KR-102964082-B1 - Novel peptides with anticancer or antibacterial effects and uses thereof

Abstract

The present invention relates to a novel peptide having an anticancer or antibacterial effect and its use. It has been confirmed that the synthesized peptide successfully exhibits desired functions with low toxicity to normal cells and low hemolytic activity, and can provide a therapeutic agent with potential applications for antibacterial and anticancer treatments.

Inventors

• 장원희
• 이병조
• 목창수
• 성정석
• 신민경

Assignees

• 동국대학교 산학협력단

Dates

Publication Date

20260513

Application Date

20230102

Claims (18)

1. A peptide having anticancer and antibacterial effects, composed of the amino acid sequence of Sequence List 1 or Sequence List 3.
2. An anticancer pharmaceutical composition comprising the peptide of claim 1 as an active ingredient.
3. An antimicrobial pharmaceutical composition comprising the peptide of claim 1 as an active ingredient.
4. In claim 2, The above anticancer pharmaceutical composition is characterized by exhibiting an anticancer effect against one or more cancers selected from the group consisting of colorectal cancer, lung cancer, breast cancer, breast adenocarcinoma, glioblastoma, gastric cancer, liver cancer, pancreatic cancer, uterine cancer, esophageal cancer, bladder cancer, head and neck cancer, leukemia, thyroid cancer, papillary thyroid cancer, lymphoma, blood cancer, rectal cancer, prostate cancer, ovarian cancer, kidney cancer, brain cancer, and skin cancer.
5. In claim 3, The above antimicrobial pharmaceutical composition is characterized by having an antimicrobial effect against one or more bacteria selected from the group consisting of Gram-positive bacteria, Gram-negative bacteria, and antibiotic-resistant bacteria.
6. In claim 5, An antimicrobial pharmaceutical composition characterized in that the above-mentioned Gram-positive bacteria are one or more selected from the group consisting of Enterococcus faecalis , Micrococcus luteus, Pseudomonas aeruginosa , and Staphylococcus aureus .
7. In claim 5, An antimicrobial pharmaceutical composition characterized in that the above-mentioned Gram-negative bacteria are one or more selected from the group consisting of Escherichia coli , Pseudomonas aeruginosa , and Salmonella typhimurium.
8. In claim 5, An antimicrobial pharmaceutical composition characterized in that the above antibiotic-resistant bacteria is Methicillin-resistant Staphylococcus aureus (MRSA) or Vancomycin-resistant Enterococcus (VRE).
9. An anticancer quasi-drug composition comprising the peptide of claim 1 as an active ingredient.
10. An antimicrobial quasi-drug composition comprising the peptide of claim 1 as an active ingredient.
11. delete
12. A peptide having an antibacterial effect composed of the amino acid sequence of Sequence List 2.
13. An antibacterial pharmaceutical composition comprising the peptide of claim 12 as an active ingredient.
14. In claim 13, The above antimicrobial pharmaceutical composition is characterized by having an antimicrobial effect against one or more bacteria selected from the group consisting of Gram-positive bacteria, Gram-negative bacteria, and antibiotic-resistant bacteria.
15. In claim 14, An antimicrobial pharmaceutical composition characterized in that the above-mentioned Gram-positive bacteria are one or more selected from the group consisting of Enterococcus faecalis , Micrococcus luteus, Pseudomonas aeruginosa , and Staphylococcus aureus .
16. In claim 14, An antimicrobial pharmaceutical composition characterized in that the above-mentioned Gram-negative bacteria are one or more selected from the group consisting of Escherichia coli , Pseudomonas aeruginosa , and Salmonella typhimurium.
17. In claim 14, An antimicrobial pharmaceutical composition characterized in that the above antibiotic-resistant bacteria is Methicillin-resistant Staphylococcus aureus (MRSA) or Vancomycin-resistant Enterococcus (VRE).
18. An antimicrobial quasi-drug composition comprising the peptide of claim 12 as an active ingredient.

