160 results about "Inosamycins" patented technology

There is disclosed herein a composition for treating gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhea, chronic idiopathic nausea, IBD-associated constipation and diarrhea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinsons disease, MS, Alzheimers Disease, Motor Neurone Disease or autism, the composition comprising: (i) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (ii) at least one anti-clostridial agent selected from the above combined with an opioid blocking agent. There is also disclosed herein a method of treating various gastrointestinal or neurological disorders, constipation, functional constipation, irritable bowel syndrome, diverticulitis, travelers diarrhea, chronic idiopathic nausea, IBD-associated constipation and diarrhea, pseudo-obstruction, diabetic gastroparesis, cyclic vomiting, reflux oesophagitis, autism enteropathy, flatulence, halitosis, chronic fatigue, bloating, proctalgia fugax, Parkinsons disease, MS, Alzheimers Disease, Motor Neurone Disease or autism, the method comprising administering orally, via enema or by suppository: (i) a composition of the invention; (ii) at least two anti-clostridial agents selected from the group consisting of: vancomycin, vancomycin derivatives, a multi-valent polymer of vancomycin, aminoglycosides, nitroimidazoles, ansamysins, nifuroxazide, colchicine, prucalopride, prokinetic agent and 5-aminosalicylic acid; or (iii) at least one anti-clostridial agent selected from the above and an opioid blocking agent to a patient in need of such treatment.

The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

A novel group of aminoglycosides which share some structural features of currently available aminoglycosides with regard to the backbone, while also having significant structural differences. The similarity enables these aminoglycosides to be highly potent and effective antibiotics, while the significant differences enable these aminoglycosides to reduce or even block antibiotic resistance.

The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

Colloidal compositions, loaded with non-covalently bonded antibiotics, can be efficiently used for the treatment of severe bacterial pneumonia and other serious lung infections such as tuberculosis. Such formulations, comprised of biodegradable nanoparticles or nanocapsules with incorporated antibiotics, show a significant increase in antibacterial activity, extended and sustained drug release and a decrease in frequency of the drug administration. Antibiotics of various types, such as aminoglycosides, glycopeptides and others can be successfully incorporated into a nanoparticulate colloidal delivery system.

The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5″ position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides can be represented by the general formula I:or a pharmaceutically acceptable salt thereof, wherein R1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.

The present invention provides methods for identifying target genes whose partial or complete functional inactivation potentiates the activity of an antibiotic agent, e.g., a quinolone antibiotic. The invention further provides methods for identifying agents that modulate expression of target genes or that modulate activity of expression products of target genes. Agents identified according to various methods of the invention potentiate the activity of antibiotics such as quinolones, aminoglycosides, peptide antibiotics and β-lactams. Also provided are agents that suppress and / or retard resistance to antibiotics. The inventive methods provide potentiating agents and compositions comprising potentiating agents and antibiotics. Such agents and compositions can be used for inhibiting growth or survival of a microbial cell or of treating a subject suffering from or susceptible to a microbial infection.

The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

The present invention provides a bone marrow stem cell protection solution, which is mainly prepared by dissolving a hypoxic protection agent, heparin sodium and an aminoglycoside antibiotic in a DMEM / F12 culture medium aqueous solution, wherein per mL of the DMEM / F12 culture medium aqueous solution can respectively dissolve 5-10 mg of the hypoxic protection agent, 0.01-0.05 U of the heparin sodium and 50-200 U of the aminoglycoside antibiotic, and the concentration of the DMEM / F12 culture medium aqueous solution is 30-40 mg / ml. According to the present invention, the bone marrow stem cell protection solution has advantages of stable performance, safety and no toxicity, can effectively protect bone marrow stem cells, can make bone marrow stem cells be preserved for a long time and can maintain the cell activity in vitro, can maintain the original multidirectional differentiation ability, and can expand the clinical application of bone marrow stem cells, wherein the bone marrow stem cells can be transported to most domestic cities and neighboring countries by using the existing transportation tools.

The invention discloses a preparation method and an application of a sensor for simultaneously detecting four aminoglycoside antibiotics and belongs to the technical field of novel function materials and biosensor analysis. According to the invention, a reference electrode is printed by the use of a silver paste and four working electrodes and a counter electrode are printed by the use of a conductive carbon paste on a rectangular substrate surface coated with a layer of a polyester film. Thus, a four-channel screen-printed electrode is prepared. The preparation method is characterized in that antibodies of four aminoglycoside antibiotics including streptomycin, gentamycin, kanamycins and spectinomycin are respectively fixed on surfaces of the four working electrodes by the use of a Pt nanoparticle-sulfated graphene-carboxymethyl chitosan conductive composite nano-material; and after the detection liquids are dripped, the four working electrodes are connected with a multichannel electrochemical workstation detection circuit so as to realize simultaneous detection of the four aminoglycoside antibiotics. The sensor provided by the invention is simple to prepare and convenient to process, requires low cost, and is convenient to carry. The detection method is simple and rapid and has high sensitivity and good specificity.

