147 results about "Macrocyclic lactone" patented technology

The invention discloses trichoderma asperellum TS7-1 capable of efficiently degrading macrolide antibiotics and application of the trichoderma asperellum TS7-1, and belongs to the technical field of microorganisms. The preservation number of the trichoderma asperellum TS7-1 is CGMCC (China General Microbiological Culture Collection Center) No. 41372. The Trichoderma asperellum TS7-1 (CGMCC No.41372) provided by the invention has high-efficiency degradation capability on various macrolide antibiotics (erythromycin, roxithromycin and azithromycin), the removal rates of the Trichoderma asperellum TS7-1, roxithromycin and azithromycin in 36h all reach 85% or above, and the Trichoderma asperellum TS7-1 has high-concentration antibiotic tolerance, degradation rate and degradation spectrum obviously superior to those of other strains in the prior art. The trichoderma asperellum TS7-1 is directly separated from a natural soil body which is not polluted by antibiotics, has no animal and plant pathogenicity hidden danger, has no microbial toxicity to degradation products of macrolide antibiotics, avoids secondary pollution, and has excellent environmental safety.

The invention discloses a bacteriostatic composition which comprises a synergist and a bacteriostatic agent, the synergist is ethyl phenylacetate or a derivative thereof, and the bacteriostatic agent is selected from hydrogen peroxide, beta-lactam antibiotics, macrolide antibiotics and aminoglycoside antibiotics. The synergist disclosed by the invention is wide in synergistic effect spectrum range, and has a remarkable synergistic bacteriostatic effect when being combined with hydrogen peroxide, amoxicillin, ampicillin, benzylpenicillin potassium, erythromycin, azithromycin and amikacin; the antibacterial effect is weak when the compound is independently used, but the virulence of staphylococcus aureus can be remarkably reduced, the formation of hemolysin, staphylococcus flavin, enterotoxin and a biofilm can be inhibited, and meanwhile, the selective pressure on bacteria is favorably reduced due to the relatively low antibacterial activity, so that the occurrence of drug resistance is delayed; the method is suitable for various application scenes such as food processing industry.

The present invention relates to the field of analytical chemistry, and discloses a mass spectrum ionization element for macrolide antibiotic detection and a preparation method thereof, the mass spectrum ionization element comprises: a conductive substrate made of stainless steel; the adsorption layer is attached to at least part of the surface of the substrate, the adsorption layer is formed by a boric acid functionalized covalent organic framework, and the boric acid functionalized covalent organic framework is of a polycyclic structure composed of repeated units shown in the formula I in the specification. The mass spectrum ionization element is uniform in coating, high in selectivity on macrolide enriched antibiotics in a complex matrix and high in enrichment capacity, an eluent of the mass spectrum ionization element can be used for detection based on a liquid chromatography method and can also serve as a mass spectrum ion source solid substrate, mass spectrum detection is conducted through electrospray ionization, the detection steps are simple, and the mass spectrum ionization element is suitable for mass spectrum detection. And the detected background noise is low.

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 provides a synergistic treatment method for intensifying aerobic compost humification and preventing and controlling pollution based on a molecular sieve 13X, and relates to the field of solid waste treatment. The method comprises the following steps: mixing livestock and poultry manure with composting auxiliary materials, adjusting the water content and the carbon nitrogen ratio, adding a molecular sieve 13X, and then carrying out conventional aerobic composting so as to strengthen humification, gas emission reduction and resistance gene removal in the composting process; the humic acid HA in the obtained compost rotten product is increased by 18.1% compared with that in a control group, and the humate-rich ratio is increased by 59.6%; the cumulative emissions of CO2, CH4, N2O, NH3, H2S, MeSH and Me2S are respectively reduced by 13.1%, 14.8%, 25.7%, 20.4%, 33.6%, 21.9% and 20.7% compared with the control group; the relative abundance of tetracycline resistance genes, aminoglycoside resistance genes, macrolide resistance genes and clindamycin resistance genes in a compost product is reduced by 72.7%, 92.6%, 87.1% and 86.2% respectively compared with a control group, and the relative abundance of a movable genetic element MGEs is reduced by 94.1% compared with the control group; according to the method, efficient recycling and harmlessness of the organic solid waste can be synchronously achieved, and gas emission in the composting process is reduced.

The present invention provides a method for enhancing the removal of resistance genes and promoting humification in aerobic composting. The method comprises the following steps: mixing livestock and poultry manure with a composting auxiliary material, adjusting the moisture content to 55%-65%, and adding a MnFe2O4 additive to obtain a composting raw material; aerobically composting the material, turning the compost every 2-3 days during a temperature rise period and a high temperature period, and every 7 days during a temperature fall period and a mature period, with the aerobic composting time being 20-30 days. Compared with a conventional composting method, the relative abundances of sulfonamide, tetracycline, macrolide, and aminoglycoside resistance genes in the mature compost obtained by the method are reduced by 60%-73%, 50%-57%, 20%-80%, and 45%-66%, respectively, and the humic acid (HA) content is increased by about 15%. Meanwhile, the method achieves efficient harmlessness and resource utilization of organic solid waste, and has the potential for large-scale production.

