201 results about "Betalactam antibiotics" patented technology

Substituted bicyclic beta-lactams of Formula I: (I), are β-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds can be employed with a β-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.

A method for enhancing the oral bioavailability of a prodrug ester by formulating the ester as a non-emulsified formulation with lecithin; as well as a pharmaceutical composition of at least one antibiotic and lecithin in a non-emulsified formulation; a method of treating infections with the non-emulsified formulation, and a method for preparing tablets by direct compression of blends of drugs with lecithin are disclosed. Non-emulsified formulations include solids, tablets, capsules, lozenges, suspensions, elixirs and solutions, and exclude emulsions, liposomes, lipid matrix systems and micro-emulsions. A suitable prodrug ester is a cephalosporin β-lactam antibiotic such as cefditoren pivoxil, and a suitable non-emulsified formulation is a solid formulation.

The present invention relates to carbocephem antibiotics and pharmaceutically acceptable salts thereof useful for the treatment of bacterial infections, in particular infections caused by methicillin-resistant Staphylococcus spp. bacteria.

Stabilized preparations which contain a beta-lactam antibiotic having an esterified carboxyl group attached directly to the mother nucleus, an oil and a phosphate.

The invention discloses an antibiotic compound, which comprises the following parts: at least one beta-lactam antibiotics and at least one ion chelant to inhibit the generation of particle or at least one buffer component or at least one ion chelant and at least one buffer component. The compound can build with at least one aminoglycoside antibiotics in the same container as the drug to control microbe infection.

The present invention relates to eukaryotic cells which have the ability to convert L-arabinose into D-xylulose 5-phosphate. The cells have acquired this ability by transformation with nucleotide sequences coding for an arabinose isomerase, a ribulokinase, and a ribulose-5-P-4-epimerase from a bacterium that belongs to a Clavibacter, Arthrobacter or Gramella genus. The cell preferably is a yeast or a filamentous fungus, more preferably a yeast is capable of anaerobic alcoholic fermentation. The may further comprise one or more genetic modifications that increase the flux of the pentose phosphate pathway, reduce unspecific aldose reductase activity, confer to the cell the ability to directly isomerise xylose into xylulose, increase the specific xylulose kinase activity, increase transport of at least one of xylose and arabinose into the host cell, decrease sensitivity to catabolite repression, increase tolerance to ethanol, osmolarity or organic acids; and / or reduce production of by-products. The cell preferably is a cell that has the ability to produce a fermentation product such as ethanol, lactic acid, 3-hydroxy-propionic acid, acrylic acid, acetic acid, succinic acid, citric acid, amino acids, 1,3-propane-diol, ethylene, glycerol, -lactam antibiotics and cephalosporins. The invention further relates to processes for producing these fermentation products wherein a cell of the invention is used to ferment arabinose into the fermentation products.

The invention discloses a method, a special kit and test paper strips for detecting beta-lactam antibiotics based on penicillin-binding protein. The receptor kit used for detecting beta-lactam antibiotics comprises: protein represented by SEQ ID NO: 1, enzyme labeled ampicillin and a standard substance solution, wherein the standard substance is penicillin G. The kit and colloidal gold test paper strips provided by the invention have advantages of high sensitivity, high accuracy, high precision, low cost, simple operation, short detection period, simple storage, and long shelf-life. The kit and colloidal gold test paper strips are suitable for various work units. With the kit and colloidal gold test paper strips, simultaneous and rapid detections of large batches of samples can be realized, and on-site high flux rapid detections can be realized. Therefore, the kit, the colloidal gold test paper strips and the method provided by the invention play an important role in the detections of beta-lactam antibiotics.

The invention provides a preparation method and application of a product obtained by coupling penicillin with carrier protein, as well as a beta-lactam type penicillin antibody. Animals are immunized with penicillin artificial antigen coupled in the invention so as to prepare the antibody which can be used for detecting beta-lactam type penicillin in foods. The preparation method comprises the following steps: immune BALB / C mouse spleen cells and SP2 / 0 mouse myeloma cells are fused; beta-lactam type antibiotics coupled with the carrier protein are used as coating antigen to screen positive hybridoma; hybridoma capable of stably transferring culture and secreting anti-beta-lactam type antibiotic antibodies through cell clones is obtained; and an ascites monoclonal antibody is prepared. The prepared monoclonal antibody is utilized to establish a direct competitive ELISA method having high specificity, sensitivity and accuracy to the beta-lactam type antibiotics, as well as an immune colloidal gold test strip. The preparation method for the product obtained by coupling penicillin with carrier protein, as well as the beta-lactam type antibiotic antibodies can serve the rapid detection of beta-lactam type antibiotic residue in foods.

