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

A technology for rheumatoid arthritis and a compound is applied in the preparation of Sutherlandin-5-p-hydroxybenzoate and its application in the preparation of rheumatoid arthritis drugs, which can solve the problems of high treatment cost, heavy social burden and the like, and achieves the The effect of highlighting substantive features

Active Publication Date: 2021-04-20
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 sutherlandin-5-p-hydroxybenzoate and its application in the preparation of drugs for treating rheumatoid arthritis
  • Preparation of sutherlandin-5-p-hydroxybenzoate and its application in the preparation of drugs for treating rheumatoid arthritis
  • Preparation of sutherlandin-5-p-hydroxybenzoate and its application in the preparation of drugs for treating rheumatoid arthritis

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 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 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 pressur...

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 preparation method of a compound Sutherlandin-5-p-hydroxybenzoate, and the application of the compound in the preparation of medicines for treating rheumatoid arthritis. Sutherlandin‑5‑p‑hydroxybenzoate is a new compound purified and prepared by the applicant of the present invention from the traditional Chinese medicine Sorbaria sorbifolia (L.) A. Brown. It can significantly inhibit the PEG in the serum of rats with adjuvant arthritis 2 and NO level, and its activity is stronger than that of tripterygium glycosides in the same dose, and can be used to prepare medicines for treating rheumatoid arthritis. The chemical structure, preparation method and anti-RA activity of the compound are disclosed for the first time, so it has outstanding substantive features.

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 (NSAIDs), glucocorticoids, disease-modifying antirheumatic drugs, biologic...

Claims

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Application Information

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Patent Type & Authority Patents(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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