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Application of ginkgolic acid in preparation of products for prevention and/or treatment of allergic diseases

A technology of ginkgolic acid and products, applied in allergic diseases, medical raw materials derived from Ginkgo biloba, skin diseases, etc.

Active Publication Date: 2017-09-22
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the existing Syk inhibitors are chemically synthesized small molecules, and Syk inhibitors derived from traditional Chinese medicine are rarely reported.

Method used

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  • Application of ginkgolic acid in preparation of products for prevention and/or treatment of allergic diseases
  • Application of ginkgolic acid in preparation of products for prevention and/or treatment of allergic diseases
  • Application of ginkgolic acid in preparation of products for prevention and/or treatment of allergic diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Embodiment 1, the application of ginkgolic acid (C15:1) in inhibiting spleen tyrosine kinase (Syk) activity

[0057] 1. Determination of Syk inhibitory activity

[0058] 1. Take a 384-well plate, add 4 μL of SYK enzyme solution and 2 μL of test sample solution (ginkgolic acid C15:1), mix well and incubate at 30°C for 20 minutes. At the same time, the test sample solution (staurosporine) was used as a positive control.

[0059]SYK enzyme solution is made up of solvent and solute, solvent is water, solute and its concentration are respectively: 3ng / μL SYK enzyme (British Abcam company, ab60886), 20mM MgCl 2 , 0.1 mg / ml BSA, 50 μM DTT, 40 mM Tris buffer (pH 7.5).

[0060] Test sample solution (ginkgolic acid C15:1) is made up of solvent and solute, and solvent is water, and solute and concentration thereof are respectively: ginkgolic acid (C15:1) prepared in 1mmol / L embodiment 1, 20mM MgCl 2 , 0.1 mg / ml BSA, 50 μM DTT, 40 mM Tris buffer (pH 7.5).

[0061] Test sample s...

Embodiment 2

[0075] Embodiment 2, the application of ginkgolic acid (C15:1) in inhibiting mast cell degranulation

[0076] 1. Determination of inhibition of mast cell degranulation activity

[0077] 1. RBL-2H3 mast cells (purchased from the American ATCC cell bank, CRL-2256 TM ) were suspended in EMEM medium (purchased from Lonza (China) Investment Co., Ltd., LONZA12-611F) containing 10% FBS, 100 U / ml penicillin and 100 μg / ml streptomycin, and the cell density was adjusted to 2.0×10 4 per well, seeded in 96-well plate, 180 μL per well, at 37°C, 5% CO 2 Incubate for 24 hours in a cell culture incubator.

[0078] 2. Then add 20 μL of DNP-IgE (Sigma, D8406) solution (solvent: 0.1M phosphate buffer, pH 7.4) to the cells in each well for sensitization for 12 hours, so that the final concentration of DNP-IgE is 100 ng / ml; discard the culture Solution, use PBS buffer solution (NaCl8.0g; KCl 0.2g; NaCl 2 HPO 4 1.44g; KH 2 PO 4 0.24g; add distilled water to 1000ml, pH 7.4), wash twice, a...

Embodiment 3

[0110] Embodiment 3, the application of ginkgolic acid (C13:0) in inhibiting Syk activity

[0111] 1. Determination of Syk inhibitory activity

[0112] The ginkgolic acid C15:1 in Step 1 of Example 1 was replaced with ginkgolic acid C13:0, and other steps were kept unchanged, and the Syk inhibitory activity of ginkgolic acid (C13:0) was detected.

[0113] The result is as Figure 7 shown. The inhibitory rate of ginkgolic acid (C13:0) was 48.17% at the concentration of 33.33μM. Under the same conditions, the inhibitory rate of the positive drug staurosporine at a concentration of 50nM was 52.96%.

[0114] 2. Study on the dose-effect relationship of ginkgolic acid (C13:0) on Syk inhibitory activity

[0115] The ginkgolic acid C15:1 in Step 2 of Example 1 was replaced by ginkgolic acid C13:0, and other steps were kept unchanged, and the dose-effect relationship of ginkgolic acid (C13:0) on Syk inhibitory activity was investigated.

[0116] Dose-response curve such as Figur...

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Abstract

The invention discloses a traditional-Chinese-medicine active compound with the Syk inhibitory activity and its preparation method and application. It is found that the active compound, namely ginkgolic acid C15:1 or ginkgolic acid C13:0, has the spleen tyrosine kinase (Syk) inhibition activity, research further shows that the active compound has the effect of inhibiting mastocyte degranulation, the traditional-Chinese-medicine active compound ginkgolic acid C15:1 is obtained from ginkgo medicinal materials for the first time, and it is verified that the traditional-Chinese-medicine active compound ginkgolic acid C15:1 has the Syk inhibition activity and the mastocyte degranulation inhibition activity. The effective component and chemical component of the active compound ginkgolic acid C15:1 or ginkgolic acid C13:0 are simple, the action target is clear, the Syk activity can be directly inhibited, the mastocyte degranulation is inhibited, the action mechanism of the ginkgolic acid C15:1 or ginkgolic acid C13:0 is easier to illuminate in pharmacological research, and the ginkgolic acid has a potential application value in the prevention and treatment of allergic asthma and provides a new medicine selection for the prevention and treatment of allergic asthma.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine chemistry, and more specifically relates to a compound found in the traditional Chinese medicine Ginkgo that can directly act on spleen tyrosine kinase (Syk) and inhibit the enzyme activity. The compound has the activity of inhibiting mast cell degranulation, The compound and its preparation have the potential to prevent and treat allergic diseases such as asthma. Background technique [0002] Allergic asthma (Bronchial asthma) is a chronic airway inflammatory disease characterized by infiltration of various cells in the lungs, especially mast cells, eosinophils, and T lymphocytes, and airway hyperresponses to various stimulating factors. In susceptible persons, this kind of inflammation can cause recurrent symptoms such as shortness of breath, wheezing, coughing and chest tightness. [0003] Studies have shown that mast cells play a very important role in the pathology of allergic ast...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/16A61K31/60A61P37/08A61P11/06A61P11/02A61P17/00
CPCA61K31/60A61K36/16
Inventor 王星张宇昕乔延江
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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