63 results about "Macrolide resistance" patented technology

According to the scheme, the invention provides the recombinant macrolide enzyme as well as the preparation method and the application thereof, the amino acid sequence of the recombinant macrolide enzyme is as shown in SEQ ID NO.1, and the recombinant macrolide enzyme is derived from an EreC esterase family of enterobacter hormaechei and is obtained through site-specific mutagenesis; the mutation sites are as follows: glutamic acid at the 44th site is mutated into asparagine, tyrosine at the 55th site is mutated into proline, proline at the 76th site is mutated into arginine, phenylalanine at the 153rd site is mutated into alanine, and serine at the 219th site is mutated into glutamic acid. The method is expected to remove macrolide antibiotic pollution, and has good economic benefits and practical values.

The invention relates to a novel 16-membered macrolide compound 13alpha-O-alpha-L-oleandrosyl-23-alpha-hydroxy-25-isopropyl milbemycin beta3, a preparation method of the novel 16-membered macrolide compound 13alpha-O-alpha-L-oleandrosyl-23-alpha-hydroxy-25-isopropyl milbemycin beta3, and an application of the novel 16-membered macrolide compound 13alpha-O-alpha-L-oleandrosyl-23-alpha-hydroxy-25-isopropyl milbemycin

The invention discloses a method for preparing an ester compound and a macrolide compound, and belongs to the technical field of organic chemistry, the preparation method of the ester compound is as follows: in an organic solvent, an alpha-carbonyl alkenyl ester compound reacts with alcohol or phenol under the catalytic condition of alkali to obtain the ester compound; the preparation method of the macrolide compound comprises the following step: in an organic solvent, carrying out intramolecular hydroxyl reaction on an alpha-carbonyl alkenyl ester compound under the catalysis condition of alkali or acid, thereby obtaining the macrolide compound. The method is wide in substrate range, high in practicability and high in yield, racemization of a carboxylic acid alpha-chiral center can be inhibited in intermolecular esterification reaction and macrocyclic lactonization reaction, and the method can be applied to total synthesis of a Brevicidine natural product containing a 13-membered cyclic ester peptide core structure; the method disclosed by the invention has the advantages of mild reaction conditions, simplicity, easiness in operation, wide substrate adaptability, no racemization of the product and the like.

According to the scheme, the recombinant macrolide enzyme and the preparation method and application thereof are provided, the amino acid sequence of the recombinant macrolide enzyme is shown as SEQ ID NO.1, and the recombinant macrolide enzyme is obtained by site-directed mutagenesis of an erythromycin esterase family protein sequence derived from enterobacter hormaechei; the mutation sites are as follows: the 44 glutamic acid is mutated into asparagine, the 55 tyrosine is mutated into proline, the 153 proline is mutated into alanine, and the 219 serine is mutated into glutamic acid, so that the specific macrolide lactonase which is efficient, stable, easy to prepare on a large scale and more suitable for environmental requirements is prepared, and macrolide antibiotic pollution is removed; and the method has good economic benefits and practical values.

The invention discloses a novel Fe-C-N-coated Au material and a preparation method and application thereof.According to the Fe-C-N-coated Au material, iron monatomic nano-enzyme Fe-C-N serves as a core, gold nanoparticles are loaded on the surface, the Fe-C-N nanoparticles and a HAuCl4 aqueous solution are stirred at low temperature, then an ice-cold NaBH4 solution is slowly added into a mixed solution, and the Fe-C-N-coated Au material is obtained after reaction and treatment. The novel Fe-C-N-coated Au material disclosed by the invention can be used for rapidly and sensitively detecting the azithromycin or macrolide drug-resistant gene ermB.

The application discloses a preparation method and application of a cobalt monatomic doped strontium titanate composite material, and belongs to the field of water treatment. The cobalt doped strontium titanate composite catalytic material is composed of a cobalt metal doped strontium titanate material. A preparation process uses tetrabutyl titanate and a nitrate as reactants, ethylene glycol and water as solvents, and prepares strontium titanate (SrTiO3: STO) through a hydrothermal method. Then, cobalt monatomic atoms are doped into the strontium titanate through cobalt chloride (a cobalt source) by using an electrostatic adsorption method, so as to form cobalt doped strontium titanate (Co-STO). The material can efficiently activate an oxidant peracetic acid and rapidly degrade various antibiotic pollutants, and especially performs well in degrading quinolone, tetracycline and macrolide antibiotics. The catalytic material has the advantages of low cost, renewability and environmental protection, and is very suitable for being applied to a deep treatment process of pharmaceutical wastewater.

