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KR-20260062104-A - Pharmaceutical composition for preventing or treating pulmonary fibrosis comprising myristic acid as an active ingredient

KR20260062104AKR 20260062104 AKR20260062104 AKR 20260062104AKR-20260062104-A

Abstract

The present invention relates to a pharmaceutical composition for the prevention or treatment of pulmonary fibrosis comprising myristic acid as an active ingredient. It was found that when myristic acid is treated, the expression of fibrosis-related markers in fibroblast cell lines decreases at both protein and transcriptional levels, and cell migration is inhibited, so it is expected to be usefully utilized for the treatment of pulmonary fibrosis.

Inventors

  • 송진우

Assignees

  • 재단법인 아산사회복지재단
  • 울산대학교 산학협력단

Dates

Publication Date
20260507
Application Date
20241024

Claims (6)

  1. A pharmaceutical composition for the prevention or treatment of pulmonary fibrosis, comprising myristic acid as an active ingredient.
  2. In paragraph 1, A pharmaceutical composition in which the above-mentioned pulmonary fibrosis includes idiopathic pulmonary fibrosis.
  3. In paragraph 1, The above composition is a pharmaceutical composition that inhibits the gene or protein expression level of a fibrosis-related marker.
  4. In paragraph 3, A pharmaceutical composition wherein the above fibrosis-related marker is one or more selected from the group consisting of fibronectin, collagen-1, and α-SMA.
  5. In paragraph 1, The above composition is a pharmaceutical composition that inhibits the cell migration of fibroblasts.
  6. A kit for the prevention or treatment of pulmonary fibrosis comprising the composition of claim 1 and instructions.

Description

Pharmaceutical composition for preventing or treating pulmonary fibrosis comprising myristic acid as an active ingredient The present invention relates to a pharmaceutical composition for the prevention or treatment of pulmonary fibrosis comprising myristic acid as an active ingredient. Pulmonary fibrosis is a disease in which lung tissue is damaged and scarred, becoming thick and hardened, preventing the lungs from functioning normally. As pulmonary fibrosis worsens, breathing gradually becomes shorter. In many cases, the exact cause of pulmonary fibrosis cannot be identified, and this type of fibrosis is called idiopathic pulmonary fibrosis (IPF). There are various types of pulmonary fibrosis, including idiopathic pulmonary fibrosis; pulmonary fibrosis caused by diseases such as autoimmune diseases like rheumatoid arthritis, viral infections, and gastroesophageal reflux disease (GERD); familial pulmonary fibrosis (familial PF); and pulmonary fibrosis caused by harmful substances such as asbestos, silica, dust, radiation therapy, and smoking. Symptoms of pulmonary fibrosis primarily include shortness of breath (especially during exercise), chronic dryness, dry cough, fatigue, tightness accompanied by chest pain, loss of appetite, and rapid weight loss. In this case, pulmonary fibrosis may be diagnosed based on symptoms of shortness of breath that progress with overexertion, and sometimes a faint inspiratory crackling sound may be heard at the base of the lungs during auscultation. While chest X-rays may appear normal or abnormal, abnormal lung features can be observed on CT scans. Treatment strategies for pulmonary fibrosis vary and are individualized depending on the patient's condition and symptoms, but a cure for the disease has not yet been found. Figure 1 shows the results of confirming the concentration range of myristic acid that does not affect cell viability using a CCK-8 assay. Figures 2a to 2d show that the protein expression levels of fibrosis-related markers were reduced in fibroblast cell lines treated with myristic acid. Figures 2e to 2g show that the transcription levels of fibrosis-related markers were reduced in fibroblast cell lines treated with myristic acid. Figure 3a shows a decrease in cell migration of fibroblast cell lines treated with myristic acid, and Figure 3b is a graph quantifying this. The inventors of the present invention have identified the possibility that myristic acid can be a target for the treatment of pulmonary fibrosis by demonstrating that myristic acid has the potential to regulate fibrosis, which is a major mechanism of pulmonary fibrosis. Accordingly, the present invention provides a pharmaceutical composition for the prevention or treatment of pulmonary fibrosis comprising myristic acid as an active ingredient. In the present invention, “fatty acid” is a carboxylic acid having a long aliphatic chain that is saturated or unsaturated in chemistry, particularly in biochemistry. Most naturally occurring fatty acids have unbranched chains composed of an even number of carbon atoms, ranging from 4 to 28. Fatty acids generally exist in organisms primarily in the form of esters, consisting of three main classes: triglycerides, phospholipids, and cholesteryl esters, rather than existing alone. In these ester forms, fatty acids are an important energy source in animals and an important structural component in cells. When fatty acids in plasma circulate in the blood in a state other than ester, these fatty acids are called non-esterified fatty acids (NEFA) or free fatty acids (FFA). Free fatty acids are always bound to transport proteins such as albumin. In the present invention, “miristic acid” is interchangeably named “tetradecanoic acid (IUPAC name)” and is a saturated fatty acid having the chemical formula CH₃ ( CH₂ ) ₁₂COOH , which may be represented by the following structural formula, but is not limited thereto (Cas no.: 544-63-8). In the present invention, myristic acid may include not only myristic acid but also pharmaceutically acceptable salts. Accordingly, the present invention provides a pharmaceutical composition for the prevention or treatment of pulmonary fibrosis comprising myristic acid or a pharmaceutically acceptable salt thereof as an active ingredient. Salts and esters of myristic acid are generally called myristates. Myristic acid was named after the scientific name of nutmeg (Myristica fragrans) and was first isolated in 1841 by the Scottish scientist Lyon Playfair. Myristic acid possesses sufficient hydrophobicity to infiltrate into the fatty acid acyl core of the phospholipid bilayer of eukaryotic cell membranes. In this way, myristic acid acts as a lipid anchor in biological membranes. According to various epidemiological studies in humans, myristic acid and lauric acid are the saturated fatty acids most closely associated with human plasma cholesterol concentrations; this implies that an increase in plasma triglycerides correlates with an incr