A new class of paromomycin-derived aminoglycosides, which exhibit efficient stop-codon mutation suppression activity, low toxicity and high selectivity towards eukaryotic cells are provided. Also provided are chemical and chemo-enzymatic processes of preparing these paromomycin-derived aminoglycosides and intermediates thereof, as well as pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders.

The present invention provides a pharmaceutical composition that includes: (a) at least one of a non-aminoglycoside antibiotic and an anti-inflammatory agent; and (b) a biofilm-dissolving agent. The present invention also provides for methods of killing or inhibiting the growth of a fungus by contacting the fungus with a composition of the present invention, methods of killing or inhibiting the growth of a virus by contacting the virus with a composition of the present invention, methods of killing or inhibiting the growth of a bacteria by contacting the bacteria with a composition of the present invention, methods of treating a disorder in a mammal by administering the composition of the present invention to the mammal, methods for preserving contact lens by contacting the contact lens with a composition of the present invention, methods for cleansing surgical or dental instrument by contacting the fungus with a composition of the present invention, and kits that include (a) a container that includes the pharmaceutical composition of the present invention, and (b) a drug delivery device.

The present invention provides aminoglycosides and pharmaceutical compositions that include the aminoglycosides. The aminogylcosides are useful to treat or prevent infectious diseases (e.g., bacterial infections) in a mammal (e.g., human).

The invention discloses a method for simultaneously analyzing various aminoglycoside compound residues in agricultural and animal products. The method comprises the following steps: weighing a sample;adding an ammonium acetate buffering solution; after carrying out oscillation and extraction, carrying out centrifuging; separating an extracting solution obtained by centrifuging and regulating to asuitable range by utilizing a PH (Potential of Hydrogen) meter; purifying by adopting dispersed solid-phase extraction and a solid-phase extraction small column. Ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS / MS), electrospray ionization (ESI) and multi-reaction monitoring (MRM) scanning modes are adopted. Compared with other similar methods, the method disclosed by the invention has the advantages of simplicity in operation and high sample flux; eight types of aminoglycoside compounds including streptomycin, dihydrostreptomycin, spectinomycin, gentamicin, apramycin, kanamycin, amikacin and neomycin are detected at the same time; the detection efficiency is greatly improved, and rapid qualitative and quantitative detection can be rapidly carried out; the detection limit can completely meet domestic and overseas laws and regulations and limitation requirements, and powerful support is provided for food safety guarantees and import and export of the agricultural and animal products of China.

This invention is for an improved process to co-encapsulate hydrophobic drugs and hydrophilic drugs in phospholipid liposomes. Non-toxic supercritical or near-critical fluids with / without polar cosolvents are utilized to solubilize phospholipid materials and hydrophobic drugs, and form uniform liposomes to encapsulate hydrophobic drugs and hydrophilic drugs.DNA topoisomerase I (Top1) is the target of camptothecin, and novel Top1 inhibitors are in development as anticancer agents. Top1 inhibitors damage DNA by trapping covalent complexes between the Top1 catalytic tyrosine and the 3′-end of the broken DNA. Tyrosyl-DNA phosphodiesterase (Tdp1) can repair Top1-DNA covalent complexes by hydrolyzing the tyrosyl-DNA bond. Inhibiting Tdp1 has the potential to enhance the anticancer activity of Top1 inhibitors and to act as antiproliferative agents. It has been recently reported that neomycin inhibits Tdp1 more effectively than the related aminoglycosides paromomycin and lividomycin A. Inhibition of Tdp1 by neomycin is observed both with single- and double-stranded substrates but is slightly stronger with duplex DNA, which is different from aclarubicin, which only inhibits Tdp1 with the double-stranded substrate. Inhibition by neomycin can be overcome with excess Tdp1 and is greatest at low pH. Aminoglycoside antibiotics and the ribosome inhibitors thiostrepton, clindamycin-2-phosphate, and puromycin are the first reported pharmacological Tdp1 inhibitors. The development of Tdp1 inhibitors as anticancer agents can be envisioned as combinations of Tdp1 and Top1 inhibitors. Moreover, Tdp1 inhibitors might also be effective by themselves as anticancer agents. In addition, Tdp1 inhibitors might be valuable as anti-infectious agents.This invention can produce a co-encapsulated combination drug product consisting of a topoisomerase 1 inhibitor such as camptothecins including neat camptothecin and its derivatives irinotecan, topotecan and other derivatives, and a tyrosyl-DNA phosphodiesterase (Tdp1) such as aminoglycoside antibiotics including neomycin and tetracycline, and the ribosome inhibitors thiostrepton, clindamycin-2-phosphate, and puromycin.

The invention relates to a kit for quickly detecting a drug resistance gene of pneumophila pathogenic bacteria, which comprises a gene chip capable of detecting 24 main drug resistance genes of pneumophila pathogenic bacteria and a reaction system for multiple asymmetric PCR reactions. The 24 drug resistance genes are derived from aminoglycosides, quinolones, extended spectrum beta-lactamases (ESBLs), cephalosporins (AmpC), carbapenems and drug resistance genes with vancomycin resistance and methicillin resistance causing membrane permeability transition. The kit can be used for directly detecting drug resistance genes of pneumophila pathogenic bacteria in clinical samples, is simple and quick to operate, does not need culture or drug sensitive tests, gains valuable time for reasonable application of antibiotics to a great extent, and is worthy of clinical popularization and application.

