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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., achieve low toxicity and side effects, and increase specificity. resistance, to avoid the effect of accumulation

Inactive Publication Date: 2010-10-27
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] The preparation of embodiment 1 polypeptide-cisplatin conjugate

[0046] Add 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 into a 25 ml round bottom flask. 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 subchloride was added, and the solution was lyophilized to obtain the product.

Embodiment 2

[0047] Example 2 Anti-lung cancer pharmacodynamics study of polypeptide-cisplatin conjugates in vivo

[0048] 1 Materials and methods

[0049]1.1 cells

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

[0051] 1.2 Experimental animals

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

[0053] 1.3 Main Reagents and Drugs

[0054] High-glucose DMEM medium was purchased from Gibco; imported fetal bovine serum was purchased from Hyclone; test drug: H001, homemade injection; positive control drug: cisplatin, produced by Bayer, Germany, batch...

Embodiment 3

[0104] Example 3 Experimental Study on the Pharmacodynamics of Polypeptide-Cisplatin Conjugates Against Colon Cancer in Vitro

[0105] 1 Materials and methods

[0106] 1.1 Cell lines

[0107] The SW1116 human colon cancer cell line was provided by the Shanghai Cell Institute of the Chinese Academy of Sciences.

[0108] 1.3 Main Reagents and Drugs

[0109] High-glucose DMEM medium was purchased from Gibco; imported fetal bovine serum was purchased from Hyclone; test drug: H001, homemade 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 and 5% CO 2 Cultured in a constant temperature incubator, the cells grow as a single layer of adherent cells. When the adherent cells reach 80%-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 noantigenicity, 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 its preparation method and application. Background technique [0002] Cisplatin, whose English name is Cisplatin, is the first metal complex with anticancer activity first discovered in 1965 by American scientist B. Rosenborg et al. In 1965, he accidentally discovered the fact that the "inert platinum electrode" can cause the mycelial growth of bacteria, thus launching the research on the anticancer properties of cis-dichlorodiplatinum. Cisplatin is a heavy metal complex in which divalent platinum is combined with two chlorine atoms and two ammonia molecules, similar to a bifunctional alkylating agent. Studies have found that the main action site of cisplatin is in 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 concentrati...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/06C07K1/04A61K47/48A61K33/24A61P35/00A61K47/64
Inventor 臧林泉
Owner 臧林泉
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