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Hemsleya amabilis cucurbitane tetracyclotriterpene compounds, pharmaceutical composition containing compounds and application thereof

A cucurbitane-type, tetracyclic triterpene technology, applied in the direction of drug combination, medical preparations containing active ingredients, steroids, etc.

Active Publication Date: 2015-07-15
INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The applicant has disclosed several cucurbitane-type tetracyclic triterpene compounds in the patent documents with publication numbers CN103665082A and CN103626824A, and disclosed its application in the preparation of anticancer drugs, but its anticancer effect is still greatly improved space

Method used

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  • Hemsleya amabilis cucurbitane tetracyclotriterpene compounds, pharmaceutical composition containing compounds and application thereof
  • Hemsleya amabilis cucurbitane tetracyclotriterpene compounds, pharmaceutical composition containing compounds and application thereof
  • Hemsleya amabilis cucurbitane tetracyclotriterpene compounds, pharmaceutical composition containing compounds and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 1. Extraction and separation

[0034] Take 4 kg of dried snow gall tubers, crush them and extract them 3 times with ethanol under reflux, 2 hours each time. Concentrate the extract to obtain extract, add water to suspend, and then extract with petroleum ether, ethyl acetate and water-saturated n-butanol in sequence. The ethyl acetate part was subjected to repeated silica gel column chromatography, gel column chromatography, and ODS column chromatography, and the eluents were chloroform:acetone, chloroform:methanol, chloroform:methanol:water, and pure methanol, respectively. The n-butanol fraction was first subjected to D101 macroporous resin column chromatography, and eluted with 20%, 40%, 60%, and 80% ethanol solutions in sequence. A total of 11 compounds were obtained from the crude extract, 5 of which were new cucurbitacin compounds.

[0035] The following is the extraction and separation method in the previous application:

[0036] Snow gallbladder (Hemsleya amab...

preparation Embodiment 1

[0074] [Formulation Example 1] Tablet

[0075] Tablets are prepared according to methods known in the art, each containing the following ingredients:

[0076] Compound 1 [structural formula (I) represents compound (R 1 =CHO,R 2 =CH 3 , R 3 =OH)] 2mg,

[0077] Lactose 80mg, magnesium stearate 10mg, polyvinylpyrrolidone 18mg.

preparation Embodiment 2

[0078] [Formulation Example 2] Tablet

[0079] Tablets are prepared according to methods known in the art, each containing the following ingredients:

[0080] Compound 4 [compound represented by structural formula (II) (R=H)] 2 mg,

[0081] Lactose 80mg, magnesium stearate 10mg, polyvinylpyrrolidone 18mg.

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Abstract

The invention relates to novel hemsleya amabilis cucurbitane tetracyclotriterpene compounds disclosed as structural formula (I) or structural formula. The invention also relates to a pharmaceutical composition using the compounds as active ingredients and application of the compounds and pharmaceutical composition in drugs for treating lung adenocarcinoma, colon cancer and prostate cancer.

Description

technical field [0001] The invention relates to a new class of compounds, specifically a cucurbitane-type tetracyclic triterpene compound, a pharmaceutical composition containing the compound and applications thereof. Background technique [0002] Hemsleya amabilis Diels, also known as chrysanthemum tortoise lotus and golden pot, are the dried root tubers of Hemsleya amabilis Diels and several plants of the same genus. This product is bitter and cold in nature, enters the two meridians of stomach and large intestine, and has the effects of clearing away heat and detoxification, antibacterial and anti-inflammatory. There are 31 species of Eucalyptus in the world, except for 2 species produced in India and Vietnam, they are mainly distributed in my country's Yunnan, Guizhou and Sichuan provinces. Many plants in this genus are commonly used traditional Chinese medicines. The main components of the plant of the genus Electra are oleanane-type pentacyclic triterpenes and their s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J17/00A61K31/704A61P35/00
CPCC07J17/005
Inventor 姚庆强周玲邓志鹏李莹郑重飞孙敬勇牟艳玲刘拥军
Owner INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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