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Peptide - cisplatin conjugate and preparation method and application thereof

A technology for the synthesis of conjugates and solid-phase peptides, which is applied in the preparation methods of peptides, chemical instruments and methods, peptides, etc., can solve the problems of human immune response, allergic symptoms, small molecular weight, etc. resistance, to avoid the effect of accumulation

Inactive Publication Date: 2013-02-13
臧林泉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, because of its large molecular weight, cisplatin drugs are likely to cause immune reactions in the human body and produce allergic symptoms. Therefore, the cisplatin complexes for preparing anti-tumor drugs should also have the feature of relatively small molecular weight.

Method used

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  • Peptide - cisplatin conjugate and preparation method and application thereof
  • Peptide - cisplatin conjugate and preparation method and application thereof
  • Peptide - cisplatin conjugate and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 Preparation of polypeptide-cisplatin conjugate

[0046] In a 25 ml round bottom flask were added 10 ml of DMF, 25 mg (0.017 mol) of LLADTTHHRPWT, 3.5 mg (0.019 mmol) of 1,2-dibromoethane and 15 mg of anhydrous sodium carbonate. Stir at room temperature for 24 hours. 10 mg (0.028 mol) of bis(2-phthalimide)ethylamine was added, and stirring was continued for 24 hours. 1 ml of 80% aqueous hydrazine solution was added, and stirring was continued for 3 days. Add 10 ml of 70% acetone solution and filter. The precipitate was washed with 70% acetone solution. The precipitate was dissolved in 3 mL of water, 4.5 mg (0.017 mmol) of platinum chloride was added, and the solution was lyophilized to obtain the product.

Embodiment 2

[0047] Example 2 In vivo anti-lung cancer pharmacodynamics study of polypeptide-cisplatin conjugate

[0048] 1 Materials and methods

[0049]1.1 Cells

[0050] The NCI-H1299 human lung cancer cell line was provided by the Shanghai Institute of Cell Research, Chinese Academy of Sciences.

[0051] 1.2 Experimental animals

[0052] SPF grade healthy male Balb-c nude mice, 5 to 6 weeks old, weighing 16 to 20 g, were provided by the Guangdong Provincial Medical Laboratory Animal Center, certificate number: SCXK (Guangdong) 2008-0002. In the IVC system of the New Drug Screening and Pharmacodynamic Evaluation Center of the College of Pharmacy, Guangdong University of Pharmacy, the temperature was 25°C, and the humidity was 70-80%.

[0053] 1.3 Main reagents and drugs

[0054] High-glucose DMEM medium was purchased from Gibco Company; imported fetal bovine serum was purchased from Hyclone Company; test drug: H001, self-made for injection; positive control drug: cisplatin, produced...

Embodiment 3

[0104] Example 3 Experimental study on pharmacodynamics of polypeptide-cisplatin conjugate against colon cancer in vitro

[0105] 1 Materials and methods

[0106] 1.1 Cell line

[0107] SW1116 human colon cancer cell line, provided by Shanghai Institute of Cell Research, Chinese Academy of Sciences.

[0108] 1.3 Main reagents and drugs

[0109] High-glucose DMEM medium was purchased from Gibco Company; imported fetal bovine serum was purchased from Hyclone Company; test drug: H001, self-made for injection; positive control drug: cisplatin, produced by Bayer, Germany, batch number: BXF 23E3.

[0110] 1.4 Cell culture and passage

[0111] Human colon cancer cells SW1116 were cultured in high-glucose DMEM medium containing 10% fetal bovine serum at 37°C, 5% CO 2 Cultured in a constant temperature incubator, the cells grow in a single layer adherent, and when the adherent cells reach 80% to 90% confluence, they are digested and passaged with 0.25% trypsin containing 0.01% EDTA...

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Abstract

The invention discloses a peptide - cisplatin conjugate which is prepared by taking a peptide containing 12 amino acids as a carrier and coupling the pipetide with anticancer drug cisplatin, and the invention makes initial research on the pharmacological properties of the peptide - cisplatin conjugate. Cisplatin is widely applied to traditional cancer treatment, but the advantages of great toxic and side effect and the like thereof restrict the application thereof in the treatment. Therefore, to reduce the toxic and side effect of cisplatin is the key to improve the cisplatin medicine. The peptide - cisplatin conjugate obtained by the coupling of peptide and the cisplatin through chemical reaction has small molecular weight when being used for preparing anti-tumor disease medicine, has no antigenicity, does not cause allergic reaction, helps the medicine to display tumor targeting property, takes envoplakin, CD63 and other antigen as the targets, kills tumors with high efficiency, promotes the apoptosis of tumor cells and reduces the toxic and side effect.

Description

technical field [0001] The invention relates to the field of preparation of anticancer drugs, in particular to a polypeptide-cisplatin conjugate and a preparation method and application thereof. Background technique [0002] Cisplatin, the English name of Cisplatin, is the first metal complex with anticancer activity first discovered in 1965 by American scientist B. Rosenborg et al. His accidental discovery in 1965 of the fact that "inert platinum electrodes" can cause bacterial hyphal growth led to research into the anticancer properties of cis-dichlorodiplatinum. Cisplatin is a heavy metal complex with two chlorine atoms and two ammonia molecules combined with divalent platinum in the center, similar to a bifunctional alkylating agent. Studies have found that the main action site of cisplatin is the purine and pyrimidine bases of DNA, which can inhibit the DNA replication process of cancer cells and damage the structure of the cell membrane. High concentrations of cisplat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K7/08C07K1/06C07K1/04A61K47/48A61K33/24A61P35/00A61K47/64
Inventor 臧林泉
Owner 臧林泉
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