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Marine-derived polyketone compound hypoxone A, preparation method thereof, and application of hypoxone A in preparation of anti-inflammatory drugs

A technology of anti-inflammatory drugs and compounds, applied in the field of medicine and biology, can solve the problems of unsatisfactory clinical efficacy and large side effects of drugs, and achieve significant anti-inflammatory effects

Active Publication Date: 2020-06-02
GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the clinical efficacy of quite a few anti-inflammatory drugs on the market is far from reaching the ideal level, and some drugs have serious side effects.

Method used

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  • Marine-derived polyketone compound hypoxone A, preparation method thereof, and application of hypoxone A in preparation of anti-inflammatory drugs
  • Marine-derived polyketone compound hypoxone A, preparation method thereof, and application of hypoxone A in preparation of anti-inflammatory drugs
  • Marine-derived polyketone compound hypoxone A, preparation method thereof, and application of hypoxone A in preparation of anti-inflammatory drugs

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Experimental program
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Effect test

Embodiment 1

[0029] 1. Isolation, purification and identification of marine fungus Hypoxylon rubiginosum FS521

[0030] The marine fungus Hypoxylon rubiginosum FS521 of the present invention was isolated from marine sediments in the South China Sea (115°34'45"E, 15°58'38"N, water depth 4188 meters) in October 2012, and was identified by ITS sequence analysis , the GenBank gene accession number is: MN636334, after blast comparison and homology analysis, the strain was identified as Hypoxylonrubiginosum, numbered FS521.

[0031] 2. Solid fermentation of Hypoxylon rubiginosum FS521

[0032] Inoculate the activated deep-sea fungus Hypoxylon rubiginosum FS521 mycelium into potato dextrose liquid medium (per liter of medium is prepared by the following method: boil 200g of potatoes with 500mL of pure water, boil for 20min, filter to obtain potato juice, and then add Glucose 20g, KH 2 PO 4 3g, MgSO 4 1.5g, vitamin B 1 10mg, made up to 1000mL with water, and sterilized), cultivated at 28°C...

Embodiment 2

[0045] The anti-inflammatory activity of compound hypoxone A was tested by Griess method.

[0046] 1. Reagents for the test: the compound hypoxone A prepared by the present invention was dissolved in dimethyl sulfoxide (DMSO) to obtain a mother solution with a concentration of 10 mM, and then diluted to the required concentration with DMEM medium. The positive control was indomethacin aqueous solution.

[0047] The cell line used in this experiment is mouse macrophage RAW264.7.

[0048] 2. Experimental method: Griess method was used to determine the effect of the compound on the release of nitric oxide (NO) in the RAW264.7 cell inflammation model induced by bacterial lipopolysaccharide (LPS), so as to evaluate the anti-inflammatory activity of the compound. Take the RAW264.7 cells in the logarithmic growth phase, digest them with trypsin, stain with trypan blue and count. After the trypan blue exclusion test detects that the cell viability is greater than 95%, use fresh DMEM ...

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Abstract

The invention discloses a marine-derived polyketone compound hypoxone A, a preparation method thereof, and an application of the hypoxone A in the preparation of anti-inflammatory drugs. The compoundhypoxone A is prepared by being separated from a fermentation culture of a marine fungus Hypoxylon rubigosum FS5211. Tests prove that the IC50 value of the compound hypoxone A on inhibition of nitricoxide (NO) generation by a lipopolysaccharide (LPS) induced mouse macrophage RAW264.7 inflammation model is 21.44 + / -0.88 [mu]M, and the compound hypoxone A shows relatively remarkable anti-inflammatory activity and can be used for preparing the anti-inflammatory drugs.

Description

technical field [0001] The invention belongs to the field of medical biotechnology, and in particular relates to a compound hypoxone A, a preparation method thereof and an application in preparation of anti-inflammatory drugs. Background technique [0002] Inflammation is a series of complex defense responses of the animal body against various endogenous or exogenous injury factors locally or throughout the body. Acute inflammatory response is usually beneficial, through which damage factors can be limited or eliminated, and damaged tissue can be repaired. However, chronic inflammation is associated with many chronic human diseases, such as atherosclerosis, obesity, metabolic syndrome, diabetes, neurodegenerative diseases, etc. Moreover, chronic inflammation plays an important role in the occurrence and development of tumors, is one of the important biological malignant behaviors of tumors, and is called the seventh characteristic of tumors. From the perspective of epidemi...

Claims

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Application Information

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IPC IPC(8): C07C69/16C07C67/56C12P7/62A61K31/216A61P29/00
CPCC07C69/16C07C67/56C12P7/62A61P29/00C07C2602/10
Inventor 陈玉婵张婕刘洪新章卫民李赛妮
Owner GUANGDONG INST OF MICROBIOLOGY GUANGDONG DETECTION CENT OF MICROBIOLOGY
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