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Antibacterial compound and application thereof

A compound, antifungal technology, applied in the field of medicinal chemistry

Active Publication Date: 2015-08-05
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, in recent decades, whether in the field of agriculture, breeding or human medicine, the abuse of antibiotics has brought huge challenges to the ecosystem and global medical and health problems

Method used

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  • Antibacterial compound and application thereof
  • Antibacterial compound and application thereof
  • Antibacterial compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] 1. Fermentation of lead compounds

[0040] Bacillus subtilis (Bacillus subtilis) ZJU007 CGMCC NO.4140 was fermented, separated and purified to obtain the lead compound Chlorotetaine, as follows:

[0041] i medium

[0042] (1) Incline medium: LB medium.

[0043] (2) Seed medium (g L -1 ): glucose 15, yeast powder 10, K 2 HPO 4 1. MgSO 4 0.5, FeSO 4 0.01, NaCl 10, add CaCO after adjusting pH 7.0 3 0.4.

[0044] (3) Fermentation medium (g L -1 ): yeast powder 2.72, soluble starch 26.67, (NH 4 ) 2 SO 4 3.95,K 2 HPO 4 2.4, NaCl 10, MgSO 4 0.5, CaCO 3 0.72, CuSO 4 0.02, FeSO 4 0.02, MnSO 4 0.02, pH 6.5.

[0045] (4) Candida albicans medium (g L -1 ): glucose 20, peptone 10, agar 20.

[0046] ii method

[0047] Strain culture conditions Take 1 cycle of activated strains and put them into a seed bottle, fill 100mL medium in a 500mL Erlenmeyer flask with an initial pH value of 7.0, and culture at 200r / min at 30°C for 24h. Then the seed solution i...

Embodiment 2

[0078] Utilize the novel antibacterial compound Chlorotetaine-Lys that embodiment 1 obtains to carry out in vitro antifungal experiment, concrete steps are as follows:

[0079] (1) Five strains of common fungal pathogenic bacteria purchased from China Microbial Culture Collection Center were activated and cultured in vitro; the above five strains of common fungal pathogenic bacteria were respectively Candida albicans (ATCC10231), Aspergillus niger (preserved in the laboratory), Candida parapsilosis (JCM1785), Candida krusei (CBS573), Candida pseudopolymorpha (ATCC 26012)

[0080] The formula of the fermentation medium of Candida and Aspergillus niger is: 4% glucose and 1.0% peptone. The above five common fungal pathogenic bacteria were placed in the above medium at 28° C. and cultured for 18-24 hours.

[0081] (2) Using a 96-well plate, the novel antimicrobial compound is formulated to a final concentration of 100 μg / mL to 0.2 μg / mL by the double dilution method;

[0082] (3...

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Abstract

The invention discloses an antibacterial compound and application thereof. The formula of the compound is showed in formula (I). The method is characterized in that bacillus subtilis with the ZJU007 CGMCC No. 4140 is used to obtain a lead compound Chlorotetaine, a drug delivery process is used as the theoretical basis to perform homologous modeling so as to build the virtual structure of small molecule peptide transport proteins, the virtual structure of the small molecule peptide transport proteins is used to optimize the structure of the lead compound Chlorotetaine to obtain a tripeptide compound with a fungus resisting capability. The antibacterial compound has the advantages that the compound can resist candida funguses such as candida albicans, candida parapsilosis, candida krusei and polymorphic candida, and minimal inhibitory concentration (MIC) can reach 0.81 microgram / mL; the compound can also resist aspergillus funguses such as aspergillus niger, and MIC can reach 1.63 microgram / mL.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to an antibacterial compound and its application. Background technique [0002] The invention and use of antibiotics is one of the greatest inventions in the 20th century. Its wide application in the field of antibacterial has relieved a lot of human suffering and brought great blessings. However, in recent decades, whether in the field of agriculture, breeding or human medicine, the abuse of antibiotics has brought huge challenges to the ecosystem and global medical and health issues. At the same time, with the continuous outbreak of drug-resistant strains and the continuous improvement of the public's requirements for public health, people's requirements for new antibiotics, especially new antifungal drugs, are becoming more and more urgent. [0003] Antimicrobial peptides (AMPs) are a class of positively charged amphiphilic (having both hydrophobic and hydrophilic pa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K5/09A61K38/06A61P31/10
Inventor 吴绵斌王涛林建平杨立荣
Owner ZHEJIANG UNIV
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