The invention relates to a method for analyzing pollutants in hospital wastewater based on liquid chromatography-high resolution mass spectrometry. The method comprises the following steps: S1, enriching pollutants in hospital wastewater through solid-phase extraction of four specific solid-phase extraction columns, and then analyzing and detecting a liquid to be detected through a specific chromatographic column, a specific liquid chromatography and a high-resolution mass spectrometry which are connected in series; the identification of various pollutants (medicines and metabolites thereof) in the hospital wastewater is realized, so that a data basis is provided for subsequent fingerprint analysis. Specifically, the analysis method provided by the invention can identify 34 kinds of substances, including sulfonamide antibiotics, macrolide antibiotics, cephalosporin antibiotics, quinolone antibiotics, beta-lactam antibiotics, aminoglycoside antibiotics and carbamazepine and metabolites thereof.

The application discloses a biosynthesis gene cluster of a polyene macrolide natural product mandimycin, and a natural product and application of the biosynthesis gene cluster, wherein the nucleotide sequence of the biosynthesis gene cluster is shown as SEQ ID NO. 1, and the compound structural formula of the natural product mandimycin and mandimycin B is shown as formula I and formula II. The natural product mandimycin can target fungal cell membrane phospholipid molecules, especially phosphatidylinositol, cause important ion efflux in fungal cells, and lead to fungal cell death. The natural product mandimycin and mandimycin B have strong in-vivo and in-vitro antibacterial activity and a broad antibacterial spectrum on various WHO-published multiple drug-resistant fungal key pathogens, including candida, aspergillus, cryptococcus, mucor and fusarium.

To provide a technique relating to total secretion regulation of sebaceous gland cells.SOLUTION: The present invention provides a total secretion regulator comprising a compound selected from the group consisting of oligosaccharides and macrolide compounds as an active ingredient.SELECTED DRAWING: None

We report improved adjuvant compounds that have an aryl 2-aminoimidazole structure for macrolide potentiation against a virulent strain of gram-negative bacteria, AB5075. Compounds were discovered to retain significant adjuvant activity at 10 μM, lowering the minimum inhibitory concentration (MIC) of clarithromycin (CLR) from 8-fold to 128-fold or greater. 2-Aminoimidazole compounds linked to aryl groups via either an amide or urea linker showed significantly improved activity over control compounds.

Provided herein are synthetic methods and intermediates useful in the preparation of polyketides, including 12-membered ring macrolides. These synthetic methods and intermediates provide scalable access to polyketides, including polyketides with potent bioactive splicing modulator activity and therapeutic potential, including treating various types of cancer. The polyketides include 12-membered ring macrolides, including Compound A, Compound B, and pladienolides, including pladienolide A, pladienolide B, pladienolide C, pladienolide D, pladienolide E, pladienolide F, and pladienolide G.

This invention discloses a method for controlling potato scab, relating to the field of crop cultivation methods. The method includes: Step S1, preparing a coating agent: mixing a first active ingredient and a second active ingredient, wherein the first active ingredient is selected from neonicotinoid insecticides or macrolide insecticides, and the second active ingredient is selected from at least one of methoxyacrylates, organosulfur compounds, or inorganic copper fungicides; Step S2, seed potato coating treatment: mixing the coating composition with potato seed potatoes to ensure the composition is uniformly adhered to the seed potato surface; Step S3, sowing. This invention, through the synergistic combination of insecticides and fungicides, controls pathogens and pests at the source, combining growth-stage control and soil treatment to construct a comprehensive, multi-effect control method, improving control efficacy, reducing pesticide usage, and achieving highly efficient control of potato scab.

