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Hemsleya cucurbitane tetracyclic triterpenoid compound, pharmaceutical compositions containing same and application of compound and pharmaceutical composition

A cucurbitane-type, tetracyclic triterpenoid technology, which can be used in drug combinations, medical preparations containing active ingredients, steroids, etc., can solve the problems of less research on anticancer activity and the like

Active Publication Date: 2014-03-26
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

Pharmacological studies have shown that snow gallbladder has antibacterial effect, anti-tumor effect, and anti-HIV activity in vitro. There are many domestic studies on the chemical components of this plant, but there are few studies on anti-cancer activity.

Method used

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  • Hemsleya cucurbitane tetracyclic triterpenoid compound, pharmaceutical compositions containing same and application of compound and pharmaceutical composition
  • Hemsleya cucurbitane tetracyclic triterpenoid compound, pharmaceutical compositions containing same and application of compound and pharmaceutical composition
  • Hemsleya cucurbitane tetracyclic triterpenoid compound, pharmaceutical compositions containing same and application of compound and pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] 1. Extraction and separation

[0036] snow gall ( Hemsleya amabilis Diels) dried rhizome 9kg, 95% ethanol heating reflux extraction 3 times, each time 2h, combine the extracts and concentrate under reduced pressure to obtain 2018g ethanol extract, suspend with equal volume of water, and use ethyl acetate, n-butanol successively Extract to get 700g of ethyl acetate extract. 300 g of ethyl acetate was subjected to silica gel column chromatography, chloroform-methanol gradient elution (98:2, 95:5, 93:7, 90:10, 85:15, 80:20, 100:0) to obtain 14 fractions (Fr .A-Fr.N). Fr.D (69g) was recrystallized repeatedly to obtain compound 5 (4.8g). Fr.E was subjected to silica gel column chromatography, dichloromethane-methanol gradient elution (98:2, 96:4, 94:6, 92:8, 90:10, 80:20, 100:0) to obtain 6 fractions (Fr .E1-6). Fr.E5 (800mg) and Fr.E6 (12g) were subjected to SephadexLH-20 column chromatography (methanol-water, 45:55) and ODS column chromatography (methanol-water, 60:40...

preparation Embodiment 1

[0071] [Formulation Example 1] Tablet

[0072] Tablets are prepared according to methods known in the art, each containing the following ingredients:

[0073] Structural formula ( ) means compound (R 1 = H, R 2 =H) 2mg,

[0074] Lactose 80mg, magnesium stearate 10mg, polyvinylpyrrolidone 18mg.

preparation Embodiment 2

[0075] [Formulation Example 2] Tablet

[0076] Tablets are prepared according to methods known in the art, each containing the following ingredients:

[0077] Structural formula ( ) means compound (R 1 =β-D-Glc,R 2 =Ac) 1mg,

[0078] Structural formula ( ) means compound (R=Ac) 1mg,

[0079] Lactose 80mg, magnesium stearate 10mg, polyvinylpyrrolidone 18mg.

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PUM

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Abstract

The invention relates to a Hemsleya cucurbitane tetracyclic triterpenoid compound with a structural formula (I) which is described in the specification. In the structural formula (I), R1 is H and R2 is H; or, R1 is beta-D-Glc, and R2 is Ac. The invention further relates to a pharmaceutical composition with the compound as an active component and application of the compound and the pharmaceutical composition in drugs used for treating lung adenocarcinoma and colorectal carcinoma.

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] Cancer is an enemy that endangers human life. At present, 8.7 million new cancer patients are diagnosed every year in the world, and the number of deaths due to it reaches 6-7 million, accounting for one-tenth of the total death toll of the population. The incidence of cancer in our country is equally astonishing. According to the statistics of the World Health Organization, about 1.6 million new cancer cases and 1.3 million people die from cancer every year in our country. The number of cancer deaths is also increasing year by year. my country has become a high-incidence area for liver cancer, lung cancer, colon cancer, pancreatic cancer and other cancers, and the cancer mortality rate remains high. [0003] There are currently n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J17/00C07J9/00A61K31/575A61K31/704A61P35/00
Inventor 姚庆强周玲邓志鹏徐晓婷白虹孙敬勇
Owner INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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