A method for enhancing resistance gene removal and promoting humification in an aerobic compost, which method comprises mixing livestock and poultry manure with compost auxiliary materials, adjusting the water content, adding an MnFe2O4 additive, and then performing aerobic composting for 20-30 days. Compared with conventional composting methods, the mature compost product obtained by means of the method exhibits a 60%-73% reduction in the relative abundance of sulfonamide resistance genes, a 50%-57% reduction in tetracycline resistance genes, a 20%-80% reduction in macrolide resistance genes, and a 45%-66% reduction in aminoglycoside resistance genes, and shows approximately a 15% increase in humic acid HA. This method achieves both efficient harmless treatment and resource utilization of organic solid waste.

The present invention is directed to a stable, efficacious and palatable chewable veterinary composition comprising as active ingredient an isoxazoline compound of Formula (I),a stabilized macrocyclic lactone, pyrantel and excipients.

The invention provides a compound as shown in a formula (I), and a stereoisomer, a tautomer, an isotope label, nitrogen oxide, a solvate, a polymorphic substance, a metabolite, ester, pharmaceutically acceptable salt or prodrug thereof, or a pharmaceutical composition thereof, which have better antibacterial and anti-inflammatory effects, can be used as an antibiotic, and can be used for preparing a pharmaceutical preparation for preventing and treating diseases. The compound can treat infection caused by pathogenic microorganisms resistant to erythromycin and telithromycin, and simultaneously acts on double targets of ribosome and topoisomerase.

The invention belongs to the technical field of microbial pharmacy, and discloses a polyketone macrolide compound generated by genetically engineered streptomyces as well as a preparation method and application thereof. The polyketone macrolide compound disclosed by the invention is a cinnamyl streptomycin derivative, has cell proliferation inhibition activity better than that of a natural product Cinnamomycin A-D, can exert anti-tumor activity by inhibiting activity of human exonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) and activating an inherent immune pathway, can be prepared into a medicine or a medicinal composition, and can be used for preparing medicines or medicinal compositions. The compound is used for treating tumors and related diseases.

The present application relates to the field of polymer chemistry and biomedical technology, and particularly relates to a macrocyclic lactone polymer shown in formula (I) which is used for preventing or treating hyperproliferative diseases, including liver cancer, leukemia, breast cancer, colon adenocarcinoma, gastric cancer, lung cancer, Barrett's esophageal cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymphoma, kidney cancer, brain cancer, nerve cancer, nasopharyngeal cancer, oral cancer, bladder cancer, colorectal cancer and melanoma, and has the potential to be developed into a new type of antitumor drug.

The invention describes an extended-release composition comprising PLGA or PLA polymeric microspheres comprising an isoxazoline, preferably sarolaner, and a macrocyclic lactone, preferably moxidectin, and wherein the composition further comprises at least one pharmaceutically acceptable excipient; and uses thereof.

The present invention relates to a pyrazine macrolide compound and the use thereof. Specifically disclosed is a compound as represented by formula I or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits activity against bacteria, mycoplasmas, or chlamydias, and is useful for preventing and / or treating diseases caused by bacteria, mycoplasmas, or chlamydias. Further, the compound of the present application can achieve an antibacterial activity comparable to or better than that of azithromycin or solithromycin at a lower dosage. Furthermore, the compound of the present application achieves a superior antibacterial effect on Gram-positive bacteria. Still furthermore, the compound of the present application exhibits a better inhibitory activity against mycoplasmas and a lower hepatotoxicity.

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 ester derivatives of brefeldin A represented by Formula (I) in the inhibition of tumor proliferation. The compounds are prominent in the prevention or treatment of hyperproliferative diseases, including liver cancer, leukemia, breast cancer, colon adenocarcinoma, gastric cancer, lung cancer, Bart's esophageal cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymphoma, kidney cancer, brain cancer, nerve cancer, nasopharyngeal cancer, oral cancer and colorectal cancer, and have the potential to be developed as antitumor agents.

The invention belongs to the field of medicines, and relates to a macrolide derivative as well as a preparation method and application thereof. The macrolide derivative is a compound as shown in a structural general formula (I), a salt thereof or an optical isomer thereof: (I), wherein R1 is selected from NR8R9, a C3-C8 nitrogen-containing aliphatic ring and a substituted C3-C8 nitrogen-containing aliphatic ring. The macrolide derivative disclosed by the invention has better chemical stability than 17-glucoside spinosad, and has a better tumor inhibition effect in a human body environment, so that the macrolide derivative is expected to be used as an anti-tumor potential drug.

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.

Disclosed are a method for producing pladienolide D that includes a step that reacts a compound represented by formula (A1) with a compound represented by formula (B1) in the presence of a metal catalyst to obtain a compound represented by formula (C1) (in the formulas, X means hydrogen, optionally substituted boryl, optionally substituted stannyl, or optionally substituted silyl, R4 is hydrogen, etc., R5 is optionally substituted benzoyl, etc., and R1 and R2 each independently are hydrogen, etc.) and crystals of a solvate of pladienolide D.

