding amino acid in each cycle step:

[0145] Fmoc-Asn(Tre)-OH, Fmoc-Ala-OH, Fmoc-Glu(OtBu)-OH,

[0146] Fmoc-Glu(OtBu)-Ort,

[0147] Fmoc-Val-OH, Fmoc-Val-OH, Fmoc-Glu(OtBu),

[0148] Fmoc-Arg(Pbf)-OH, Fmoc-Arg(Pbf)-OH, Fmoc-Glu(OtBu)-OH,

[0149] Fmoc-Arg(Pbf)-OH, Fmoc-Leu-OH, Fmoc-Asp(OtBu)-OH,

[0150] Fm...

Embodiment 3

[0158] Embodiment three drug efficacy experiment

[0159] Using Zidaxian as a positive control, the effect of the sample on the production of cytokines by T lymphocytes was detected to determine whether the sample has a regulatory effect on the immune activity of T lymphocytes and the strength of the effect.

[0160] [Experimental principle]

[0161] Among the lymphocytes cultured in vitro, T lymphocytes can activate T lymphocytes after being stimulated by mitotic proconcanavalin A (ConA, Concanavalin A), and produce cytokine synthesis, cytokine receptor expression, cell differentiation and cell proliferation. Changes in cell behavior. The production of cytokines and the proliferative response of cells are the reflection of the functional state and cell activation of immune cells. The detection method has the characteristics of reliability, good repeatability and simplicity, so it has been widely used to judge the influence of samples on the function of T lymphocytes through...

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Abstract

The invention relates to the method for producing long-acting thymus peptide 1 derivant and its salt for medical use, and the usage of them. The long-acting thymus peptide derivant is consisting of thymus peptide derivant and carbowax with covalent links, of which the structure is showed as the instruction defined. The prosoma thymus peptide 1 derivant modifying carbowax can be produced by the means of chemosynthesis and restructuring DNA.

Description

technical field [0001] The present invention relates to the preparation and application of long-acting thymosin 1 derivatives. It specifically relates to polyethylene glycol-modified thymosin 1 derivatives. technical background [0002] The thymus is an important immune organ in the body and plays an important role in the development of the lymphatic system and maintaining the normal function of the immune system. Especially, it has special significance in anti-infection, anti-tumor, autoimmune diseases and organ transplantation. As the body ages, the thymus gradually shrinks and degenerates, and the incidence of tumors, infections, and immune diseases gradually increases. In recent years, foreign scholars have purified thymosin into several individual components, and found that the biological activity of thymosin 1 is 10-1000 times higher than that of thymosin mixture. Thymosin 1 belongs to the fifth component of thymosin, which has an immunoregulatory effect. It can ind...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61P37/04C07K17/02
CPCA61K47/48215A61K47/60A61P1/16A61P31/12A61P31/16A61P35/00A61P37/04
Inventor 钟慧娟
Owner JIANGSU HANSOH PHARMA CO LTD
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