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A kind of thiomacrolide compound and its preparation method and anti-aquaculture disease fungus activity application

A technology of macrolides and macrolides, which is applied in the field of microbial medicine and medicinal chemistry, and can solve problems such as no literature reports

Active Publication Date: 2020-11-27
INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] According to literature research, the two thiomacrolide compounds involved in the present invention are new compounds, which have not been reported in the literature before, nor have they been studied on their anti-aquatic disease fungus activity

Method used

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  • A kind of thiomacrolide compound and its preparation method and anti-aquaculture disease fungus activity application
  • A kind of thiomacrolide compound and its preparation method and anti-aquaculture disease fungus activity application
  • A kind of thiomacrolide compound and its preparation method and anti-aquaculture disease fungus activity application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1. Fermentative production and separation and purification of compounds 1 and 2 shown in formula I:

[0025] Cladosporium cladosporioides obtained according to the above-mentioned literature or public circulation channels was purified and inoculated on a PDA plate medium, and cultured in an incubator at 28° C. for 6 days.

[0026] An appropriate amount of bacteria on the surface of the above-mentioned PDA plate was cut, inoculated into a sterilized Erlenmeyer flask filled with solid medium, left to stand at room temperature for 48 days, and then inactivated with ethyl acetate for use.

[0027] The solid medium contains 70g of rice, 0.3g of peptone, 0.1g of corn steep liquor and 0.1% of methionine per 100mL of natural seawater.

[0028] The product obtained by fermenting and culturing the above-mentioned Cladosporium cladoides on a solid medium was ultrasonically extracted three times with ethyl acetate, and the extracts were combined and concentrated to obtai...

Embodiment 2

[0039] Embodiment 2. Aquatic pathogen inhibitory activity:

[0040] The antibacterial activity of compounds 1 and 2 represented by formula I was detected by the minimum inhibitory concentration method. Select the following two strains of aquatic disease pathogens: Edwardsiella tarda and Edwardsiella ictarda for antibacterial activity test.

[0041] 1) Antibacterial activity test (MIC method):

[0042]Minimum Inhibitory Concentration (MIC), the lowest concentration of a drug that can inhibit bacterial growth in vitro. In a 96 microwell plate, by adding different concentrations of drugs into the bacterial suspension of the bacteria to be tested, observe after incubation, if the indicator bacteria grow in a certain well, it means that the drug concentration in the well cannot inhibit the growth of the bacteria, The liquid in the hole is turbid, and the light transmittance drops obviously. On the contrary, the liquid in the hole is clear, and the decrease in light transmittance...

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Abstract

The invention relates to the technical field of medicinal chemistry and microbial medicine, specifically to thio macrolide compounds obtained from a fermented product of cladosporium cladosporioides and a separation and purification method thereof, and application in inhibiting the activity of aquatic disease bacteria. The thio macrolide compounds comprise a compound 1 and a compound 2 which are shown in formula I; the compound 1 has a molecular formula C16H26O6S and a structural formula represented by 1 in formula I, and the compound 2 has a molecular formula C16H28O7S and a structural formula represented by 2 in formula I. The compounds disclosed by the invention all have significant inhibitory activity against the aquatic disease bacterium Edwardsiella ictarda and is expected to be developed into a novel aquatic disease bacteria prevention and treatment drug.

Description

technical field [0001] The invention relates to the technical fields of medicinal chemistry and microbial medicine, in particular to a method for obtaining a thiomacrolide compound from a fermentation product of Cladosporium cladosporioides and a method for separating and purifying the same and for inhibiting aquatic diseases. applications in bacterial activity. Background technique [0002] The thiomacrolide compound with a 12-membered ring skeleton structure is a class of biologically active compounds mainly produced by Cladosporium fungi. Its structure consists of the C-2 or C-3 position in the 12-membered ring Formed by substitution of sulfur side chains, the thiomacrocyclic lactone involved in the present invention is a 12-membered ring structure substituted at the C-2 position. Cladosporium is an important genus in Ascomycota, with 189 species reported in the literature by 2016. The types of metabolites of different Cladosporium fungi were quite different. The bacte...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D313/00C12P17/08A01N43/22A01P1/00A61P31/04C12R1/645
CPCA01N43/22A61P31/04C07D313/00C12P17/08
Inventor 王斌贵张凡忠孟令红李晓明杨遂群
Owner INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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