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Hemsleya amabilis cucurbitane tetracyclic triterpene compound, pharmaceutical composition comprising compound and application of pharmaceutical composition and compound

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: 2014-03-12
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 amabilis cucurbitane tetracyclic triterpene compound, pharmaceutical composition comprising compound and application of pharmaceutical composition and compound
  • Hemsleya amabilis cucurbitane tetracyclic triterpene compound, pharmaceutical composition comprising compound and application of pharmaceutical composition and compound
  • Hemsleya amabilis cucurbitane tetracyclic triterpene compound, pharmaceutical composition comprising compound and application of pharmaceutical composition and compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 1. Extraction and separation

[0035] snow gall ( Hemsleya amabilis Diels) dried rhizomes 9 kg, 95% ethanol heating reflux extraction 3 times, 2 h each time, the extracts were combined and then concentrated under reduced pressure to obtain 2018 g ethanol extract, suspended in an equal volume of water, followed by ethyl acetate, Extract with n-butanol to obtain 700 g of ethyl acetate extract. The ethyl acetate fraction (300g) was chromatographed on a silica gel column with 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 (69 g) was obtained by repeated recrystallization 4 (4.8 g). 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. E 1-6). Fr. E 6 (12 g) was obtained by Sephadex LH-20 column chromatography (methanol-water, 45:55), ODS column chromatography (methanol-...

preparation Embodiment 1

[0069] [Formulation Example 1] Tablet

[0070] Tablets are prepared according to methods known in the art, each containing the following ingredients:

[0071] Structural formula ( ) means compound 2mg, lactose 80mg, magnesium stearate 10mg,

[0072] Polyvinylpyrrolidone 18mg.

preparation Embodiment 2

[0073] [Formulation Example 2] Tablet

[0074] Tablets are prepared according to methods known in the art, each containing the following ingredients:

[0075] Structural formula ( ) represents compound 1mg, structural formula ( ) means compound (R=H) mg,

[0076] Lactose 80mg, magnesium stearate 10mg, polyvinylpyrrolidone 18mg.

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Abstract

The invention relates to a novel hemsleya amabilis cucurbitane tetracyclic triterpene compound shown as the structural formula (I) in the specification. The invention further relates to a pharmaceutical composition using the compound as an active ingredient, as well as the application of the compound and the pharmaceutical composition in drugs for the treatment of adenocarcinoma of lung and colon 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] 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): C07J17/00A61K31/704A61P35/00A61K31/575
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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