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Dammarane type triterpene compound and preparation method and application thereof

A technology for dammarane-type triterpenes and compounds, which is applied in the field of dammarane-type triterpenoid saponins and preparations thereof, can solve problems such as no dammarane-type triterpenoids, and achieve good economic benefits and industrialization. Application prospect, simple and easy preparation method, high purity effect

Inactive Publication Date: 2013-04-03
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The types and contents of saponins contained in Gynostemma pentaphyllum show great differences due to different varieties. At present, more than 160 kinds of triterpenoid saponins have been isolated from various species of Gynostemma pentaphyllum. Marane-type tetracyclic triterpenoids, but so far, there is no relevant report on dammarane-type triterpenoids with anti-inflammatory activity isolated from tetraploid Gynostemma pentaphyllum

Method used

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  • Dammarane type triterpene compound and preparation method and application thereof
  • Dammarane type triterpene compound and preparation method and application thereof
  • Dammarane type triterpene compound and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0026] (1) Preparation of tetraploid Gynostemma pentaphyllum extract

[0027] Tetraploid Gynostemma pentaphylla whole herb was dried, crushed, 3.8kg was taken, heated and refluxed with methanol at 65-70°C for 2 hours x 3 times, the extracts were combined, methanol was recovered under reduced pressure, and 800g of extract extract was obtained;

[0028] (2) extracting triterpenoid saponins

[0029] Add 4800ml of water to 800g of the extract to dissolve, extract with equal volumes of petroleum ether, ethyl acetate, and n-butanol in sequence to obtain n-butanol extract, and recover the solvent under reduced pressure to obtain 390 g of n-butanol part extract;

[0030] (3) Separation and purification

[0031] Mix the n-butanol part extract with silica gel, load the sample on a conventional silica gel chromatography column, and use dichloromethane-methanol system at a volume ratio of 100:1, 20:1, 10:1, 5:1, 1:1 , 1:2 for gradient elution, each part of 2000ml, a total of 27 parts of...

Embodiment 2

[0039] Anti-inflammatory activity test

[0040]The anti-inflammatory activity of monomeric compounds I and II was demonstrated on the expression levels of IL-1β, IL-6 and COX-2 mRNA in lipopolysaccharide (LPS)-induced RAW264.7 mouse macrophages.

[0041] 1. Preparation of drug solution

[0042] (1) The monomer compounds I and II were respectively prepared into 100 μg / ml solutions with DMSO, and stored at -4°C;

[0043] (2) LPS: E.Coli O111: B4 (Merck Millipore, USA, product number: LPS25), made into a 100 μg / mL solution with redistilled water, and stored at -20°C.

[0044] 2. Cell line: RAW 264.7 mouse macrophages, provided by the Chinese Academy of Sciences in Shanghai.

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Abstract

The invention relates to a dammarane type triterpene glycoside compound obtained by extracting and separating from tetraploid gynostemma pentaphyllum, and a preparation method and application of the dammarane type triterpene glycoside compound. The compound, and optical isomers, medicinal salt derivatives and solvates of the compound have a purpose of preparing an anti-inflammatory drug, can be applied in self-forms, and can also be applied by forming drug compositions with acceptable carriers in pharmacy; the preparation method is simple and easy to operate; and the obtained compound is high in purity, and has a good economic benefit and an industrial application prospect.

Description

technical field [0001] The invention belongs to the field of triterpenoid compounds and their preparation and application, in particular to dammarane-type triterpene saponins extracted and separated from tetraploid Gynostemma pentaphyllum and its preparation method and application. Background technique [0002] Gynostemma pentahyllum (Thunb.) Makino is a perennial herbaceous vine belonging to the genus Gynostemma of Cucurbitaceae. The currently known literature reports on Gynostemma pentaphyllum were first seen in the Ming Dynasty "Rescue Famine Materia Medica" in which Gynostemma pentaphyllum was used as a wild vegetable. Since the 1970s, people have conducted extensive modern research and development on the chemical composition, pharmacological effects, and clinical and health care applications of Gynostemma pentaphyllum. and anti-tumor and many other biological activities, and triterpenoid saponins are considered to be the main biological active components of Gynostemma ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J17/00A61K31/7048A61P29/00
Inventor 杨飞俞良莉史海明
Owner SHANGHAI JIAO TONG UNIV
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