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Benzoxyazepine compound having antibacterial activity, and preparation method and application thereof

A technology for benzoazepines and compounds, which is applied in the field of natural compound extraction, can solve the problems of reduced efficacy of antibacterial drugs, no drugs available, and the like

Active Publication Date: 2019-01-29
福建圣维生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the face of thorny problems such as the continuous escalation of bacterial resistance, the reduction of the efficacy of antibacterial drugs, and the lack of clinical availability of drugs, the development of new anti-drug-resistant bacteria is imminent

Method used

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  • Benzoxyazepine compound having antibacterial activity, and preparation method and application thereof
  • Benzoxyazepine compound having antibacterial activity, and preparation method and application thereof
  • Benzoxyazepine compound having antibacterial activity, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] A strain was screened from Fujian Donghai sponge and named FIM06-0025. After testing, its taxonomic characteristics were as follows.

[0045] 1.1. Physicochemical properties of strains

[0046] The single colony morphology of strain FIM06-0025 in nutrient agar medium is as follows: figure 1 shown. From the scanning electron microscope figure of bacterial strain FIM06-0025 ( figure 2 ) shows that the mycelium in the base is well developed, the branches are separated, the diameter is 0.4μm, and a single spore is born on the short sporophysis.

[0047] Under sterile conditions, use an inoculation loop to inoculate the screened strain FIM06-0025 on the agar slant medium of the following ISP1-ISP7, culture at 32°C for 2-5 days, and observe and record the cultivation of the FIM06-0025 strain in different media Features (see Table 1 below).

[0048] The nutrient agar culture medium includes the following components (g / L): beef extract 3.0, peptone 10.0, yeast extract 2.0,...

Embodiment 2

[0076] The fermentation of embodiment 2 bacterial strains

[0077] Take a Platinum ring-preserved strain Verrucosispora gifhornensis FIM06-0025 and inoculate it into the seed medium, and culture it on a shaker at 26°C and 240rpm for 223 days to obtain the seeds of V.gifhornensis FIM06-0025 culture medium.

[0078] Inoculate the seed culture solution of the obtained strain FIM06-0025 into the prepared fermentation medium with an inoculum volume fraction of 5-10%, and carry out shaking table fermentation culture at 26°C and 240rpm for 4-5d to obtain Verruca Fermentation broth of V. gifhornensis FIM06-0025.

[0079] Described high asparticine agar slant medium comprises following component (g / L): Soluble starch 20.0g, asparagine 0.5g, sea salt 16.5g, NaCl 0.5g, KNO 3 1.0g, K 2 HPO 4 0.5g, MgSO 4 ·7H 2 O 0.5g, CaCO 3 1.0g, 12.0g of agar, 1000mL of seawater, natural pH value; its preparation method is to mix all components according to their content, sterilize at 121°C fo...

Embodiment 3

[0083] The extraction of embodiment 3 compound

[0084] With 50L of the fermentation broth of Verruca V.gifhornensis FIM06-0025 prepared in the above-mentioned embodiment 2, centrifuge under the condition of 4500rpm, obtain mycelium and supernatant respectively, standby;

[0085] Take the separated mycelium, add 1.5-2.0 times the volume of methanol-acetone mixed solvent (1:1, v:v) and mix well, perform ultrasonic extraction twice, control the ultrasonic temperature below 40°C, and ultrasonic time for 30 minutes; Collect the extract and concentrate under reduced pressure at a temperature lower than 40°C to remove the methanol-acetone solvent to obtain the first extract (210g); combine the obtained first extract with the above-mentioned separated supernatant, and obtain the combined solution 1.5-2.0 times the volume of ethyl acetate was added for extraction twice, followed by concentration under reduced pressure at a temperature lower than 40°C to remove ethyl acetate to obtain ...

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Abstract

The invention belongs to the technical field of natural compounds, and particularly relates to a benzoxyazepine compound having antibacterial activity, and a preparation method and an application thereof. The benzoxyazepine compound has a new structure and is prepared by fermenting and extracting V. Gifhornensis FIM06-0025, screened by the inventor. A test proves that the benzoxyazepine compound has broad-spectrum inhibition activity on Gram negative bacteria and Gram positive bacteria, especially having strong inhibition activity on Gram negative bacteria, such as helicobacter pylori and klebsiella pneumonia, and Gram positive bacteria, such as staphylococcus aureus, so that the compound can be used for preparing a broad-spectrum antibacterial medicine.

Description

technical field [0001] The invention belongs to the technical field of extraction of natural compounds, and in particular relates to a benzoazepine compound with antibacterial activity and a preparation method and application thereof. Background technique [0002] Since the discovery of the medical antibiotic penicillin in 1929 and the agricultural antibiotic blasticidin S in 1958, more than 4,000 antibiotics have been discovered around the world, playing an important role in the prevention and control of human and animal diseases and agricultural pest control, and promoting human civilization. and scientific and technological progress. [0003] However, the use of a large number of broad-spectrum antibiotics has accelerated the evolution of pathogenic bacteria, and has also led to the increasing drug resistance of pathogens, especially bacterial pathogens, which has reduced the efficacy of existing drugs. In addition, the extensive use of broad-spectrum antibiotics has als...

Claims

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Application Information

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IPC IPC(8): C07D267/02C07D267/14A61K31/553A61P31/04A61P31/10C12P17/14C12N1/20C12R1/01
CPCC07D267/02C07D267/14C12P17/14C12N1/205C12R2001/01Y02A50/30
Inventor 陈名洪江红张文龙林如谢阳方东升连云阳
Owner 福建圣维生物科技有限公司