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Smelly seven secondary metabolites and their preparation methods and their application in pharmacy

A technology for the generation and metabolites of stinky seven times, which is applied in the field of medicine, and can solve the problems of no anti-inflammatory related pharmacological activities, no reports of anti-inflammatory drugs and pharmaceutical preparations, etc.

Active Publication Date: 2022-01-11
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, so far, there is no separation of 20(S)-dammar-25-ene-24(S)-hydroperoxyl-3β,6α,12β,20-tetrol (1), 20 (S)-dammar-3-oxo-23-ene-25-hydroperoxyl-6α,12β,20-triol (2), 20(S)-dammar-12-oxo-23-ene-25-hydro-peroxyl- 3β,6α,20-triol (3), 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-12β,20-diol (4), 20(S),24(R)-epoxy -3,4-seco-dammar-25-hydroxy-12-one-3-oic acid (5),20(S),24(R)-epoxy-3,4-seco-dammar-25-hydroxy-12 -one-3-oic acid methyl ester(6), and 6α-hydroxy-22,23,24,25,26,27-hexanordammar-3,12,20-trione(7) and other compounds and their preparation methods There are no reports on its anti-inflammatory pharmacological activity, nor its use in the treatment of anti-inflammatory drugs and pharmaceutical preparations

Method used

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  • Smelly seven secondary metabolites and their preparation methods and their application in pharmacy
  • Smelly seven secondary metabolites and their preparation methods and their application in pharmacy
  • Smelly seven secondary metabolites and their preparation methods and their application in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Preparation of 20(S)-dammar-25-ene-24(S)-hydroperoxyl-3β,6α,12β,20-tetrol(1) and its application in medicine.

[0022]

[0023] Step 1: Preparation of compound 20(S)-dammar-25-ene-24(S)-hydroperoxyl-3β, 6α, 12β, 20-tetrol(1).

[0024] The air-dried stinky seven was pulverized, extracted with methanol under reflux for 3 times at 60°C, and filtered. The filtrate was concentrated in vacuo to remove the organic solvent, applied to a macroporous resin chromatography column, eluted with pure water to remove the polysaccharide, and then eluted with methanol to obtain the crude saponin. The crude saponin was applied to a silica gel chromatography column and eluted with a solvent with a volume ratio of chloroform:methanol of 7:3 to obtain three fractions, namely A, B and C. Part B continued to be applied to RP-18, and gradient elution was carried out with a solvent with a methanol:water volume ratio from 1:9 to 9:1 to obtain 8 parts, namely B1-B8, and part B3 was applied to ...

Embodiment 2

[0033] Preparation of 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-6α,12β,20-triol(2) and its application in medicine.

[0034]

[0035] Step 1: Preparation of compound 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-6α, 12β, 20-triol(2).

[0036] The air-dried stinky seven was pulverized, extracted with methanol under reflux for 3 times at 60°C, and filtered. The filtrate was concentrated in vacuo to remove the organic solvent, applied to a macroporous resin chromatography column, eluted with pure water to remove the polysaccharide, and then eluted with methanol to obtain the crude saponin. The crude saponin was applied to a silica gel chromatography column and eluted with a solvent with a volume ratio of chloroform:methanol of 7:3 to obtain three fractions, namely A, B and C. Part B was continued on RP-18, and eluted with a solvent with a volume ratio of methanol:water from 1:9 to 9:1 to obtain 8 parts, namely B1-B8, and B1 was continued on silica gel chromatography column with c...

Embodiment 3

[0045] Preparation of 20(S)-dammar-12-oxo-23-ene-25-hydro-peroxyl-3β,6α,20-triol(3) and its application in medicine.

[0046]

[0047] Step 1: Preparation of compound 20(S)-dammar-12-oxo-23-ene-25-hydro-peroxyl-3β,6α,20-triol(3).

[0048] The air-dried stinky seven was pulverized, extracted with methanol under reflux for 3 times at 60°C, and filtered. The filtrate was concentrated in vacuo to remove the organic solvent, applied to a macroporous resin chromatography column, eluted with pure water to remove the polysaccharide, and then eluted with methanol to obtain the crude saponin. The crude saponin was applied to a silica gel chromatography column and eluted with a solvent with a volume ratio of chloroform:methanol of 7:3 to obtain three fractions, namely A, B and C. Part B was continued on RP-18, and eluted with a solvent with a volume ratio of methanol:water from 1:9 to 9:1 to obtain 8 parts, namely B1-B8, and B1 was continued on silica gel chromatography column with c...

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Abstract

The present invention provides smelly seven secondary metabolites 1-7 and a preparation method thereof, a pharmaceutical composition using it as an active ingredient, and its application in the preparation of medicines for preventing inflammatory diseases, and its use in the preparation of medicines for treating inflammatory diseases. application in medicine. The present invention mainly adopts phytochemical research means to obtain the above-mentioned compound 1-7 from Smellia, and make it into solid, liquid or paste dosage form. The anti-inflammatory compound obtained in the invention is a natural product, which is non-toxic and harmless to human cells.

Description

Technical field: [0001] The invention belongs to the field of medicine, and in particular relates to a secondary metabolite of stinky seven, a preparation method thereof, and its application in an anti-inflammatory pharmaceutical composition and its application in pharmacy. Background technique: [0002] Panax notoginseng (Burk.) F.H.Chen, also known as Panax notoginseng, blood ginseng, Jinbuchang, etc., is an important traditional Chinese medicine in my country, and is often used as a tonic or a drug to regulate blood circulation. It has various pharmacological activities in cardiovascular, cerebrovascular, nervous, immune and other systems, and also has protective effects on liver damage, anti-tumor and anti-inflammatory effects. Because of its high medicinal value and economic value, it has been cultivated in my country for more than 400 years. The natural distribution area of ​​Panax notoginseng is narrow, and it only grows in the area of ​​1500-1800 meters above sea le...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J7/00C07J9/00C07D307/16A61P29/00A61K31/575A61K31/57A61K31/341
CPCC07J9/00C07J7/002C07D307/16A61P29/00
Inventor 张颖君朱宏涛尚佳欢王东杨崇仁
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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