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Cage-like monoterpene glycoside compounds derived from radix paeoniae rubra as well as preparation method and application of cage-like monoterpene glycoside compounds

A technology of compounds and monoterpene glycosides, applied in the directions of medical preparations, drug combinations, plant raw materials, etc. containing active ingredients, can solve the allergy-like diseases of red peony extract, and the patent for the preparation method of red peony compound monomers. Literature, etc.

Pending Publication Date: 2022-04-22
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no research report on the use of the above-mentioned Radix Paeoniae Rubra extract for the treatment of allergic diseases, and there is no patent document on the preparation method of the above-mentioned Radix Paeoniae Rubra Compound Monomer that can inhibit RBL-2H3 degranulation

Method used

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  • Cage-like monoterpene glycoside compounds derived from radix paeoniae rubra as well as preparation method and application of cage-like monoterpene glycoside compounds
  • Cage-like monoterpene glycoside compounds derived from radix paeoniae rubra as well as preparation method and application of cage-like monoterpene glycoside compounds
  • Cage-like monoterpene glycoside compounds derived from radix paeoniae rubra as well as preparation method and application of cage-like monoterpene glycoside compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1, the preparation of compound I, II, III, IV, V, VI

[0046] Radix Paeoniae Rubra decoction pieces 50kg, soaked in distilled water and ultrasonically extracted 3 times, 1 hour each time. The water extract was directly separated by macroporous adsorption resin, eluted with 50% ethanol, and the eluate was concentrated under reduced pressure. The part eluted with 50% ethanol continues to be separated by MCI column, eluted with 30% ethanol and 50% ethanol in turn, and the eluate is concentrated under reduced pressure, and the sample eluted with 30% ethanol is CS-3 (2000g), 50% ethanol The eluted sample was CS-4 (316 g). The residue was concentrated to no alcohol by 95% ethanol extract, extracted 5 times with an equal volume of ethyl acetate, and the extract was concentrated under reduced pressure to obtain the ethyl acetate part CS-1 (580 g) and the water phase part CS-2 (270 g). Such as figure 1 .

[0047] Our previous activity screening found that only CS-...

experiment example 1

[0065] Exploration of Cytotoxicity of Parts of Radix Paeoniae Rubra

[0066] The RBL-2H3 cells in the logarithmic growth phase were taken out from the incubator, and the cells were digested to prepare a cell suspension. Cell density was calculated using a handheld cell counter (model: scepter). Adjust the cell number to 1×10 with fresh complete medium 5 cells / ml, inoculate in 96-well plate, 200 μL per well, mix the cell suspension once for every three wells inoculated, after culturing for 24 hours, discard the supernatant, and add different concentrations (0.2 μg / ml , T2 is 2 μg / ml, T3 is 20 μg / ml) drugs to be screened, each group has 3 duplicate wells, and a normal group (cell blank wells without drugs) and zero adjustment wells (cell blank wells without inoculation) After culturing for 24 hours, discard the supernatant, add 200 μL of serum-free MTT solution (serum-free medium: 5 mg / ml: MTT=1:10), incubate for 4 hours, centrifuge at 400 g / 5 min, discard the supernatant, and...

experiment example 2

[0072] Study on the effect of Radix Paeoniae Rubra on the degranulation of RBL-2H3 cells caused by allergic reaction

[0073] Digest the cells in the logarithmic growth phase and adjust the cell density to 1×10 5 pieces / ml. 200 μL / well was added into the 96-well plate, and the zero adjustment well, the blank control well, the total enzyme well and each administration well were set. The administration wells were divided into model control group, T1, T2 and T3 groups, wherein the final administration concentration of T1 was 0.2 μg / ml, T2 was 2 μg / ml, and T3 was 20 μg / ml. Incubate overnight, add complete medium to the zero wells, normal wells and total enzyme wells for normal culture, add 200 μL of anti-DNP-IgE prepared in complete medium with a final concentration of 750ng / ml in the model group, and add drugs of various concentrations to the administration wells and anti-DNP-IgE with a final concentration of 750ng / ml in a total of 200 μL, incubated for 24 hours, centrifuged, a...

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Abstract

The invention belongs to the technical field of medicines, and relates to application of cage-like monoterpene glycoside compounds in resisting allergic diseases, in particular to application of cage-like monoterpene glycoside compounds in radix paeoniae rubra in preparing medicines for preventing and treating allergic diseases. Pharmacological experiments prove that the compounds can effectively inhibit release of hexosaminidase (beta-HEX) and histamine (HIS) in sensitized RBL-2H3 cells, and the anti-allergic effect of the compounds I-VI is stronger than that of paeoniflorin. Besides, a representative compound II shows that HIS release is reduced by combining with HDC, release of inflammatory factors is inhibited by blocking ERK1 / 2, JNK and p38 in an MAPK signal transduction pathway, and the compound II also has important significance in repairing cytoskeleton and mitochondrial membrane damage caused by anaphylactic reaction. In addition, in-vivo experiments also prove that the compound II has a protective effect on animal models with allergic diseases. Therefore, cage-like monoterpene glycosides from radix paeoniae rubra can be considered as a promising HDC and MAPK signal channel dual inhibitor from natural sources.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a compound isolated from traditional Chinese medicine Radix Paeoniae Rubra and its application in preventing and treating allergic diseases. Background technique [0002] As a chronic disease, allergic diseases seriously affect the work efficiency of patients and reduce their production capacity, which leads to the increase of social costs. Therefore, effective and safe treatment of allergic diseases is one of the major challenges facing public health. Anaphylaxis is the most urgent and potentially serious manifestation of allergic diseases. It refers to a physiological change that occurs when the body is stimulated by the same antigen again after the body responds to the antigen for the first time. . According to the "World Allergy Organization" report, people with allergic symptoms account for 30% to 40% of the total population in the world; there are a large num...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K31/7034A61P37/08A61P27/02A61P11/02A61P11/06A61K36/71A61K36/65
CPCA61K31/7048A61K31/7034A61P37/08A61P27/02A61P11/02A61P11/06A61K36/71A61K36/65
Inventor 靳洪涛林生李恩灿钟万超郝瑞瑞夏桂阳李万芳夏欢
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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