A kind of preparation method and application of aromatic crotonolactone

A technology of aromatic butenolide and structural formula, which is applied in the field of marine natural medicines, can solve problems such as adverse reactions of the kidneys, and achieve the effect of inhibiting the activity of COX-2

Active Publication Date: 2022-02-01
莱州金兴化工有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

COX-1 mainly exists in normal cells and catalyzes the production of prostaglandins that maintain normal physiological functions; COX-2 is inducible in most tissues and is an important inducing enzyme in the inflammatory process, which is the effect of non-steroidal anti-inflammatory drugs However, long-term administration of non-steroidal anti-inflammatory drugs currently on the market can cause gastrointestinal and renal adverse reactions. have played an important role and have become one of the new targets for tumor prevention and treatment

Method used

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  • A kind of preparation method and application of aromatic crotonolactone
  • A kind of preparation method and application of aromatic crotonolactone
  • A kind of preparation method and application of aromatic crotonolactone

Examples

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Effect test

Embodiment 1

[0029] Example 1 Isolation, purification and identification of strains.

[0030] Bacteria were isolated and purified from the sediments of the Mangrove Reserve in Techeng Island, Zhanjiang Aspergillus terreus SCAU011, its typical culture pictures are as follows figure 2 Shown: the colony is round, the hyphae are white, and the spores are khaki. After ITS rDNA detection, compared with Gene Bank data, identified as Aspergillus terreus fungus.

Embodiment 2

[0031] Example 2 Preparation of fermented product.

[0032] Preparation method of seed medium: Potato extract 200 mL, glucose 20 g, sea salt 30 g, dilute to 1 L with water. Put the PDB medium into twenty 500 mL Erlenmeyer flasks, about 150 mL each, sterilize at 121 °C for 25 minutes by high-pressure steam, and set aside.

[0033] Rice medium configuration method: 80 g of commercially available rice, 0.4 g of yeast extract, 0.4 g of glucose, 120 mL of sterile water, and 3.6 g of sea salt were placed in 1 L Erlenmeyer flasks, a total of 60 bottles. Autoclave at 121°C for 25 minutes and set aside.

[0034] Pick an appropriate amount of fungi with a sterile bamboo stick Aspergillus terreus The SCAU011 strain was inoculated into the seed medium, and cultured on a shaker (180 rpm) at 28°C for 3 days to obtain the seed liquid, and then inoculated 10 mL of the seed liquid into a 1 L Erlenmeyer flask containing rice medium with a pipette gun, and then After static culture at 28° C....

Embodiment 3

[0036] Example 3 Preparation of aromatic croton lactone dimer.

[0037] According to the method of Example 2, 4.0 kg of fermented rice medium was obtained, the rice medium was soaked with 95% ethanol, the ethanol was recovered from the leaching solution, and the remaining water phase was extracted with ethyl acetate, concentrated under reduced pressure to obtain the ethyl acetate extract 60g. The ethyl acetate extract was subjected to column chromatography on normal phase silica gel (100-200 mesh), with dichloromethane-methanol as the eluent, gradient elution from volume ratio 100:0 to 0:100, according to TLC The fractions were combined according to the analysis situation, and the elution solvent was recovered to obtain 7 fractions (Fr.1-Fr.7).

[0038] Fr.4 further carried out normal phase silica gel (200-300 mesh) column chromatography with dichloromethane-acetone as the eluent, and combined the fractions according to the thin layer chromatography to obtain 9 components (Fr...

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PUM

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Abstract

The invention discloses an aromatic butenolide compound, a preparation method thereof, and an application in the preparation of COX-2 inhibitors and antioxidant drugs. The present invention obtains from a strain of Aspergillus fungus Aspergillus terreus Aromatic butenolide compounds with COX‑2 inhibitory activity and antioxidant activity were isolated from the fermentation product of SCAU011 CGMCC No: 19270 (as shown in Figure 1), in the preparation of COX‑2 inhibitors and antioxidant drugs It has a good application prospect.

Description

technical field [0001] The invention belongs to the field of marine natural medicines, and in particular relates to an aromatic butenolide compound and its application in the preparation of COX-2 inhibitors and antioxidant drugs. Background technique [0002] Cyclooxygenase (COX) is a key enzyme that catalyzes the oxidation of arachidonic acid to synthesize prostaglandins. COX-1 mainly exists in normal cells and catalyzes the production of prostaglandins that maintain normal physiological functions; COX-2 is inducible in most tissues and is an important inducing enzyme in the inflammatory process, which is the effect of non-steroidal anti-inflammatory drugs However, long-term administration of non-steroidal anti-inflammatory drugs currently on the market can cause gastrointestinal and renal adverse reactions. All have played an important role and have become one of the new targets for tumor prevention and treatment. Therefore, the development of new COX-2 inhibitors is of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C12N1/14C12P17/16C07D307/83A61K31/365A61P39/06C12R1/66
CPCC12P17/162C07D307/83A61K31/365A61P39/06C12R2001/66C12N1/145
Inventor 张华鲍洁贺菲李秀秀
Owner 莱州金兴化工有限责任公司
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