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Octahydrofuro[2,3-b]pyridine-4,6-diol and its preparation method and application
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A technology of octahydrofuran and 3-b, which is applied in the field of octahydrofuran[2,3-b]pyridine-4,6-diol and its preparation, and can solve the problems of drug-resistant bacteria and the like
Active Publication Date: 2022-03-11
GUANGXI UNIV OF CHINESE MEDICINE
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[0005] At present, clinical antibiotics mainly achieve bactericidal effect by inhibiting the function of TPase, such as penicillin, cephalosporin, monobactamycin, ceftaroline, ceftodol, carbapenem, etc., but these act on the TPase functional domain Corresponding drug-resistant bacteria appear in clinical practice
However, moenomycin, which targets TGase to exert antibacterial effects, has been used in animal feeding for decades without drug resistance
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Embodiment 1
[0028] Example 1: Preparation and separation of octahydrofuro[2,3-b]pyridine-4,6-diol
[0029] 1. Microbial fermentation
[0030] Preparation of seed solution: Take 3g of sea salt, 1.5g of malt extract powder, 100mL of water, and shake well. At 121°C, autoclave for 20 minutes, let it cool down, and use it as a seed medium. The strain Epicoccum sorghinum GXIMD02001 was inoculated in the seed medium in a biological safety cabinet and sealed. It was cultured at 25° C. and 180 rpm for 72 hours as a seed solution.
[0031] Large-scale fermentation: Weigh 150g of rice and put it into a 1000mL Erlenmeyer flask, add 150mL of water containing an appropriate amount of sea salt, seal and shake well. Autoclave at 121°C for 20 minutes. After taking it out and letting it cool, add 10mL of seed solution. Ferment at 25°C for 25-40 days.
[0032] 2. Obtaining the extract
[0033] Crush and mix the fermented rice culture medium, add ethyl acetate for ultrasonic extraction 3 times, filter...
Embodiment 2
[0040] Example 2: Octahydrofuro[2,3-b]pyridine-4,6-diol inhibits glycosyltransferase (TGase) activity
[0041]Liposome II analogs (5 μM) containing dimethylaminoazobenzoyl and coumarin groups, N-acetylmurazyme (1 μg / μL), different concentrations of compounds (0, 2.5, 5, 10, 20, 30, 40 μM) were mixed in the buffer, and after adding Clostridium PBP (5 μg / mL), cultured at 37°C and 80% humidity for 2 hours, using an excitation wavelength of 355nm and an emission wavelength of 460nm to detect once every 2min Fluorescence concentration. Buffer was used in place of the liposome II analog in negative control experiments. The strength of competitive inhibition is represented by the inhibition constant Ki. The results are shown in Table 2. Octahydrofuro[2,3-b]pyridine-4,6-diol has a certain inhibitory effect on glycosyltransferase.
[0042] The inhibition constant of table 2 compound to glycosyltransferase
[0043]
Embodiment 3
[0044] Example 3: Octahydrofuro[2,3-b]pyridine-4,6-diol antibacterial activity
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Abstract
The invention discloses octahydrofuro[2,3-b]pyridine-4,6-diol and its preparation method and application. The compound can inhibit the activity of glycosyltransferase (TGase) and is effective against Staphylococcus aureus and Escherichia coli , Bacillus subtilis, Acinetobacter baumannii, Klebsiella pneumoniae and methicillin-resistant Staphylococcus aureus all have a certain inhibitory effect and can be used to prepare antibacterial drugs. The invention provides candidate compounds for new antibacterial drugs. The preparation method disclosed in the invention obtains the compound by separating the compound from the fermented culture medium of the marine fungus Epicoccum sorghinum GXIMD02001. Compared with the traditional chemical synthesis method, the method has the advantages of environmental friendliness and high efficiency.
Description
technical field [0001] The invention belongs to the technical field of biopharmaceuticals, and specifically relates to octahydrofuro[2,3-b]pyridine-4,6-diol and its preparation method and application. Background technique [0002] With the continuous increase of bacterial resistance and the depletion of terrestrial resources, antibiotics from terrestrial biological sources can no longer meet the needs of human health. In order to discover antibiotic lead compounds with significant activity and specific targets and reduce the chance of repeated research, people have gradually turned their attention to marine biological resources that are in a unique ecological environment, have many secondary metabolites, are novel, and are still underdeveloped. Hilary D. Marston et al pointed out that discovering new antibiotic drugs in unexploited marine natural products is an important way to solve antibiotic resistance (Journal of the American Medical Association, 2016, 316(11): 1193-1204...
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