Description

Novel peptides with anticancer or antibacterial effects and uses thereof The present invention provides a novel peptide having an anticancer or antibacterial effect and uses thereof. Peptides, composed of short chains of amino acids, are widely studied and utilized as promising therapeutic candidates because advancements in synthesis technology allow for rapid synthesis and easy modification. In particular, compared to other synthetic chemicals, peptides have a relatively broad target range, high target specificity, low toxicity, and few side effects. As a result of these advantages, peptides accounted for over $50 billion in the global pharmaceutical market in 2019, and the number of approvals for peptide-based drugs has steadily increased over the past 60 years. Antibiotic resistance is currently one of the most serious problems facing global health, global development, and food safety. The overuse and misuse of antibiotics have accelerated the emergence of antibiotic-resistant strains, leading to a rapid depletion of resources for the development and/or identification of new antibiotics. Another global health threat is cancer, a leading cause of death worldwide, which claimed approximately 10 million lives in 2020. The development of new treatments to combat drug-resistant bacteria and cancer is urgent, as there are limitations to treatment due to endogenous or acquired drug resistance following exposure to treatment. Figure 1 shows an overview of the deep conditional generator and generation performance. Figure 2 shows the results of comparing Random, Cond-Gen-B, and test data set sequences. Figure 3 shows the results of confirming the bacterial membrane destruction effect caused by G-ABP1, G-ABP2, and G-ACP. Figure 4 shows the results of the analysis of cytotoxicity for G-ABP1, G-ABP2, and G-ACP peptides. Figure 5 shows the results of confirming the hemolytic activity of G-ABP1, G-ABP2, and G-ACP. The present invention will be described in more detail below. The present invention provides a peptide represented by the amino acid sequence of Sequence List 1. The above peptide may have an anticancer or antibacterial effect. In addition, the present invention provides a pharmaceutical composition for anticancer or antibacterial purposes comprising the above peptide as an active ingredient. The above pharmaceutical composition may exhibit an anticancer effect against one or more cancers selected from the group consisting of colorectal cancer, lung cancer, breast cancer, breast adenocarcinoma, glioblastoma, gastric cancer, liver cancer, pancreatic cancer, uterine cancer, esophageal cancer, bladder cancer, head and neck cancer, leukemia, thyroid cancer, papillary thyroid cancer, lymphoma, hematological cancer, rectal cancer, prostate cancer, ovarian cancer, kidney cancer, brain cancer, and skin cancer, but is not limited thereto. The above pharmaceutical composition may have an antibacterial effect against one or more bacteria selected from the group consisting of Gram-positive bacteria, Gram-negative bacteria, and antibiotic-resistant bacteria, but is not limited thereto. The above Gram-positive bacteria may be one or more selected from the group consisting of Enterococcus faecalis , Micrococcus luteus, Pseudomonas aeruginosa , and Staphylococcus aureus , but are not limited thereto. The above Gram-negative bacteria may be one or more selected from the group consisting of Escherichia coli , Pseudomonas aeruginosa , and Salmonella typhimurium, but are not limited thereto. The above antibiotic-resistant bacteria may be methicillin-resistant Staphylococcus aureus (MRSA) or vancomycin-resistant Enterococcus (VRE), but are not limited thereto. In another embodiment of the present invention, the pharmaceutical composition may further comprise one or more additives selected from the group consisting of suitable carriers, excipients, disintegrants, sweeteners, coating agents, leavening agents, lubricants, lubricants, flavoring agents, antioxidants, buffers, bacteriostatic agents, diluents, dispersants, surfactants, binders, and lubricants commonly used in the manufacture of pharmaceutical compositions. Specifically, the carrier, excipient, and diluent may be lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia gum, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, and mineral oil. Solid dosage forms for oral administration include tablets, pills, powders, granules, capsules, etc. These solid dosage forms may be prepared by mixing at least one excipient, for example, starch, calcium carbonate, sucrose or lactose, gelatin, etc., with the above composition. In addition, lubricants such as magnesium stearate and talc may also be used in addition to simple excipients. Liquid preparations for oral administration include