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Steroidal compounds as well as extraction method and application thereof

A compound and steroid technology, applied in the field of steroid compounds and extraction

Active Publication Date: 2018-08-24
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the steroidal compounds extracted from Zizhi and their application in the preparation of antitumor drugs as HK2 inhibitors or IDH inhibitors have not been reported yet.

Method used

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  • Steroidal compounds as well as extraction method and application thereof
  • Steroidal compounds as well as extraction method and application thereof
  • Steroidal compounds as well as extraction method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] The extraction method of steroidal compound is characterized in that comprising the steps:

[0060] (1) Take the dry fruiting body (9.5kg) of the fungus Zizhi of the genus Ganoderma lucidum of Polyporaceae as raw material, add a volume fraction of 10 times the mass of the raw material and be 90% ethanol aqueous solution, reflux extraction twice, each extraction for 2 hours, and combine to obtain the extraction solution, the solvent is reclaimed under reduced pressure, and after concentrating, total extract (214g) is obtained;

[0061] (2) The total extract is dispersed into 5L water, extracted successively with cyclohexane, ethyl acetate and n-butanol, and the solvent is recovered under reduced pressure from the cyclohexane, ethyl acetate and n-butanol extract to obtain the cyclohexane layer respectively Extract, ethyl acetate layer extract, n-butanol layer extract and the remaining water layer samples;

[0062] (3) Cyclohexane layer extract (37g) and ethyl acetate lay...

Embodiment 2

[0083] The extraction method of steroid compound, comprises the steps:

[0084] (1) Take the dry fruiting body of the fungus Zizhi of the genus Ganoderma lucidum of Polyporaceae as raw material, add a volume fraction of 8 mass times of the raw material and be 70% ethanol aqueous solution, reflux extraction for 3 times, extract for 2 hours each time, combine to obtain the extract, and depressurize Recover solvent, obtain total extract after concentrating;

[0085] (2) The total extract is dispersed into 5 times of quality water, extracted successively with cyclohexane, ethyl acetate and n-butanol, and the solvent is recovered under reduced pressure from the cyclohexane, ethyl acetate and n-butanol extract to obtain cyclohexane respectively Alkane layer extract, ethyl acetate layer extract, n-butanol layer extract and the remaining water layer samples;

[0086](3)-(24) are the same as embodiment 1 (3)-(24).

Embodiment 3

[0088] The extraction method of steroid compound, comprises the steps:

[0089] (1) Take the dry fruiting body of the fungus Zizhi of the genus Ganoderma lucidum of Polyporaceae as raw material, add a volume fraction of 10 times the mass of the raw material and be 90% ethanol aqueous solution, reflux extraction 2 times, extract for 2 hours each time, combine to obtain the extract, and depressurize Recover solvent, obtain total extract after concentrating;

[0090] (2) The total extract is dispersed into 10 times of quality water, extracted successively with cyclohexane, ethyl acetate and n-butanol, and the solvent is recovered under reduced pressure from the cyclohexane, ethyl acetate and n-butanol extracts to obtain cyclohexane respectively Alkane layer extract, ethyl acetate layer extract, n-butanol layer extract and the remaining water layer samples;

[0091] (3)-(24) are the same as embodiment 1 (3)-(24).

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Abstract

The invention belongs to the technical field of medicines, and discloses an extraction method for steroidal components in glossy ganoderma and an application of the steroidal components. The compoundshave structures represented by a formula (I) and a formula (II) shown in the description. The compounds and compositions of the compounds disclosed by the invention have an inhibitory effect on glycolysis first rate-limiting enzyme HK-2 or isocitrate dehydrogenase (IDH1), thereby having a significant anti-tumor effect; and the compounds have good research and development prospects.

Description

technical field [0001] The invention relates to the field of traditional Chinese medicine extraction, and relates to a steroid compound, an extraction method and an application thereof. Background technique [0002] In recent years, studies have found that the overexpression of the key metabolic enzyme hexokinse 2 (HK2) in the first step of glycolysis is widespread in tumor cells, and it mainly plays the role of phosphorylating glucose in vivo. research shows, [0003] HK2 plays an important role in tumorigenesis and development; there are low levels of glucose-derived nucleotides and glutamine-derived carbon utilization in HK2 knockout lung cancer cells. The above studies suggest that HK2 is required for ATP synthesis, nucleotide synthesis, fatty acid synthesis, serine biosynthesis pathways, and carbon transfer from glycolysis to the tricarboxylic acid cycle (TCA) (Patra K C, Wang Q, Bhaskar P T , et al. Hexokinase 2 is required for tumor initiation and maintenance and it...

Claims

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Application Information

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IPC IPC(8): C07D307/93C07J9/00A61K31/365A61K31/575A61P35/00
CPCC07D307/93C07J9/00
Inventor 陈丽霞李华郑梦竹高苏钰吴灿荣鲍凤艳
Owner SHENYANG PHARMA UNIVERSITY
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