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A kind of gamma-pyrone derivative and its preparation method and application

A kind of derivative, pyrone technology, applied in the field of γ-pyrone derivatives, can solve the problems such as drugs that have not yet been seen

Active Publication Date: 2019-09-03
NINGBO UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report on the chemical structure of the compound and the activity against Botrytis cinerea, so there is no drug related to it on the market

Method used

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  • A kind of gamma-pyrone derivative and its preparation method and application
  • A kind of gamma-pyrone derivative and its preparation method and application
  • A kind of gamma-pyrone derivative and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] A kind of gamma-pyrone derivative structural formula is as shown in I:

[0024]

Embodiment 2

[0026] The preparation method of the gamma-pyrone derivative shown in I formula specifically comprises the steps:

[0027] (1) Fermentation production

[0028] Aspergillus versicolor DJ013 with the preservation number CCTCC No.M2014089 was revived by streaking, transferred to a 250mL Erlenmeyer flask containing 100mL PDB medium, and cultivated at 28°C and 180r / min for 4 days to obtain seeds Culture solution; then inoculate the seed solution into the rice medium according to the volume ratio of 10% inoculum (dissolve 80g of rice and 1g of yeast powder in 120mL of seawater, soak overnight, and then autoclave at 121°C for 20min) In a 1000mL Erlenmeyer flask, cultured at 28°C for 35 days to obtain the fermented product;

[0029] (2) Obtaining the extract

[0030] Soak the above-mentioned fermented product in 4L of methanol for 3 times, then concentrate and evaporate the methanol extract to dryness, redissolve it in 1L of water, repeat the extraction 3 times with 1L of ethyl acet...

Embodiment 3

[0039] In vitro test of resistance to Botrytis cinerea (96-well plate antibacterial method)

[0040] (1) Experimental samples

[0041] Preparation of the test sample solution: the test sample is the pure compound I isolated and purified in Example 1 above, and an appropriate amount of sample is accurately weighed, and prepared into a solution of the required concentration with DMSO for testing the activity.

[0042] (2) Experimental method

[0043] 96-well plate method: prepare 1 mg / mL DMSO sample solution of the compound to be tested, and in a 96-well plate, use sterilized PDB liquid medium to dilute to concentrations of 200, 100, 50, 25, 12.5, 6.25μg / mL solution (50μL), add an equal amount of 1×10 6 CFU bacterial suspension, the final concentration is: 200, 100, 50, 25, 12.5, 6.25, 3.13μg / mL, shake well, and all the above operations are under sterile conditions. DMSO was used as blank control and carbendazim was used as positive control, and each treatment was repeated 3 ...

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Abstract

The invention discloses a gamma-pyranone derivative and a preparation method and application thereof. The gamma-pyranone derivative is characterized in that the structural formula of the gamma-pyranone derivative is shown in formula I, and the preparation method comprises the following steps: acquiring fermentation broth which contains a novel gamma-pyranone derivative by fermental cultivation ofmarine Aspergillus sp under the deposit number of CCTCC No. M2014089; and then soaking the fermentation broth with methanol and extracting with ethyl acetate to obtain a crude extract. The crude extract is obtained by separation and purification through decompressing column chromatography on silica gel and opposite-phase semi-preparative high performance liquid chromatography. The gamma-pyranone derivative has effect of resisting botrytis cinerea, and has the advantage that the gamma-pyranone derivative can be used as a novel medicine ingredient or a lead compound of a botrytis cinerea inhibitor.

Description

technical field [0001] The invention relates to a gamma-pyrone derivative, in particular to a method for preparing a gamma-pyrone derivative with marine aspergillus and the application of the compound in the preparation of an inhibitor of Botrytis cinerea. Background technique [0002] Microorganisms have always been an important resource for the development of biopesticides. Microbial-derived biopesticides such as jinggongmycin, kasugamycin, polyoxin, agriculturalantibiotic 120, wuyiencin ( wuyiencin M), Qingfengmycin (qingfengmycin) and so on have been widely used in the control of plant diseases. But in recent years, the repeated discovery of the same chemically active substances has puzzled researchers in this field for a long time. Therefore, it has become a top priority and has very important social significance to continuously expand the screening objects, discover new agricultural antibacterial substances, and develop more agricultural antibiotics with independent i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D309/36C12P17/06A01N43/16A01P3/00C12R1/66
Inventor 张云阳丁立建何山肖烨姚佳晓严小军
Owner NINGBO UNIV
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