Panaxadiol-type triterpene saponins with anti-inflammatory activity

A technology of ginseng diol and triterpene saponins, which is applied in the direction of organic active ingredients, anti-inflammatory agents, and medical preparations containing active ingredients, etc., can solve the problems of limited growth environment and insufficient resources of Panax notoginseng, and achieve the effect of inhibiting release

Active Publication Date: 2022-04-15
TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The medicinal parts of Panax notoginseng are mainly its roots and rhizomes, but due to the limited suitable growth environment, the resources of Panax notoginseng are insufficient

Method used

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  • Panaxadiol-type triterpene saponins with anti-inflammatory activity
  • Panaxadiol-type triterpene saponins with anti-inflammatory activity
  • Panaxadiol-type triterpene saponins with anti-inflammatory activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Preparation of Notoginseng Leaf Extract

[0081] 8 kg of dried Panax notoginseng leaves were cut into pieces, heated and refluxed for 3 times with 10 times the amount of 50% ethanol solution for 3 hours, 2 hours, and 2 hours. The filtrates were combined, and the solvent was recovered under reduced pressure to obtain 2.67 kg of extract. Get extractum 2.1kg and be dissolved in 20L water, separate through D101 macroporous adsorption resin chromatographic column, elution solvent is water → 95% ethanol, thereby obtained water and 95% ethanol eluate, are respectively 760.0g and 695.0g. Among them, the 95% ethanol eluate was used as the Panax notoginseng leaf extract rich in panaxadiol-type triterpene saponins for subsequent experiments.

Embodiment 2

[0083] Preparation and structure identification of panaxadiol-type triterpene saponins 1-7

[0084] Compounds 1-7 were isolated simultaneously and thus described in one example.

[0085] 1. [Isolation and preparation of compounds 1-7]

[0086] Get the 95% ethanol eluent 150.0g that obtains in the above-mentioned embodiment 1, through silica gel column chromatography [elution solvent: CH 2 Cl 2 →CH 2 Cl 2 / MeOH (volume ratio is 100:3→100:7→10:1→8:1→3:1→2:1→1:1)→MeOH] to obtain 12 components [wherein, Fr.1( 1.3g), Fr.2(6.2g), Fr.3(2.1g), Fr.4(5.4g), Fr.5(6.8g), Fr.6(6.5g), Fr.7(56.3g ), Fr.8 (28.2g), Fr.9 (16.4g), Fr.10 (7.2g), Fr.11 (3.7g), Fr.12 (2.0g)].

[0087] Fr.6 (6.2g) was subjected to silica gel column chromatography [elution solvent: CH 2 Cl 2 -MeOH-water (volume ratio is 40:3:1→30:3:1→25:3:1→15:3:1→13:3:1→12:3:1→10:3:1→ 8:3:1→6:3:1, lower layer)→MeOH] to obtain 13 components [Fr.6-1(32.0mg), Fr.6-2(28.0mg), Fr.6-3( 40.7mg), Fr.6-4(74.5mg), Fr.6-5(757.8mg), F...

Embodiment 3

[0139] Determination of Biological Activities of Panaxadiol Type Triterpene Saponins 1~7

[0140] As immune cells distributed throughout the body, macrophages play a central role in the immune surveillance system. After pathogens enter the body, macrophages can immediately and indirectly play an immune role by releasing various inflammatory mediators. RAW264.7 cells, as a type of macrophages, are commonly used cell lines in the study of microbiology, immunology and other related subjects because of their strong ability to adhere and phagocytize antigens. Lipopolysaccharide (LPS) can stimulate RAW 264.7 cells to produce an acute inflammatory response and release various inflammatory factors such as nitric oxide (NO), which can participate in the regulation of the occurrence and development of inflammation in the body, and its content can indirectly reflect inflammation the extent to which it occurs.

[0141] The present invention adopts the RAW 264.7 cell model induced by LPS...

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Abstract

The present invention utilizes a variety of separation means, including forward and reverse phase silica gel column chromatography, macroporous adsorption resin column chromatography, gel column chromatography and preparation of high performance liquid chromatography, etc., and obtains 7 leaves of Panax notoginseng Panaxadiol-type triterpene saponins including new compounds. These 7 new compounds have been shown to have anti-inflammatory activity by activity assay, which has laid a material foundation for further pharmacological activity screening and clinical research to develop anti-inflammatory drugs with definite curative effect and less toxic and side effects.

Description

technical field [0001] The invention belongs to the field of natural medicines, and in particular relates to a class of novel panaxadiol-type triterpene saponins with anti-inflammatory activity. Background technique [0002] Inflammation is a basic pathological process in which the living tissue with vascular system is stimulated by various damage factors and is mainly a defense response. Anything that can cause tissue damage can be a cause of inflammation. The basic pathological changes of inflammation usually include degeneration, exudation and hyperplasia of local tissues. Inflammation is closely related to the occurrence and development of various diseases such as diabetes, tumors, and cardiovascular and cerebrovascular diseases. [0003] Panax notoginseng (Burk.) F.H.Chen is a plant of the genus Panax of the family Araliaceae, also known as Tianqi, blood ginseng, Tianzhi, Dianzhi, and Sanqi. It is mainly produced in Wenshan Prefecture, Yunnan, and in Guangxi, Guangdon...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61K31/704A61K36/258A61P29/00A61K8/63A61Q19/00A61K127/00
CPCC07J63/008A61K36/258A61P29/00A61K8/63A61Q19/00A61K2800/10
Inventor 张祎王涛阮静雅赵薇孙璠于海洋刘梦扬高秀梅刘二伟
Owner TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE
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