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Polypeptide and application of polypeptide in preparation of drugs for treating colitis and colorectal cancers related to colitis

A technology for colorectal cancer and colitis, applied in the field of small molecule peptides for the treatment of colitis and colitis-related colorectal cancer

Active Publication Date: 2016-12-14
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the curative effect is obvious in experimental studies, but no drug has been approved in clinical practice.

Method used

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  • Polypeptide and application of polypeptide in preparation of drugs for treating colitis and colorectal cancers related to colitis
  • Polypeptide and application of polypeptide in preparation of drugs for treating colitis and colorectal cancers related to colitis
  • Polypeptide and application of polypeptide in preparation of drugs for treating colitis and colorectal cancers related to colitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: Synthesis of Small Molecular Peptides

[0047] The amino acid sequence of the small molecule polypeptide is shown in SEQ ID NO:1.

[0048] Small molecule peptide synthesis was performed on an ABI 431A solid-phase peptide synthesizer (PE Company, USA). Methods The standard fluorenylmethoxycarbonyl (Fmoc) protocol was used, and arginine was coupled twice. Initially select 0.125mmol p-hydroxymethylphenoxymethyl polystyrene resin (HMP resin), extend the peptide chain from the carboxyl terminal to the amino terminal one by one according to the polypeptide sequence, the amount of each amino acid is 0.5mmol, and the mole of the resin The ratio is 4:1. The α-amino acids of various amino acids are protected by Fmoc, and the other side chain protection groups are: Ser (tBu), Glu (OtBu), Arg (Pmc). The first amino acid is connected to the resin with 4-lutidine, the amino acid is activated with 1-hydroxybenzotriazole and dicycloethyl carbon, and after coupling, the Fmo...

Embodiment 2

[0050] Embodiment 2: the application of small molecular polypeptide in the treatment of mouse colitis, colitis-associated colorectal cancer

[0051] 1. Animals:

[0052] C57BL6 mice, 5 weeks old, 18-20 g, were purchased from the Animal Laboratory of Nantong University, and randomly divided into an experimental group (15 mice) and a control group (15 mice) according to body weight. The experimental group was given AOM / DSS, while the control group was injected with normal saline and drank distilled water freely. No food was fasted during the experiment.

[0053] 2. Drugs:

[0054] Small molecule polypeptide treatment group: 20nmol / kg body weight of the small molecule polypeptide shown in SEQ ID NO: 1 was given for intraperitoneal injection, a total of 6 mice;

[0055] Blank group: intraperitoneal injection of the same volume of PBS as the treatment group, a total of 6 rats.

[0056] 3. Experimental method:

[0057] ①Intraperitoneal injection of AOM / DSS is a common animal mo...

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Abstract

The invention relates to the field of biotechnologies, in particular to a small molecular polypeptide. The polypeptide is provided with an amino acid sequence shown as SEQ ID NO:1. The invention further provides application of the small molecule polypeptide in preparation of drugs for treating colitis and colorectal cancers related to colitis. The colon length, tumor number and the like of a treatment group of rats are obviously lower than those of a control group through treatment of the small molecular polypeptide. The bowel tissue proliferation indexes of rats suffering from the colorectal cancers related to colitis are remarkably reduced. In addition, the small molecular polypeptide can promote enterocyte apoptosis and inhibit enterocyte proliferation in an in-vitro cell experiment. The purpose of blocking inflammatory-cancer conversion is achieved by interfering or blocking biological functions of the polypeptide FKBP11, and novel drug design and a therapeutic target are provided for relieving of colitis related tumors.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular, a small molecular polypeptide for treating colitis and colitis-associated colorectal cancer by blocking FKBP11-mediated proliferation and its application. Background technique [0002] Inflammatory bowel disease is a non-specific inflammatory bowel disease of unknown cause, including ulcerative colitis and Crohn's disease. Inflammatory bowel disease is a recurrent and protracted disease. There is still a lack of effective treatment methods, and lifelong treatment is often required, which seriously affects the physical and mental health and quality of life of patients. Colorectal cancer is the most serious complication of inflammatory bowel disease with the highest mortality rate, accounting for 10% to 15% of the deaths of patients with inflammatory bowel disease. Patients with inflammatory bowel disease who have a wider range of inflammation, more severe inflammation, younger age of o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12N9/90A61K38/52A61P1/00A61P35/00
CPCC12N9/90
Inventor 张冬梅刘晓娟王晓彤周国雄
Owner NANTONG UNIVERSITY
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