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Preparing method of sutherlandin-5-cis-p-coumarate and application of sutherlandin-5-cis-p-coumarate to preparation of drugs for treating rheumatoid arthritis

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

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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  • Preparing method of sutherlandin-5-cis-p-coumarate and application of sutherlandin-5-cis-p-coumarate to preparation of drugs for treating rheumatoid arthritis
  • Preparing method of sutherlandin-5-cis-p-coumarate and application of sutherlandin-5-cis-p-coumarate to preparation of drugs for treating rheumatoid arthritis
  • Preparing method of sutherlandin-5-cis-p-coumarate and application of sutherlandin-5-cis-p-coumarate to preparation of drugs for treating rheumatoid arthritis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The preparation of embodiment 1.Sutherlandin-5-cis-p-coumarate

[0024] Take the medicinal material of pearl plum, 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 10% ethanol concentration, 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 60% ethanol to elute 4 column volumes, collect the 60% ethanol eluted part, Concentrate, refrigerate and crystallize, filter, and dry under reduced pressure to obtain Sutherlandin-5-cis-p-coumarate coarse crystals. Dissolve the crude crystals in methanol to form a supersaturated solution, recrystallize, filter, and dry under reduced pressure to obtain.

Embodiment 2

[0025] The preparation of embodiment 2.Sutherlandin-5-cis-p-coumarate

[0026] 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 10% , 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 60% methanol to elute 4 column volumes, collect 60% methanol to wash Partially removed, concentrated, refrigerated for crystallization, filtered, and dried under reduced pressure to obtain Sutherlandin-5-cis-p-coumarate coarse crystals. Dissolve the crude crystals in methanol to form a supersaturated solution, recrystallize, filter, and dry under reduced pressure to obtain.

Embodiment 3

[0027] Example 3. Confirmation of the structure of Sutherlandin-5-cis-p-coumarate

[0028] 1. Instruments and materials

[0029] 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 Sutherlandin-5-cis-p-coumarate sample was prepared according to the steps in Example 1 above.

[0030] 2. Compound structure identification

[0031] Colorless needles (methanol), mp 94-96°C, easily soluble in dimethyl sulfoxide and methanol, slightly soluble in ethyl acetate, acetone, chloroform, water, insoluble in petroleum ether, [α]2D4-12.2(c 0.43, methanol). Positive ion ESI-MS m / z: 422[M+H] + , 444[M+Na] + , 865[2M+Na] + ; Negative ion ESI-MS m / z: 420[M-H] - , 456[M+Cl] - ,841[2M-H] - . Positive ion HR-ESI-MS m / z: found value 444.1263[M+Na] + , the calculated value is 444....

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Abstract

The invention relates to a chemical structure and preparing method of the compound sutherlandin-5-cis-p-coumarate and application of the compound to preparation of drugs for treating rheumatoid arthritis. Sutherlandin-5-cis-p-coumarate is a novel compound prepared from the traditional Chinese medicine Sorbaria sorbifolia (L.) A. Brown. through purification by the applicant of the invention. The compound can remarkably suppress the level of PEG2 and NO in serum of adjuvant arthritis rats. The activity of the compound is close to that of tripterygium glycosides of the same dose, and the compound can be used for preparing drugs for treating rheumatoid arthritis. The chemical structure, preparing method and anti-RA activity of the compound are disclosed for the first time, thus having prominent and substantive features.

Description

technical field [0001] The invention relates to the structure and preparation method of Sutherlandin-5-cis-p-coumarate, and the application of Sutherlandin-5-cis-p-coumarate 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-modi...

Claims

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Application Information

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IPC IPC(8): A61K31/7028C07H15/10C07H1/08A61P29/00A61P19/02
CPCA61K9/205A61K9/2059A61K9/4866A61K31/7028C07H1/08C07H15/10
Inventor 曲桂武吴长景荆杰曹奇志孙亚楠郝玉玲于泽秋张丽刘俊杰
Owner BINZHOU MEDICAL COLLEGE
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