39 results about "Macrolide resistance" patented technology

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 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.

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.

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 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 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.

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 a solid-phase extraction process method for detecting veterinary drug residues in an animal-derived sample, and belongs to the technical field of analysis of harmful residues in food. The method comprises the steps of sample pretreatment, solid-phase extraction column activation balance, sample loading, multi-stage washing and core collaborative elution. Especially, core collaborative elution adopts a collaborative elution method combining three-stage pH gradient elution and two-time competitive acetone pulse injection. The method comprises the following steps: firstly, eluting sulfonamides and quinolones under an acidic condition; then injecting acetone to competitively remove phospholipid; then, the tetracycline and macrolide drugs are eluted under the neutral condition; injecting acetone again for deep purification; and finally, eluting the chloramphenicol medicine under an alkaline condition. According to the method, the problem that the recovery rate and the purification degree are difficult to consider when multiple types of veterinary drug residues in the egg high-phospholipid complex matrix are synchronously detected is effectively solved, and the accuracy, the sensitivity and the reproducibility of subsequent LC-MS / MS analysis are remarkably improved.

The present invention relates to a composition and a method for rapidly and accurately detecting Mycoplasma pneumoniae and macrolide-resistant mutations thereof. Specifically, the present invention provides: a loop-mediated isothermal amplification (LAMP) primer set of SEQ ID NOs: 1 to 6 targeting the 23S rRNA gene of Mycoplasma pneumoniae; and a RHAM probe set of SEQ ID NOs: 7 to 9 specifically identifying the wild-type, the A2063G mutation, and the A2064G mutation, respectively. By using the primer and probe sets, it is possible to simultaneously determine the presence or absence of Mycoplasma pneumonia infection and the presence or absence of major macrolide resistance mutations within 30 minutes using a single reaction.

The purpose of the present invention is to provide a method for producing an animal model infected with Enterobacteriaceae bacteria such as pathogenic Escherichia coli. Provided is a method for producing an animal model infected with Enterobacteriaceae bacteria, the method comprising step (1) and step (2) in the following order. (1) A step for administering a β-lactam antibacterial agent to a non-human mammal; (2) a step including the following steps (2-1) and (2-2) in random order; (2-1) a step for administering at least one selected from the group consisting of lincomycin antibacterial agents and macrolide antibacterial agents to the non-human mammal; and (2-2) a step for administering Enterobacteriaceae bacteria to the non-human mammal

The invention belongs to the field of synthetic biology and microbial pharmacy, and particularly relates to recombinant streptomyces, a construction method of the recombinant streptomyces and application of the recombinant streptomyces in preparation of savermectin B. According to the present invention, after the aveA1 gene segment in the abamectin biosynthesis gene cluster in the streptomyces avermectin is replaced with the nemA1 gene segment in the nemadectin biosynthesis gene cluster in the streptomyces blue griseolus, the recombinant streptomyces capable of producing the 16-membered macrolide compound-Sesvermectin B (Senvermectin B), such as the recombinant streptomyces avermectin HU520-M provided by the invention, is obtained; experiments show that the savermectin B has efficient insecticidal, acaricidal and anti-parasitic activity, and shows good industrial development potential.

The present invention relates to the field of therapeutics and, more in particular, to pharmaceutical compositions for the prevention and / or treatment of bacterial infections and antibacterial-induced dysfunctions. The compositions of the present invention demonstrate high species-specificity in inhibiting the growth of a small number of bacterial species, and most importantly are effective also against multi drug resistant (MDR) clinical isolate species. Interestingly, one of those combinations pairs a non-antibiotic drug, vanillin, with an antibiotic drug, spectinomycin, to demonstrate a surprisingly strong inhibitory effect on the growth of clinically relevant Gram-negative pathogenic and multi-drug resistant E. coli isolates. A second set of compounds combines the polymyxin colistin with loperamide, a rifamycin, or a macrolide. Importantly, this invention relates to combinations that enable narrow-spectrum antibacterial therapies, constituting a major effort of current and future drug development efforts in order to prevent major side effects of antibacterial strategies. This invention also relates to pharmaceutical combinations useful to prevent an adverse effect on the gut microbiome, induced by the use of antibacterial compounds.

The application discloses a strain of macrolide antibiotic high-efficiency degradation fungus Trichoderma asperellum TS7-1 and application thereof, and belongs to the technical field of microorganisms. The preservation number of the Trichoderma asperellum TS7-1 is CGMCC No.41372. The strain Trichoderma asperellum TS7-1 (CGMCC No.41372) provided by the application has high-efficiency degradation capacity for various macrolide antibiotics (erythromycin, roxithromycin and azithromycin), and the removal rates of the three antibiotics are all above 85% within 36 hours. The high-concentration antibiotic tolerance, degradation rate and degradation spectrum of the Trichoderma asperellum TS7-1 are obviously superior to those of other strains in the prior art. The Trichoderma asperellum TS7-1 is directly separated from a natural soil body without antibiotic pollution, has no hidden danger of animal and plant pathogenicity, and has no microbial toxicity to degradation products of the macrolide antibiotics, so that secondary pollution is avoided, and excellent environmental safety is achieved.