The present invention provides an anti-parasitic composition for use in the treatment or prevention of a parasitic infection in a mammal, the anti-parasitic composition comprising a macrolide, in particular a combination of ivermectin, abamectin and doramectin. The invention also provides a method of treating a parasitic infection in a mammal by administering to the mammal an effective amount of an anti-parasitic composition comprising ivermectin, abamectin, and doramectin, and a method of preparing the anti-parasitic composition.

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.

Provided herein are pharmaceutically acceptable compositions containing macrolide antibiotics, in particular azithromycin. In particular, compositions containing azithromycin with low toxicity, especially for administration to felines, are provided herein.

The present invention relates to the field of pharmaceutical technology, and specifically to the application of a macrolide derivative in the preparation of a drug for treating heart failure. The present invention provides a new use of a macrolide derivative. Experimental results show that this macrolide derivative significantly improves the cardiac function of heart failure mice, increases the ejection fraction (EF%), fractional shortening (FS%), and cardiac output per minute (CO), without changing the heart rate (HR), is equivalent to the positive drug digoxin, and is superior to enalapril; at the same time, it has the effects of reducing the heart weight ratio, improving myocardial hypertrophy and fibrosis, and has good clinical prospects and social benefits.

Disclosed herein are macrolide compounds having senescent cell elimination activity. These compounds selectively target senescent cells and can be used to reduce or eradicate senescent cells in a subject's body and / or delay the onset of aging. These compounds also inhibit the proliferation of cancer stem cells and can be used to treat cancer, particularly to inhibit the proliferation of cancer stem cells that cause metastasis and tumor recurrence.

The application provides a macrolide derivative and a preparation method and application thereof, relates to the technical field of medicinal chemistry, and the macrolide derivative is a compound with a general structure shown in the following formula I: in the formula, A is selected from any one of alkynyl, alkenyl or piperazine; R is selected from any one of H or F; X is selected from any one of CH or N, Y is selected from any one of methyl, ethyl or cyclopropyl, and n is an integer in the range of 2-6. The macrolide derivative is connected by different lengths of ether hydrocarbons at the 3-position, thereby avoiding the problem that the instability of a synthesized compound is caused by using an ester group as a side chain to connect a quinolone group. The application successfully prepares a macrolide derivative with double targets, and the antibacterial activity of the macrolide derivative is obviously better than the antibacterial activity of erythromycin, telithromycin, clarithromycin and ciprofloxacin which only have single targets.

Provided are 13-membered macrolides for the treatment of infectious diseases. The 13-membered macrolides described herein are azaketolides. Also provided are methods for preparing the 13-membered macrolides, pharmaceutical compositions comprising the 13-membered macrolides, and methods of treating infectious diseases, and in particular, disease resulting from Gram negative bacteria using the disclosed macrolides. Formula (I)

The present invention provides a composition with a solubilizing effect, a preparation method thereof, and an application thereof. The composition comprises a solubilizing agent, a glidant, and an inclusion compound, wherein the mass ratios of the components are as follows: the mass ratio of the solubilizing agent to the inclusion compound is 1:1-1:20, and the mass ratio of the glidant to the inclusion compound is 1:100-3:20. The composition of the present invention can effectively improve the solubility of macrolides, tetracyclines, and penicillins, and the composition of the present invention does not react with the active ingredients of the drugs, ensuring that after the drugs are mixed therewith, the active ingredients of the drugs are stable, and the mixture of the drugs and the composition does not agglomerate or discolor.

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 solid phase extraction-ultra-high performance liquid chromatography-tandem mass spectrometry rapid determination method for antibiotics in aquaculture fresh water, which comprises the following steps: (1) adding an internal standard solution into aquaculture fresh water to be determined, uniformly mixing, filtering the obtained water sample, and adjusting the pH value; (2) activating a small solid-phase extraction column, enriching the water sample obtained in the step (1) through the small solid-phase extraction column, then leaching and eluting, collecting an eluent, blowing the eluent until the eluent is nearly dry, and fixing the volume by using methanol and water; and (3) feeding the solution obtained after volume metering in the step (2) into ultra-high performance liquid chromatography-tandem mass spectrometry for detection. The invention establishes a method for simultaneously detecting 37 antibiotic residues in aquaculture fresh water by solid phase extraction-ultra-high performance liquid chromatography-tandem mass spectrometry, the method comprises six common antibiotics such as tetracyclines, macrolides, fluoroquinolones, phenols, sulfonamides and cephalospores, the detection is convenient and fast, and the accuracy is high.

The present invention relates to a compound drug for preventing and treating porcine reproductive and respiratory syndrome (PRRS), belonging to the field of veterinary drugs. The present invention makes an oral pharmaceutical preparation by mixing an animal-specific macrolide drug, sodium houttuyfonate, mannan oligosaccharide peptide and pharmaceutical excipients in a certain proportion. The drug of the present invention can effectively treat acute-phase PRRS, rapidly relieve the clinical symptoms of diseased pigs and improve the survival rate.