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Elephantopin compound as well as preparation method and application thereof

A compound, the technology of Didancao, applied in the field of medicine, can solve the problems of danger of infection, large toxic and side effects, retention of water and sodium, etc.

Active Publication Date: 2020-10-30
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Steroidal anti-inflammatory drugs and non-steroidal anti-inflammatory drugs are commonly used clinically to treat inflammatory diseases. Steroidal anti-inflammatory drugs usually refer to steroidal hormones, including adrenocortical hormones, glucocorticoids, etc. These drugs have strong anti-inflammatory effects , but there are serious side effects such as water and sodium retention, risk of infection, etc., and the clinical use is limited
Non-steroidal anti-inflammatory drugs are a class of anti-inflammatory drugs that do not contain a steroidal structure. They are well tolerated, but their long-term use is limited by severe gastrointestinal adverse reactions, and severe cases may even cause digestive problems. tract bleeding and perforation
Because the existing anti-inflammatory drugs have problems such as single effect and high toxicity and side effects, they can no longer meet the clinical needs, and there is an urgent need to develop a safer and more effective anti-inflammatory drug
[0004] At present, the extract of Echinacea is a plant extract that is recognized as having medicinal effects, and there are few related studies. The research mainly focuses on its crude extract and effective parts. The crude extracts and effective parts that can be obtained by different extraction methods are different. , due to technical reasons, several kinds of galactones have been found at present, which cannot meet the clinical demand for ideal anti-inflammatory drugs. The applicant used the extraction process and preparation technology developed by itself to re-extract and synthesize After sorting out, a series of new dicholide compounds were found, and this series of dicholides had the same parent ring structure, and had stronger anti-inflammatory activity, which filled the gap in this field

Method used

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  • Elephantopin compound as well as preparation method and application thereof
  • Elephantopin compound as well as preparation method and application thereof
  • Elephantopin compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] The preparation of general formula (I) compound (total lactone):

[0072] Get the whole herb 20kg of dried Elephantopus scaber and use 10 times the amount of 95% ethanol to reflux extract 3 times, each time for 3 hours, combine the extracts, reclaim the ethanol, and get 1400g of dry extract, extract (dry extract ) is dissolved with about 5L of 30% ethanol, and is separated by macroporous resin HP-20 column chromatography, and is successively eluted with an equal volume of 50%, 90% ethanol-water gradient, each eluting 3 column volumes, and collecting 90% ethanol The solvent was recovered to obtain 127g of 90% ethanol. Purify the 90% ethanol part with silica gel column (200-300 mesh column chromatography silica gel, the mass ratio of sample to silica gel is 1:10), and perform gradient washing with petroleum ether-acetone (5:1,3:1,) 4 column volumes for each gradient elution, collecting petroleum ether-acetone (3:1) eluate, recovering the solvent, and obtaining the crude ...

Embodiment 2

[0074] The preparation of general formula (I) compound (total lactone):

[0075] Get 9.0kg of dried E. scaber whole herb and extract 3 times by cold soaking with 10 times the amount of 95% ethanol, 2 days each time, combine the extracts, reclaim ethanol, and obtain 270g of dry extract, extract ( dry extract) was dispersed by adding about 2.5L of water, added twice the volume of ethyl acetate for extraction, extracted 5 times, got the ethyl acetate part, recovered the solvent, and obtained 35g of ethyl acetate extract. Purify the ethyl acetate extract by chromatography on a silica gel column (200-300 mesh column chromatography silica gel, the mass ratio of sample to silica gel is 1:15), and carry out gradient washing with petroleum ether-acetone (5:1, 3:1) 5 column volumes for each gradient elution, collecting the petroleum ether-acetone (3:1) eluate, recovering the solvent, and obtaining the crude extract of the compound of general formula (I). The crude extraction is separat...

Embodiment 3

[0077] The difference from Example 1 is that the extract is Elephantopus tomentosus, the medicinal part is the whole herb, and the solvent used is methanol. Obtain general formula (I) total lactone 30g.

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Abstract

The invention discloses an elephantopin compound. The structural general formula of the elephantopin compound is shown in the specification, and the elephantopin compound is extracted from flowers, roots, stems and leaves or whole herbs of elephantopus plants, has excellent anti-inflammatory activity which is not reported by the compound, and is stronger than that of an elephantopus scaber whole extract and an effective part of the elephantopus scaber whole extract; the invention also provides a preparation method of the compound and application of the compound in anti-inflammatory drugs, especially in preparation of neuroinflammatory drugs, and the compound is suitable for industrial production.

Description

technical field [0001] The invention relates to the application of a dichotilide compound in the preparation of anti-inflammatory drugs, which belongs to the field of medicine. Background technique [0002] Inflammation is a complex immune defense response involving a variety of cells and factors, which can occur in tissues and organs anywhere in the body, and is a common clinical pathological process. Studies have shown that inflammation is associated with many diseases, such as the inflammatory cytokine CRP can promote the occurrence and development of atherosclerosis (AS) and tumor necrosis factor-α (tumor necrosis factor-α, TNF-α) on The occurrence of osteoporosis plays an important role and the "inflammation theory" of diabetes has been widely recognized. Many infectious diseases and autoimmune diseases, malignant tumors, cardiovascular diseases, diabetes and other chronic non-communicable major diseases belong to the category of inflammatory diseases. An important pu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/08A61K31/365A61P29/00A61P25/28
CPCC07D493/08A61P29/00A61P25/28
Inventor 邹忠梅张涛付露于猛齐云李凌宇
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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