Isopentenylated flavonoid compound sinoflavonoids as well as preparation method and application thereof

A technology of prenylated flavonoids and peach seven, which is applied in the field of medicine to achieve the effect of good reproducibility, significant economic and social benefits, and high purity

Inactive Publication Date: 2020-07-31
HENAN UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] In view of the above situation, in order to overcome the defects of the prior art, the purpose of the present invention is to provide a kind of prenylated flavonoids amygdone and its preparation method and application, which can effectively solve the problem of extracting isopentene from lotus lobata. The problem of ylated flavonoids apricotone and its use in the preparation of anti-prostate cancer drugs

Method used

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  • Isopentenylated flavonoid compound sinoflavonoids as well as preparation method and application thereof
  • Isopentenylated flavonoid compound sinoflavonoids as well as preparation method and application thereof
  • Isopentenylated flavonoid compound sinoflavonoids as well as preparation method and application thereof

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Embodiment 1

[0013]In the specific implementation of the present invention, a method for preparing the prenylated flavonoid compound apricotone, using 9 kg of lobular lotus medicinal material as raw material, extracting 3 times with 18 L of ethanol with a volume concentration of 95% by heating and refluxing, the extraction temperature at 95°C, each extraction time is 1.5h (hour, the same below), recover ethanol under reduced pressure to obtain extract-like ethanol extract, suspend in 3.2L of distilled water, and successively add petroleum ether, dichloromethane, ethyl acetate Ester and n-butanol were extracted 3 times, 3.2 L each time, and the time was 1.5 h; the ethyl acetate extraction part was separated by silica gel column chromatography, and the volume ratio was 100:0, 100:5, 100:7, 100: 10. 100:30, 100:50, 100:70, 100:100, 100:200, 0:100 petroleum ether-acetone mixed solvent system for gradient elution, each gradient uses 13L eluent, the flow rate is 15mL / min, every 500mL volume is ...

Embodiment 2

[0015] In the specific implementation of the present invention, a method for preparing the prenylated flavonoid compound apricotine, using 6 kg of the lobular lotus medicinal material as the raw material, is heated and refluxed 3 times with ethanol that is 5 times the weight of the raw material and has a volume ratio of 75%. , the extraction temperature is 90°C, and each extraction time is 2h (hours, the same below), and the ethanol is recovered under reduced pressure to obtain an extract-like ethanol extract, which is suspended in 2L of distilled water, and is sequentially mixed with petroleum ether, dichloromethane, acetic acid Ethyl and n-butanol were extracted 3 times, 2 L each time, and the time was 1.5 h; the ethyl acetate extraction part was separated by silica gel column chromatography, and the volume ratio was 100:0, 100:5, 100:7, 100: 10. 100:30, 100:50, 100:70, 100:100, 100:200, 0:100 petroleum ether-acetone mixed solvent system for gradient elution, each gradient us...

Embodiment 3

[0017] In the specific implementation of the present invention, a method for preparing the prenylated flavonoid compound apricotone, using 8 kg of the lobular lotus medicinal material as raw material, extracting 3 times with 24 L of ethanol with a volume concentration of 85% by heating and refluxing, the extraction temperature At 92°C, each extraction time is 1.8h, recover ethanol under reduced pressure to obtain extract-like ethanol extract, suspend in 2.8L of distilled water, and extract with petroleum ether, dichloromethane, ethyl acetate, and n-butanol in sequence 3 times, 2.8L each time, the time is 1.8h; the ethyl acetate extraction part was separated by silica gel column chromatography, and the volume ratios were 100:0, 100:5, 100:7, 100:10, 100:30, 100:50, 100:70, 100:100, 100:200, 0:100 petroleum ether-acetone mixed solvent system for gradient elution, each gradient uses 11.7L eluent, the flow rate is 13mL / min, every 450mL The volume is fractions, and 260 fractions ar...

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Abstract

The invention relates to isopentenylated flavonoid compound sinoflavonoids as well as a preparation method and application thereof. The method can be used for effectively solving the problem of extracting the isopentenylated flavonoid compound sinoflavonoids from fructus podophylli, and preparing of the products into anti-prostate cancer drugs. The isopentenylated flavonoid compound sinoflavonoidscomprise Sinoflavanonoid NF I, Sinoflavanonoid NG II, Sinoflavanonoid NH III, Sinoflavanonoid NI IV which are extracted from fructus podophylli. The novel isopentenylated flavonoid compound sinoflavonoids NF-NI have cytotoxic activity on human prostate cancer cell strain PC-3, have the prospect of being prepared into anti-prostatic cancer medicine; the repeatability of the preparation method is high; the purity of obtained compounds is high; it in favor of further pharmacological and clinical research of the compounds, and the medicinal value of the fructus podophylli medicine and a new way for preparing the anti-prostatic cancer medicine are developed.

Description

technical field [0001] The invention relates to medicine, in particular to a prenylated flavonoid compound apricotone which is extracted from lotus lobata and used to prepare anti-prostate cancer drugs and its preparation Methods and applications. Background technique [0002] Prostate cancer is the most common malignant tumor of the genitourinary system in men, and its incidence is increasing in most countries. Fast malignant tumors. After the age of 50, with the increase of age, the incidence of prostate cancer increases rapidly, and it has become one of the problems that seriously affect the health of elderly men. At present, there is no clear method for radically curing prostate cancer. Surgery and radiotherapy are commonly used clinical treatments, but both have certain limitations. The survival rate after treatment is not high, and there are many complications. Synthetic anti-prostate cancer drugs widely used in clinical practice generally have side effects such as ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/04C07D493/14C07D407/04C07D311/40C07D311/28A61P35/00
CPCC07D493/04C07D493/14C07D407/04C07D311/40C07D311/28A61P35/00
Inventor 王俊敏刘延霆孙彦君冯卫生陈辉陈豪杰赵晨韩瑞杰潘如意柴站
Owner HENAN UNIV OF CHINESE MEDICINE
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