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4'-N-demethyl-vicenistatin as well as preparation method and application thereof

A methyltransferase and drug technology, applied in the fields of botanical equipment and methods, biochemical equipment and methods, applications, etc., can solve the problems of increasing the probability of repeated discovery of strains and secondary metabolites, and difficulty in research and development of microbial-derived drugs.

Active Publication Date: 2022-01-11
SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In recent years, the research and development of microbial-derived drugs has gradually become difficult. Terrestrial microbial resources, mainly soil actinomycetes, have undergone long-term, high-intensity, and large-scale screening for nearly 80 years, resulting in repeated discoveries of strains and secondary metabolites. greatly increased odds

Method used

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  • 4'-N-demethyl-vicenistatin as well as preparation method and application thereof
  • 4'-N-demethyl-vicenistatin as well as preparation method and application thereof
  • 4'-N-demethyl-vicenistatin as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Construction of embodiment 1 methyltransferase gene mutant strain SCSIO Mla-L010 / ΔvicG

[0045] 1. Construction of S.parvus SCSIO Mla-L010 Genomic Library and Screening of Cosmids Containing Methyltransferase Genes

[0046] 1.1 Construction of S.parvus SCSIO Mla-L010 Genomic Library

[0047] The S.parvus SCSIO Mla-L010 genomic library was constructed with reference to the SuperCos1 Cosmid Vector Kit (Agilent) and Gigapck III XL packingExtract (Epicentre) operating manuals. After submerged culture of S.parvus SCSIO Mla-L010 strain for 2 days, the cells were collected by centrifugation, and genomic DNA was extracted by phenol-chloroform extraction. Take a suitable concentration of high-purity DNA and add a certain concentration of Sau3AI enzyme, and react for a certain period of time to digest the genomic DNA into a suitable fragment size, which can be tested on a nucleic acid gel, and the digested product is extracted and purified with phenol-chloroform and dephosphoryl...

Embodiment 2

[0062] Example 2 Separation and structure identification of 4'-N-demethyl-vicenistatin

[0063] The fermentation culture of the 4'-N-demethyl-vicenistatin production bacterial strain SCSIO Mla-L010 / ΔvicG was prepared using the scale fermentation conditions described in Example 1, and the mycelium precipitate and fermentation surface were separated by centrifugation (4000r / min, 15min). Serum. Add 3 times the volume of acetone to the mycelium precipitate for extraction, repeat the extraction 3 times, and concentrate the extract under reduced pressure to form an extract. An equal volume of butanone was added to the fermentation supernatant for extraction three times, and the extract was concentrated under reduced pressure to form a concentrated extract. Combine the above two parts of concentrated extracts, add silica gel to mix the sample, and then perform normal phase silica gel column chromatography, and use chloroform / methanol system to carry out gradient elution according to...

Embodiment 3

[0067] Example 3 4'-N-demethyl-vicenistatin measures the minimum inhibitory concentration of a series of active indicator strains

[0068] The antibacterial activity of vicenisatin and 4'-N-demethyl-vicenistatin was evaluated by the broth microdilution method. Dissolve vicenisatin, 4'-N-demethyl-vicenistatin, and positive controls vancomycin (Vancomycin), ampicillin (Ampicillin), and amphotericin B (Amphotericin B) in dimethyl sulfoxide (DMSO) to prepare the final The drug solution with a concentration of 1.6mg / mL should be stored in a -20°C refrigerator for later use.

[0069] Select Mueller-Hinton (MH) broth liquid medium to cultivate the active test strain, its formula is as follows beef extract powder 300g / L, soluble starch 15g / L, casein acid hydrolyzate 17.5g / L, adjust the pH value to 7.3, Sterilize at 121°C for 30 minutes for later use.

[0070]Dilute the overnight cultured test bacteria solution with MH medium until the absorbance value at 600nm wavelength is approxim...

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Abstract

The invention discloses 4'-N-demethyl-vicenistatin as well as a preparation method and application thereof, and belongs to the technical field of natural products. According to the present invention, the N-demethylation vicenatistatin derivative 4'-N-demethylation-vicenistatin is separated from the N-methyltransferase inactivated mutant strain SCSIO Mla-L010 / [delta] vicG of S.parvus SCSIO Mla-L010, the test result shows that the 4'-N-demethylation-vicenistatin has significant inhibitory activity on a variety of fungi and bacteria, the important value of the 4'-N-demethylation-vicenistatin in the development of anti-infection drugs is displayed, the antibacterial activity of the 4'-N-demethylation-vicenistatin on fungi Candida albicans is 2-4 times stronger than the antibacterial activity of vicenistatin on fungi Candida albicans, and the derivative with the structure has better patent medicine potential. In addition, the 4'-N-demethyl-vicenistatin also shows relatively strong cytotoxic activity on a plurality of cancer cells, and has the potential of being developed into an anti-tumor drug.

Description

Technical field: [0001] The invention belongs to the technical field of natural products, and specifically relates to 4'-N-demethyl-vicenistatin and its preparation method and application. Background technique: [0002] Broad-spectrum, high-efficiency, and low-toxicity antibiotics have always been considered one of the greatest inventions of mankind in the 20th century. As the main antibiotic-producing bacteria, many secondary metabolites produced by actinomycetes have been developed and utilized as antibacterial drugs with clinical application value in medical and health, such as erythromycin and vancomycin, which are used in clinical anti-infection antibiotics. (vancomycin), daptomycin (daptomycin), etc. However, due to the widespread abuse and misuse of antibiotics in the world, the emergence of antibiotic resistance is becoming more and more frequent, and pathogenic microorganisms can easily acquire drug resistance genes from the environment, which leads to the effectiv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/02A61K31/7052A61P35/00A61P31/04A61P31/10A61P35/02C12N15/76C12N15/54C12N1/21C12R1/465
CPCC07H17/02A61P35/00A61P31/04A61P31/10A61P35/02C12N15/76C12N9/1007C12Y201/01Y02A50/30
Inventor 李青连鞠建华梁智铖李骏凌春耀
Owner SOUTH CHINA SEA INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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