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Norditerpenoid compound as well as preparation method and application thereof

A compound, the technology of norditerpene, applied in the fields of medicinal chemistry and microbial medicine, can solve the problems of no literature reports

Active Publication Date: 2018-11-23
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 norditerpene compounds involved in the present invention are new compounds, and there is no literature report before

Method used

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  • Norditerpenoid compound as well as preparation method and application thereof
  • Norditerpenoid compound as well as preparation method and application thereof
  • Norditerpenoid compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Embodiment 1. Fermentative production and separation and purification of compounds 1 and 2 shown in formula I:

[0024] The marine fungus Aspergillus wentii (Aspergillus wentii) (size 2.5 cm × 2.5 cm) was inoculated in 300 mL PDB liquid medium grown in plate culture medium, and fermented on a shaker (200 rpm) at 28°C for 7 days. The obtained bacterial liquid was inserted into a 30L PDB liquid medium, fermented in a 50L fermenter for 1 day, then inserted into a 300L PDB liquid medium as a seed liquid and fermented in a 500L fermenter for 7 days, and the fermentation product was repeatedly soaked and extracted with ethyl acetate, combined The extract is concentrated to obtain a fermented crude extract

[0025] The formula of the PDB liquid medium is: 200 grams of potato powder, 20 grams of glucose, 5 grams of peptone, 3 grams of yeast extract powder and 35 grams of sea salt per liter of water.

[0026] The crude extract was subjected to reduced-pressure silica gel column...

Embodiment 2

[0034] Example 2. Activity of inhibitors against aquatic pathogens.

[0035] The antibacterial activity of compounds 1 and 2 represented by formula I was detected by the minimum inhibitory concentration method. Select the following three aquatic pathogenic strains: Edwardsiella tarda, Vibrio harveyi or Vibrio parahaemolyticus for antibacterial activity test.

[0036] 1) Antibacterial activity test (MIC method):

[0037] Minimum Inhibitory Concentration (MIC), the lowest concentration of a drug that can inhibit bacterial growth in vitro. In a 96-well plate, add different concentrations of drugs into the bacterial suspension of the bacteria to be tested, and 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 ...

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Abstract

The invention relates to the technical field of pharmaceutical chemistry and microbial medicines, and in particular relates to a norditerpenoid compound obtained from a fermentation product of Aspergillus wentii, a separation and purification method for the norditerpenoid compound and application of the norditerpenoid compound in the aspect of inhibiting the activity of aquatic disease bacteria. The norditerpenoid compound comprises a compound 1 and a compound 2 as shown in the formula I; the compound 1 and the compound 2 are a pair of isomers; the molecular formula of each of the compound 1 and the compound 2 is C19H26O3; the bacteriostatic activity tests show that the compound 1 and the compound 2 have outstanding inhibitory activity on the aquatic disease bacteria such as Edvardsiella tarda, Vibrio harveyi and Vibrio parahaemolyticus, and the minimum inhibitory concentration (MIC) of each of the compound 1 and the compound 2 is 8.0 microgram / mL, and the norditerpenoid compound is expected to be developed into a novel aquatic disease bacteria prevention and treatment drug. The formula I is shown in the description.

Description

technical field [0001] The invention relates to the technical fields of medicinal chemistry and microbial medicine, in particular to a method for obtaining norditerpene compounds from the fermentation product of the marine fungus Aspergillus wentii and its preparation method for separation and purification, and for inhibiting the activity of aquatic disease bacteria application. Background technique [0002] Marine microbial secondary metabolites have rich structural diversity and significant biological activity, and are an important source of drug lead compounds. Norditerpene compounds with a 20-Nor-isopimarane skeleton structure are a class of biologically active compounds mainly produced by fungi. [0003] According to literature research, the two norditerpene compounds involved in the present invention are new compounds, which have not been reported in the literature before. Contents of the invention [0004] The object of the present invention is to provide a nordit...

Claims

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Application Information

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IPC IPC(8): C07C49/743C12P7/26A01P1/00C12R1/66
CPCC07B2200/07C07C49/743C12P7/26C07C2603/26
Inventor 王斌贵李晓栋李鑫李晓明
Owner INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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