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Di-sesquiterpene compound derived from marine fungi, preparation method of di-sesquiterpene compound and application of di-sesquiterpene compound in preparation of anti-inflammatory drugs

A technology of sesquiterpenes and marine fungi, applied in biochemical equipment and methods, fungi, and methods based on microorganisms, etc., can solve problems such as adverse reactions and damage, and achieve the effect of low cost, abundant sources, and simple methods

Active Publication Date: 2019-07-05
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these anti-inflammatory drugs have certain clinical anti-inflammatory effects, long-term large-scale use will cause a series of adverse reactions, such as gastric mucosal damage, liver damage, kidney damage, etc.

Method used

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  • Di-sesquiterpene compound derived from marine fungi, preparation method of di-sesquiterpene compound and application of di-sesquiterpene compound in preparation of anti-inflammatory drugs
  • Di-sesquiterpene compound derived from marine fungi, preparation method of di-sesquiterpene compound and application of di-sesquiterpene compound in preparation of anti-inflammatory drugs
  • Di-sesquiterpene compound derived from marine fungi, preparation method of di-sesquiterpene compound and application of di-sesquiterpene compound in preparation of anti-inflammatory drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The compound of the present invention can be isolated from the cell of marine fungus Aspergillus sp. ZJ-68. The marine fungus is isolated from the leaves of the mangrove plant Candela in Zhanjiang Mangrove Reserve in Guangdong Province; the specific steps are as follows:

[0025] 1. Seed culture:

[0026] 1.1 Preparation of seed medium: 200g of potatoes, 20g of glucose, 1L of tap water, equally distributed in five 500mL Erlenmeyer flasks, and extinguished at 121°C for 30 minutes.

[0027] 1.2 Cultivation of seeds: Inoculate the strains of marine fungi into the seed medium, place them on a shaker at a speed of 200 rpm at a temperature of 28° C., and cultivate them for 72 hours to obtain a seed culture solution.

[0028] 2. Fermentation culture:

[0029] 2.1 Preparation of fermentation medium: 6000g of northeast rice, 180g of sea salt, 6L of tap water, extinguished at 121°C for 30 minutes.

[0030] 2.2 Fermentation culture: Aseptically transfer 5 mL of the seed solutio...

Embodiment 2

[0034] The new compounds I, II and III in Example 1 were analyzed for structural testing, and the following experimental data were obtained:

[0035] New compound I:C 25 h 38 o 5 , HRESI-MS: [M-H] － (experimental value 417.26500);

[0036] New compound II:C 25 h 36 o 4 , HRESI-MS: [M-H] － (experimental value 399.35500);

[0037] New compound Ⅲ:C 25 h 34 o 3 , HRESI-MS: [M-H] － (experimental value 381.24404).

[0038] See Table 1 for the NMR data of compounds I, II and III.

[0039] Table 1 NMR data (125MHz / 500MHz, TMS, ppm) of compounds Ⅰ, Ⅱ and Ⅲ

[0040]

[0041]

Embodiment 3

[0043] Compounds I, II and III in Example 1 were tested for anti-inflammatory activity of macrophages in vitro:

[0044] 1. Cell culture and treatment: RAW 264.7 cells were cultured in vitro, using DMEM high-glucose medium containing 10% FBS, at 37°C and 5% carbon dioxide concentration for routine maintenance and passage.

[0045] 2. Compound intervention: adjust the RAW 264.7 cell density to 1×10 5 cells / well and in the logarithmic growth phase, adding LPS (final concentration 1 μg / mL) to induce macrophages to be in an inflammatory state, using DMSO to prepare the compound to be tested or indomethacin into different drug concentrations, each concentration was set at 3 parallel wells, and set positive control wells (only LPS added), negative control wells (cells and medium), and blank control wells (medium). After culturing for 24 hours, take 50 μL of the cell supernatant and add it to a new 96-well plate, add 50 μL of reagents I and II of the NO detection kit, and use the Gr...

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Abstract

The invention belongs to the technical field of pharmaceutical compounds, and particularly discloses a di-sesquiterpene compound derived from marine fungi, a preparation method of the di-sesquiterpenecompound and application of the di-sesquiterpene compound in preparation of anti-inflammatory drugs. The structural formula of the di-sesquiterpene compound is shown in formulas I, II and III, and the di-sesquiterpene compound is prepared by fermenting marine fungus Aspergillus sp. ZJ-68, wherein the marine fungus Aspergillus sp. ZJ-68 was preserved in Guangdong Culture Collection Center on Jan.21, 2019 with the preservation number of GDMCC No: 60541; the production of NO induced by LPS can be significantly inhibited by compounds I, II, and III, specifically, IC50 is 16.48 micrometer, 20.7 micrometer and 24.4 micrometer, respectively, and the IC50 of the positive control indomethacin was 37.5 micrometer. Therefore, the di-sesquiterpene compound can be used for preparing the anti-inflammatory drugs and has the clinical application potential of anti-inflammatory treatment.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical compounds, in particular to a class of sesquiterpene compounds derived from marine fungi with anti-inflammatory activity, a preparation method thereof, and an application in the preparation of anti-inflammatory drugs. Background technique [0002] Inflammation is the defense response of living tissue with vascular system to various inflammatory factors, and is the immune response of the body to foreign components. The basic pathological changes include deterioration, exudation, and hyperplasia. The clinical manifestations are local redness, swelling, heat, pain, and dysfunction, and there are systemic reactions such as fever, leukocytosis, and monocyte-macrophage system hyperplasia. Under normal circumstances, the body's inflammatory response helps to remove pathogenic factors, phagocytize necrotic cells, and prevent further damage. However, an excessive inflammatory response will backfire...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C49/757C07D303/32A61P29/00C12P15/00C12N1/14C12R1/66
CPCC07C49/757C07D303/32A61P29/00C12P15/00C07C2603/36C12R2001/66C12N1/145
Inventor 佘志刚蔡润林蒋红明莫亚玲
Owner SUN YAT SEN UNIV
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