Application of a compound in the preparation of antiallergic drugs

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

Active Publication Date: 2022-07-05
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 a compound in the preparation of antiallergic drugs
  • Application of a compound in the preparation of antiallergic drugs
  • Application of a compound in the preparation of antiallergic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

specific Embodiment approach

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

[0031] 1. RT-PCR: RBL-2H3 (5×10 5 / per well) were seeded in 6-well plates, incubated with anti-DNP IgE overnight to sensitize, 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, Düsseldorf, Germany) according to the manufacturer's instructions. Use Honor TM ⅡStrandcDNA Synthesis Kit to synthesize cDNA. use terabytes Premix Ex Taq TM (Tokyo, Japan) reagents to quantify mRNA levels.

[0032] 2. Western blotting to detect the...

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 Medical Laboratory Animal Center), in RPMI (Hyclone) 10% FBS (Gibico), 1% double antibody, 10ng / ml IL-3 and SCF Culture for 4-6 weeks.

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

[0041] 3. Release of β-aminoglycosidase: inoculate BMMC in a 24-well plate, incubate with anti-DNP IgE overnight to sensitize, incubate with T-5224 for one hour, stimulate with DNP-HSA (sigma) for 30 minutes, and take 50ul The clear reacted with 50ul of substrate at 37℃ for 90min. The absorbance was measured at 405nm. After discarding the supernatant, add 500u...

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PUM

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Abstract

The invention discloses the application of a compound in the preparation of antiallergic medicine, characterized in that the molecular formula of the compound is C 29 H 27 NO 8 , its chemical structural formula is: the present invention finds that the compound T-5224 can significantly inhibit the release of β-aminoglycosidase in mast cells, has the effect of significantly inhibiting the degranulation of mast cells, and can significantly inhibit allergy in mice reaction. This fully shows that the T-5224 compound can be used to prepare antiallergic drugs and has broad application prospects.

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 Manifested as red and swollen skin, itching, runny nose and shortness of breath, etc., it poses a constant health threat to the people's statement. [0003] Mast cells play a key role in inducing and maintaining inflammation. They are mainly distributed in the parts of the body in contact with the external environment, such as the skin, digestive tract, intestinal and reproductive tract mucosa, etc. These parts are the first host cells that come into contact with allergens one. It has a high-affinity Ig...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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