The invention discloses a defect engineering modified composite catalyst as well as a preparation method and application thereof, and belongs to the technical field of environmental material preparation. The preparation method comprises the following steps: (1) performing reduction heat treatment on a titanium silicalite molecular sieve in a hydrogen-containing inert atmosphere to obtain an oxygen vacancy-containing titanium silicalite molecular sieve; and (2) stirring and mixing the oxygen vacancy-containing titanium silicalite molecular sieve solution and the ferric salt solution, centrifuging the product, washing with water, washing with alcohol, and drying to obtain the defect engineering modified composite catalyst. The titanium silicalite molecular sieve is firstly subjected to reduction heat treatment to construct oxygen vacancies, then iron ions are specifically anchored on the oxygen vacancies, the composite catalyst with excellent photocatalytic activity and stability is prepared, the composite catalyst is used for treating macrolide antibiotics in water, and efficient degradation of antibiotic wastewater is achieved.

This invention relates to agricultural biological control technology, aiming to provide a bamectin-degrading strain, Ldeb-1, and its application in enhancing the resistance of parasitic wasps. This strain is deposited at the China Center for Type Culture Collection (CCTCC), with the deposit name *Stenotrophomoans maltophilia* Ldeb-1 and the Latin taxonomic name *Stenotrophomoans maltophilia*, and the accession number CCTCC NO: M 20252462. The 16S rRNA gene sequence of the strain is shown in SEQ ID NO: 1. This invention provides a novel strain with outstanding degradation activity against the next-generation macrolide insecticide bamectin, offering a highly targeted and precise tool for addressing bamectin pesticide residue problems. Introducing a strain derived from a specific parasitic wasp species into its own species can enhance the parasitic wasps' intrinsic resistance to bamectin, representing a green, safe, and sustainable technology.

A macrolide compound and a preparation method and application thereof are provided. The macrolide compound has a structure represented by Formula I. A pharmaceutical composition or a veterinary pharmaceutical composition, which includes the macrolide compound with a structure represented by Formula I, is also provided. Moreover, a pharmaceutical preparation, which includes the macrolide compound with a structure represented by Formula I, is provided. The macrolide compound, veterinary pharmaceutical composition and pharmaceutical preparation can be used to treat pathogen infections, especially to treat pathogen infections in animals, with a significant effect.

The invention discloses a preparation method of a tGmR bacterial sensor, a product of the tGmR bacterial sensor and application of the tGmR bacterial sensor. The tGmR bacterial sensor contains recombinant plasmids pET-mpR-tetR-mpA-tetM. The biosensor disclosed by the invention can realize real-time, low-cost and biological related detection on chemical pollutants; the genetic stability is better; resistance genes tetM and mpphA are introduced, so that the detection sensitivity and the tolerance to high-concentration antibiotics are improved; on the basis of bacteria, the bio-available concentration of tetracycline and macrolide antibiotics can be detected at the same time; the detection limit of the tGmR bacterial sensor on tetracycline is 11.1 [mu] g / L, the LOD of the tGmR bacterial sensor on erythromycin is 16.3 [mu] g / L, and in addition, the tGmR bacterial sensor can simultaneously detect the erythromycin with the maximum of 125 [mu] g / L and the tetracycline with the maximum of 250 [mu]

This invention discloses a magnetic organic polymer for the enrichment and extraction of macrolide antibiotics, its preparation, and its application. The magnetic organic polymer has a core-shell structure, with magnetic Fe3O4 nanoparticles as the core and a Tb-PDAN organic polymer formed by the reaction of trimesin and terephthalonitrile as the shell. This magnetic organic polymer can be used as an adsorbent for the enrichment and extraction of macrolide antibiotics in water, enabling qualitative and / or quantitative detection of macrolide antibiotics. The magnetic organic polymer of this invention can simultaneously, rapidly, and efficiently extract 16 macrolide antibiotics from water and is reusable, making it of significant importance for advancing the monitoring of macrolide antibiotics in water.

Disclosed herein are macrolide compounds having senolytic activity. These compounds selectively target senescent cells, and may be used to reduce or eradicate senescent cells in a subject, and / or delay the onset of aging. These compounds also inhibit propagation of cancer stem cells, and may be used to treat cancer, and in particular inhibit the propagation of cancer stem cells responsible for metastasis and tumor recurrence. Formulae (I) & (II):