Amphiphilic polypeptide P13 and preparation method thereof

An amphiphilic, P13 technology, applied in the field of peptides, can solve problems such as reducing drug utilization, achieve high drug utilization, and improve the effect of acid-base buffering capacity

Active Publication Date: 2018-11-06
ANHUI UNIVERSITY OF TECHNOLOGY AND SCIENCE
View PDF4 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the amphiphilic polypeptide disclosed in this patent is easily digested by lysosomes in the body, which reduces the utilization rate of the drug

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Amphiphilic polypeptide P13 and preparation method thereof
  • Amphiphilic polypeptide P13 and preparation method thereof
  • Amphiphilic polypeptide P13 and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0054] The present invention also provides a method for preparing the above-mentioned amphiphilic polypeptide P13, comprising:

[0055] 1) Soak the matrix resin in the solvent, then add N, N-diisopropylethylamine (DIEA), aspartic acid Fmoc-Asp (OtBu)-OH to carry out contact reaction, then wash, head, remove protection, and finally washing until ninhydrin is detected as blue to obtain a secondary resin;

[0056] 2) The secondary resin is subjected to multiple modification treatments with various compounds in turn to obtain a tertiary resin; each modification process is as follows: the secondary resin and the compound are mixed in 1-hydroxybenzotriazole (HoBt), benzotriazole-N, N, N', N'-tetramethyluronium hexafluorophosphate (HBTU) in the presence of contact reaction, and then through deprotection, washing until ninhydrin is detected as Blue to obtain a tertiary resin; the compounds in a single modification process are independently Fmoc-Gly-OH, Fmoc-Arg(pbf)-OH, Fmoc-His(OtBu...

Embodiment 1

[0076] 1) Soak 0.25g of 2-chlorotrityl chloride resin in 5mL, 15°C DCM for 10min, then add 0.3mLDIEA, 0.08gFmoc-Asp(OtBu)-OH, react at 15°C for 30min, and then wash;

[0077] 2) Add 5mL DCM, 0.3mL methanol and 0.3mL DIEA to the reaction system for capping treatment, then add piperidine for deprotection, and then wash the reaction system until ninhydrin is detected as blue;

[0078] 3) Add 0.2g Fmoc-Gly-OH, 0.2g HoBt, and 0.2g HBTU to the reaction system and contact with it for 30 minutes at 15°C. After washing, add piperidine for deprotection, and wash the reaction system again until it passes ninhydrin detection It is blue; sequentially add 0.5g Fmoc-Arg(pbf)-OH, 0.5g Fmoc-His(OtBu)-OH, 0.2g Fmoc-Gly-OH, 0.2g Fmoc-Ala-OH and react at 15°C for 30min;

[0079] 4) Wash with DMF, DCM and methanol in sequence, then dry at 30°C for 1 h to powder, add 10 mL of cutting solution A (the volume ratio of TFA, TIS, EDT and water is 95:1.5:1.5:2) to cut the resin and Peptide chain, add ic...

Embodiment 2

[0082] 1) Soak 0.25g of 2-chlorotrityl chloride resin in 5mL, 20°C DCM for 20min, then add 0.5mLDIEA, 0.2gFmoc-Asp(OtBu)-OH, react at 20°C for 60min, and then wash;

[0083] 2) Add 10mL DCM, 0.5mL methanol and 0.5mL DIEA to the reaction system for capping treatment, then add piperidine for deprotection, and then wash the reaction system until ninhydrin is detected as blue;

[0084] 3) Add 0.4g Fmoc-Gly-OH, 0.3g HoBt, and 0.3g HBTU into the reaction system and contact with the reaction for 60min at 20°C. After washing, add piperidine for deprotection, and wash the reaction system again until it is detected by ninhydrin It is blue; sequentially add 0.6g Fmoc-Arg(pbf)-OH, 0.6g Fmoc-His(OtBu)-OH, 0.4g Fmoc-Gly-OH, 0.4g Fmoc-Ala-OH and react at 20°C for 60min;

[0085] 4) Wash with DMF, DCM, and methanol in sequence, then dry at 30°C for 1 h to powder, add 12 mL of cutting solution A (the volume ratio of TFA, TIS, EDT, and water is 95:2:2:1) to cut the resin and Peptide chain, add...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention discloses amphiphilic polypeptide P13 and a preparation method thereof and belongs to the field of polypeptide. The amphiphilic polypeptide disclosed by the invention has amino acid sequences with hydrophilic segments DGRHHH and lyophobic segments, the lyophobic segments consist of L and A amino acids, and specifically, the amino acid sequences are DGRHHHLLLAAAA. The invention further provides a method for preparing the amphiphilic polypeptide P13. The method is a solid phase synthesis method. The amphiphilic polypeptide P13 disclosed by the invention has active targeting recognition upon cancer cells, meanwhile has a sponge proton effect, that is, an escape capability, and has great values in development and application of drug delivery carriers.

Description

technical field [0001] The invention belongs to the field of polypeptides, and more specifically relates to an amphipathic polypeptide P13 and a preparation method thereof. The amphiphilic polypeptide has active target recognition and proton sponge effect on cancer cells. Background technique [0002] In recent years, the incidence of malignant tumors has continued to rise for many years, and it has become a public health problem and even a social problem that must be attached great importance to. There are more than 10 million new cancer cases in the world every year, and the death toll exceeds 7 million. In my country, there are currently 3.5 million new cancer patients every year, and the annual cancer death toll reaches 2.5 million. Accompanied by aging population, environmental problems, and unhealthy life The incidence of cancer is increasing at an average annual rate of 3% to 5%. In some cities, cancer has surpassed cardiovascular disease and has become the "number on...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08C07K1/36C07K1/34C07K1/16C07K1/06C07K1/04
CPCC07K7/08
Inventor 葛飞乔茜茜晋珍珍朱龙宝陶玉贵
Owner ANHUI UNIVERSITY OF TECHNOLOGY AND SCIENCE
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap