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Small molecule peptides and their uses

A technology of small molecule peptides and amino acids, applied in peptides, medical preparations containing active ingredients, peptide/protein components, etc., can solve problems such as frequent occurrence of drug resistance

Active Publication Date: 2021-06-08
青岛联正科技集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, there are few effective drugs against parasitic diseases, and drug resistance occurs frequently

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] A small molecular polypeptide, the amino acid sequence of the small molecular polypeptide is shown in SEQ ID No.1;

[0016] SEQ ID No. 1: DDQQYVDDRNKFYYVSTEE.

[0017] The isoelectric point of the small molecule polypeptide is 3.7.

[0018] The molecular weight of the small molecule polypeptide is 2414.48.

[0019] The preparation method of the small molecule polypeptide:

[0020] Choose amino acid-King resin as the carrier (resin), fully swell the resin with dichloromethane, add the first Fmoc-protected amino acid, wash with dimethylformamide several times, use appropriate concentration of DBLK, Fmoc-protecting group Then, wash it several times with dimethylformamide, wash away DBLK, weigh the appropriate condensing agent benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate and activate The reagent methylmorpholine and the second Fmoc-protected amino acid (Fmoc-ASp-OH) at the C-terminus (Fmoc-ASp-OH) were coupled, and the ninhydrin detection method was use...

Embodiment 2

[0022] 1. Experimental method

[0023] Add 1 mL to a sterile test tube at a concentration of 1×10 6 Each / mL of the bacterial solution, add 1 mg of the small molecule polypeptide provided by the present invention, and culture at 37°C for 24 hours, collect the culture medium and dilute it in multiples, the dilution factor is 10 times, and detect the number of viable bacteria by the coating culture method.

[0024] 2. Experimental results:

[0025] Table 1 The bactericidal rate (%) of the small molecule polypeptide of the present invention

[0026] bacteria ATCC 6538 ATCC 25922 ATCC 10231 ATCC 9372 Sterilization rate 99.5% 99.7% 99.7% 99.9%

[0027] It can be seen from Table 1 that the small molecule polypeptide provided by the present invention is effective against Staphylococcus aureus (ATCC 6538), Escherichia coli (ATCC 25922), Candida albicans (ATCC 10231), Bacillus subtilis var. 9372) have strong bactericidal properties, with a bactericidal r...

Embodiment 3

[0029] The anti-parasitic activity of the products of the present invention was assessed using fluorescent cell sorting analysis (FACS) to quantify parasite cultures of erythrocytes. The polypeptide obtained in Example 1 was dissolved in 1 ml DMSO, and then mixed with 25 mmol / L 4-hydroxyethylpiperazineethanesulfonic acid buffer, 32mmol / L NaHCO 3 Dilute 200 times with RPMI 1640 cell culture medium made with 10% human plasma. The sample solution was subsequently prepared into 11 different concentrations by 2-fold dilution, 1ml, 2×10 6 / ml of parasites were added to the solution and placed in 5% CO at 37°C 2 Cultivate in the incubator for 48h. Add 1ml of 3% diamidinophenylindole solution, incubate for another 18 hours, and measure the number of red blood cells with a fluorescent cell differential analyzer. The inhibition rate of different concentrations of samples against parasites can be obtained, and the IC can be calculated. 50 value.

[0030] Table 2 The half effective co...

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PUM

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Abstract

The invention discloses a small molecule polypeptide, the amino acid sequence of the small molecule polypeptide is shown in SEQ ID No.1. The invention also provides the application of the small molecule polypeptide. The polypeptide of the invention has good anti-parasitic activity, antibacterial activity, strong stability, easy structure regulation and obvious application potential.

Description

technical field [0001] The invention relates to a small molecule polypeptide. More specifically, the present invention relates to a small molecule polypeptide with antiparasitic and antibacterial activities. Background technique [0002] As a common disease, parasitic diseases have affected the health of people all over the world. For example, malaria has become a serious social problem in tropical and subtropical regions such as Africa, Asia, and Latin America. About 200 million people are infected with malaria every year, and more than half a million people die. Currently, there are not many effective drugs against parasitic diseases, and drug resistance occurs frequently. Therefore, it is extremely urgent to find new drugs for parasitic diseases. In particular, it is of great significance to find a drug that has both parasitic activity and other biological activities. Contents of the invention [0003] One object of the present invention is to provide a small molecul...

Claims

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Application Information

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IPC IPC(8): C07K7/08A61K38/10A61P33/00A61P31/10A61P31/04
CPCA61K38/00C07K7/08
Inventor 李培源苏炜霍丽妮陈睿
Owner 青岛联正科技集团有限公司
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