Application of rutin oligomer in preparation of tumor targeting product and rutin oligomer-bortezomib tumor targeting drug delivery system

A tumor-targeting, bortezomib technology, applied in the field of bioengineering, achieves the effects of mild conditions, specific accumulation, and simple preparation process

Pending Publication Date: 2022-07-26
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there have been few reports on the tumor targeting function of oligorutin

Method used

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  • Application of rutin oligomer in preparation of tumor targeting product and rutin oligomer-bortezomib tumor targeting drug delivery system
  • Application of rutin oligomer in preparation of tumor targeting product and rutin oligomer-bortezomib tumor targeting drug delivery system
  • Application of rutin oligomer in preparation of tumor targeting product and rutin oligomer-bortezomib tumor targeting drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: Enzymatic synthesis of oligorutin

[0047] Weigh rutin and suspend it in 39mL of double-distilled water, dissolve laccase in 1mL of PBS buffer, add the laccase solution to the above rutin suspension, the final concentration of rutin is 0.005g / mL, laccase The final concentration of acetonitrile was 0.2U / mL, and the reaction was stirred at 200rpm for 24h at room temperature. After the reaction, a reaction solution was obtained. In order to remove the laccase in the reaction solution, 120mL of acetonitrile was added, and centrifuged at 12,000rpm for 30min to obtain the supernatant, and the volume was reduced by rotary evaporation. , using a 3kDa ultrafiltration tube and deionized water at 7500rpm for ultrafiltration and centrifugation for 15min, ultrafiltration 3 times to remove small molecular oligomer rutin, and obtain oligomer rutin by freeze-drying.

[0048] The mass of the obtained oligomer rutin accounts for the percentage of the input rutin mass, which is...

Embodiment 2

[0052] Example 2: Preparation of oligomeric rutin-bortezomib tumor-targeted drug delivery system

[0053] The oligomeric rutin prepared in Example 1 was added to the Tris-HCl buffer with a concentration of 10 mM and mixed to make an oligomeric rutin solution with a concentration of 1 mg / mL; bortezomib was dissolved in DMSO to prepare a concentration of 1 mg / mL. is 30 mg / mL bortezomib mother solution; the bortezomib mother liquid is added to the oligomer rutin solution, the mass ratio of oligomer rutin and bortezomib is 8:1; the reaction is stirred at 25°C and 200 rpm for 16h, and the reaction ends After 3 kDa ultrafiltration tubes and deionized water were used for ultrafiltration and centrifugation at 7500 rpm for 10 min, ultrafiltration was performed for 3 times, the supernatant and the flow-through liquid were collected, and the supernatant was lyophilized to obtain an oligomeric rutin-bortezomib tumor-targeted drug delivery system. .

[0054] The above-mentioned flow-throu...

Embodiment 3

[0058] Example 3: Oligomeric rutin tumor cell targeting and enrichment of intracellular acidic organelles

[0059] Confocal laser was used to observe the distribution of fluorescently labeled oligorutin and fluorescently labeled acidic organelles in various cells. The specific operation steps are as follows:

[0060] (1) Oral epithelial cancer cells KB, prostate cancer cells PC3, liver cancer cells HepG2, and normal liver cells L-O2 were cultured according to routine operations, the cells were cultured to 70% confluence, digested, collected and counted, and the cells were divided into 1 × 10 5 The number of cells / well was seeded in a laser confocal petri dish, placed at 37°C, 5% CO 2 Incubate overnight in incubator;

[0061] (2) Replace the new complete medium, and add 50 μL of oligomer rutin-aminofluorescein (4 mg / mL) prepared in Example 1 into a laser confocal culture dish, and place it in a cell incubator at 37°C, 5% CO 2 Incubate in the dark for 2h;

[0062] (3) Add 2 ...

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Abstract

The invention relates to an application of rutin oligomer in preparation of a tumor targeting product and a rutin oligomer-bortezomib tumor targeting drug delivery system. It is proved for the first time that the rutin oligomer synthesized through an enzymic method has the tumor cell targeting capacity, and the fluorescently-labeled rutin oligomer can selectively enter tumor cells and can be enriched in acidic organelles in the cells. According to the invention, the anti-tumor drug bortezomib is connected to the rutin oligomer through a pH-sensitive covalent bond, so that a water-soluble targeting drug delivery system which has tumor targeting ability and can respond to a tumor microenvironment and pH condition drug release of acidic organelles in cells is constructed; the bortezomib can release drugs under the tumor microenvironment and the pH condition of acidic organelles, and tumors are inhibited through the inhibition effect of bortezomib on tumor cell proteasomes.

Description

technical field [0001] The invention relates to an application of oligomer rutin in the preparation of tumor targeting products and an oligomer rutin-bortezomib tumor targeting drug delivery system, belonging to the technical field of bioengineering. Background technique [0002] Compared with traditional methods such as surgery, radiation therapy, chemotherapy and hormone therapy, tumor targeted therapy has the advantages of improving drug selectivity, reducing toxic side effects, increasing availability and controlling drug release. Natural biomaterials have the advantages of low toxicity, low antigenicity and good biocompatibility as targeted delivery vehicles for drugs. Rutin is a common dietary polyphenol flavonol compound formed by the flavonol quercetin and rutinobiose (α-L-rhamnosyl-1,6-β-D-glucose). Glycosides. Rutin has anti-inflammatory, anti-tumor, immune regulation, antioxidant and antidepressant functions, and has been clinically used for the adjuvant treatme...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K38/05A61P35/00C12P19/00C12Q1/02
CPCA61K47/545A61K38/05A61P35/00C12P19/00G01N33/5011
Inventor 徐莉肖敏洪伟英张赫男王洋
Owner SHANDONG UNIV
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