Acid-responsive anticancer peptide and preparation method thereof

An anti-cancer peptide and responsive technology, which is applied in the field of artificially synthesized anti-cancer peptides and their acid-responsive nanoparticles, can solve the problems of low bioavailability, hindering anti-cancer peptides, and low selectivity, and achieve shielding of cytotoxicity, Improved stability, good targeting effects

Active Publication Date: 2022-03-25
SUN YAT SEN MEMORIAL HOSPITAL SUN YAT SEN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Low selectivity, normal tissue cytotoxicity, hemolytic toxicity, instability in serum, low bioavailability, and the need for intratumoral administration are still the main bottlenecks that hinder the application of anticancer peptides in tumor therapy

Method used

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  • Acid-responsive anticancer peptide and preparation method thereof
  • Acid-responsive anticancer peptide and preparation method thereof
  • Acid-responsive anticancer peptide and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0048] The present invention will be further described below in conjunction with the examples, but not as a limitation to the protection scope of the present invention.

[0049] Description of name and corresponding abbreviation or code:

[0050] The anticancer peptide of this example is called Peptide for short, and the code name in the synthesis route is C12-PButLG-CA;

[0051] The acid-responsive anticancer peptide nanoparticles of this embodiment are referred to as R Peptide, the code name in the synthetic route is: (PEO

[0052] -PPO-CDM) 2 -C12-PButLG-CA;

[0053] The non-acid-responsive anticancer peptide nanoparticles of this embodiment are referred to as NR Peptide, the code name in the synthetic route is: (PEO-

[0054] PPO-SA) 2 -C12-PButLG-CA;

[0055] 1. Peptides, R Peptide and NR Preparation of Peptides

[0056] 1.1 Synthesis and characterization of Peptide

[0057] The synthesis circuit diagram of Peptide is as follows figure 1 Shown, concrete synthe...

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Abstract

The invention discloses an artificially synthesized anticancer peptide and an acid responsive nanoparticle precursor thereof. The nanoparticle is formed by connecting an anti-cancer peptide and an amphiphilic monomethyl polyethylene glycol-polypropylene glycol polymer through an acid-responsive chemical bond. Tests prove that the anti-cancer peptide can kill tumor cells through membrane rupture activity, and has the advantages of excellent broad-spectrum anti-cancer activity and drug resistance. The nanoparticles are selectively sensitive to a tumor subacid environment, can completely release anti-cancer peptides, and play an active role of a targeted tumor cell line. And the polypeptide has the advantages of hemolysis resistance, high plasma stability, low in-vivo systemic toxicity, systemic drug delivery and the like. The nanoparticle has a remarkable inhibition effect on various tumor cells including triple negative breast cancer, and particularly has a relatively good clinical application potential on drug-resistant triple negative breast cancer.

Description

technical field [0001] The invention relates to the technical field of biopharmaceuticals, in particular to an artificially synthesized anticancer peptide and acid-responsive nanoparticles thereof. Background technique [0002] Drug resistance and poor selectivity have always been problems to be solved urgently for chemotherapeutic anticancer drugs. Taking breast cancer subtype triple negative breast cancer (Triple Negative Breast Cancer, TNBC) as an example, due to the low expression or deletion of estrogen receptor, progesterone receptor and human epidermal growth factor (HER2) receptor, endocrine and anti-HER2 Targeted monoclonal antibody therapy is ineffective for TNBC, and chemotherapy is still the standard treatment for TNBC. However, since TNBC has a high degree of tumor heterogeneity, and the expression of drug efflux pumps such as ATP-binding cassette transporters is significantly excessive, drug resistance is prone to occur, resulting in decreased chemotherapy sen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K38/08A61K47/60A61K47/69A61P35/00B82Y5/00B82Y40/00
CPCC07K7/06B82Y5/00B82Y40/00A61K38/08A61K47/60A61K47/6935A61P35/00
Inventor 姚燕丹鲍燕熊梦华钟翠玉李杰刘穗萍
Owner SUN YAT SEN MEMORIAL HOSPITAL SUN YAT SEN UNIV
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