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Application of dammarane triterpenes derivative and drug composition containing dammarane triterpenes derivative

A technology of dammarane triterpenoids and derivatives, applied in the field of medicinal chemistry, can solve problems such as Gynostemma pentaphyllum that cannot be further explained

Inactive Publication Date: 2009-09-16
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, the existing studies (see above) all focus on the anti-hepatic fibrosis pharmacological activity of the total saponins of Gynostemma pentaphylla from a single place of origin. This compound cannot fundamentally solve the problem of uncertain curative effect brought about by differences in origin and planting conditions, which is not conducive to the further development of Gynostemma pentaphyllum as a new anti-hepatic fibrosis drug with high technical content and application value.

Method used

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  • Application of dammarane triterpenes derivative and drug composition containing dammarane triterpenes derivative
  • Application of dammarane triterpenes derivative and drug composition containing dammarane triterpenes derivative
  • Application of dammarane triterpenes derivative and drug composition containing dammarane triterpenes derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 1000 grams of Gynostemma pentaphyllum was refluxed with 5L petroleum ether and extracted 3 times for 3 hours each time, and the obtained dregs were extracted 3 times with methanol refluxed for 3 hours each time. Concentrate the methanol extract under reduced pressure to obtain 70 g of Gynostemma pentaphyllum extractum, mix the samples with Gynostemma pentaphyllum extractum and silica gel, carry out gradient column chromatography elution with chloroform:methanol 100:10-100:50, and 100:20 elution fraction Concentrate under reduced pressure to obtain 15g, then eluted with MeOH with Sephadex LH-20 to remove flavonoids, then eluted with water: acetone 9:1-2:1 gradient through MCI resin column, combined 9:1 eluted fractions 1g was recovered under reduced pressure, and then MeOH:H 2 O=6:4 via RP-C 18 320 mg of pure compound 1 was obtained by elution, with a yield of 0.46%. Combined MCI resin 8:1 eluted fractions were recovered under reduced pressure to obtain 1.2g, and then ...

Embodiment 2

[0037] Compound 1 (1 g) obtained in Example 1 was hydrolyzed with 2N hydrochloric acid for 2 hours, distributed with equal volumes of ethyl acetate and water, after three extractions, the organic phases were combined, washed successively with saturated aqueous sodium carbonate solution and saturated brine , and then dried over anhydrous sodium sulfate overnight. Concentrated under reduced pressure to obtain 490 mg of crude compound 5, which was eluted through a silica gel column with petroleum ether: acetone = 9:1 to obtain 250 mg of pure compound 5 with a yield of 48.3%.

Embodiment 3

[0039] Compound 2 (1 g) obtained in Example 1 was hydrolyzed with 2N hydrochloric acid for 2 hours, distributed with equal volumes of ethyl acetate and water, after three extractions, the organic phases were combined, and washed successively with saturated aqueous sodium carbonate and saturated brine , and then dried over anhydrous sodium sulfate overnight. Concentrated under reduced pressure to obtain 451 mg of crude compound 6, which was eluted through a silica gel column with petroleum ether: acetone = 8:1 to obtain 210 mg of pure compound 6 with a yield of 40.5%.

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Abstract

The invention provides the application of a dammarane triterpenes derivative with the structure shown as the following formula (I), a drug composition containing the dammarane triterpenes derivative, and application thereof. The dammarane triterpenes derivative and the drug composition which can induce the apoptosis of hepatic stellate cells can be used for preparing drugs for preventing or treating hepatic fibrosis and hepatocirrhosis.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular, the invention relates to the use of dammarane triterpene derivatives and a pharmaceutical composition containing the derivatives. Background technique [0002] Liver fibrosis is an important pathological feature of chronic liver disease. Viruses, alcohol, autoimmune diseases and other etiologies can cause liver cell necrosis, regeneration and persistent fibrous proliferation, eventually leading to cirrhosis. It has been confirmed that liver fibrosis is a reversible disease, while liver cirrhosis is irreversible. Therefore, in the treatment of chronic liver disease, the prevention and treatment of liver fibrosis plays an important role. [0003] In recent decades, people have been looking for drugs for the treatment and / or prevention of liver fibrosis, and some drugs for the treatment of liver fibrosis have been developed, such as colchicine, salvianolic acid, soft liver tablets...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K31/58A61K36/424A61P1/16
Inventor 胡立宏沈旭蒋华良杨正毅陈静徐吉庆王旭陈琦冈虞靓
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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