A new class of dimeric 2-aminoimidazole (2-AI) compounds that potentiate macrolide antibiotics against A. baumannii. A parent dimer lowers the MIC of clarithromycin (CLR) from 32 μg / mL to 1 μg / mL at a concentration of 7.5 μM (3.4 μg / mL), while a structure activity relationship (SAR) study on the dimeric 2-AI scaffold resulted in the identification of several compounds with increased activity. Substitution of fluorine on a central phenyl ring resulted in the most potent activity, with the lead compound, containing a fluorine ortho to each of the 2-AIs, that lowered the CLR MIC to 2 μg / mL against AB5075 at 1.5 μM (0.72 μg / mL), exceeding the activity of both the parent dimer and the lead aryl-2-AI. Furthermore, these dimeric 2-AI analogs exhibit favorably low mammalian cell toxicity.

The invention relates to the field of medicines, in particular to a hydroxypyridone coupled macrolide compound shown in a formula (I) or a formula (II) and application of the hydroxypyridone coupled macrolide compound in preparation of an antibacterial agent and a bacterial biofilm inhibitor. In-vivo and in-vitro pharmacological verification shows that most of the hydroxypyridone coupled macrolide compounds have antibacterial activity, can be used for preparing antibacterial agents and anti-biofilm agents, and have the potential of being developed into novel antibacterial drugs.

This invention relates to the field of agricultural biological control technology, specifically disclosing a novel bafilomycin analogue with antifungal activity, its preparation method, and its application. The bafilomycin analogue is a novel natural compound obtained by fermentation culture of Streptomyces sp. TH21, component activity tracing, and subsequent separation and extraction. This type of compound exhibits good activity against plant pathogenic fungi and has the potential to be developed into a novel, highly efficient, and environmentally friendly biological fungicide.

The application discloses a synergistic bactericidal composition, comprising the following components: a toona sinensis extract: 16-2048 mu g / mL; a macrolide antibiotic: 0.0625-4096 mu g / mL; the bacteria are staphylococcus aureus or methicillin-resistant staphylococcus aureus, and the macrolide antibiotic is erythromycin or azithromycin. The application further discloses a use of the synergistic bactericidal composition in preparation of a medicine for treating skin and soft tissue infections. The composition provided by the application can convert the traditional macrolide antibiotics such as erythromycin and azithromycin which only have a bacteriostatic effect into a preparation which has clear bactericidal activity on staphylococcus aureus and drug-resistant strains thereof. After the toona sinensis extract is combined with the antibiotic, a synergistic effect is exhibited, and the concentration of the toona sinensis extract and the antibiotic required when the toona sinensis extract and the antibiotic are used alone can be greatly reduced.

The invention relates to a molecular marker of drug-resistant mycobacterium abscessus based on fusA gene mutation and application of the molecular marker, and belongs to the technical field of biological medicines. The invention provides a group of molecular markers for detecting the drug resistance of mycobacterium abscessus. The molecular markers are mutations on a fusA gene of the mycobacterium abscessus, including fusA1318Agt; g, fusA 1613 G gt; a, fusA18721883 dup GGGCGACGTGAT, and the number of the GGGCGACGTGAT is 1: 1. The invention finds that when the mycobacterium abscessus generates fusA1613 G gt; when A is mutated, cross resistance is generated to aminoglycoside drugs, macrolide drugs and tetracycline drug tigecycline. The fusA < 1318 > A < gt > is generated; the mycobacterium abscessus with mutations of G and fusA18721883 dup GGGCGACGTGAT is resistant to aminoglycoside drugs and tigecycline, and meanwhile, the mycobacterium abscessus has lateral sensitivity to macrolide drugs. The mycobacterium abscessus with mutations of G and fusA18721883 dup GGGCGACGTGAT is resistant to aminoglycoside drugs and tigecycline. The method is of great significance to clinical molecular diagnosis and medication.

