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Nucleic acid aptamer derivative and application thereof in preparation of medicament carrier

A technology of nucleic acid aptamers and derivatives, applied in biochemical equipment and methods, microbial measurement/testing, drug combination, etc., can solve problems such as difficult chemical modification and transformation, easy to cause immune response, and limit wide application, etc., to achieve Reduced toxicity, no immune activity and toxicity, high application value effect

Active Publication Date: 2011-01-12
谭蔚泓
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the antibodies used for targeted delivery of drugs are derived from animals or fused monoclonal cells, which need to be produced through biological processes. The preparation is cumbersome, high cost, poor stability, and difficult to chemically modify and transform; at the same time, antibodies also have large molecular weight, tissue Poor penetrating power, easy to cause immune reaction and other problems limit its wide application

Method used

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  • Nucleic acid aptamer derivative and application thereof in preparation of medicament carrier
  • Nucleic acid aptamer derivative and application thereof in preparation of medicament carrier
  • Nucleic acid aptamer derivative and application thereof in preparation of medicament carrier

Examples

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Effect test

Embodiment 1

[0041] 1. Preparation of nucleic acid aptamers and their derivatives

[0042] Three kinds of nucleic acid aptamer derivatives were artificially synthesized, and 1 GC, 29 GCs and 50 GCs were introduced into the 5' end of the nucleic acid aptamer TLS11a respectively. TLS11a-(GC) 1 As shown in sequence 3 of the sequence listing. TLS11a-(GC) 29 As shown in sequence 4 of the sequence listing. TLS11a-(GC) 50 As shown in sequence 5 of the sequence listing.

[0043] Three control nucleic acid aptamer derivatives were artificially synthesized, and 1 GC, 29 GC and 50 GC were introduced into the 5' end of the nucleic acid aptamer TD05, respectively. TD05-(GC) 1 As shown in sequence 6 of the sequence listing. TD05-(GC) 29 As shown in sequence 7 of the sequence listing. TD05-(GC) 50 As shown in sequence 8 of the sequence listing.

[0044] The nucleic acid aptamer TLS11a shown in sequence 1 of the sequence listing and the control nucleic acid aptamer TD05 shown in sequence 2 were...

Embodiment 2

[0053] 1. Aptamer TLS11a and aptamer derivative TLS11a-(GC) 29 preparation of

[0054] In order to embed more doxorubicin, a long GC sequence (composed of 29 GCs connected sequentially) was introduced at the 5' end of the nucleic acid aptamer TLS11a, thereby obtaining a nucleic acid aptamer derivative TLS11a-(GC ) 29 . TLS11a-(GC) 29 As shown in sequence 4 of the sequence listing.

[0055] The nucleic acid aptamer TLS11a shown in sequence 1 of the sequence listing was artificially synthesized. The artificially synthesized nucleic acid aptamer derivative TLS11a-(GC) shown in sequence 4 of the sequence listing 29 .

[0056] 2. Preparation and characterization of nucleic acid aptamer derivative-drug complex

[0057] 1. Preparation of nucleic acid aptamer derivative-drug complex

[0058] In the binding buffer, the nucleic acid aptamer derivative TLS11a-(GC) 29 Mix with doxorubicin at a ratio of 1:25 (molar ratio), and incubate with stirring at room temperature for 3 hours...

Embodiment 3

[0077] Determination of Chemosensitivity of Hepatoma Cell LH86 to Doxorubicin or Aptamer Derivative-Drug Complex Using CellTiter AQueous Single Solution Cell Proliferation Assay Kit (Promega, Madison, WI, USA) was performed. CellTiter AQueous single solution reagent: 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, internal salt; MTS and an electron coupling reagent ( thiophenazine, PES). The details are as follows: 100 μL of liver cancer cells LH86 (about 5×10 4 Cells / mL) were inoculated on 96-well plates (n=3) and grown overnight at 37°C (5% CO 2 , FBS-free DMEM medium), and then add 100 μL of the following DNA strands:

[0078] (1) TLS11a; set four concentration gradients, respectively with TLS11a-(GC) in the nucleic acid aptamer derivative-drug complex in (4) 29 The concentrations were the same, namely 40, 100, 200, 300 nM, respectively.

[0079] (2)TLS11a-(GC) 29 ; Four concentration gradients are set, respectively with TL...

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Abstract

The invention discloses a nucleic acid aptamer derivative and application thereof in preparation of a medicament carrier. The derivative is the single-chain DNA represented by formula (I); a nucleic acid aptamer is represented by the sequence 1 of a sequence list; and n is equal to 1 to 50. The nucleic acid aptamer derivative provided by the invention is liver cancer cell targeted, so that the nucleic acid aptamer derivative can serve as the medicament carrier for targeted administration of liver cancer cells in a human body to specifically kill the liver cancer cells and greatly reduce the toxicity of an anti-cancer medicament to the organism. The nucleic acid aptamer derivative provided by the invention can be chemically synthesized in a large scale and has the advantages of easy connection with medicament molecules, low cost, relatively low molecular weight, no immune activity or toxicity, and good stability. The prepared medicinal composition is stable. The medicinal composition (targeted medicament) provided by the invention has a strong bonding force with the liver cancer cells, can greatly reduce the toxic and side effects during chemical treatment of liver cancer and has very high application value. The formula (I) is: 5'-(CG)n-nucleic acid aptamer-3'.

Description

technical field [0001] The invention relates to nucleic acid aptamer derivatives and their application in the preparation of drug carriers. Background technique [0002] Liver cancer is one of the most prevalent and highly lethal cancers in the world. At present, the effective treatment methods for patients with early liver cancer are mainly surgical resection and liver transplantation. Traditional chemotherapy is not effective for patients with liver cancer, and traditional drugs usually bring fatal side effects to patients due to lack of specificity to liver cancer cells. In order to overcome these problems and improve the selectivity of chemotherapy, it is necessary to develop targeted drugs that are administered specifically in tumor regions. [0003] Tumor cell-targeted drug delivery is an effective way to improve the efficacy of tumor therapy and reduce side effects. Conjugating drugs to tumor cell-specific ligands is the main method of targeted drug delivery. For ...

Claims

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Application Information

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IPC IPC(8): C12N15/115C12Q1/68C12Q1/02A61K47/48A61P35/00A61K31/704A61K47/54
Inventor 谭蔚泓方晓红刘晨
Owner 谭蔚泓
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