Aspergillus sydowii MNP-2 and application of aspergillus sydowii MNP-2 in synthesis of dibenzoxane compounds

A technology of MNP-2 and Aspergillus polymosa, which is applied to medical preparations containing active ingredients, methods based on microorganisms, fungi, etc., can solve the problems of no compound synthesis method, and achieve the effect of improving activity and simple separation process

Active Publication Date: 2022-07-15
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Due to the special heterocyclic structure of this type of compound, there is no report on the synthesis method of this compound, and this compound is also isolated from Aspergillus polydoctoris for the first time

Method used

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  • Aspergillus sydowii MNP-2 and application of aspergillus sydowii MNP-2 in synthesis of dibenzoxane compounds
  • Aspergillus sydowii MNP-2 and application of aspergillus sydowii MNP-2 in synthesis of dibenzoxane compounds
  • Aspergillus sydowii MNP-2 and application of aspergillus sydowii MNP-2 in synthesis of dibenzoxane compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1. Screening and identification of strain MNP-2

[0023] 1. Screening of strain MNP-2

[0024] Primary screening: 200 g of ore collected from the North Pole (longitude 73.8, latitude -168.9) was placed in a 15 mL centrifuge tube, 5 mL of sterile water was added, and sonicated at room temperature and 40 KHz for 5 min. After standing for stratification, the supernatant was collected. Put them into PDA plates, cultivate them in a 28°C incubator for 3-4 days, and select single colonies after the cells grow out. The final concentration composition of PDA plate medium is: glucose 20g / L, potato 200g / L, agar 18g / L, the solvent is distilled water, and the pH is natural.

[0025] Re-screening: inoculate the single colony from the primary screening into the PDA plate, incubate at 28°C for 3-4 days, and repeat the screening until the size, shape and color of the colony are basically the same, and finally the strain MNP-2 is obtained.

[0026] 2. Identification of strains ...

Embodiment 2

[0034] Example 2: Fermentation culture of strain MNP-2

[0035] (1) Activation culture: The strain MNP-2 was inserted into the PDA slant medium, and cultivated in a 28°C incubator for 3-4 days to obtain activated strains; the final concentration of the PDA slant medium was as follows: glucose 20g / L, potato 200g / L L, agar 18g / L, distilled water as solvent, natural pH.

[0036] (2) Seed cultivation: pick an inoculated loop from the activated colony in step (1) and inoculate it into the PDB seed medium, and shake it for 3 days at 200 rpm and 28°C to obtain seed liquid; the PDB seed medium is finally The concentration composition is: glucose 20g / L, potato 200g / L, the solvent is distilled water, and the pH is natural.

[0037] (3) Fermentation culture: connect 0.83L of the seed liquid obtained in step (2) to the surface of the 16.6kg rice medium with an inoculum of 0.05mL / g volume concentration, stir evenly, and leave it to ferment for 30 days in the dark at room temperature. day...

Embodiment 3

[0038] Example 3: Dibenzo[b,e]oxa Extraction, separation and identification of compound (I)

[0039] 1. Extraction and separation of compound (I)

[0040] The whole fermentation mixture prepared in Example 2 was added to 30L of ethyl acetate (the amount of ethyl acetate was calculated as 1.8ml / g based on the quality of the rice medium before fermentation), the room temperature, 40kHz ultrasonic extraction for 20min, filtered, and the filtrate was concentrated under reduced pressure to No liquid flows out to obtain crude extract extract; after dissolving all crude extract extract with 500mL of methanol, silica gel column (silica gel particle size 200-300 mesh, column height 120cm, diameter 10cm, column height 50cm) is used to carry out For separation and purification, the dichloromethane:methanol with volume ratios of 1:0, 100:1, 50:1, 20:1, 10:1, 4:1, and 0:1 was used as the eluent, and the elution rates were 60mL / min, the elution volume is 10 column volumes, and the efflue...

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Abstract

The invention discloses Aspergillus sydowii MNP-2 and application thereof in synthesis of dibenzo [b, e] oxa compounds, the Aspergillus sydowii MNP-2 can produce the dibenzo [b, e] oxa compounds at high yield, and the strain is easy to culture and convenient for amplification fermentation, and has potential of industrial and large-scale production. A high-yield dibenzo [b, e] oxa compound (I) is separated from an aspergillus sydowii MNP-2 fermentation product, the yield is 4.3 mg/g, and the separation process is simple. The dibenzo [b, e] oxa compound (I) has anti-tumor activity, and can be subjected to structural modification in the later stage to prepare a derivative of the compound to greatly improve the activity of the compound, so that anti-tumor drugs are prepared.

Description

(1) Technical field [0001] The present invention relates to a dibenzoxan The preparation of compounds, especially polyAspergillus polyphylla MNP-2 and in the synthesis of dibenzoxan applications in compounds. (2) Background technology [0002] Dibenzo[b,e]oxa These compounds have special heterocyclic structures. To date, more than 85% of biologically active compounds are composed of heterocyclic structures. Aspergillus fungi are a class of filamentous fungi that are widely distributed in different habitats in nature. The metabolites of Aspergillus fungi are characterized by complexity, diversity, and novelty, and their compounds mainly include polysaccharides, alkaloids, polyketones, diketopyrazines, and anthraquinones. These metabolites have antibacterial, anticancer, antioxidant, antiviral and other biological activities. Natural products are an important source of drugs. In recent decades, among the more than 1,000 drugs approved by the FDA, 49.3% are directly or...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12N1/14C12P17/08C07D313/12A61K31/365A61P35/00C12R1/66
CPCC12P17/08C07D313/12A61K31/365A61P35/00
Inventor 章华伟符志杨胡哲刘子君魏斌王鸿
Owner ZHEJIANG UNIV OF TECH
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