CN-121673366-B - Small molecule peptide and application

Abstract

The invention discloses a small molecular peptide and application thereof, relates to the technical field of medicinal chemistry, and aims to overcome the defects of low safety and insufficient reliability in the prior art, wherein the amino acid sequence of the small molecular peptide is shown as SEQ ID NO. 1. The invention provides a safe and efficient new choice for preventing, relieving and treating inflammation.

Inventors

• WU DAN
• YAN PENGFEI
• WANG LIANGYU
• FANG LI
• LIU CHUNLEI

Assignees

• 吉林农业大学

Dates

Publication Date

20260512

Application Date

20260210

Claims (4)

1. 1. The small molecular peptide is characterized in that the amino acid sequence of the small molecular peptide is shown as SEQ ID NO. 1.
2. 2. The use of the small molecule peptide according to claim 1, for the preparation of a medicament for the prevention, alleviation and/or treatment of inflammation, wherein the inflammation is lipopolysaccharide-induced inflammation.
3. 3. The use of the small molecule peptide of claim 2, wherein the pharmaceutical dosage form is at least one of an injection, a tablet, an oral liquid, a granule or a capsule.
4. 4. A pharmaceutical composition comprising the small molecule peptide of claim 1.

Description

Small molecule peptide and application Technical Field The invention relates to the technical field related to medicinal chemistry. More particularly, the invention relates to a small molecule peptide and application thereof. Background Inflammation is a defensive reaction of an organism to stimulus such as infection and injury, but excessive or continuous inflammatory reaction can cause tissue injury, induce various diseases such as infectious diseases and autoimmune diseases and seriously threaten human health. Lipopolysaccharide (LPS) is a key component of the cell wall of gram-negative bacteria, is a common clinical inflammation inducer, can induce excessive production of Reactive Oxygen Species (ROS) by activating immune cells such as macrophages, down regulate antioxidant enzyme activities such as superoxide dismutase (SOD) and Catalase (CAT), promote release of pro-inflammatory cytokines such as Nitric Oxide (NO) and IL-alpha (interleukin-alpha), IL-6 (interleukin-6) and IL-1 beta (interleukin-1 beta), activate signal pathways such as NF- κB (nuclear factor- κB) and MAPK (mitogen activated protein kinase), finally lead to amplification of inflammatory cascade reaction, and related pathological mechanisms become the core direction of inflammation research. At present, the clinically commonly used anti-inflammatory drugs comprise non-steroidal anti-inflammatory drugs, glucocorticoids and the like, but the long-term use of the anti-inflammatory drugs is easy to cause side effects such as gastrointestinal damage, immunosuppression and the like, and the safety is insufficient. The natural small molecular active peptide has the advantages of good biocompatibility, low toxic and side effects, easy absorption and the like, and gradually becomes a research hot spot in the anti-inflammatory field. However, the anti-inflammatory peptides found in the prior art have the problems of undefined action mechanism, unstable anti-inflammatory activity, insufficient targeting for LPS induced inflammation and the like, and the actions of most peptide drugs only stay in the primary anti-inflammatory activity verification, lack of elucidation of deep mechanisms such as signal path regulation and control, metabolic network intervention and the like, and are difficult to meet the clinical demands of safe and efficient anti-inflammatory drugs. Therefore, there is a need to design a solution that overcomes the above drawbacks. Disclosure of Invention The invention aims to provide a small molecular peptide and application thereof, and provides a safe and efficient new choice for preventing, relieving and treating inflammation. To achieve these objects and other advantages and in accordance with one aspect of the present invention, there is provided a small molecule peptide having an amino acid sequence shown in SEQ ID NO. 1. According to another aspect of the present invention there is also provided the use of a small molecule peptide for the manufacture of a medicament for the prevention, alleviation and/or treatment of inflammation. Further, the inflammation is lipopolysaccharide-induced inflammation. Further, the dosage form of the medicine is at least one of injection, tablet, oral liquid, granule or capsule. According to another aspect of the present invention, there is also provided a pharmaceutical composition characterized by comprising said small molecule peptide. The invention at least comprises the following beneficial effects: The small molecule peptide PYYFH has remarkable anti-inflammatory advantages and practical value. Firstly, the safety is high, the medicine has no toxicity to RAW264.7 cells in the concentration range of 50-1200 mu g/mL, the biocompatibility is good, the side effects of gastrointestinal damage, immunosuppression and the like of the traditional anti-inflammatory medicine are avoided, and the medicine is suitable for long-term use. Secondly, the anti-inflammatory targeting is strong and the mechanism is clear, through stable combination with a key inflammatory factor IL-6, NF- κB and MAPK signal channels are regulated and controlled, so that SOD and CAT activities can be improved to improve oxidative stress, and the release of NO, IL-alpha, IL-6 and other pro-inflammatory factors can be inhibited, meanwhile, through non-targeted metabonomics, the activity can regulate and control a core metabolism channel through Tyrosyl-Tyrosine and sn-Glycerol-phosphate, inflammatory cascade reaction induced by LPS is blocked in a multidimensional way, and the anti-inflammatory effect is stable and reliable. The small molecular peptide provides a safe and efficient new choice for preventing, relieving and treating the LPS induced inflammation, and has important clinical application prospect and popularization value. Additional advantages, objects, and features of the invention will be set forth in part in the description which follows and in part will become apparent to those having ordinary skill in the art u