Actinomycin compound as well as preparation method and application thereof

A technology of actinomycin and compounds, which is applied in the field of actinomycin compounds and their preparation, can solve problems such as limiting the application range of drugs, slow metabolism of actinomycin D, and accumulation of toxicity, so as to solve the problem of drug sources, Low cost, rapid growth effect

Inactive Publication Date: 2019-02-26
YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the strong toxicity of actinomycin D limits the scope of application of this type of drug, and pharmacological studies have shown that actinomycin D metabolizes slowly in the body and accumulates in the host cell nucleus, which will also directly lead to the accumulation of toxicity

Method used

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  • Actinomycin compound as well as preparation method and application thereof
  • Actinomycin compound as well as preparation method and application thereof
  • Actinomycin compound as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] The isolation and identification of embodiment 1 Streptomyces S011

[0050] 1. Isolation of bacteria

[0051] Healthy plant samples were rinsed with running water, then air-dried at room temperature for 48 hours, and cleaned ultrasonically at 160W for 5 minutes to remove soil and organic residues on the plant surface. The surface disinfection of plant samples was carried out according to the following procedures: soaking in 70% ethanol for 5 minutes, soaking in 2% sodium hypochlorite for 5 minutes, soaking in 10% sodium bicarbonate for 10 minutes, and cleaning the samples with sterile water three times after each operation. The surface-sterilized plant samples were dried in a sterile environment and treated at 80°C for 30 minutes, then the plant samples were crushed with a sterile pulverizer and spread on the surface of the isolation medium, and the isolated strains were cultivated at 28°C. After the actinomycetes grew out, the single clone was picked and purified on t...

Embodiment 2

[0055] Embodiment 2 Application of Streptomyces S011 to produce actinomycin D and actinomycin compounds (desmethylactinomycin B)

[0056] 1. Strain fermentation

[0057] (1) Seed culture: inoculate the spores of Streptomyces S011 on the enrichment medium, and culture at a constant temperature of 28°C for 3-5 days to obtain the strain.

[0058] (2) Fermentation culture: Pour the sterilized PDA medium into a sterilized petri dish while it is hot, 25 mL / plate, set it upside down for later use. Bacteria were picked with a sterilized bamboo stick, inoculated on PDA medium, and incubated at a constant temperature of 28°C for 11 days.

[0059] 2. Separation and purification of active ingredients

[0060] (1) After 11 days of fermentation, cut the agar into pieces in a glass container, soak overnight with ethyl acetate: methanol: glacial acetic acid = 80:15:5, and then extract ultrasonically. After filtration, the extract is concentrated under reduced pressure to recover the solvent...

Embodiment 3

[0068] The biological activity application of embodiment 3 compound 6 and 8

[0069] 1. Determination of antibacterial activity in vitro

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Abstract

The invention discloses an actinomycin compound as well as a preparation method and application thereof. A streptomycete used for producting the actinomycin compound is Streptomyces sp.S011 and is preserved in CGMCC (China general microbiological culture collection center) on June 6, 2018, and the preservation No. is CGMCC No.15910. The chemical structural formula of the actinomycin compound is shown as the formula (I) in the original specification. The method for producing the actinomycin compound, which is provided by the invention, comprises a step of fermenting the streptomycete S011; an actinomycin D and the actinomycin compound (a demethylation actinomycin B) can be produced in a large scale through industrial fermentation, wherein the demethylation actinomycin B is a new compound, the two compounds have good antibacterial property and cytotoxic activity, therefore, the method is wide in application prospect.

Description

technical field [0001] The invention belongs to the technical field of microbiology and organic chemistry, and in particular relates to an actinomycin compound and its preparation method and application. Background technique [0002] Although antibacterial drugs have played a huge role in overcoming the infection and threat of pathogenic bacteria to human beings, with the extensive use of antibacterial drugs, drug-resistant bacteria continue to emerge, and even super-resistant bacteria. At present, the time interval between the clinical application of antibiotics and the emergence of drug-resistant strains is getting shorter and shorter. Compounds with new antibacterial mechanisms are increasingly difficult. Therefore, it is imminent to find antibacterial active ingredients with new mechanisms of action. Finding antibacterial active ingredients (especially anti-drug-resistant bacteria ingredients) from new raw materials has gradually become the focus of research and develop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12N1/20C07K7/06C12P21/02A61K38/08A61P35/00A61P31/04A61P31/10C12R1/465
CPCA61K38/00A61P31/04A61P31/10A61P35/00C07K7/06C12P21/02C12N1/205C12R2001/465
Inventor 张晓梅赵庆黄之镨靳锦赵玉瑛马伟光
Owner YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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