This invention discloses a screening and detection method for antibiotic residues in organic fertilizers, relating to the field of trace residue detection. The detection method includes the following steps: S1, mixing the organic fertilizer sample with a buffer solution to obtain an extract; S2, adding a divalent calcium ion compound to the extract, mixing well, allowing it to stand, centrifuging, discarding the supernatant, and collecting the precipitate; S3, adding an alkaline releasing agent to the precipitate to dissolve it, centrifuging, collecting the supernatant, and obtaining a release solution; S4, reacting the release solution with a colorimetric reagent, measuring the visible light absorbance, and calculating the antibiotic content based on a standard curve. This method not only completely avoids the destruction of antibiotics by strong acids but also transforms humic acid from an interfering substance into an enrichment tool, thereby significantly improving the extraction rate. It is simple to operate and low in cost, thus providing a novel solution for the detection of macrolide antibiotic residues in organic fertilizers.

The present invention relates to a macrolide compound, and a preparation method therefor and the use thereof. Specifically disclosed is a compound as shown in formula I or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits a significant antibacterial activity, comprising the antibacterial activity against bacteria resistant to macrolide drugs such as azithromycin. The compound described herein has a low hepatotoxicity and superior safety compared to other macrolide compounds. The compound can be used for infectious diseases, etc.

The application belongs to the technical field of medicine, and discloses a kind of amidine compound and its preparation method and application in treating bacterial infection, specifically discloses a kind of amidine compound and its pharmaceutically acceptable salt and preparation method and application in treating bacterial infection as shown in the following general formula (I).The amidine compound of the application is used in the preparation of products for enhancing the activity of other antibiotics.The antibiotics include macrolide drugs, pleuromutilin drugs, quinolone drugs, rifamycin drugs, dihydrofolate reductase inhibitor drugs, oxazolidinone drugs, lincosamide drugs, capreomycin drugs, mupirocin drugs and fusidic acid drugs.

The invention discloses an organic fertilizer for reducing antibiotics and antibiotic resistance genes in livestock and poultry manure based on combination of catalytic pretreatment and decay-promoting compost and a preparation method of the organic fertilizer, and relates to the technical field of organic fertilizer and organic solid waste recycling. The method comprises the following steps: firstly, adding a composite catalyst to treat the livestock and poultry manure, and then uniformly mixing the livestock and poultry manure with an acidic fermentation ingredient and a fermentation inoculant for promoting decomposition and composting. The degradation rate of typical antibiotics such as sulfonamides, quinolones, tetracyclines, macrolides and the like in pig manure and cow dung can reach 100%, the degradation rate of typical antibiotic resistance genes such as sulfonamides, quinolones, tetracyclines, macrolides and the like in pig manure and cow dung can reach 95%, and through the synergistic effect of catalytic pretreatment and biological treatment, the degradation rate can reach 100%, and the degradation rate of typical antibiotics such as sulfonamides, quinolones, tetracyclines, macrolides and the like in pig manure and cow dung can reach 95%. The problems that traditional compost antibiotics and antibiotic resistance genes are not thoroughly removed, and the composting period is long are solved, efficient, rapid and low-environmental-risk recycling of the livestock and poultry manure is achieved, and a reliable technical approach is provided for producing high-humic-acid organic fertilizer.

The invention relates to a suspension concentrate composition, the suspension concentrate comprising: a) at least one macrolide active substance; b) at least one aromatic hydrocarbon sulfonate condensed with formaldehyde; and c) ammonium sulfate. The invention also relates to the use of the suspension concentrate composition in pest control. The invention further relates to a method for increasing the stability of a macrolide active compound in a suspension concentrate formulation, the method comprising the use of a combination of an aromatic hydrocarbon sulfonate condensed with formaldehyde and ammonium sulfate in the formulation.

The invention discloses a method for measuring the concentration of macrolide antibiotics in domestic sewage. The method comprises the following steps: enriching and purifying macrolide compounds in a treated domestic sewage sample through a non-polar divinyl phenyl neutral polymer solid-phase extraction column and a hydrophilic group-containing polystyrene / divinyl benzene copolymer bonded piperazine group solid-phase extraction column which are connected in series, concentrating, and fixing the volume; and separating the target compound by liquid chromatography, and detecting by a triple quadrupole mass spectrometry detector to obtain the concentration of the macrolide antibiotics in the domestic sewage. The method overcomes the defects of traditional detection, reduces the interference of the matrix effect of the water sample on the internal standard, improves the quantitative accuracy, does not involve expensive materials, can obtain reagent consumables in situ, and saves the detection cost.

