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Heptapeptide prepared from thymopentin and pidotimod, and synthetic method

A synthesis method and product technology, which are applied in the preparation methods of peptides, chemical instruments and methods, peptides, etc., can solve the problems of high price and difficulty in wide-scale promotion and application, and achieve the promotion of specific reactions and non-specific reactions. The effect of immune response, good clinical value

Inactive Publication Date: 2009-10-14
JILIN MINGZHIYUAN BIOTECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although thymosin has a good immune enhancing effect, it is difficult to be widely used in animal husbandry because of its high price.

Method used

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  • Heptapeptide prepared from thymopentin and pidotimod, and synthetic method
  • Heptapeptide prepared from thymopentin and pidotimod, and synthetic method
  • Heptapeptide prepared from thymopentin and pidotimod, and synthetic method

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Embodiment 1

[0035]

[0036] 1NH 2 Preparation of -Arg(Mtr)-Lys(Boc)-Asp(OtBu)-Val-Tyr(tBu)-Resin In the synthesis of Fmoc-Arg(Mtr)-Lys(Boc)-Asp(OtBu)-Val-Tyr(tBu )-Resin, use 2.0ml of pyridine, 2.0ml of acetic anhydride to react with nitrogen bubbling at room temperature for 2hr to block the unreacted amino group on Lys. Chloromethane was washed three times each (25ml / time), then 40ml of 50% piperidine / DMF solution was used to remove the Fmoc protecting group, the reaction was carried out under nitrogen bubbling for 1hr at room temperature, dried by suction, washed with methanol, N,N-dimethylmethane Amide and dichloromethane each wash the resin three times (25ml / time), take a small amount of resin in a test tube, add a small amount of ninhydrin / potassium cyanide / phenol mixed solution to qualitatively detect whether Fmoc is completely removed, and heat it in a boiling water bath for 2min, as the solution The color is dark blue-purple (opaque), which means that the removal of Fmoc is mo...

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Abstract

A heptapeptide, a product of thymopentin and pidotimod, and a synthesis method thereof, belong to the technical field of chemical pharmacy, and the synthesis method is as follows: connecting thymopentin and pidotimod through an amide bond to synthesize heptapeptide through a solid-phase synthesis method. peptide. The beneficial effect is that: pidotimod is an artificially synthesized high-purity dipeptide, which can not only promote non-specific immune response, but also promote specific response. It is a multiphase broad-spectrum immune booster. The carboxyl group of pidotimod and the amino group of thymopentin arginine form an amide bond to connect the two together to form a new compound, because thymopentin starts from the amino terminal of arginine in the metabolic process Therefore, after connecting pidotimod, it is equivalent to protecting the amino terminus, and changing the traditional thymopentin dosage form will have good clinical value.

Description

technical field [0001] The invention belongs to the technical field of chemical pharmacy. Background technique [0002] 1. Overview of Thymopentin [0003] The synthetic thymopentin (TP5 for short) is a fragment of amino acid residues at positions 32-36 of thymopoietin, but it has all the same physiological functions and pharmacological effects as "thymopoietin". Novel immunomodulators with modulating effects. It mainly induces T cells and binds to T cell-specific receptors to increase the level of intracellular cAMP, thereby inducing a series of intracellular responses to regulate immune function. It also has a good anti-aging effect, which mainly works by enhancing the activity of superoxide dismutase in serum. This product is used for the treatment of tumors, immunocompromised and autoimmune diseases. [0004] 1) Pharmacological effects of thymopentin [0005] TP5 can normalize the imbalanced immune function of the body and promote the growth and differentiation of t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/06C07K1/04
Inventor 王恩思梁涌涛梁铁王明哲柳忠辉延向前
Owner JILIN MINGZHIYUAN BIOTECH
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