The invention discloses a kit test method of beta-lactam antibiotics residue in milk, comprising the following steps: performing once activation to bacillus stearothermophilus, then culturing the activated bacillus stearothermophilus in a production culture medium at 50-65 DEG C for 24-36h while stirring in a rotation speed of 100-150rpm, centrifugalizing to collect bacteria mire, adding agarose bromcresol purple solution, mixing evenly to ensure the number of spore in each kit reach 1.00*10<7>-2.50*10<8>cfu, subpackaging the spore in porous reaction vessels at 60-70 DEG C, covering aluminum-plastic film, placing upside down, sealing, placing the vessels in aluminum-plastic packages and storing in dark place while keeping from wet. The kit has the advantage of easy operation, high sensibility, good repeatability, low cost and high throughput, can be stored at 4-8 DEG C for 12-18 months and can be used to test beta-lactam antibiotics residue in milk.

The invention relates to bacillus stearothermophilus and a method for carrying out antibiotic residue detection by utilizing the same. The preservation number of the screened strain is CGMCC NO.3287; and the antibiotic residue detection method which is established by taking the strain as indicator bacteria comprises the following steps of: rejuvenating and activating the strain; preparing spore suspending liquid in enrichment; preparing a purple culture solution; embedding bacillus; detecting a sample, and the like. The strain CGMCC NO.3287 is stable, easy to store and prepare, highly sensitive to B-lactam antibiotic, good in homogeneity and dispersibility in a culture medium, grows fast at 65 DEG C and has fast metabolism and acid production. Compared with a TIC method and a fermentation test method, the method has convenient operation, high sensitivity, 2-3h time-consumption which is shorter than 4h of national similar methods and is easy to judge the result; compared with a commercial kit, the bacillus stearothermophilus has low cost which is equal to 1 / 7 of the kit in price; and the method is simple and practicable and can be operated in a common laboratory.

The invention provides feruloyl esterase and a preparing method and application thereof. A feruloyl esterase gene coming from a soil macro gene library have the nucleotide sequence and amino acid sequence shown in SEQ ID NO.1 and SEQ ID NO.2. The gene contains a tetrapeptide SXXK sequence motif which is rarely seen, and after the esterase gene is inserted into plasmid pET28a(+), the gene is transformed into escherichia coli BL21(DE3) to achieve heterogeneous expression. The molecular weight of purified recombinase (DLFae4) is 38.3 kDa. Besides, it is put forward for the first time that novel feruloyl esterase can hydrolyze penbritin, penicillin, cefazolin and other lactam antibiotics. As is shown by site-directed mutagenesis experiments, a catalysis triplet of DLFae4 is composed of serine(S11), histidine (H74) and aspartic acid (D302), and the mutation of any of serine (S11), histidine (H74) and aspartic acid (D302) can cause loss of the catalysis capability of DLFae4. DLFae4 has a high hydrolytic activity on methyl ferulate and has good heat stability. In the presence of cellulase, DLFae4 can obviously increase the amount of ferulic acid released from destarched wheat bran. Due to peculiar activities and enzymatic characteristics of novel feruloyl esterase, novel feruloyl esterase can be applied to feed, paper making, food, pharmacy and other fields.

The invention provides novel non-β-lactam inhibitors of β-lactamases. In particular, the invention provides boronic acid-based compounds set forth in the specification. These compounds may be used with β-lactam antibiotics to bacterial infection, particularly, β-lactam-antibiotic-resistant bacterial infections. These compounds are also antibacterial agents by themselves. The invention further provides methods of using such compounds. Finally, the invention provides a pharmaceutical composition comprising these compounds.

This invention provides beta-lactam antibiotic-containing tablets capable of being orally taken either as such owing to their being small-sized, hence still easily swallowable, or, in the case of administration to the aged encountering some difficulty in swallowing, in the form of dispersions resulting from easy self-disintegration upon being dropped into water in a glass as well as a method of producing the same. The tablets of this invention comprise, on the per-tablet basis, 60-85% by weight of a beta-lactam antibiotic, 1-10% by weight of low-substituted hydroxypropylcellulose and / or crosslinked polyvinylpyrrolidone as a disintegrator, and 0.5-2% by weight of a binder. Granules to be compressed for tableting are prepared using water or an aqueous solution of ethanol or the like.

