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Novel salmon calcitonin analogue and preparation method as well as use thereof

A salmon calcitonin and analog technology, applied in the preparation method of peptide, calcitonin, chemical instruments and methods, etc., can solve the problems of pain, poor metabolic stability of natural calcitonin, inconvenient treatment of patients, etc. Potential effects of increased stability, increased degree of alpha helix, reduced degradation

Active Publication Date: 2013-02-06
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 preparation method as well as use thereof
  • Novel salmon calcitonin analogue and preparation method as well as use thereof
  • Novel salmon calcitonin analogue and preparation method as well as use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Preparation of Salmon Calcitonin Analogs

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

[0037]

[0038] 1. Solid phase synthesis

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

Embodiment 2

[0048] Example 2 The drug effect test of salmon calcitonin analogue (prepared by the method of Example 1) in reducing blood calcium

[0049]Get 30 healthy Wistar rats (female), body weight 200 ± 15g, fasted for 16 hours before the experiment, and randomly divided into 3 groups, 10 each in blank group, salmon calcitonin group and salmon calcitonin analog group. Subcutaneous injection in the abdomen, normal saline injection in the blank control group, 0.05 μg / kg in the salmon calcitonin group and salmon calcitonin analog group. Before the administration and 1, 2, 4, 8, and 12 hours after the administration, blood was collected from the orbit, and the blood calcium value in the sample was determined with o-cresolphthalein complexing agent. according to:

[0050] The calculation method of (blank group blood calcium value-administration group blood calcium value) / blank group blood calcium value calculates the level of reducing blood calcium. The results show (Table 1) that the sa...

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PUM

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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 invention relates to an analog of salmon calcitonin and a preparation method thereof. Background technique [0002] Natural calcitonin is a biologically active polypeptide secreted by the parathyroid cells of mammals or the hind cheeks of vertebrates, and is the main regulator of calcium metabolism in organisms. Among them, Calcitonin (Salmon) has a remarkable curative effect and has been widely used clinically as a preventive drug for treating metabolic bone diseases such as osteoporosis. [0003] Natural calcitonin has an amidated carboxyl terminus with an intramolecular disulfide bond between the cysteine ​​residues at positions 1 and 7. The chemical structure of natural salmon calcitonin is: [0004] [0005] Natural calcitonin has poor metabolic stability in vivo. After intramuscular or subcutaneous injection, salmon calcitonin has a half-life of 70 to 90 minutes and needs daily injection, which brings inconvenience and pain to the treatm...

Claims

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Application Information

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