Small molecule polypeptide ZY4 and application thereof

A technology of small molecular polypeptide, ZY4, applied in the field of biomedicine, can solve the problems of complex antibacterial peptide antibacterial mechanism, leakage of bacterial contents, permeability change, etc., and achieve significant therapeutic effect, growth inhibition, and small molecular weight effect

Active Publication Date: 2015-10-14
四川莱真生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The antibacterial mechanism of antimicrobial peptides is complex, but most of the theories believe that the mechanism involves the interaction between the cationic and hydrophobic properties of antimicrobial peptides and negatively charged microbial cell membranes. After the antimicrobial peptides come into contact with bacterial cell membranes, they cause changes in membrane permeability. , or form a transmembrane hole in the bacterial cell membrane, and finally cause the bacterial content to leak out and die

Method used

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  • Small molecule polypeptide ZY4 and application thereof
  • Small molecule polypeptide ZY4 and application thereof
  • Small molecule polypeptide ZY4 and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1: Preparation of small molecule polypeptide ZY4

[0019] 1. Weigh 0.2g of the resin and place it in a dry and clean reaction tube, add an appropriate amount of N,N-dimethylamide (DMF) and activate for 30 minutes. Weigh 1 mmol of the first amino acid residue, add 150 mg of 4-dimethylaminopyridine (DMAP) into the reaction tube, and react with DMF for 3 hours as a solvent. After the reaction is completed, wash with DMF for 3-6 times, and add appropriate pyridine and acetic anhydride , the volume ratio is 1:1, react for 30 minutes, and wash with DMF 3-6 times after the reaction is completed. Then use piperidine to elute the protective group Fmoc of the amino acid, elution twice, each 15min, then wash 4 times with DMF, wash 2 times with methanol;

[0020] 2. Weigh 3mmol of the second amino acid and 3mmol of HBTU in a reaction tube, add 0.5ml of DIEA, react for 40min, wash with DMF 3-6 times, add piperidine solution to elute the protective group Fmoc of the amino ac...

Embodiment 2

[0023] Example 2: Antibacterial experiment of small molecule polypeptide ZY4

[0024] 1. Prepare Escherichia coli, Candida albicans, Staphylococcus aureus, Bacillus subtilis, Staphylococcus hemolyticus, Staphylococcus epidermidis, and Staphylococcus coli respectively, culture at 37°C for 18 hours, and set aside;

[0025] 2. Prepare the small molecule polypeptide ZY4 solution with a concentration of 0.8-20 μg / ml, sterilize and dry a circular qualitative filter disc with a diameter of 5-7 mm, and then immerse it in the above-mentioned small molecule polypeptide ZY4 solution with different concentrations;

[0026] 3. Prepare high-column broth agar medium, sterilize, and set aside;

[0027] 4. Melt the tall column broth agar medium, cool to 50°C, add Escherichia coli, Candida albicans, Staphylococcus aureus, Bacillus subtilis, hemolytic Staphylococcus, Staphylococcus epidermidis, and Staphylococcus kosheri respectively 1ml , shake evenly, pour into a sterile plate, and shake gent...

Embodiment 3

[0036] Example 3: Therapeutic effect of small molecule polypeptide ZY4 on mouse ear acne model

[0037] 1. Cultivate Propionibacterium acnes ATCC11817 with brain heart infusion medium, cultivate to logarithmic phase, wash with normal saline twice, and resuspend in normal saline to 5×10 8 CFU / ml;

[0038] 2. Select male mice with a weight of 18g, Kunming species, and randomly divide them into 3 groups, 6 mice in each group, which are respectively treatment group, positive control group, and negative control group. Anesthetized with appropriate sodium, and then intradermally injected 20 μl / mouse of the resuspended bacterial solution in the left ear of the mouse;

[0039]3. The small molecule polypeptide ZY4 and clindamycin were prepared into 2 mg / ml ointment with polyethylene glycol and glycerin, respectively, wherein the weight ratio of polyethylene glycol and glycerin was 5:1, and rubbed on the skin of the left ear of the mouse On the surface, the small molecule polypeptide ...

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Abstract

The present invention discloses a small molecule polypeptide ZY4 and an application thereof in preparing drugs for acne treatment, anti-infection and anti-tumor, and cosmetics. The small molecule polypeptide ZY4 contains seventeen amino acid residues with a molecular weight of 2374.0 Da and an isoelectric point of 10.74, and has an amino-acid sequence as SEQ ID:1 shows. According to the invention, the small polypeptide ZY4 is artificially synthesized and has the advantages of small molecular weight and convenient artificial synthesis. Through experiment, the polypeptide ZY4 has proved a significant antimicrobial effect and has a remarkable therapeutic effect for acne. The polypeptide ZY4 can also inhibit the growth of tumor cells and has a killing effect on the tumor cells. The small molecule polypeptide ZY4 can be applied to preparing drugs for acne treatment, anti-infection and anti-tumor, and cosmetics.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to the application of small molecular polypeptide ZY4 in the preparation of acne, anti-infection and anti-tumor drugs and cosmetics. Background technique [0002] Acne is a chronic inflammation of the pilosebaceous glands. It is a common inflammatory skin disease in adolescence. It usually occurs on the cheeks, forehead, cheeks and nasolabial folds, followed by the chest, back and shoulders. Its onset is mainly related to sex hormones. acne levels, massive secretion of sebaceous glands, proliferation of Propionibacterium acnes, abnormal keratinization of pilosebaceous ducts, and inflammation. During adolescence, the lipid composition of the skin surface changes, and the male hormone increases, resulting in hyperkeratosis of the sebaceous follicle duct, and the epithelial cells shed on the hair follicle wall are mixed with sebum, embolized in the hair follicle mouth, f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08A61P35/00A61P31/04A61P17/10
CPCC07K7/08A61P17/10A61P31/04A61P31/10A61P35/00A61K38/00A61K38/10Y02A50/30A61K47/10
Inventor 赖仞容明强杜彦军
Owner 四川莱真生物科技有限公司
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