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Oleanane-type pentacyclic triterpene compound of Xiacao, pharmaceutical composition containing the compound and application thereof

An oleanane-type, pentacyclic triterpenoid technology, which can be used in drug combinations, medical preparations containing active ingredients, steroids, etc., can solve the problem of anti-tumor drug resistance, large toxic and side effects, and low cancer efficacy , unsatisfactory effects, etc.

Inactive Publication Date: 2016-09-07
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] In recent years, although important progress has been made in the research and development and application of anticancer drugs, and chemotherapy for certain types of tumors has achieved outstanding curative effects, there is still no effective drug to cure most cancer patients
Although chemotherapy drugs have a certain curative effect, many antineoplastic drugs have developed drug resistance and severe side effects during clinical application; the curative effect of Chinese patent medicines on cancer is generally low, such as Shenlian Capsules for lung cancer and gastric cancer. 3.5%, the remission rate of Ruanjian Oral Liquid on liver cancer lesions was 6.0%, and the curative effect was not ideal

Method used

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  • Oleanane-type pentacyclic triterpene compound of Xiacao, pharmaceutical composition containing the compound and application thereof
  • Oleanane-type pentacyclic triterpene compound of Xiacao, pharmaceutical composition containing the compound and application thereof
  • Oleanane-type pentacyclic triterpene compound of Xiacao, pharmaceutical composition containing the compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment 1

[0023] 1. Extraction and separation

[0024] Xiacao (Gypsophila oldhamiana Miq.) was naturally dried and crushed, 5 kg was extracted with methanol in a Soxhlet extractor, the extract was concentrated under reduced pressure to obtain 1000 g of methanol extract, dissolved in water, and then successively washed with petroleum ether (60 ℃~90℃), ethyl acetate and n-butanol extraction to obtain 19g of petroleum ether extract, 45g of ethyl acetate extraction and 165g of n-butanol extract. The ethyl acetate portion was chromatographed on a silica gel column, eluted with a gradient of chloroform-methanol (100:0~80:20), and eluted repeatedly through Sephadex LH-20 column chromatography (methanol), and preparative HPLC to obtain compound 1 (15.7 mg), compound 2 (13.4 mg), compound 3 (7.5 mg), compound 4 (11.4 mg).

[0025] Obtain two new oleanane type pentacyclic triterpenoids (compound represented by structural formula (I, III) of the present invention) and two oleanane type pentacycli...

Embodiment 1

[0037] The four oleanane-type pentacyclic triterpenoids obtained in Example 1 were dissolved with dimethyl sulfoxide (DMSO, final concentration 0.8%) respectively, and were mixed with RPMI1640 medium containing 15% calf serum Dubbed 1mg / ml for use, diluted to the required concentration when used. The positive control drug was Doxorubicin.

[0038] 1.2 Cell lines and reagents

[0039] H460 (human lung adenocarcinoma), SGC-7901 (human gastric adenocarcinoma), the above cell lines were purchased from the Cell Bank of the Chinese Academy of Sciences, and were preserved by the Pharmacology Department of the Institute of Materia Medica, Shandong Academy of Medical Sciences. DMEM high-glucose medium was purchased from Gibco, USA. Calf serum and non-essential amino acids were purchased from Hyclone Company. Trypsin and MTT reagent were purchased from Sigma.

[0040] 1.3 Experimental method

[0041] Using the conventional MTT method, the two tumor cells were cultured with 10% calf...

preparation experiment example 1

[0051] Preparation experiment example 1 tablet

[0052] Tablets are prepared according to methods known in the art, each containing the following ingredients:

[0053] 2 mg of the compound represented by the structural formula (I), 70 mg of lactose, 8 mg of magnesium stearate, and 15 mg of polyvinylpyrrolidone.

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Abstract

The invention relates to novel gypsophila elegans oleanane type pentacyclic triterpenoids represented by structure formulae (I, II, III and IV). The invention further relates to a pharmaceutical composition containing the components serving as active components, and application of the compounds and the pharmaceutical composition in medicines for treating gastric adenocarcinoma and adenocarcinoma of the lung. The structure formulae are shown in the specification.

Description

technical field [0001] The present invention relates to a new class of compounds, specifically a oleanane type pentacyclic triterpene compound, a pharmaceutical composition containing the compound and its application. Background technique [0002] Cancer is an enemy that endangers human life. With the acceleration of industrialization and urbanization and the aggravation of environmental pollution, the number of deaths from cancer in the country has also increased year by year, and cancer has become a global public health problem. 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] In recent years, although important progress has been made in the development and application of anticancer drugs, and chemotherapy for certain types of tumors has achieved outstanding curative effects, there is still no effective drug to cure most cancer patients. Altho...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00C07J71/00A61K31/585A61K31/56A61P35/00
CPCC07J63/008C07J71/0005
Inventor 孙敬勇解龙霄牟艳玲王燕郑志伟张浩超王菊王风玲刘爱芹
Owner INST OF PHARMACY SHANDONG PROV ACAD OF MEDICAL SCI
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