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Penicillazine derivative, and preparation and use thereof

A derivative and post-reaction technology, applied in the field of penicillazine derivatives, can solve problems such as enzyme inhibitor drugs that have not yet been seen, and achieve the effect of broad application prospects.

Active Publication Date: 2011-04-20
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 inhibitors with medicinal value have been obtained from marine fungi

Method used

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  • Penicillazine derivative, and preparation and use thereof
  • Penicillazine derivative, and preparation and use thereof

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Experimental program
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Embodiment Construction

[0010] In preparing the compounds of the present invention, the following steps are taken:

[0011] (1) Carry out strain culture to marine fungus Penicillium sp.386 in culture medium earlier, used medium contains glucose 1.0% (percentage by weight, the same below), yeast extract 0.1%, peptone 0.2%, agar 1.0%, chlorine Sodium chloride 0.3%, the rest is water, when used, it is made into a test tube slope, and the above-mentioned fungal strains are cultivated at 30° C. for 5 days.

[0012] The strain medium contains 0.1%-5.0% of glucose (percentage by weight, the same below), 0.01%-1% of yeast extract, 0.01%-1% of peptone, 0.1%-3.0% of agar, and 0.05% of sodium chloride. 5%, the rest is water. The culture temperature is 15-35° C., and the culture time is 3-10 days.

[0013] (2) The fungus Penicillium sp.386 bacterial classification after above-mentioned cultivation carries out fermentation culture, and the fermentation medium used contains glucose 1.0%, yeast extract 0.1%, pept...

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Abstract

The invention provides a penicillazine derivative and the preparation method and the application thereof. The preparation method comprise the following steps: culturing strains of marine fungi in a culture medium, fermentation culturing the fungi in a fermentation culture medium, filtering the obtained fermented solution to remove thalli; heating to concentrate the filtrate and extracting with anorganic solvent; carrying out the chromatographic separation and concentrating the eluate to obtain penicillazine; and adding an alkylation or acylation reagent and reacting to obtain the penicillazine derivative. The penicillazine derivative derived from the marine fungihas an enzyme inhibiting activity, can effectively inhibit Alpha-glucosidase, and can be applied for developing enzyme inhibiting pharmaceuticals. The raw material can be produced in a large scale, and the application prospect is wide.

Description

technical field [0001] The invention relates to a penicillazine derivative having enzyme inhibitory activity and containing a dumbazine ring structure, a preparation method and application thereof. 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 inhibitors with medicinal value have been obtained from marine fungi. Contents of the invention [0003] The object of the present invention is to provide a penicillazine derivative derived from marine fungus, its preparation method and its application as an enzyme inhibito...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D413/12C12P17/16A61K31/5355A61P43/00
Inventor 王长云邵长伦林永成佘志刚
Owner OCEAN UNIV OF CHINA
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