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Algal epiphytic fungus chlorinated depside cyclic ether compound, and preparation and application thereof

A technology of chlorinated depsipepsyl acid cyclic ether and daisylated phenolic acid cyclic ether, applied in the field of chlorinated depsipepsyl acid cyclic ether compounds of epiphytic seaweed fungi and their preparation and application

Inactive Publication Date: 2013-09-18
DALIAN JIAOTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, in clinical treatment, it is found that the drug resistance of pathogenic microorganisms is getting stronger and stronger, especially the infection caused by methicillin-resistant Staphylococcus aureus (MRSA). It is getting more and more serious, and many traditional antibiotics have basically lost their curative effect; in addition, it is found in clinical treatment that the drug resistance of tumors is also increasing, and the phenomenon of multidrug resistance appears. It is necessary to find new antibiotics and anti-tumor drugs to meet the needs of clinical drug development

Method used

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  • Algal epiphytic fungus chlorinated depside cyclic ether compound, and preparation and application thereof
  • Algal epiphytic fungus chlorinated depside cyclic ether compound, and preparation and application thereof
  • Algal epiphytic fungus chlorinated depside cyclic ether compound, and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 3

[0050] Inhibition of Gram-positive drug-resistant bacteria activity test:

[0051] Staphylococcus aureus is a very common germ that sometimes enters the body and causes an infection. The infection can range from mild sores and pimples on the skin to pneumonia or blood infection. Infections caused by staph bacteria are usually treated with the penicillin-type antibiotic methicillin, which is very effective in most cases. However, some staphylococcus strains have developed resistance to methicillin, that is, methicillin-resistant Staphylococcus aureus (MRSA). The first case of MRSA was discovered in the United Kingdom in 1961, and then it spread around the world at an alarming rate. It is the most common Gram-positive drug-resistant bacteria in clinical practice. Important target pathogenic microorganisms for the development of new antibiotics.

[0052] Method: The international standard micro broth dilution method (National Committee for Clinical Laboratory Standards. 2003. ...

Embodiment 4

[0055] DNA damage repair experiments targeting Escherichia coli:

[0056] The mechanism of the DNA damage repair experiment is to use two strains of E. coli donated by the E. coli strain bank of Yale University in the United States to carry out the control antibacterial test. One strain is wild-type E. coli AB1157 with normal DNA damage repair genes, and the other strain is DNA damage repair genes. For defective Escherichia coli AB3027, if the test sample shows significant selective inhibition to the defective strain, it indicates that the sample may have a DNA damage mechanism. Since many antibacterial and antitumor drugs have a DNA damage mechanism, the control The test can be used to screen antibacterial and antitumor drug candidates.

[0057] Method: The chlorinated depsipeptide was determined by the international standard broth dilution method (National Committee for Clinical Laboratory Standards. 2003. Methods for dilution antimicrobial susceptibility tests for bacteria ...

Embodiment 5

[0060] Insecticidal activity test:

[0061] Artemia (brine shrimp), also known as saltwater Artemia, belongs to the phylum Arthropoda, Crustacea, Anocaria, Salina Artemia, Artemia genus, is a fish bait organism with high economic value, and is also a kind of For important experimental animals that are more sensitive to toxins, the 2nd to 3rd instar larvae cultured in the laboratory can be used to evaluate the activity of insecticides.

[0062] Insecticidal activity test method (see the applicant's paper Toxicology Mechanisms and Methods, 2012, 22(1), 23-30 for details).

[0063] Artemia hatching and collection: Frozen Artemia eggs that have been stimulated and revived by indoor natural light are added to the hatching tank of a double-chamber connector culture device for cultivation. The connector is filled with seawater (30g / L) prepared from natural coarse sea salt. Dosing amount is 1g / L, first close the channel of the connector. After hatching at 28°C for 24 hours under lig...

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Abstract

The invention relates to the field of antibacterial antibiotics, antitumor drugs and insecticides, in particular to algal epiphytic fungus chlorinated depside cyclic ether compound, and preparation and application thereof. As a structural formula (I) shows, the preparation method includes: inoculating aspergillus unguis DLEP2008001 to a medium for static fermentation, subjecting fermentation broth to ethyl acetate extraction, extracting mycelia from organic solvent, subjecting crude extract to gradient silica gel chromatography via organic solvent after merger, detecting via thin layer chromatography, and continuously subjecting elution fractions eluted according to a gradient eluent volume ratio of 1:2 to silica gel column, reversed-phase column and gel column chromatography, isolation and purification to target compound. The compound is capable of inhibiting methoxyl penicillin resistant staphylococcus aureus, selectively inhibiting DNA (deoxyribonucleic acid) damage, remedying defective genotype escherichia coli, killing young brine shrimps and inhibiting growth of a human lung cancer cell line A-549, and has potential uses as antibacterial antibiotics, antitumor drugs and insecticides.

Description

technical field [0001] The invention relates to the fields of antibacterial antibiotics, antitumor drugs and insecticides, in particular to a chlorinated depsipepsyl acid cyclic ether compound of algae epiphytic fungus and its preparation and application. Background technique [0002] At present, in clinical treatment, it is found that the drug resistance of pathogenic microorganisms is getting stronger and stronger, especially the infection caused by methicillin-resistant Staphylococcus aureus (MRSA) is becoming more and more serious, and many traditional antibiotics have basically lost their efficacy; in addition, clinical treatment It is found that the drug resistance of tumors is also increasing, and multi-drug resistance is emerging. The existing anti-tumor drugs are becoming more and more inadequate in clinical chemotherapy. Therefore, it is necessary to find new types of antibiotics and anti-tumor drugs to meet the needs of clinical drug development. need. In additi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C12P17/02C07D321/10A61P31/04A61P35/00A01P7/00C12R1/66
CPCY02A50/30
Inventor 张翼穆军冯妍
Owner DALIAN JIAOTONG UNIVERSITY