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Polypeptide derivatives, nanofibers and their applications

A technology of nanofibers and peptide derivatives, applied in the direction of nanotechnology, nanotechnology, nanotechnology for materials and surface science, etc., can solve the problems of complex synthesis process, unfavorable long-term storage, poor water solubility, etc., and achieve simple preparation process , Improve organizational retention rate, low cost effect

Active Publication Date: 2021-04-06
克尔维特(福州)医疗科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its polypeptide chain length is 16 peptides, the synthesis process is more complicated and the yield is lower; the most important thing is that the hydrogel formed by its self-assembly is a white opaque gel, which has poor water solubility, and a small amount of precipitation occurs after 3 to 5 days. good for long term storage

Method used

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  • Polypeptide derivatives, nanofibers and their applications
  • Polypeptide derivatives, nanofibers and their applications
  • Polypeptide derivatives, nanofibers and their applications

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preparation example Construction

[0060] The polypeptide derivatives are synthesized by the known FMOC-short peptide solid-phase synthesis method. Specifically, the preparation method of the polypeptide derivative includes the following steps:

[0061] (1) The C-terminal of the Fmoc-amino acid is bound to the resin;

[0062] (2) removal of Fmoc protecting group, washing;

[0063] (3) The C-terminal of the next Fmoc-amino acid is coupled to the N-terminal of the amino acid or polypeptide on the resin, and washed;

[0064] (4) Repeat steps (2) to (3) until the last amino acid coupling is completed, remove the Fmoc protecting group, and wash;

[0065] (5) X-OH is coupled and washed with the N-terminal of the polypeptide on the resin;

[0066] (6) The polypeptide derivative is excised from the resin to obtain a crude product;

[0067] (7) Use high performance liquid chromatography to purify the crude product.

[0068] According to the second aspect of the present invention, the present invention provides nano...

preparation Embodiment 1

[0094] Synthesis and Preparation of Peptide Derivative Nap-FFGSSSR and Its Nanofibers

[0095] (1) Solid phase synthesis of Nap-FFGSSSR

[0096] Specific steps are as follows:

[0097] 1) Weigh 0.5mmol 2-Cl-Trt resin in a solid-phase synthesizer, add 10mL of anhydrous dichloromethane (hereinafter referred to as DCM), place on a shaker and shake for 5min to fully swell the 2-Cl-Trt resin ;

[0098] 2) Remove the DCM from the solid-phase synthesizer equipped with 2-Cl-Trt resin with ear washing ball;

[0099] 3) Dissolve 0.75 mmol of Fmoc-Arg in 10 mL of anhydrous DCM, add 0.75 mmol of DIPEA, then transfer to the above-mentioned solid-phase synthesizer, add 0.75 mmol of DIPEA, and react at room temperature for 1 h;

[0100] 4) Sealing: Remove the reaction liquid in the solid-phase synthesizer with ear washing balls, then wash with 10 mL of anhydrous DCM, 1 min each time, and wash 5 times in total. Add the prepared volume ratio of anhydrous DCM: DIPEA: methanol = 17:1:2 solut...

Embodiment 1

[0116] Activity Test of Hydrogel of Peptide Derivative Nap-FFGSSSR at the Cell Level

[0117] (1) Promoting the proliferation of mouse myoblasts (C2C12)

[0118] 1) Raise the temperature of the water bath to 37°C in advance, put the medium, serum, etc. into the water bath to preheat, and at the same time turn on the ultra-clean bench UV lamp for half an hour;

[0119] 2) Take out the frozen mouse myoblast C2C12 cells from the liquid nitrogen tank, quickly place them in a water bath at 37°C to thaw the cells, and then quickly transfer them to an ultra-clean bench for the following operations: transfer the cell-containing solution with a pipette Carefully transfer the liquid container to a centrifuge tube containing the medium, centrifuge for 3 minutes, remove the supernatant, resuspend with DMEM medium containing 10% fetal bovine serum, transfer to a petri dish, and then place it in a 37°C incubator to cultivate;

[0120] 3) Observe the state of the cells the next day. After ...

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Abstract

The present invention provides a polypeptide derivative, nanofiber and application thereof. The polypeptide derivative can effectively simulate the biological activity of IGF-1 protein as a substitute for IGF-1 protein, and the production process is relatively simple and the yield is relatively high. High, good storage stability. The sequence of the polypeptide derivative is X-Phe-Phe-Gly-Ser-Ser-Ser-Arg, wherein the end group X is Nap or Npx, Phe is in L configuration or D configuration at the same time, and the rest are in L configuration type. The water mixture of the polypeptide derivative is heated and cooled to form nanofibers. The polypeptide derivative can be combined with IGF-1 protein receptor, and is used for treating muscle atrophy and atherosclerosis.

Description

technical field [0001] The invention relates to a polypeptide derivative, nanofiber and application thereof. Background technique [0002] Insulin-like growth factor I (IGF-1) is a growth hormone that plays a vital role in human development, growth, metabolism and homeostasis, and has been extensively studied clinically and in the field of life science research. [0003] Atherosclerosis is an important cause of cardiovascular diseases such as myocardial infarction, coronary heart disease, hypertension, and stroke, and has become one of the main diseases that endanger human health. According to the latest statistics from the World Health Organization (WHO), the number of deaths from cardiovascular and cerebrovascular diseases accounts for 48% of the total number of non-communicable diseases, which is more than twice the number of deaths from cancer. Low circulating levels of IGF-1 have been associated with increased atherosclerotic complications in most observational studies...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K14/65C07K1/16C07K1/04B82Y30/00A61K38/08A61K9/00A61K9/06A61P21/00A61P9/10
CPCA61K9/0092A61K9/06A61K38/08A61P9/10A61P21/00B82Y30/00C07K14/65
Inventor 杨志谋王玲商宇娜
Owner 克尔维特(福州)医疗科技有限公司