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Lipoic-acid-modified nanometer polypeptide carrier and preparation method and application thereof

A kind of lipoic acid and nano technology, which is applied in the field of medicine and achieves the effects of low composition, low cytotoxicity and simple operation

Active Publication Date: 2016-07-06
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] At present, there is no lipoic acid-modified polypeptide that can target the drug-resistant nano-delivery carrier of breast cancer

Method used

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  • Lipoic-acid-modified nanometer polypeptide carrier and preparation method and application thereof
  • Lipoic-acid-modified nanometer polypeptide carrier and preparation method and application thereof
  • Lipoic-acid-modified nanometer polypeptide carrier and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Example 1: Synthesis of lipoic acid-modified 9-peptide

[0063] The 9-peptide amino acid sequence modified by lipoic acid (LA): HisHisHisArgArgArgArgArgArg (His, histidine; Arg, arginine) (SEQ ID NO: 1), LA-HR, was synthesized by Shanghai Jier Biochemical Co., Ltd. by peptide solid-phase synthesis and named LA-H 3 R 6 , the synthetic LA-HR was purified by preparative high-performance liquid chromatography, and its purity reached more than 95%. LA- is lipoic acid, R is arginine, H is histidine, and the amino acids are connected by peptide bonds to form a 9-peptide.

Embodiment 2

[0064] Example 2: Preparation of lipoic acid-modified polypeptide nanocarrier LAHRss

[0065] Dissolve 50 mg of lipoic acid-modified polypeptide LAHR and different amounts of cysteine ​​hydrochloride in 10 ml of methanol, add sodium hydroxide solution to adjust the pH to 7.0, stir and react for 12 hours, and the reaction temperature is 10-30°C. The amount of cysteine ​​is respectively: 2.5%, 5%, 10%, 20%.

[0066] As shown in Table 1, LAHRss with different molecular weights were prepared according to the ratio of LAHR to cysteine. The obtained solution was dialyzed for 12 hours through a dialysis bag with a molecular weight cut-off of 1000. The dialysate was distilled water, and the dialysate was replaced every 4 hours. The obtained dialysis product was lyophilized and stored at -20°C, and the lyophilized carrier could be stored for a long time under reconstitution conditions. The synthesized carrier was subjected to H NMR spectroscopy 1 H-NMR (600M) detection, molecular we...

Embodiment 3

[0071] Example 3: Preparation of LAHRss in pDNA Nanomicelles

[0072] The carrier (LAHRss) and luciferase expression plasmid pEGFP (Shanghai Innovation Biotechnology Co., Ltd.) were dissolved in water to prepare aqueous solutions, and the nitrogen-phosphorus ratio (N / P) was 2.5, 5, 10, 20, 40, 80, respectively. The nanocomposites were prepared and vortexed for 10 seconds, then left to stand for 30 minutes to obtain nanomicelles. The average particle size of nano micelles is related to N / P. When N / P=40, the best particle size is obtained, and the particle size is between 80-300. For details, see figure 2 . The Zeta potential of nanomicelles increases with the increase of N / P, and is stable at 0-30mV when N / P is greater than 2.5, see image 3 .

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Abstract

The invention relates to the field of medical technologies, in particular to a lipoic-acid-modified nanometer polypeptide carrier and a preparation method and application thereof.The lipoic-acid-modified nanometer polypeptide carrier is composed of arginine, histidine, lipoic acid and cysteine.A disulfide bond contained in lipoic acid is adopted for cross-linking, a formed polypeptide polymer can be rapidly degraded in cells and will not accumulate in the cells, and arginine and cysteine in polypeptide are in-vivo amino acid and are free of toxic and side effects to the human body.A CCK-8 cell proliferation test shows that the prepared nanometer carrier has low cell toxicity and meanwhile has good capacity of co-delivery of a gene and chemotherapy drugs; the nanometer carrier can specifically enhance the sensitivity of drug-resistant cells to the chemotherapy drugs in breast cancer drug-resistant treatment and promote apoptosis of breast cancer cells, and therefore becomes a targeted, efficient and low-toxicity nanoscale delivery system in breast cancer drug-resistant treatment.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to a lipoic acid-modified nano-polypeptide carrier and a preparation method and application thereof. Background technique: [0002] Breast cancer is one of the malignant tumors that threaten women's health. At present, surgery is still the main treatment for breast cancer, combined with radiation therapy and chemotherapeutic drug therapy (chemotherapy for short). Chemotherapy plays a key role in the treatment of breast cancer. , but in clinical application, breast cancer cells often have multidrug resistance (multidrug resistance, MDR), which leads to the failure of chemotherapy. Therefore, reversing breast cancer drug resistance has become a key technology. The introduction of nanotechnology not only realizes the targeted treatment of tumors, reduces the toxic and side effects, but also effectively realizes the reversal of drug-resistant breast cancer cells. Therefore, it is of...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K48/00A61K45/06A61K31/704A61K31/337A61K31/675A61P35/00
CPCA61K31/337A61K31/675A61K31/704A61K45/06A61K48/0041
Inventor 高申胡楚玲顾芬芬姚翀高原宫春爱夏清明张丽娟田泾曹伟李佳飞
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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