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Amphiphilic polypeptide DGRGGGAAAA and preparation method thereof, and novel anticancer drug delivery system and preparation method thereof

A delivery system and anti-cancer drug technology, applied in the preparation method of peptides, anti-tumor drugs, drug combinations, etc., can solve the problems of targeted drug delivery technology to be improved, and achieve mild operating conditions, easy access to raw materials, and easy operation steps simple effect

Active Publication Date: 2017-11-21
ANHUI POLYTECHNIC UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Efficient and accurate target recognition technology can target cancer cell receptors and bind drugs to them. However, how to preserve highly effective and active drugs until they can be delivered to cancer cell receptors is a key problem in cancer treatment, and it is also a key issue in drug development. and application bottlenecks
The technology of targeted recognition of cancer cells and the stability technology of active drugs are currently being continuously improved and perfected; however, due to the limitations of these two technologies, the targeted drug delivery technology that combines the two technologies needs improvement

Method used

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  • Amphiphilic polypeptide DGRGGGAAAA and preparation method thereof, and novel anticancer drug delivery system and preparation method thereof
  • Amphiphilic polypeptide DGRGGGAAAA and preparation method thereof, and novel anticancer drug delivery system and preparation method thereof
  • Amphiphilic polypeptide DGRGGGAAAA and preparation method thereof, and novel anticancer drug delivery system and preparation method thereof

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preparation example Construction

[0032] The invention provides a method for preparing the amphiphilic polypeptide DGRGGGAAAA, the preparation method comprising:

[0033] 1) In the presence of a solvent, mix the resin with Fmoc-Asp(Otbu)-OH (fluorenylmethoxycarbonyl-aspartic acid-4-tert-butyl ester), DIEA (N,N-diisopropylethylamine) Perform a contact reaction followed by washing;

[0034] 2) Capping the reaction system, then adding piperidine for deprotection, and then washing until the reaction system is detected as blue by ninhydrin;

[0035] 3) In the presence of a solvent, G (glycine), HoBt (1-hydroxybenzotriazole), and DIC (N,N-diisopropylcarbodiimide) are added to the reaction system for contact reaction, and then Wash until the reaction system is detected as blue by ninhydrin;

[0036] 4) Add R (arginine), G (glycine), and A (alanine) to the reaction system in turn for contact reaction, then add piperidine for deprotection (remove the last Fmoc on A), and finally wash Until the reaction system is det...

Embodiment 1

[0077] (1) Preparation of amphiphilic polypeptide DGRGGGAAAA

[0078] a. Weigh 1g of 2-cl resin (the degree of substitution of resin drug loading is 0.5), soak it in 20mL of DCM at 20°C for 2min, then wash once with DMF and DCM; use 20mL of DCM as solvent, weigh 0.2g of DCM Fmoc-Asp(Otbu)-OH, react with 1mL of DIEA, 1g of 2-cl resin at 20°C for 1.5h, and then wash twice with DMF; use 20mL of DCM+1mL of methanol+1mLDIEA at 20°C for 30min, and use Wash 3 times with DMF; deprotect with 15mL piperidine at 20°C, react for 15min, then wash 4 times with DMF until ninhydrin is detected as blue;

[0079] b. Add 0.4gG and 0.5g HoBt to the system, add 1mL DIC as catalyst, 20mL DMF as solvent, react at 20°C for 1h, then wash 3 times until ninhydrin is detected as blue; add 0.9g R, 0.4 g G, 0.5g A at 20°C, each amino acid was reacted for 45 minutes;

[0080] c. After all the amino acid sequences are connected, add 15mL of piperidine and deprotect at 20°C for 15min. After the reaction, wa...

Embodiment 2

[0084] (1) Preparation of amphiphilic polypeptide DGRGGGAAAA

[0085] a. Weigh 1g of 2-cl resin (the degree of substitution of resin drug loading is 0.5), soak it in 20mL of DCM at 20°C for 2min, then wash once with DMF and DCM; use 20mL of DCM as solvent, weigh 0.3g of Fmoc-Asp(Otbu)-OH, react with 1mL of DIEA, 1g of 2-cl resin at 25°C for 2h, then wash twice with DMF; use 20mL of DCM+1mL of methanol+1mLDIEA at 20°C for 45min, wash with DMF Wash 3 times; deprotect with 15mL piperidine at 25°C, react for 15min, then wash 4 times with DMF until ninhydrin is detected as blue;

[0086] b. Add 0.5gG and 0.5g HoBt to the system, add 1mL DIC as catalyst, 20mL DMF as solvent, react at 20°C for 1h, then wash 3 times until ninhydrin is detected as blue; add 1.2g R, 0.5 g G, 0.8g A at 25°C, each amino acid was reacted for 60 minutes;

[0087] c. After all the amino acid sequences are connected, then add 15mL piperidine and deprotect at 25°C for 15min. After the reaction, wash and the ...

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Abstract

The invention discloses an amphiphilic polypeptide DGRGGGAAAA and a preparation method thereof, and a novel anticancer drug delivery system and a preparation method thereof; the preparation method of the amphiphilic polypeptide DGRGGGAAAA comprises: 1) using DMF (dimethyl formamide) as a solvent, DCM (dichloromethane) as an expanding agent and DIC (diisopropyl carbodiimide) as a catalyst to synthesize DGRGGGAAAA by a solid-phase synthetic process; 2) mixing the DGRGGGAAAA and doxorubicin (DOX), dissolving the mixture in water, subjecting the system to multiple dialysis, centrifuging the dialyzed system, and removing supernate to obtain the novel anticancer drug delivery system. The novel anticancer drug delivery system has significantly improved efficiency, and has the advantages of high targeting action, small side effect, low toxicity and the like.

Description

technical field [0001] The present invention relates to anticancer drugs, in particular to amphiphilic polypeptide DGRGGGAAAA and its preparation method, novel anticancer drug delivery system and its preparation method. Background technique [0002] All organs in the human body are composed of cells. Orderly cell growth and differentiation meet the body's needs and maintain good health. However, if the cells continue to divide, no longer under the control of the body, and reproduce indefinitely, these extra large numbers of cells form a tumor. Cells of malignant tumors can invade and destroy adjacent tissues and organs. Also, cancer cells can break out of the tumor and enter the blood or lymphatic system, becoming life-threatening. [0003] At present, many anti-tumor drugs have been developed, and all of them have effective pharmacological activities, but their poor solubility, will be cleared quickly in the body, and have certain toxicity and side effects, which limit t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C07K1/02C07K1/06A61K9/107A61K47/42A61K31/704A61P35/00
CPCA61K9/1075A61K31/704A61K47/42C07K7/06Y02P20/55
Inventor 葛飞乔茜茜陶玉贵朱龙宝李婉珍宋平
Owner ANHUI POLYTECHNIC UNIV
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