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Application of abietane type diterpene compounds

A compound and diterpenoid technology, applied in the field of rosinane-type diterpenoids, to achieve the effect of wide application prospects

Active Publication Date: 2019-03-05
SHANGHAI UNIV OF T C M
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are relatively few reports on the use of this compound. So far, there has been no relevant report on the use of scrodentoid A in the preparation of drugs that inhibit mast cell degranulation, let alone the use of scrodentoid A in the preparation of mast cell stabilizers and in the preparation of preventive or / and therapeutic factors. Drugs or health food related reports on allergic diseases caused by mast cell degranulation

Method used

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  • Application of abietane type diterpene compounds
  • Application of abietane type diterpene compounds
  • Application of abietane type diterpene compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Preparation of scrodentoid A

[0039] a) Take Scrophulariaceae serrata as raw material, add 8 times the amount of 95wt% ethanol aqueous solution, reflux extraction 3 times, each time for 2 hours; combine the filtrates, concentrate under reduced pressure to obtain a liquid extract; suspend the obtained liquid extract In water, extract 4 times with dichloromethane; combine the extracts, concentrate under reduced pressure to an extract, and obtain a crude extract;

[0040] b) The crude extract is separated by silica gel column chromatography, gradient elution is carried out with petroleum ether and ethyl acetate according to the volume ratio of 100:0 to 50:50, TLC thin layer analysis, the fractions containing scrodentoid A are collected, and the Concentrate under pressure to obtain the crude product of scrodentoidA;

[0041] c) The crude product of scrodentoid A is separated by MCI column, gradient elution is carried out with methanol and water according to the...

Embodiment 2

[0046] Example 2: Detecting the release of β-hex in mast cells, and analyzing the impact of scrodentoid A (abbreviated as SDA) on the release of β-hex from mast cells

[0047] Detect the effect of scrodentoid A on IgE-mediated release of β-hex from BMMC cells: use BMMC cells, add anti-mouse-DNP-IgE overnight, after drug intervention, then add DNP-BSA to stimulate BMMC cells to degranulate, detect The release amount of β-hex, all data are expressed as mean±SE, n=3, *P<0.05, **P<0.01, ***P<0.001.

[0048] (1) BMMC cell culture

[0049] Extract the bone marrow of C57BL / 6 mice, use BMMC cell special culture medium at 37°C, 5% CO 2 Four weeks in the incubator.

[0050] (2) Cell sensitization

[0051] Add 0.1 μg / ml anti-mouse-DNP-IgE to BMMC cells, at 37°C, 5% CO 2 Incubate overnight in the incubator.

[0052] (3) Dosing intervention

[0053] After 24 hours, different concentrations (2.5, 5, 10, 25 μM) of scrodentoid A or positive drug (10 μM PP2) were added to intervene for 3...

Embodiment 3

[0062] Example 3: Detecting the release of lipid mediators in mast cells and analyzing the impact of scrodentoid A (abbreviated as SDA) on the release of mast cell lipid mediators

[0063] Detect the effect of scrodentoid A on IgE-mediated release of lipid mediators from BMMC cells: use BMMC cells, add anti-mouse-DNP-IgE overnight, after drug intervention, then add DNP-BSA to stimulate BMMC cells to release lipid mediators, Detect its LTC 4 and PDG 2 All data are expressed as mean±SE, n=3, *P<0.05, **P<0.01, ***P<0.001.

[0064] (1) BMMC cell culture

[0065] Extract the bone marrow of C57BL / 6 mice, use BMMC cell special culture medium at 37°C, 5% CO 2 Cultured in the incubator for four weeks, the mast cell purity was detected to be higher than 99%.

[0066] (2) Cell sensitization

[0067] Add 0.1 μg / ml anti-mouse-DNP-IgE to BMMC cells, at 37°C, 5% CO2 Incubate overnight in the incubator.

[0068] (3) Dosing intervention

[0069] After 24 hours, different concentrations...

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PUM

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Abstract

The invention discloses an application of abietane type diterpene compounds. The formula of the abietane type diterpene compounds is represented by the formula I. At least one of the compounds represented by the formula I, and hydrates, pharmaceutically acceptable salts, tautomer, stereoisomer, and precursor thereof is taken as an active component to prepare drugs or health care food for inhibiting mast cell de-granulation. The results of experiments show that the compounds represented by the formula I can prominently inhibit mast cell de-granulation, can be used as an active component to prepare drugs or health care food for inhibiting mast cell de-granulation, further can be used as an active component to prepare a mast cell stabilizer, and can be used to prepare drugs or health care food for preventing or / and treating allergic diseases caused by mast cell de-granulation.

Description

technical field [0001] The invention relates to a new application of an abietane-type diterpene compound and belongs to the technical field of medicine. Background technique [0002] Allergy, also known as an allergic disease, is an overreaction of the immune system caused by substances in the environment that are not harmful to humans (McConnell T H. The nature of disease: pathology for the health professions[M]. Lippincott Williams&Wilkins, 2007 ). Common allergic diseases mainly contain hay fever, food allergy, atopic dermatitis and allergic asthma etc. (Kay A B.Allergy and allergic diseases[J].New England Journal of Medicine,2001,344(1):30- 37), the main symptoms are skin redness, itching, runny nose and shortness of breath. With the development of modern industrialization, allergy has become the sixth largest disease in the world, which is posing a continuous health threat to people. According to media reports, about 22% of the world's population suffers from allergi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P37/08A61P17/00A61P11/06C07C49/747C07C45/78C07C45/79C07C45/80
CPCA23L33/105A23V2002/00A61K31/122C07C45/78C07C45/79C07C45/80C07C49/747A23V2200/304A23V2250/20
Inventor 李医明张刘强钱菲郭夫江
Owner SHANGHAI UNIV OF T C M
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