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Cyclic lipopeptide antibiotic and preparation and application thereof

A cyclolipopeptide and antibiotic technology, applied in the field of biomedicine, can solve the problems of not being able to administer alone, no oral dosage form, high price, etc., and achieve the effect of high medical application value, obvious prevention and treatment effect, and excellent toxicity.

Inactive Publication Date: 2013-02-06
WUXI NO 4 PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Terbinafine has low curative effect and cannot be administered alone; polyenes have serious adverse reactions; azoles can only inhibit but not kill fungi; although echinocandins are effective for Candida and Aspergillus, and The safety is high, but it faces two major problems of no oral dosage form and high price, which limits their clinical application

Method used

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  • Cyclic lipopeptide antibiotic and preparation and application thereof
  • Cyclic lipopeptide antibiotic and preparation and application thereof
  • Cyclic lipopeptide antibiotic and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Preparation of cyclolipopeptide antibiotic cyclononapeptide

[0033] (1) Transfer strain B7 from a glycerol tube stored in a -80°C refrigerator to nutrient agar medium, and culture at 32°C for 24-72 hours;

[0034] (2) Put the activated strain into 50mL seed culture medium in a 250mL Erlenmeyer flask, shake and culture at 32°C and 220rpm for 24h, which is the first-grade seed solution;

[0035](3) Put the first-grade seed solution into 200mL seed medium in a 500mL Erlenmeyer flask, and culture it at 32°C and 220rpm for 24 hours with shaking to obtain the second-grade seed solution;

[0036] (4) Put the secondary seed liquid into a 2L Erlenmeyer flask containing 500mL of fermentation medium at an inoculum amount of 5%-10% (v / v), and culture at 28°C and 200rpm for 96h with shaking to obtain a fermentation broth.

[0037] Nutrient agar medium, prepared as follows: beef extract 3g, peptone 10g, sodium chloride 5g, agar 17g, distilled water 1000mL, pH7.2;

[003...

Embodiment 2

[0044] Example 2 Determination of cyclolipopeptide antibiotic cyclononapeptide

[0045] The product prepared in Example 1 The relevant parameters of the compound cyclolipopeptide antibiotic cyclononapeptide are as follows:

[0046] Appearance: white powder after freeze-drying;

[0047] Molecular weight: 1100;

[0048] Molecular formula: C 54 h 92 N 12 o 12 ;

[0049] ESI-MS spectrum: see figure 1 ;

[0050] ESI-MS-MS spectrum: see figure 2 .

[0051] According to the above characteristics, it can be inferred that the compound is a new cyclolipopeptide antibiotic containing nine amino acids, and it is named cyclononapeptide. The antibiotic is another new cyclolipopeptide antibiotic isolated from Paenibacillus for the first time at home and abroad. The compound showed significant inhibitory activity against all tested Gram-positive (staphylococcus) and negative (pseudomonas and Escherichia coli) pathogenic bacteria and fungi (Candida albicans). Experiments in mice s...

Embodiment 3

[0052] Example 3 Determination of in vitro antibacterial activity of cyclolipopeptide antibiotic cyclononapeptide

[0053] Use Mueller Hinton broth medium to prepare cyclic nonapeptide antibiotics at a concentration of 256 μg / mL, and adjust the concentration of cyclic nonapeptides to 256, 128, 64, 32, 16, 8, 4, 2, 1, 0.5 μg / mL.

[0054] Add 50 μL of doubly diluted cyclic nonapeptide antibiotic solution to the 1st to 10th wells of a 96-well polystyrene plate, and add 50 μL of Mueller Hinton broth medium (acid hydrolyzed casein 17.5 g / L) to the 11th well , beef extract powder 2g / L, starch 1.5g / L) as a growth control, and 100 μL of Mueller Hinton broth medium was added to the 12th well as a negative control. The control antibiotic was polymyxin B.

[0055] After culturing the indicator bacteria for 24 hours, dilute to 10 with Mueller Hinton broth medium 6 cells / mL, add 50 μL of diluted bacterial solution to the 1st to 11th wells, seal and incubate in an incubator at 37°C for 2...

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Abstract

The invention relates to a novel cyclic lipopeptide antibiotic (cyclic nonapeptide avermectin) and preparation and application thereof, belonging to the technical field of biomedicine. The fermentation medium is inoculated with paenibacillus, the paenibacillus is cultured at 28-35 DEG C for 24-96 hours, the fermentation broth is centrifuged to take the supernatant, the supernatant is adsorbed by a macroporous adsorption resin, and separation and purification are performed further to obtain the cyclic lipopeptide antibiotic which can be used for preparing the bacterial-infection resisting medicament. The invention provides the cyclic nonapeptide avermectin with higher toxicity than polymyxin B and higher medical application value and the preparation and application of the cyclic nonapeptide avermectin. The experiments in vitro prove that the compound can inhibit all the tested Gram-positive and negative pathogens including the multiple and super medicament resisting bacteria significantly, and the in-vivo experiments prove that the compound can prevent and treat the mouse septicemia caused by theextended-spectrum medicament resisting pseudomonas aeruginosa significantly.

Description

technical field [0001] The invention relates to a novel cyclolipopeptide antibiotic-cyclic nonapeptide and its preparation and application, belonging to the technical field of biomedicine. Background technique [0002] Due to the widespread use or abuse of antibiotics, antibiotics that once played a significant role in the treatment of bacterial infectious diseases have been widely ineffective. Many common bacteria are increasingly resistant to commonly used antibiotics. At present, bacterial drug resistance has seriously threatened human health. Multidrug-resistant bacteria such as methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, and extended-spectrum β-lactamases (ESBLs)-producing Escherichia coli and Klebsiella have become a major factor in hospital transmission and fatality rates. High pathogens. The rapid emergence of vancomycin-resistant enterococci (VRE) has exacerbated people's concerns about the problem of drug resistanc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06C12N1/20C12P21/02A61K38/08A61P31/04C12R1/01
Inventor 黄朝晖
Owner WUXI NO 4 PEOPLES HOSPITAL
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