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Novel salmon calcitonin analogue and its preparation method and use

A technology of salmon calcitonin and analogues, which is applied to the preparation method of peptides, calcitonin, chemical instruments and methods, etc., can solve the problems of poor metabolic stability of natural calcitonin, inconvenient treatment and pain of patients, and achieve chemical Increased stability, increased degree of alpha helix, reduced potential for degradation

Active Publication Date: 2016-08-24
CHINESE PEPTIDE CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Natural calcitonin has poor metabolic stability in the body. After intramuscular or subcutaneous injection, salmon calcitonin has a half-life of 70 to 90 minutes and requires daily injections, which brings inconvenience and pain to the treatment of patients.

Method used

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  • Novel salmon calcitonin analogue and its preparation method and use
  • Novel salmon calcitonin analogue and its preparation method and use
  • Novel salmon calcitonin analogue and its preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Preparation of salmon calcitonin analog

[0036] According to the conventional method of solid-phase synthesis, the amino acids with protective groups are attached to the resin one by one, and then the catalyst is used to catalyze the cyclization, then the protective group is removed and the polypeptide is cut from the resin to prepare the preferred salmon calcitonin of the following formula analog:

[0037]

[0038] 1. Solid phase synthesis

[0039] Choose 0.402g Fmoc-Rinke Amide MBHA resin (degree of substitution: 0.373mmol / g) to prepare, soak the resin in DMF at room temperature for 60 minutes, arrange the amino acids with Fmoc protection in sequence in the synthesizer for activation and connection, and obtain figure 1 The product of compound 2 in the compound, the structure is:

[0040]

[0041] 2. Catalytic cyclization

[0042] The compound obtained in the above steps was washed twice with DCM (20ml) and DCE (20ml) respectively, then soaked with DCE (8ml) for 30mi...

Embodiment 2

[0048] Example 2 Salmon calcitonin analog (prepared by the method of Example 1) to reduce blood calcium efficacy experiment

[0049] Thirty healthy Wistar rats (females), weighing 200±15g, were fasted for 16 hours before the experiment, and were randomly divided into 3 groups, the blank group, the salmon calcitonin group and the salmon calcitonin analog group, each with 10 rats. The administration was administered by subcutaneous injection into the abdomen, the blank control group was injected with physiological saline, and the administration dose of the salmon calcitonin group and the salmon calcitonin analog group was 0.05 μg / kg. The blood was taken from the orbit before the administration and 1, 2, 4, 8, and 12 hours after the administration, and the blood calcium value in the sample was measured with the o-cresolphthalein complexing agent. according to:

[0050] (Blank group blood calcium value-administration group blood calcium value) / Blank group blood calcium value calculati...

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Abstract

The invention relates to a novel salmon calcitonin analogue and a preparation method thereof. Compared with a natural salmon calcitonin, the chemical stability of a compound provided by the invention is improved and the pharmacological activity of the natural salmon calcitonin is kept. The salmon calcitonin analogue provided by the invention has the following chemical structure.

Description

Technical field [0001] The present invention relates to analogs of salmon calcitonin and a preparation method thereof. Background technique [0002] Natural calcitonin is a biologically active polypeptide secreted by mammalian parathyroid cells or the hindgills of vertebrates, and is the main regulator of calcium metabolism in organisms. Among them, salmon calcitonin (Calcitonin (Salmon)) has a significant curative effect and has been widely used clinically as a preventive drug for the treatment of metabolic bone diseases such as osteoporosis. [0003] Natural calcitonin has an amidated carboxyl terminal, and there is an intramolecular disulfide bond between the cysteine ​​residues at position 1 and 7. The chemical structure of natural salmon calcitonin is: [0004] [0005] Natural calcitonin has poor metabolic stability in the body. After intramuscular or subcutaneous injection of salmon calcitonin, the half-life is 70 to 90 minutes and requires daily injections, which brings inc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/585C07K1/107A61K38/23A61P19/02A61P19/08A61P19/10A61P5/18
Inventor 李湘
Owner CHINESE PEPTIDE CO
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