The invention aims to provide a method for preparing a rapid detection kit based on penicillin-binding protein PBP6 beta-lactam antibiotic receptor assay as well as a used detection method, aiming at solving the problem of sieve leakage in the process of detecting beta-lactam medicines in a traditional ELISA method. The invention discloses a method for preparing a detection kit based on penicillin-binding protein PBP6 beta-lactam antibiotic receptor assay as well as an indirect competitive receptor assay method for detecting the content of beta-lactam drugs in milk by adopting the detection kit based on penicillin-binding protein PBP6 beta-lactam antibiotic receptor assay. The methods have the beneficial effects that by utilizing the characteristic that the penicillin-binding protein 6 can be specifically bound to the beta-lactam drugs, the drugs can be specifically identified in a buffer liquid system or a sample matrix extracting solution and are not influenced by other antibiotics such as macrolides, quinolones and tetracyclines.

The invention relates to a method of rapidly degrading a beta-lactam antibiotic in water. The method concretely comprises the following steps: adding a certain quantity of peroxymonosulfate (PMS) as an oxidant in waste water which contains a beta-lactam antibiotic (such as cephalexin, i.e. CFX) at normal temperature and normal pressure, uniformly stirring, carrying out reaction for a period of time under a neutral condition while keeping a pH value of a system, and removing a pollutant with oxidative degradation. According to the method provided by the invention, the peroxymonosulfate as the oxidant has very high selectivity to the beta-lactam antibiotic, directly oxidizes and removes the pollutant without an additional persulfate activation step, is rapid in degradation with very little influence caused by other organic matters in a water body, and is more beneficial to removing the beta-lactam antibiotic in a polluted water body.

The invention relates to antisense oligonucleotides aiming to methicillin-resistant Staphylococcus aureus (MRSA) resistance gene mecR1 / mecA and blaR1 / blaZ and a preparation of the drugs with the antisense oligonucleotides and the application thereof. The antisense oligonucleotides comprise antisense phosphorothiate oligodeoxynucleotide (PS-ODNs) and thiodeoxyribozyme (PS-DRz). The invention is characterized in that the combination of the specificity and the various areas of MRSA resistance gene mecR1 / mecA and blaR1 / blaZ blocks the expression of the resistance gene, the base sequence of the antisense nucleic acid is PS-ODNs01-40, the antisense nucleic acid can combine with the specific site of the target gene, thereby inhibiting the expression of the resistance gene, causing MRSA to restore the sensitivity of the lactam antibiotics and achieving the purpose of effective fighting with the drug resistance of MRSA.

The invention discloses a PBP-1A affinity beta-lactam antibiotic electrochemical biological sensor, and a making method and an application thereof. The electrochemical biological sensor is characterized in that the surface of a glassy carbon electrode is commonly modified by graphene, penicillin G and nafion. The making method comprises the steps of bare electrode polishing, cleaning and activating, and concretely comprises: sequentially adding graphene and penicillin G to the surface of the glassy carbon electrode in a dropwise manner, well mixing, carrying out blow drying at 37DEG C, adding nafion in a dropwise manner, naturally air-drying the surface, immersing the electrode in 5wt% bovine serum albumin, placing the immersed electrode in an oven, drying at 37DEG C for 30min, taking out the electrode, washing the electrode with a PBS solution to obtain a glassy carbon electrode with the surface modified by graphene-penicillin G-nafion as a work electrode, placing the work electrode in a system solution, carrying out DPV detection, and determining the concentration of beta-lactam antibiotics in a sample to be detected according to a standard curve. The electrochemical biological sensor has the advantages of high sensitivity, fast detection speed, low detection limit, high efficiency and cheapness.

A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.

The invention discloses an animal bifidobacterium and a composition thereof, and belongs to the technical field of microbe application. The preservation number of the animal bifidobacterium provided by the invention is CGMCC No.4521 and is preserved in General Microbiology Center of Chinese Culture Collection Committee in Beijing on December 29, 2010. The animal bifidobacterium provided by the invention has a symplastic growth effect on lactobacillus casei, streptococcus faecium and bacillus cereus and has tolerance on carbostyril, aminoglycoside and monocyclic beta-lactam antibiotics, and the animal bifidobacterium is suitable for use in food, drugs and / or health care products.

The invention relates to a therapy of an infection with a drug resistant bacterium wherein a characteristic of multivalent phenol derivatives and / or extracts from “Tara” which enhance the activity of β-lactam antibiotics on the drug resistant bacteria is utilized. Specifically, the invention relates to an enhancer of β-lactam antibiotics comprising a multivalent phenol derivative or its pharmaceutically acceptable salt, a pharmaceutical composition comprising a β-lactam antibiotic and a multivalent phenol derivative and / or extract from “Tara” for the therapy of an infection with a drug resistant bacterium, a disinfectant for the same, and a functional food comprising a multivalent phenol derivative and / or extract from “Tara”.

