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Preparation of 2s-cardiospermin-5-benzoate and its application in the preparation of drugs for treating rheumatoid arthritis

A technology for rheumatoid arthritis and medicine, applied in the application field of preparing medicine for treating rheumatoid arthritis, can solve the problems of high treatment cost, heavy social burden and the like, and achieve the effect of highlighting substantive characteristics

Active Publication Date: 2021-05-25
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 (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 2s-cardiospermin-5-benzoate and its application in the preparation of drugs for treating rheumatoid arthritis
  • Preparation of 2s-cardiospermin-5-benzoate and its application in the preparation of drugs for treating rheumatoid arthritis
  • Preparation of 2s-cardiospermin-5-benzoate and its application in the preparation of drugs for treating rheumatoid arthritis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The preparation of embodiment 1.2S-cardiospermin-5-benzoate

[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, carry out stage elution according to the concentration of methanol from low to high, collect the eluted part with a methanol concentration of 10-15%, concentrate, and crystallize , filtered, and dried under reduced pressure to obtain coarse crystals of 2S-cardiospermin-5...

Embodiment 2

[0026] The preparation of embodiment 2.2S-cardiospermin-5-benzoate

[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 the sample to the D-101 non-polar macroporous adsorption resin column, first use 20% methanol solution to elute 5 column volumes to remove impurities, then use 80% methanol to elute 4 column volumes, collect 80% 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 in stages according to the concentration of methanol from low to high, and collected the eluted part with a methanol concentration of 10-15%. Concentrate, crystallize, filter, and dry under reduced p...

Embodiment 3

[0028] Example 3. Confirmation of the structure of 2S-cardiospermin-5-benzoate

[0029] 1. Instruments and materials

[0030] Jasco P-1020 digital polarimeter, Agilent TOF / 6500 high-resolution mass spectrometer, Shimadzu UV-2401 visible-ultraviolet spectrophotometer, Bruke Avance III 500 NMR spectrometer for NMR, and Yanaco MP53 melting point analyzer (melting point is not Correction). The 2S-cardiospermin-5-benzoate 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, (c 0.49, methanol). Positive ion ESI-MS m / z: 380[M+H] + , 402[M+Na] + , 781[2M+Na] + ; Negative ion ESI-MS m / z: 378[M-H] - , 414[M+Cl] - ,757[2M-H] - . Positive ion HR-ESI-MS m / z: measured value 402.1159[M+Na] + , the calculated value is 402.1165 (C 18 h ...

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Abstract

The present invention relates to the chemical structure and preparation method of a compound 2S-cardiospermin-5-benzoate, and the application of the compound in the preparation of drugs for treating rheumatoid arthritis. 2S-cardiospermin-5-benzoate 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 2S-cardiospermin-5-benzoate, and the application of 2S-cardiospermin-5-benzoate 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, biological agents...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H15/04C07H1/08A61K31/7032A61P29/00A61P19/02
CPCC07H1/08C07H15/04
Inventor 曲桂武吴长景孙书勤孙亚楠刘俊杰曹奇志荆杰
Owner BINZHOU MEDICAL COLLEGE
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