CN-122005520-A - Application of avenanthramide D in preparation of angiogenesis inhibiting drugs

Abstract

The invention discloses an application of avenanthramide D in preparing an angiogenesis inhibiting drug, and relates to the technical field of biological medicines. According to the invention, the oat anthracene amide D is used for interfering HUVEC cells, and the stem cell viability, the apoptosis rate and the angiogenesis capacity are detected, so that the oat anthracene amide D can inhibit the proliferation of the HUVEC cells, promote the apoptosis of the HUVEC cells and inhibit the angiogenesis of the HUVEC cells. Further experiments have found that avenanthramide D reduces endothelial barrier integrity by reducing protein expression of Vascular Endothelial Growth Factor A (VEGFA) and platelet endothelial cell adhesion molecule-1 (CD 31) in HUVEC cells, resulting in a blockage of angiogenesis.

Inventors

• LUO YU
• LUO HANJIANG
• LI QINGHUA
• CHEN MIN
• CHEN WENQING

Assignees

• 桂林医科大学第一附属医院

Dates

Publication Date

20260512

Application Date

20260129

Claims (10)

1. 1. Application of avenanthramide D in preparing angiogenesis inhibiting medicines.
2. 2. The use of the avenanthramide D according to claim 1 for the preparation of a drug for inhibiting angiogenesis, wherein the active ingredient of the drug is avenanthramide D.
3. 3. The use of avenanthramide D according to claim 2 for the preparation of a medicament for inhibiting angiogenesis, characterized in that the concentration of avenanthramide D in the medicament is 25 μm-100 μm.
4. 4. The use of a avenanthramide D according to claim 2 for the preparation of an angiogenesis inhibiting drug, characterized in that said avenanthramide D has a molecular formula of C 16 H 13 NO 4 and a molecular weight of 283.28.
5. 5. The use of a avenanthramide D according to claim 4 for the preparation of a medicament for inhibiting angiogenesis, characterized in that said avenanthramide D is 2- [ (E) -3- (4-hydroxyphenyl) acrylamido ] benzoic acid.
6. 6. The application of the avenanthramide D in preparing an angiogenesis inhibiting medicine according to claim 5, wherein the avenanthramide D has a CAS number of 115610-36-1 and a structural formula shown in a formula (1): (1)。
7. 7. The use of an avenanthramide D according to any one of claims 1-6 for the preparation of an angiogenesis inhibiting drug, wherein the drug is in the form of a tablet, capsule, granule, drop, lyophilisate, ointment or injection.
8. 8. The use of a avenanthramide D according to claim 7 for the preparation of a medicament for inhibiting angiogenesis, said medicament further comprising a pharmaceutically acceptable adjuvant.
9. 9. The use of the avenanthramide D according to claim 8 for preparing an angiogenesis inhibiting drug, wherein the auxiliary material includes at least one of a solvent, an emulsifier, a dispersant, a wetting agent, an adhesive and a stabilizer.
10. 10. The use of a avenanthramide D according to claim 7 for the preparation of a medicament for inhibiting angiogenesis, said medicament further comprising a pharmaceutically acceptable carrier.

Description

Application of avenanthramide D in preparation of angiogenesis inhibiting drugs Technical Field The invention relates to the technical field of biological medicines, in particular to application of avenanthramide D in preparation of angiogenesis inhibiting medicines. Background Angiogenesis refers to the biological process of forming a new capillary network from endothelial cells of existing blood vessels by budding, dividing, migrating and remodelling. This is a critical physiological activity of the body in development, repair and regeneration. Angiogenesis is regulated by a precision "on-off" system consisting of pro-angiogenic factors and inhibitory factors. Among these, vascular endothelial growth factor is the core "on" signal, while angiostatin, endostatin, etc. are "off" signals. In physiological conditions, this system remains in dynamic balance, and once unbalanced, causes disease. Angiogenesis is twofold in disease. On the one hand, it is required to inhibit the abnormal growth of the cells in tumors and eye diseases, and on the other hand, it is required to promote the functional regeneration of the cells in diseases such as myocardial infarction, limb ischemia and the like. Human Umbilical Vein Endothelial (HUVEC) cells are typical representations of human vascular endothelial cells and are widely used in vascular biology, angiogenesis and drug screening studies. Abnormal proliferation, migration and luminal formation of HUVECs are key steps in pathological angiogenesis and are closely related to the development and progression of a variety of diseases, such as growth and metastasis of solid tumors, age-related macular degeneration, diabetic retinopathy, rheumatoid arthritis, psoriasis, atherosclerosis, and the like. At present, inhibitors (such as VEGF monoclonal antibodies, small molecule tyrosine kinase inhibitors and the like) aiming at angiogenesis are clinically applied to the treatment of partial cancers and eye diseases, but the problems of large individual difference in curative effect, easiness in generation of drug resistance, strong toxic and side effects, limited administration route, high cost and the like still exist. Therefore, the development of angiogenesis inhibitors with novel mechanisms of action, higher efficacy or lower toxic side effects is an important direction in the current field of angiogenesis drug development. The oat anthracene amide is a special nitrogenous phenolic acid derivative in oat and silkworm eggs, belongs to non-steroid natural components, and has the characteristics of antioxidation, anti-inflammation and antiallergic. It is mainly distributed in oat bran and contains more than 40 structural analogues, wherein the content of the analogues is higher in three forms of alkaloid A, B, C. The composition is in the form of brown clear liquid in cosmetics, is soluble in 1, 3-butanediol, and can be used for substituting glucocorticoid for anti-allergic antipruritic skin care product. Avena sativa anthramide D (Avenanthramide D) is a phenolic acid found in Avena sativa. At present, AVENANTHRAMIDE D has not been reported on the inhibition of angiogenesis. Disclosure of Invention In order to solve the technical problems, the invention aims to provide an application of the avenanthramide D in preparing an angiogenesis inhibiting drug, wherein the principal active ingredient of the drug is the avenanthramide D, namely 2- [ (E) -3- (4-hydroxyphenyl) acrylamide ] benzoic acid, which can inhibit HUVEC cell proliferation, promote HUVEC cell apoptosis and inhibit HUVEC cell angiogenesis. AVENANTHRAMIDE D can reduce the integrity of endothelial barrier by inhibiting the protein expression of VEGFA and CD31 in HUVEC cells, thereby preventing angiogenesis, and is expected to be applied to the preparation of various medicaments for preventing or treating diseases related to pathological angiogenesis, thereby having better application prospect. The technical scheme for solving the technical problems is as follows: the invention aims to provide an application of avenanthramide D in preparing an angiogenesis inhibiting drug. The invention has the beneficial effects that oat anthracene amide D (Avenanthramide D) is used for interfering Human Umbilical Vein Endothelial (HUVEC) cells, and the influence of AVENANTHRAMIDE D on HUVEC cell proliferation, apoptosis and angiogenesis capacity is detected through a CCK8 experiment, a flow cytometry (Annexin V-FITC/PI double-dyeing method) and an in-vitro lumen formation experiment. Experimental results show that AVENANTHRAMIDE D can inhibit HUVEC cell proliferation, promote HUVEC cell apoptosis and inhibit HUVEC cell angiogenesis. Further, it was found experimentally that AVENANTHRAMIDE D decreased endothelial barrier integrity by decreasing protein expression of Vascular Endothelial Growth Factor A (VEGFA) and platelet endothelial cell adhesion molecule-1 (CD 31) in HUVEC cells, resulting in blocked angiogenesis. AVENANTHRAMIDE D plays