The invention discloses macrolactone compounds or salts of the macrolactone compounds, as well as a synthesis method, a pharmaceutical composition and application of the macrolactone compounds or salts. The invention provides a macrolactone compound 1, a macrolactone compound 1' or salts of the macrolactone compound 1 and the macrolactone compound 1', a pharmaceutical composition containing the macrolactone compound 1, the macrolactone compound 1' or the salts of the macrolactone compound 1 and the macrolactone compound 1' and application of the pharmaceutical composition in preparing a drug for inhibiting methicillin-resistant staphylococcus aureus. When one or more of the macrolactone compound 1, the macrolactone compound 1', the salt of the macrolactone compound 1 and the salt of the macrolactone compound 1' are jointly used in combination with beta-lactam antibiotics, the inhibiting effect of the beta-lactam antibiotics on the methicillin-resistant staphylococcus aureus can be obviously increased. The macrolactone compounds and the salts thereof are novel synergists having good in-vitro synergistic effect, can alleviate the drug resistance of the methicillin-resistant staphylococcus aureus to the beta-lactam antibiotic and are drug having good market development prospects.

The invention relates to a penicillin G acylase mutant constructed by genetic engineering. In comparison with wild type penicillin G acylase from achromobacter (Achromobacter sp.CCM 4824), the synthesis performance of the penicillin G acylase mutant is improved substantially, the maximum synthetic product / hydrolysate value S / H reaches 22.3 and is 3.9 times that of wild type enzyme, and various beta-lactam antibiotics can be efficiently synthesized catalytically. When the ratio of side chains to mother nucleus is 1.05:1, the conversion rate of the mother nucleus 6-APA, 7-ADCA, 7-ACCA and 7-APRA reaches 99.0% or above, and the penicillin G acylase mutant has wide industrial application prospects.

The invention discloses a method for preparing a penicillin binding protein combined with beta-lactam antibiotic and a special recombinant bacterium. The recombinant bacterium is prepared by the following steps of: importing the coding gene of the penicillin binding protein into initial escherichia coli to obtain recombinant escherichia coli. Experiments prove that the method for preparing the penicillin binding protein has high yield, and the problems of low yield and difficulty in preparation in the prior art are solved. Therefore, the method has significance.

The invention provides a beta-lactam antibiotic detection card which comprises a sample pad, a golden label pad containing beta-lactam antibiotic captured monoclonal antibody, a nitrocellulose membrane which sequentially comprises a detection line beta-lactam antibiotic coated polyclonal antibody and a quality control line rabbit antimouse IgG, an absorption pad and a lining plate. The invention also provides a performance detection and quality control method for the beta-lactam antibiotic detection card. The beta-lactam antibiotics can be accurately, simply and rapidly detected on the site, and the detection result consistency of the detection card is guaranteed.

The invention belongs to the field of food detection and in particular relates to a kit for quantitatively detecting beta-lactamase residue in milk. The kit for quantitatively detecting beta-lactamase residue in milk is characterized in that the kit comprises an elisa plate enveloped with penicillin-binding proteins, marker coupled beta-lactam antibiotics, a skim milk powder freeze dried product of which the substrate reference 1 is beta-lactam antibiotics and which has the concentration of 0ppb, a skim milk powder freeze dried product of which the substrate reference 2 is beta-lactam antibiotics containing calibration concentration, and a beta-lactam antibiotic standard substance. The kit has high specificity and sensitivity, beta-lactam with the concentration of about 0.5U / ml can be detected, and the linear detection range is 1-16 U / ml; intra-batch CV percent of the kit is less than 10 percent, the inter-batch CV percent is less than 20 percent, and high precision is reflected; the detection steps are simple, the time consumption is low, and the cost is low; according to the kit, the beta-lactamase residue can be accurately, quantitatively and rapidly detected at high throughput, and the requirements of enterprises and detection mechanisms are met.

The invention relates to a selenium nano composite material capable of overcoming multi-drug-resistant bacterial infection. The selenium nano composite material comprises nano-selenium composite particles, which are obtained by coating mannose modified chitosan on the outer surface of a complex of selenium nano particles and beta-lactam antibiotics, and are of a spherical structure, wherein selenium nanoparticles and beta-lactam antibiotics are arranged in the nano-selenium composite particles, mannose-modified chitosan is arranged on the outer surface of the nano-selenium composite particles,the average particle size of the nano-selenium composite particles is 40-80 nm, and the thickness of shells of the mannose-modified chitosan on the surface is smaller than or equal to 5 nm. The invention also provides a selenium nano composite material capable of overcoming multi-drug-resistant bacterial infection, and application of the selenium nano composite material in a nano antibacterial material. The nano antibacterial material prepared by the invention inhibits the expression of a drug efflux pump of multi-drug-resistant bacteria and the activity of beta-lactamase, and chitosan is used for embedding selenium nanoparticles and antibiotics, so that the dispersity and stability of the nano material are favorably improved.