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Mixed-source terpene compounds as well as separation method and application thereof

A technology of compounds and mixed terpenes, applied in the field of microbial medicine, can solve the problems of no neuraminidase activity, research, no literature reports, etc.

Active Publication Date: 2018-07-20
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 three mixed-source terpene compounds involved in the present invention are new compounds, which have not been reported in the literature before, nor have they been studied on neuraminidase activity

Method used

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  • Mixed-source terpene compounds as well as separation method and application thereof
  • Mixed-source terpene compounds as well as separation method and application thereof
  • Mixed-source terpene compounds as well as separation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Embodiment 1. Fermentative production and separation and purification of compounds 1, 2 and 3 shown in formula I:

[0026] The marine fungus Aspergillus ustus used in the present invention is isolated from sea squirt tissue, purified and cultivated on rice solid medium. The formula of rice solid medium is: rice 70g, corn steep liquor 0.2g, peptone 0.3g, yeast powder 0.5g, monosodium glutamate 0.6g , seawater 100ml.

[0027] Strain Aspergillus ustus (size 2.5 cm x 2.5 cm) was fermented in batches in rice solid medium in a 1000ml Erlenmeyer flask, the fermentation product was stirred and crushed, soaked and extracted with ethyl acetate for 3-4 times, and the combined extract was concentrated to obtain a fermented crude Extract.

[0028] The crude extract was subjected to vacuum silica gel column (200–300 mesh) chromatography, and the gradient was 20:1 to 1:1 (v / v) petroleum ether-ethyl acetate and the gradient was 20:1 to 1:1 ( v / v) Dichloromethane-methanol was used as ...

Embodiment 2

[0038] Example 2. Neuraminidase inhibitor activity.

[0039] Neuraminidase inhibitor screening kit (including neuraminidase detection buffer, neuraminidase, neuraminidase fluorescent substrate, Milli-Q water) was used to test neuraminidase inhibitory activity. Neuraminidase is a special glycoprotein on the surface of influenza virus and an important target of influenza drugs, so the screening of its inhibitors has become a common method for screening potential anti-influenza drugs.

[0040] The operation steps are as follows: Accurately weigh the sample of the pure product compound shown in formula I prepared in the above example, and prepare solutions of the required concentration with dimethyl sulfoxide (DMSO), respectively, and the concentrations of the positive control Tamiflu and the sample are both 200 μM .

[0041] Preparation of sample detection: Add 70 μl neuraminidase detection buffer, 10 μl neuraminidase, the neuraminidase inhibitor sample or the positive control Tam...

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Abstract

The invention relates to the technical field of microbial medicine, in particular to mixed-source terpene compounds obtained from a fermentation product of Aspergillus ustus, a separation and purification method of the mixed-source terpene compounds and application of the mixed-source terpene compounds to the aspect of inhibiting the neuramidinase activity. The mixed-source terpene compounds include a compound 1, a compound 2 and a compound 3 shown as a formula I, wherein the molecular formula of the compound 1 is C33H34O12; the molecular formula of the compound 2 is C32H38O11; the molecular formula of the compound 3 is C25H28O8; shown as the formula, activity test shows that the compounds have obvious inhibition activity on neuramidinase; the median inhibitory concentrations (IC50) are respectively 5.28, 8.95 and 10.72 muM; the compound is hopeful to become novel anti-influenza virus potential medicine. The formula is shown in the description.

Description

technical field [0001] The invention relates to the technical field of microbial medicine, in particular to an application in the aspect of obtaining mixed-source terpene compound from the fermentation product of marine fungus Aspergillusustus and its separation and purification method, and inhibiting neuraminidase activity. Background technique [0002] Marine microbial secondary metabolites have rich structural diversity and significant biological activity, and are an important source of drug lead compounds. Mixed terpene compounds with Austin skeleton structure are a class of biologically active compounds mainly produced by fungi, most of which contain oxygen bridges in their molecular structures. Artemia has certain inhibitory activity, and its inhibitory activity on neuraminidase shown in this experiment makes it a potential active molecule against influenza virus. [0003] According to literature research, the three mixed-source terpene compounds involved in the prese...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/22A61P31/16C12P17/18C12N1/14C12R1/70
CPCC07B2200/07C07D493/22C12P17/181C12N1/145C12R2001/70
Inventor 王斌贵李莉李晓明
Owner INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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