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Preparation of Sutherlandin-5-p-hydroxybenzoate, and applications of Sutherlandin-5-p-hydroxybenzoate in preparation of rheumatoid arthritis treatment drugs

A technology for rheumatoid arthritis and compounds, applied in the preparation of Sutherlandin-5-p-hydroxybenzoate and its application in the preparation of drugs for the treatment of rheumatoid arthritis, which can solve the problems of high treatment cost and heavy social burden

Active Publication Date: 2017-07-25
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 (non-steroidalanti-inflammatory drugs, NSAIDs), glucocorticoids, disease-modifying antirheumatic drugs, biological preparations and herbal preparations, etc., although they have certain curative effects , but most of them have strong toxic and side effects, and there is still a big gap between this and the ideal antirheumatic drug that needs to be taken for a long time

Method used

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  • Preparation of Sutherlandin-5-p-hydroxybenzoate, and applications of Sutherlandin-5-p-hydroxybenzoate in preparation of rheumatoid arthritis treatment drugs
  • Preparation of Sutherlandin-5-p-hydroxybenzoate, and applications of Sutherlandin-5-p-hydroxybenzoate in preparation of rheumatoid arthritis treatment drugs
  • Preparation of Sutherlandin-5-p-hydroxybenzoate, and applications of Sutherlandin-5-p-hydroxybenzoate in preparation of rheumatoid arthritis treatment drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] The preparation of embodiment 1.Sutherlandin-5-p-hydroxybenzoate

[0026] 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 elution system, and carry out stage elution according to the methanol concentration from low to high, collect the eluted part with a methanol concentration of 20-30%, concentrate, and crystallize , filtered, and dried under reduced pressure to obtain coarse crystals of Sutherlandin...

Embodiment 2

[0027] The preparation of embodiment 2.Sutherlandin-5-p-hydroxybenzoate

[0028] 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 the 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 to wash The eluted part was dried under reduced pressure and placed on a 100-200-mesh silica gel column, using dichloromethane-methanol as the elution system, and eluted step by step according to the methanol concentration from low to high, and collected the eluted part with a methanol concentration of 20-30%. Concentrate, crystallize, filter, and dry under reduced ...

Embodiment 3

[0029] Example 3. Confirmation of the structure of Sutherlandin-5-p-hydroxybenzoate

[0030] 1. Instruments and materials

[0031] 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) ). Sutherlandin-5-p-hydroxybenzoate samples were prepared according to the steps in Example 1 above.

[0032] 2. Compound structure identification

[0033] Colorless needle crystal (methanol), mp 79-81℃, 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 418.1104[M+Na] + , the calculated value is 418.1114 (C 18 h 21 NO 9 Na[M+Na] + ...

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Abstract

The present invention relates to the chemical structure and the preparation method of a compound Sutherlandin-5-p-hydroxybenzoate, and applications of the compound in preparation of rheumatoid arthritis treatment drugs. According to the present invention, Sutherlandin-5-p-hydroxybenzoate is the new compound purified and prepared from a traditional Chinese medicine Sorbaria sorbifolia (L.) A. Brown., can significantly inhibit the PEG2 level and the NO level in the serum of adjuvant arthritis rats, has strong activity compared to the same dose of tripterygium glycosides, and can be used for preparing rheumatoid arthritis treatment drugs; and the chemical structure, the preparation method and the anti-RA activity of the compound are firstly disclosed, such that the compound has prominent substantive characteristics.

Description

technical field [0001] The invention relates to the structure and preparation method of Sutherlandin-5-p-hydroxybenzoate and the application of Sutherlandin-5-p-hydroxybenzoate in the preparation of medicines 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 (non-steroidalanti-inflammatory drugs, NSAIDs), glucocorticoids, disease-m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/10C07H1/08A61P19/02A61P29/00
CPCC07H1/08C07H15/10
Inventor 曲桂武刘俊杰吴长景曹奇志孙亚楠伊鹏于泽秋
Owner BINZHOU MEDICAL COLLEGE
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