Application of Hyperforin derivant in preparing drugs

A technology of hypericin and hypericin ethyl ester is applied in the field of hypericin derivatives to achieve the effect of good therapeutic effect

Inactive Publication Date: 2011-01-05
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, in terms of anti-tumor, there are no reports about hyperforin ethyl ester and hyperforin-N, N dicyclohexylamine salt

Method used

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  • Application of Hyperforin derivant in preparing drugs
  • Application of Hyperforin derivant in preparing drugs
  • Application of Hyperforin derivant in preparing drugs

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0030] One, the preparation method of the extract rich in hyperforin

[0031] (1) Take the above-ground part containing Hypericum perforatum (Hypericum perforatum L.), extract 4-10 times the dry weight of the medicinal material each time with a polar solvent containing 1-5% composite stabilizer at room temperature and stir for 2-6 hours , leaching 2-3 times; said polar solvent is alcohols (usually methanol, ethanol, propanol or isopropanol), ketones (usually acetone), ketone water mixed solvent or ketone alcohol water with any The mixed solvent of ratio; Said composite stabilizer is the mixture of VC or VC derivative and VE or VE derivative and organic acid, and the mixing ratio is VC or VC derivative: VE or VE derivative: organic Acid=20~200: 20~200: 1 (mass ratio); Said organic acid is usually any one in citric acid, benzoic acid, tartaric acid or their combination in any proportion;

[0032] (2) Concentrate the above obtained extract to a crude drug content of 0.1-1 g / ml, ...

Embodiment 1

[0045] Embodiment 1, the preparation that is rich in the extract of hyperforin

[0046] The Hypericum perforatum medicinal material is pulverized, and 300 g of medicinal material powder is taken, and 800 milliliters of acetone leaching containing 1% compound stabilizer (stabilizer is composed of VC: VE: citric acid=50: 100: 1) with 800 milliliters of acetone extraction is carried out altogether 3 times, each The next day, combine the acetone extracts, recover the acetone to 1000 ml, and then add 250 ml of distilled water. Extract with 1300 milliliters of petroleum ether, extract 2 times in total, combine petroleum ether phase and add vitamin E to the content of 1%. Concentrate to 600 ml and extract twice with 500 ml of 50% ethanol, and discard the ethanol phase. The petroleum ether phase was basified with 800 ml of 1% NaOH in 50% ethanol, and the petroleum ether phase was discarded. Use 10% hydrochloric acid to adjust the alkali-alcoholic solution to pH = 2, then extract 3 t...

Embodiment 2

[0047] Embodiment 2, the synthesis of hyperforin ethyl ester

[0048] The extract of hypericin perforatum was dissolved in pyridine solution, after it was completely dissolved, acetic anhydride was added to the solution, stirred and reacted in the dark at room temperature, dried, and after 24 hours of reaction, thin-layer chromatography showed that the reaction was relatively complete, and the raw material point was almost complete. disappear. Ice water was added to the reaction mixture to stop the reaction.

[0049] Add n-hexane-diethyl ether mixture (3:1) for extraction three times, combine the organic phases, and successively wash with saturated NaHCO 3 Wash with saturated brine. Anhydrous sodium sulfate was dehydrated overnight, the solid sodium sulfate was removed by filtration, and the filtrate was concentrated to dryness to obtain a brownish yellow solid. Through silica gel column chromatography (100-200 mesh), first elute with petroleum ether, and then elute with pe...

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PUM

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Abstract

The invention discloses an application of Hyperforin ethyl ester with a structure I1 and / or Hyperforin-N, N dicyclohexyl ammonium with a structure I2 in preparing drugs capable of treating tumor. The pharmacological pharmacodynamics experiment proves that the Hyperforin ethyl ester and the Hyperforin-N, N dicyclohexyl ammonium of the invention have the action of specific proliferation inhibition, apoptosis induction, cell cycle influence and the like on human tumor cells cultured in vitro and provide new drug selection for clinic tumor therapy.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the application of two hyperforin derivatives, namely hyperforin ethyl ester and hyperforin-N,N dicyclohexylamine salt, in pharmaceuticals. Background technique [0002] Malignant tumors are common and one of the major diseases that seriously threaten human life and quality of life. In 2000, there were about 10 million new cancer cases worldwide, 6.2 million deaths, and 22.4 million existing cases. The incidence of cancer has been on the rise for nearly 30 years in the late 20th century. According to the current trend, the World Health Organization (WHO) predicts that by 2020, with the global population reaching 8 billion, there will be 20 million new cancer cases, including deaths It will reach 12 million, and cancer will become the first killer of human beings in the new century. Statistics show that the common malignant tumors of human life and health in my country include: lung ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/22A61K31/122A61K31/13A61P35/00A61P35/02
Inventor 杨得坡王一飞刘劲芸刘忠王冬梅孙凤
Owner SUN YAT SEN UNIV
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