Application of ingenane diterpene compound in preparation of antitumor drug

A technology of ingenuin and anti-tumor drugs, applied in anti-tumor drugs, drug combinations, organic chemistry and other directions, can solve problems such as small toxic and side effects, achieve low toxic and side effects, low medicinal material yield, good anti-breast cancer cells Active and selective effects

Active Publication Date: 2015-05-20
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, in the drug market for the treatment of breast cancer, there are basically no natural product drugs with significant efficacy, low toxicity and side effects, and strong targeting. activity report

Method used

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  • Application of ingenane diterpene compound in preparation of antitumor drug
  • Application of ingenane diterpene compound in preparation of antitumor drug
  • Application of ingenane diterpene compound in preparation of antitumor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation and Activity of Total Ingenue Parts

[0049] 1. Separation of total ingenins

[0050] Preparation process: 10 kg of Gansui medicinal material, 8 times the amount (mass ratio) of 95% (volume percentage) ethanol, reflux extraction for 2 hours, filter, then add 6 times the amount of 95% ethanol for reflux extraction for 1 hour, filter, combine the filtrate, and recover Until there is no alcohol smell, add an equal volume of ethyl acetate for extraction, let stand to separate layers, extract three times, combine the ethyl acetate layers, recover the solvent, concentrate to dryness, add weight to the extract and dissolve it in methanol with a volume ratio of 1:1, 0.45 μm microporous membrane filtration, reversed-phase gel C18 (YMC GEL-ODS) column chromatography on the filtrate, respectively using 75% MeOH (methanol), 85% MeOH, 95% MeOH, MeOH, isopropanol , dichloromethane elution, the volume ratio of the extract weight (g) to the eluent is 1g:500ml, co...

Embodiment 2

[0073] The preparation of embodiment 2 ingenia diterpenoids

[0074] 1. Separation of ingenoids:

[0075] Preparation process: 10 kg of kansui medicinal material, 10 times the amount (mass ratio) of 95% (volume percentage) methanol, reflux extraction for 3 hours, filtered, then added 8 times the amount of methanol for reflux extraction for 2 hours, filtered, combined filtrates, recovered to nothing Alcoholic smell, add an equal volume of dichloromethane to extract, let stand to separate layers, extract three times, combine the dichloromethane layers, recover the solvent, concentrate to dryness, add weight to volume of the extract and dissolve it in methanol with a volume ratio of 1:1, 0.45μm Pore ​​membrane filtration, reversed-phase gel C18 (YMC GEL-ODS) column chromatography, eluted with volume concentrations of 60% acetone, 75% acetone, 85% acetone, acetone, isopropanol, and dichloromethane, respectively, The volume ratio of the extract weight (g) to the eluent is 1g:500ml...

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Abstract

The invention discloses an application of an ingenane diterpene compound in preparation of antitumor drug. The ingenane diterpene compound is one or more of the ingenane diterpene compound shown in a formula (1). The ingenane diterpene compound can obviously inhibit the propagation activity of breast cancer cells, compared with a traditional tumor therapeutic method, tumor inhibitory effect is good, toxic and side effects are little, targeting property is strong, the ingenane diterpene compound has no damage to normal cells, security can be guaranteed at maximum degree, the ingenane diterpene compound provides a latent novel medicine development purpose for treating breast cancer, and can be a further research as an anti-breast cancer candidate medicine.

Description

technical field [0001] The present invention relates to the application of an ingenoid compound, in particular to the application of an ingenoid compound in the preparation of antitumor drugs. Background technique [0002] Cancer is the number one malignant disease that seriously threatens human life, and breast cancer has become one of the cancers that threaten women's health the most. With the development of modern society and economy, unhealthy living environment factors caused by various social problems and family problems have increased the incidence of female breast cancer year by year. At present, there are an average of 1.3 million new breast cancer cases in the world every year, and in recent years there have been continuous An upward trend. In recent years, the growth rate of the incidence of breast cancer in my country is 1-2 percentage points higher than that of high-incidence countries, and it shows a clear trend of rejuvenation. [0003] Breast cancer is a gene...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/231A61K31/22A61P35/00C07C69/587C07C69/28C07C67/48
CPCY02P20/582
Inventor 果德安吴婉莹侯晋军杨洲姚帅龙华丽笪娟蔡录影
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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