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Preparation of 2r-cardiospermin-5-p-hydroxybenzoate and its application in the preparation of drugs for treating rheumatoid arthritis

An arthritic and rheumatoid technology, applied to the preparation of 2R-cardiospermin-5-p-hydroxybenzoate and its application in the preparation of rheumatoid arthritis drugs, can solve the problems of heavy social burden and high treatment cost

Active Publication Date: 2020-11-03
BINZHOU MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The treatment of RA patients requires long-term medication to control the course of the disease and improve symptoms, and the cost of treatment is high and the social burden is heavy
At present, the drugs used clinically to treat RA mainly include non-steroidal anti-inflammatory drugs (NSAIDs), glucocorticoids, disease-modifying antirheumatic drugs, biological agents and herbal preparations, etc., although they have certain However, most of them have strong toxic and side effects, and there is still a big gap between this and the ideal anti-rheumatoid drug that needs to be taken for a long time

Method used

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  • Preparation of 2r-cardiospermin-5-p-hydroxybenzoate and its application in the preparation of drugs for treating rheumatoid arthritis
  • Preparation of 2r-cardiospermin-5-p-hydroxybenzoate and its application in the preparation of drugs for treating rheumatoid arthritis
  • Preparation of 2r-cardiospermin-5-p-hydroxybenzoate and its application in the preparation of drugs for treating rheumatoid arthritis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1. Preparation of 2R-cardiospermin-5-p-hydroxybenzoate

[0025] Take the pearl plum medicinal material, crush it into the coarsest powder, add 20 times the amount of 95% ethanol, soak and extract 1 to 3 times, about 10 hours each time, combine the extracts, filter, dealcoholize and concentrate to about 20% ethanol concentration, and add samples On the AB-8 type weakly polar macroporous adsorption resin column, first use 20% ethanol solution to elute 5 column volumes to remove impurities, then use 95% ethanol to elute 4 column volumes, collect the 95% ethanol eluted part, After drying under reduced pressure, put on a 100-200-mesh silica gel column, use dichloromethane-methanol as the eluting system, and carry out stage elution according to the methanol concentration from low to high, collect the eluted part with a methanol concentration of 15-25%, concentrate, and crystallize , filtered, and dried under reduced pressure to obtain coarse crystals of 2R-cardiosp...

Embodiment 2

[0026] Embodiment 2. Preparation of 2R-cardiospermin-5-p-hydroxybenzoate

[0027] Take the pearl plum medicinal material, crush it into the coarsest powder, add 20 times the amount of methanol, soak and extract 1 to 3 times, about 10 hours each time, combine the extracts, filter, dealcoholize and concentrate to an appropriate volume, and replenish water until the alcohol concentration is about 20% , add sample to D-101 non-polar macroporous adsorption resin column, first use 20% methanol solution to elute 5 column volumes to remove impurities, then use 90% methanol to elute 4 column volumes, collect 90% methanol wash The eluted part was dried under reduced pressure and put on a 100-200-mesh silica gel column, using dichloromethane-methanol as the elution system, and carried out stage elution according to the methanol concentration from low to high, and collected the eluted part with a methanol concentration of 15-25%. Concentrate, crystallize, filter, and dry under reduced pre...

Embodiment 3

[0028] Example 3. Confirmation of the structure of 2R-cardiospermin-5-p-hydroxybenzoate

[0029] 1. Instruments and materials

[0030] Jasco P-1020 digital polarimeter, Agilent TOF / 6500 high-resolution mass spectrometer, Shimadzu UV-2401 visible-ultraviolet spectrophotometer, NMR is Bruke Avance III 500NMR spectrometer, melting point analyzer is Yanaco MP53 (melting point is not corrected) ). The 2R-cardiospermin-5-p-hydroxybenzoate sample was prepared according to the procedure in Example 1 above.

[0031] 2. Compound structure identification

[0032] Colorless viscous oil (methanol), easily soluble in dimethyl sulfoxide and methanol, slightly soluble in ethyl acetate, acetone, chloroform, water, insoluble in petroleum ether, Positive ion ESI-MS m / z: 396[M+H] + , 418[M+Na] + ; Negative ion ESI-MS m / z: 394[M-H] - , 430[M+Cl] - ,789[2M-H] - . Positive ion HR-ESI-MS m / z: measured value 418.1108[M+Na] + , the calculated value is 418.1114 (C 18 h 21 NO 9 Na[M+Na] + ...

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Abstract

The invention relates to chemical structure and a preparation method of a compound 2R-cardiospermin-5-p-hydroxybenzoate as well as an application of the compound in preparing medicines for treating rheumatoid arthritis. The 2R-cardiospermin-5-p-hydroxybenzoate, as a novel compound purified and prepared from a conventional traditional Chinese medicine, namely Sorbaria sorbifolia (L.) A. Brown, by the inventor, can be used for obviously inhibiting PEG2 and NO levels in serum of a mouse with adjuvant arthritis, and the compound is close to tripterygium glycosides at an equivalent dosage in activity; therefore, the compound can be used for preparing the medicines for treating and resisting the rheumatoid arthritis. The chemical structure and the preparation method of the compound as well as anti-RA (rheumatoid arthritis) activity of the compound are disclosed for the first time, therefore outstanding substantive features are guaranteed.

Description

technical field [0001] The invention relates to the structure and preparation method of 2R-cardiospermin-5-p-hydroxybenzoate, and the application of 2R-cardiospermin-5-p-hydroxybenzoate in the preparation of drugs for treating rheumatoid arthritis. Background technique [0002] Rheumatoid arthritis (RA) is a heterogeneous, systemic, autoimmune disease with symmetrical polyarthritis as the main clinical manifestation. Qualitative autoimmune disease. RA is one of the main causes of human incapacity and disability. The average incidence rate in the world is 0.2% to 1.2%, and the prevalence rate in my country is 0.2% to 0.93%. The treatment of RA patients requires long-term medication to control the course of the disease and improve symptoms, and the cost of treatment is high and the social burden is heavy. At present, the drugs used clinically to treat RA mainly include non-steroidal anti-inflammatory drugs (NSAIDs), glucocorticoids, disease-modifying antirheumatic drugs, bio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7028C07H15/10C07H1/08A61P29/00A61P19/02
CPCA61K9/205A61K9/2059A61K9/4866A61K31/7028C07H1/08C07H15/10
Inventor 孙书勤曲桂武张菡菡吴长景孙亚楠伊鹏荆杰
Owner BINZHOU MEDICAL COLLEGE
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