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Alkaloid compounds, method for preparing same and applications as enzyme inhibitors

A compound and alkaloid technology, applied in the field of alkaloid compounds with enzyme inhibitory activity and their preparation, can solve problems such as enzyme inhibitors that have not yet been seen, and achieve the effect of not being limited by resources and having broad application prospects

Active Publication Date: 2011-04-13
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the particularity of the marine environment, marine fungi can provide metabolites that terrestrial fungi cannot provide, but so far no enzyme inhibitor products with medicinal value have been obtained from marine fungi

Method used

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  • Alkaloid compounds, method for preparing same and applications as enzyme inhibitors
  • Alkaloid compounds, method for preparing same and applications as enzyme inhibitors
  • Alkaloid compounds, method for preparing same and applications as enzyme inhibitors

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Embodiment Construction

[0010] Preparation of Compounds of the Invention

[0011] (1) The medium used for the culture of the fungus Penicillium sp.386 contains 1.0% glucose (percentage by weight, the same below), 0.1% yeast extract, 0.2% peptone, 1.0% agar, 0.3% sodium chloride, and the rest is water , when used to make a test tube slant, fungal strains were cultured at 30 ° C for 5 days.

[0012] The strain culture medium contains glucose 0.1%-5.0% (weight percentage, the same below), yeast extract 0.01%-1%, peptone 0.01%-1%, agar 0.1%-3.0%, sodium chloride 0.05%- 5%, the rest is water. (2) The used fermentation medium of the fermentation culture of fungus Penicillium sp.386 contains glucose 1.0% (percentage by weight, the same below), yeast extract 0.1%, peptone 0.2%, sodium chloride 0.3%, all the other are water, fungal strains in Cultured at 28°C for 30 days.

[0013] The fermentation medium contains 0.1%-5.0% of glucose (weight percentage, the same below), 0.01%-1% of yeast extract, 0.01%-1% ...

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Abstract

The invention relates to an alkaloid compound, a method for preparing the alkaloid compound and an application of the alkaloid compound as enzyme inhibitor. During preparation, strain culture is first carried out to a marine fungus in a culture medium, and then fermentation culture is carried out to the fungus in a fermentation culture medium; obtained fermentation liquid is filtered to eliminatemycelium; filtrate is heated, concentrated and extracted through ethyl acetate; chromatographic separation is carried out, and after obtained eluent is concentrated, penicillazine is obtained; bromine or manganese dioxide is added to a solution dissolving the Penicillazine, and then Penicillazines 1 and 2 are respectively obtained after reaction; or acetic anhydride is added to a solution dissolving the Penicillazine 2, and then Penicillazines 3 and 4 are obtained after reaction. An alkaloid derivative derived from the marine fungus can effectively inhibit human topoisomerase I, can be used for developing enzyme inhibitor medicine, and has raw materials that can be produced in large scale.

Description

technical field [0001] The invention relates to an alkaloid compound with a novel dumbazine ring structure, in particular to a class of alkaloid compound with enzyme inhibitory activity and its preparation method and application. Background technique [0002] Since penicillin was prepared from fungi in 1929, fungal metabolites have become a rich source of drugs, and the vast majority of clinically used antibiotics are derived from fungi and bacteria. The metabolites of fungi also have other medicinal value, such as anti-tumor, treatment of cardiovascular diseases, enzyme inhibitors, etc. Due to the particularity of the marine environment, marine fungi can provide metabolites that terrestrial fungi cannot provide, but so far no enzyme inhibitor products with medicinal value have been obtained from marine fungi. Contents of the invention [0003] The object of the present invention is to provide an alkaloid compound derived from marine fungi, its preparation method and its ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D413/12C12P17/16A61K31/536A61P43/00C12R1/80
Inventor 邵长伦王长云林永成佘志刚
Owner OCEAN UNIV OF CHINA
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