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Application of compound in preparation of anti-allergic drugs

A compound and anti-allergic technology, which can be applied in drug combinations, allergic diseases, pharmaceutical formulations, etc., can solve the problems of poor curative effect, large side effects, and few types of anti-allergic drugs, and achieve the suppression of allergic reactions, wide application prospects, and suppression of hypertrophy The effect of cell degranulation

Active Publication Date: 2021-06-08
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide an application of a compound in the preparation of anti-allergic drugs in view of the deficiencies of the prior art, aiming to solve the problems of fewer types of existing anti-allergic drugs, poor curative effect and relatively large side effects

Method used

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  • Application of compound in preparation of anti-allergic drugs
  • Application of compound in preparation of anti-allergic drugs
  • Application of compound in preparation of anti-allergic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Inhibitory effect of T-5224 on rat basophil (RBL-2H3) degranulation:

specific Embodiment approach

[0030] Rat basophils have a good anaphylactic immune response in the study of allergy diagnosis and immunotherapy. RBL-2H3 has a high affinity IgE receptor. They can be activated to secrete histamine and other transmitters by clustering these receptors or synergizing with calcium ionophores. This cell line is widely used to study biochemical pathways of mast cell FcERI and secretion. The specific implementation is as follows:

[0031] 1. RT-PCR: RBL-2H3 (5×10 5 / well) were inoculated in 6-well plates, incubated overnight with anti-DNP IgE for sensitization, incubated with T-5224 for one hour, and stimulated with DNP-HSA (dinitrophenylated human serum albumin) for 4 hours. Total RNA was extracted with the RNeasy Mini Kit (Qiagen, Dusseldorf, Germany) according to the manufacturer's instructions. Use Honor TM ⅡStrandcDNA Synthesis Kit synthesizes cDNA. Use TB Premix Ex Taq TM (Tokyo, Japan) reagents for quantification of mRNA levels.

[0032] 2. Detection of p-c Fos pr...

Embodiment 2

[0038] T-5224 inhibits degranulation of bone marrow-derived mast cells (BMMCs)

[0039] 1. Cell culture: BMMCs were isolated from Balb / c mice (purchased from Guangdong Provincial Medical Experimental Animal Center), in RPMI (Hyclone) 10% FBS (Gibico), 1% double antibody, 10ng / ml IL-3 and SCF Culture for 4-6 weeks.

[0040] 2. CCK8 detection of cell toxicity to T-5224: seed BMMC (1×104 / well) in a 96-well plate, add T-5224 after 24 hours, and continue to incubate for 24 hours. Then add 10ul CCK8 reagent, incubate for 1 hour, and finally measure the absorbance (OD value) with a microplate reader at a wavelength of 450nm.

[0041] 3. Release of β-aminoglycosidase: Inoculate BMMC in a 24-well plate, incubate with anti-DNP IgE overnight for sensitization, incubate with T-5224 for one hour, stimulate with DNP-HSA (sigma) for 30min, take 50ul on The supernatant was reacted with 50ul of the substrate at 37°C for 90min. The absorbance was measured at 405nm. After the supernatant was ...

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PUM

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Abstract

The invention discloses an application of a compound in preparation of anti-allergic drugs, and is characterized in that the molecular formula of the compound is C29H27NO8, and the chemical structural formula of the compound is shown in the specification. The study finds that the compound T-5224 can obviously inhibit release of beta-aminoglycosidase in mast cells, has an obvious effect of inhibiting degranulation of the mast cells, and can obviously inhibit the allergic reaction in mice. Therefore, the T-5224 compound can be used for preparing the anti-allergic drugs and has a wide application prospect.

Description

technical field [0001] The invention relates to the technical field of antiallergic drugs, in particular to the application of a compound in the preparation of antiallergic drugs. Background technique [0002] Allergy is a state of hypersensitivity of the immune system to substances in the normal environment. It can occur in multiple organs and tissues. Common clinical diseases include hay fever, food allergy, atopic dermatitis, allergic asthma, etc. The symptoms are mainly It manifests as red and swollen skin, itching, runny nose and shortness of breath, etc., which brings continuous health threats to people's statements. [0003] Mast cells play a key role in inducing and maintaining inflammation. They are mainly distributed in the parts of the body that are in contact with the external environment, such as the skin, digestive tract, intestinal tract, and reproductive tract mucosa. These parts are the first host cells that come into contact with allergens one. It has a h...

Claims

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Application Information

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IPC IPC(8): A61K31/423A61P37/08
CPCA61K31/423A61P37/08
Inventor 陈家杰王慧娜吉坤美
Owner SHENZHEN UNIV
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