The invention relates to a transcription factor-based cell-free biosensor and an application thereof in water environment antibiotic detection. Firstly, a cell-free biosensor containing TetR or MphR is constructed, the cell-free biosensor comprises a DNA template, a transcription factor TetR or MphR, RNA polymerase and a DFHBI-1T fluorescent probe, the DNA template comprises a reporter gene capable of being combined with the fluorescent probe, and an operon corresponding to the transcription factor TetR or MphR is arranged on the upstream of the reporter gene; the biosensor can respond to tetracycline or macrolide antibiotics, and further, the content of the antibiotics can be measured according to the change of fluorescence intensity in a cell-free biosensor system. The invention provides the cell-free biosensor with high sensitivity and high stability, and the biosensor can realize high-efficiency detection under different water body conditions and realize stronger environmental adaptability.

The application belongs to the technical field of medicine, and discloses a kind of amidine compound and its preparation method and application in treating bacterial infection, specifically discloses a kind of amidine compound and its pharmaceutically acceptable salt and preparation method and application in treating bacterial infection as shown in the following general formula (I).The amidine compound of the application has the use in preparing the product for enhancing the activity of other antibiotics.The antibiotics include macrolide drugs, pleuromutilin drugs, quinolone drugs, rifamycin drugs, dihydrofolate reductase inhibitor drugs, oxazolidinone drugs, lincosamide drugs, capreomycin drugs, mupirocin drugs and fusidic acid drugs.

Provided are methods, compositions, and systems for detecting nucleic acids of macrolideresistant Mycoplasma genitalium. The illustrated method can involve real-time nucleic acid amplification, and further can involve processing real-time run curve data using a derivative-based analytical method to distinguish macrolide-resistant M. genitalium from macrolide-sensitive M. genitalium. Advantageously, the disclosed technique reduces the incidence of false-positive identification of macrolide resistance.

The invention belongs to the technical field of biological detection, genotype detection of a mutation site of Bordetella pertussis 23S rRNA A2047G is realized based on a PCR-melting curve method, and then macrolide antibiotic resistant Bordetella pertussis is detected, and the following technical scheme is adopted: the detection kit for the macrolide antibiotic resistant Bordetella pertussis has the advantages that the genotype of the mutation site of the Bordetella pertussis 23S rRNA A2047G mutation site is detected; the kit comprises a reaction solution, a detection solution, a sensitive positive control, a drug-resistant positive control and a blank control. The detection method comprises the following steps: S1, taking a bordetella pertussis DNA sample as a template, simultaneously using sensitive positive control, drug-resistant positive control and blank control, and using the macrolide antibiotic drug-resistant bordetella pertussis detection kit in the patent for detection; and S2, data processing: after the reaction is finished, performing result judgment through a melting curve of the sample.

The invention discloses an application of macrolide derivatives in preparation of drugs for resisting poxviridae viruses. It is found that the macrolide derivative T8 can reduce the replication level of LSDV, and the derivative is low in toxicity, has no toxic or side effect on MDBK cells, can serve as an inhibitor for efficiently resisting bovine nodular skin disease viruses, provides a powerful theoretical basis and a practical basis for further research and development of antiviral drugs, and has good application prospects. Wide application prospects are realized in the fields of breeding industry and biological medicines.

This invention discloses a method for degrading residual antibiotics in fermentation waste containing macrolide antibiotics. The method includes using antibiotic fermentation residue as the degradation raw material, stainless steel beads as the grinding medium, and oxidants and co-oxidants as ball milling aids. The mixture is ground and reacted in a ball mill jar to complete the treatment of the fermentation residue. The antibiotic content in the ball-milled residue is reduced to below 99%, with the antibiotics losing their anti-viability, and the residue can be further used for the re-fermentation of erythromycin. This invention features a short process route, low reagent consumption and cost, simple operation, and the entire process is carried out under solid-phase conditions without solvents, resulting in high degradation efficiency. It is a method for treating macrolide antibiotic fermentation residue with good prospects for widespread application.