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Antibacterial compound derived from fungal metabolites, preparation method and application

A compound and antibacterial drug technology, applied in the field of antibacterial compounds, can solve problems such as depletion, resource scarcity, and fewer wild plants, and achieve the effect of inhibiting growth and alleviating the depletion of plant resources

Active Publication Date: 2021-09-17
HUBEI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 1. Extracting chemical components from plants has been an important means of discovering active compounds in the past few decades, but with the deepening of people's research, there are gradually fewer wild plants available for large-scale research, which is likely to cause resource scarcity or even depletion
[0006] 2. The irrational use or even abuse of antibiotics has led to the emergence of drug-resistant Staphylococcus epidermidis. Drug-resistant Staphylococcus epidermidis infection has become a difficult problem, and effective drugs are urgently needed to combat drug-resistant antibiotics

Method used

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  • Antibacterial compound derived from fungal metabolites, preparation method and application
  • Antibacterial compound derived from fungal metabolites, preparation method and application
  • Antibacterial compound derived from fungal metabolites, preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation of embodiment 1 antibacterial compound

[0040] 1. Fermentation and extraction

[0041]Inoculate the Aspergillus spp. stored at 4°C on high-temperature sterilized potato dextrose agar medium (PDA medium), activate it in an incubator at 28°C for 7 days, and use it as a seed plate. Mix 10.0kg rice with water at a ratio of 1:1, sterilize at 121°C and 15psi for 30 minutes, add Aspergillus nigeri after cooling to room temperature, seal with sterile parafilm, ferment at a constant temperature of 25°C for 30 days, then add ethyl acetate to stop the cultivation and fermentation . Use 20L of 95% ethanol to extract the fermented product, concentrate the extract under reduced pressure to obtain 200g of crude extract, then sequentially extract with equal volumes of ethyl acetate: water and petroleum ether: 95% methanol, and recover the solvent from the 95% methanol extraction part to obtain 40g extract.

[0042] 2. Separation

[0043] 40g of the methanol part ex...

Embodiment 2

[0047] The structural identification of embodiment 2 compound

[0048] The structures of compounds 1-4 were obtained by nuclear magnetic resonance (NMR) and computational ECD methods.

[0049] 1. Physical and chemical data

[0050] 2′S-formoic acid A (compound 1): brown powder; HRESIMS[M+H] + m / z 213.0175 (calculated value C 10 h 9 o 5 ,213.0763); ;UV(CH 3 OH)λ max (logε)=225(4.726), 241(4.538), 350(4.122)nm; IR(KBr)ν max 3237,2957,2874,1649,1588,1477,1410cm –1 ; 1 H and 13 See Table 1 for CNMR data.

[0051] 8-methoxymellein (compound 2): brown needle-like crystals; m / z calculated value C 11 h 12 o 3 : 192.0786; 1 H and 13 See Table 1 for C NMR data.

[0052] Conidiogenone C (compound 3): yellow oily liquid; m / z calculated value C 20 h 30 o 2 :302.2246; 1 H and 13 CNMR data, see Table 2.

[0053] n-hexacos-5,8,11-trienoic acid (compound 4): colorless oily liquid; m / z calculated value C 26 h 46 o 2 :490.3498; 1 H and 13 C NMR data, see Table 2. I...

Embodiment 3

[0065] Embodiment 3 has the application research of the compound of antibacterial activity

[0066] Gram-negative bacteria (Escherichia coli, Salmonella) and Gram-positive bacteria (Staphylococcus epidermidis, Staphylococcus aureus) were selected as the targets, and the antibacterial activity of the compounds was evaluated by the micro broth dilution method.

[0067] Inoculate Escherichia coli, Salmonella, Staphylococcus epidermidis and Staphylococcus aureus into 10ml of culture solution, and when the bacteria enter the logarithmic growth phase, dilute them with NB broth until the McFarland turbidity is 0.5, and the number of bacteria at this time is 10 8 CFU / mL, then diluted 1:1000, treated with compound 1, 2, 3 or 4 respectively, placed in a constant temperature incubator at 37°C for 16-24h, and observed the results.

[0068] Bacterial culture: Escherichia coli, Salmonella, Staphylococcus epidermidis and Staphylococcus aureus were grown in NB medium. Culture the bacteria in...

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Abstract

The invention belongs to the technical field of biological medicines, and particularly relates to an antibacterial compound derived from fungal metabolites, a preparation method and application. According to the invention, endophytic fungus Aspergillius westerdijkiae derived from a traditional Chinese medicine Hypericum perforatum L is cultured and fermented to obtain a secondary metabolite, a new compound 1 and known compounds 2-4 are separated from fermentation metabolites of the strain, gram-negative bacteria (escherichia coli and salmonella) and gram-positive bacteria (staphylococcus epidermidis and staphylococcus aureus) are selected as research objects, the antibacterial activity of the compounds is evaluated by adopting a trace broth dilution method, and the results show that the compounds 1-4 have certain bacteriostatic activity and can be expected to be developed into antibacterial drugs.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to an antibacterial compound derived from a fungal metabolite, a preparation method and an application. Background technique [0002] Staphylococcus epidermidis is a Gram-positive coccus belonging to the Bacteroidaceae family, which exists on human skin and mucous membranes. In the past, Staphylococcus epidermidis was considered not to be pathogenic to humans, but now it is considered to be a common and important pathogenic bacteria, and the phenomenon of drug resistance is becoming more and more serious, causing difficulties in treatment. When the human body's resistance decreases or Staphylococcus epidermidis leaves the skin and mucous membranes and other normal living parts, it will cause many infections and endanger the human body when it arrives at abnormal parasitic parts. Today, drug-resistant S. epidermidis infection has become a thorny problem in valve repa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C65/01C07C57/03C07C62/38C07D311/76A61K31/201A61K31/192A61K31/19C12P17/06C12P7/42C12P7/26C12P7/40A61P31/04C12R1/66
CPCC07C65/01C07C57/03C07C62/38C07D311/76C12P17/06C12P7/42C12P7/26C12P7/40A61P31/04C07C2603/97Y02A50/30
Inventor 胡琳珍肖雪洋江雯童周周慧胡天卉罗梦颖
Owner HUBEI UNIV