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Preparation method of two aspergillus terreus ketone compounds and application of aspergillus terreus ketone compounds as antitumor drugs

A technology of terrein and compounds, applied in the field of medicine, to achieve the effects of inhibiting proliferation, inducing cell apoptosis, and broad application prospects

Active Publication Date: 2020-09-01
MINJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Faced with the huge threat to human life brought by more and more diverse diseases, the existing drugs can no longer meet the fight against the diseases, and the demand for research and development of new drugs is increasing day by day

Method used

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  • Preparation method of two aspergillus terreus ketone compounds and application of aspergillus terreus ketone compounds as antitumor drugs
  • Preparation method of two aspergillus terreus ketone compounds and application of aspergillus terreus ketone compounds as antitumor drugs
  • Preparation method of two aspergillus terreus ketone compounds and application of aspergillus terreus ketone compounds as antitumor drugs

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Experimental program
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Effect test

Embodiment 1

[0022] Separation and purification of formula I compound of the present invention

[0023] (1) Fermentation of mutant strains

[0024] CGMCC no. 19630 Aspergillus terreus mutant strain was inserted into seawater oligotrophic starch medium, and cultured on a shaker at 28°C and 150 rpm for 7 days.

[0025] (2) Extraction and separation of compounds

[0026] After the fermentation, the fermentation culture obtained in step (1) was filtered, and the bacterial liquid was extracted 3 times with ethyl acetate; the mycelium was soaked in dichloromethane / methanol (2:1), concentrated, and washed Extracted 3 times, combined extracts, concentrated under reduced pressure to obtain crude extract. The extract was first subjected to rapid decompression normal phase silica gel column chromatography, respectively with petroleum ether / ethyl acetate 10:1, 6:1,3:1, 1:1 and ethyl acetate / methanol 1:0, 9: 1 mobile phase gradient elution, a total of six components (Fr.1−Fr.6). Fr.5 was further se...

Embodiment 2

[0033] Cytotoxic activity test of formula I compound of the present invention

[0034] According to the literature method, the cytotoxic activity of the compound of formula I was tested by MTT or SRB method. The tested cell lines include human lung cancer cell A549, human cervical cancer cell Hela, human liver cancer cell Hep G2, human breast cancer cell MCF-7, and human colon cancer cell HCT-116. Doxorubicin was used as a positive control. Observe the Hoechst staining results, repeat the experiment three times, and calculate the IC of the compound on tumor cells 50 value.

[0035] The results showed that the compound of formula Ⅰ had a good inhibitory effect on Hep G2, and its IC 50 The values ​​are 376 nM and 697nM respectively, and the Hoechst staining results are shown in the attached figure.

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Abstract

The invention relates to a preparation method of two aspergillus terreus ketone compounds and application of the aspergillus terreus ketone compounds as antitumor drugs. The two aspergillus terreus ketone compounds are aspergillus terreus ketone B and aspergillus terreus ketone C; the compoundshavea structure shown as a formula I. The invention provides two natural products with good anti-tumor activity; the two compounds are generated by a histone deacetylase gene hdaA deletion strain CGMCC No.19630, can significantly inhibit proliferation of human hepatoma carcinoma cells Hep G2 and induce apoptosis, are used for treating diseases such as hepatoma carcinoma, and have broad application prospects.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a preparation method of two aspergillus terreus ketone compounds and their application as antitumor drugs. Background technique [0002] With the improvement of people's living standards, the spectrum of human diseases has quietly changed. Faced with the huge threat to human life brought by more and more diverse diseases, the existing drugs can no longer meet the fight against the diseases, and the demand for research and development of new drugs is increasing day by day. In recent decades, more and more scientists regard the ocean as an important treasure house of medicinal biological resources. Its special habitat often makes marine natural products have novel skeletons and unique mechanisms of action, and become an important resource for the development of new anti-tumor drugs. . As an important group of microorganisms, marine fungi provide an innumerable chemical base fo...

Claims

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Application Information

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IPC IPC(8): C07C49/577A61P35/00C12P7/26C12R1/66
CPCC07C49/577A61P35/00C12P7/26C07C2601/10
Inventor 姚光山
Owner MINJIANG UNIV
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