Bi-functional targeting antineoplastic polypeptide and application thereof

An anti-tumor, dual-function technology, applied in the direction of anti-tumor drugs, peptides, specific peptides, etc., to reduce the economic burden

Inactive Publication Date: 2006-12-27
NANJING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, none of the numerous studies is related to this application, so two polypeptides with different functions can be hybridized through the present invention, and have guiding and long-lasting functions, especially in the treatment of tumors, which will be of great importance. significance

Method used

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  • Bi-functional targeting antineoplastic polypeptide and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: Preparation of polyethylene glycol diacid (PEG-DA) and polyethylene glycol diacid activated ester (PEG-DA-NHS)

[0023] Dissolve 30g of PEG6000 and 2.5g of succinic acid in 100ml of chloroform. After reflux for 48 hours, remove the organic solvent, add ether to precipitate, and dry in vacuum to obtain 27.5g of PEG-DA.

[0024] 15.5g of PEG-DA was dissolved in 50ml of dichloromethane, 1.04g of dicyclohexylcarbodiimide (DCC) and 0.602g of N-hydroxysuccinimide in 50ml of tetrahydrofuran were added, reacted at room temperature for 24 hours, filtered, and the filtrate Add diethyl ether to precipitate and dry in vacuo to obtain 14.9 g of PEG-DA-NHS.

Embodiment 2

[0025] Example 2: Preparation of PMO-1 Half or all of the mice were male. The tumor-bearing mice that had been inoculated with Lewis lung cancer cells were killed, and their ascites was extracted by aseptic operation, and diluted at a ratio of 1:3 to prepare a cell suspension, and 0.2ml of tumor cells were subcutaneously injected into the right forelimb armpit of each experimental mouse. Suspension, no less than 10 tumor cells 5 , 24 hours after tumor implantation, the administration groups were injected intravenously with different doses, with normal saline as the negative control group, CTX as the positive control group, AOP-1 peptide was continuously injected for 10 days, PEG-AOP-1 peptide and PMO-1 Peptides were injected every 3 days for a total of 4 times. The mice were sacrificed 4 days after drug withdrawal, the subcutaneous tumor mass was dissected, the tumor weight was weighed, and the tumor inhibition rate was calculated. The results are shown in Table 2.

[0026]...

Embodiment 6

[0028] Example 6: Determination of PMO-1's resistance to experimental tumor metastasis in vivo

[0029] The mice were randomly divided into 3 groups, 6 in each group, respectively:

[0030] 1) PMO-18μmol / kg group (sample and cell suspension were injected separately in the left and right tail veins)

[0031] 2) PMO-116 μmol / kg (sample and cell suspension are injected separately into the left and right tail veins)

[0032] 3) Normal saline control group

[0033] B16 cells in the logarithmic growth phase were taken, digested and prepared with serum-free medium to make 2.5×10 4 Cell suspension, each mouse in the normal saline group was injected with 0.2ml (5×10 4 cell / only), 1), 2) group animals were first injected with 0.5ml of sample solution into the left tail vein, and then injected with 0.2ml of cell suspension into the right tail vein (5×10 4 cell / only). 28 days after inoculation, the animals were sacrificed by dislocation of the neck, weighed, and the lungs were dissec...

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Abstract

The invention pertains to pharmacy field, comprising connecting two polypeptides of different functions with a carrier molecule of polyethylene glycol(PEG). One polipeptide thereof is a cell adhesive peptide with a seaquence of Glu-Ile-Leu-Asp-Val, and the other polipepetide thereof is an antitumor oligopeptide with a seaquence of Tyr-X-Glu-Pro-Gly-Pro-Y-Ala,in which X is Leu or Ile, and Y is Thr or Ser. The synthesized hybrid molecule is called guiding double functional antitumor polypeptide, possessing a suppression function for tumour cell growth and transfer, and can be used in antitumor pharmacy.

Description

1. Technical field: [0001] The invention belongs to the technical field of polypeptide pharmacy. 2. Background technology: [0002] Although protein and peptide drugs have the advantages of strong specificity and high timeliness, they are quickly cleared in the body, especially small molecule peptides are quickly filtered out through the kidneys, and are rapidly hydrolyzed by numerous proteolytic enzymes in the body, thus Generally, the half-life is very short. Under such circumstances, how to prolong the half-life of these drugs in the body has become a hot spot in the research of protein and peptide drugs in recent years, especially γ-interferon modified with polyethylene glycol (PEG). After becoming a long-acting drug for the treatment of hepatitis C, it has driven a large number of clinically applied protein and peptide drugs to use PEG to obtain long-acting drugs. However, none of the many studies is related to this application, so two polypeptides with different func...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48C07K17/08A61K38/08A61P35/00A61K47/60A61K47/64
Inventor 王新昌王文刚陈钧辉曾名嘉聂永军李俊张冬梅
Owner NANJING UNIV
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