The present invention provides a transgenic cotton (including hybrid cotton) seed purity identification method. Said method incldues the following steps: using aminoglycoside antibiotics (kanamycin, etc) to prepare seed-soaking aqueous solution with proper concentration, soaking seed, using fresh water sand containing no salt content as germinating bed, sowing, then retaining required temp. and humidity required for germination, after about 7 days the cotton seedling cotyledon is completely patulous, investigating cotton seedling and counting, according to the yellow spot rate identifying purity of seed. It is simple, has no need of disinfecting cotton seed, has no need of making sterile operation and can directly use running water to prepare seed-soaking solution.

The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.

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 provides a placenta and umbilical cord cell protective solution. The protective solution is mainly prepared by dissolving a mycoplasma inhibitor and aminoglycoside antibiotics with an aqueous solution of MEM-alpha medium. 1 mL of the aqueous solution of MEM-alpha medium is respectively used for dissolving 10-30 mg of the mycoplasma inhibitor and 180-240 U of the aminoglycoside antibiotics. Concentration of the aqueous solution of MEM-alpha medium is 10-15 mg / mL. The protective solution provided by the invention not only can effectively kill or inhibit formation of mycoplasma and prevent placenta cell or umbilical cord cell infection, but also can provide a stable osmotic pressure environment for placenta or umbilical cord cells through addition of protective components. Then, human environment can be effectively simulated, and cell survival rate is raised. Meanwhile, nutrients can be provided for storing and transporting cells within a short period of time; immune performance of cells is enhanced; cell infection is prevented; cell viability is effectively improved; and cell transport time is prolonged.

The invention relates to the microbial field, and discloses corynebacterium glutamicum strains and application thereof. A corynebacterium glutamicum MHZ-0510 strain has a preservation number CGMCC No.7939; a corynebacterium glutamicum MHZ-0511 strain has a preservation number CGMCC No.7940; the two strains have significantly improved ability of fermentation for generating L-glutamine, compared with that of the original strain of wild type of corynebacterium glutamicum B498, and can be widely applied to fermentation production of L-glutamine. The corynebacterium glutamicum strains involved in the invention are obtained by screening aminoglycoside antibiotics, such as streptomycin and neomycin, have resistance to the aminoglycoside antibiotics including streptomycin and neomycin, and have improved ability to synthesis of L-glutamine, thus increasing the yield of L-glutamine. Therefore, aminoglycoside antibiotics can be widely applied to screen of L-glutamine.

The invention discloses primers and a kit for detecting the aminoglycoside drug-resistance genes of bacteria, and belongs to the technical field of microbiological detection. The sequences of the primers provided by the invention are shown in SEQ ID NO: 1-10, and by comparing the aminoglycoside drug-resistance gene sequence of multiple bacteria and clinic isolated strains in the gene sequence library of NCBI, the specific primers designed at conserved sites are capable of rapidly detecting the five aminoglycoside drug-resistance genes of aac(3)-II, aac(6')-Ib, aph(3')-III, ant(3')-1a and ant(4')-1a5 of multiple bacteria. The invention further discloses a kit containing the primers and used for detecting the aminoglycoside drug-resistance genes of bacteria, wherein the kit is capable of rapidly and accurately detecting the aminoglycoside antibiotic-related drug-resistance genes of bacteria.

The invention relates to a slow-releasing agent of antibiotics containing aminoglycoside, comprising slow-releasing micro-sphere containing slow-releasing findings and aminoglycoside antibiotics, and special dissolvent containing suspending adjuvant agent such as sodium carboxymethyl cellulose with the adhesive degree being 100cp-3000cp (at 20-30 Deg. C). The slow-releasing findings comprises EVAc, polyphenyl, PLA, PLGA, decanedioic acid copolymer, albumen glue and gelatin; the slow-releasing micro-sphere can be produced to slow-releasing implanting agent and unguent agent. When the slow-releasing implanting agent and injection is placed or injected into bacteria, the medicine can be released slowly for more than 5-30 days, and toxicity is dramatically reduced at the same time when effective medicine concentration is got and maintained. The said slow-releasing agent is specially effective for chronic medullitis, bedsore, intractable ulcer on skin, diabetes femoral head necrosis and other abscessus, which are caused by Staphylococcus, Streptococcus, Streptococcus, acne Propionibacteriaceae, Enterobacter, Enterobacter, gonotoxin or parameningococcus.

The invention relates to an enzyme-linked immunodetection method of aminoglycoside antibiotics in animal-derived foods, belonging to the immnunoassay field. The invention utilizes a carbodiimide method to synthesize immunogen (NM)L-(KM)m-(GM)n-(SM)k-BSA with multiple antigen determinants, such as aminoglycoside antibiotics, by four steps, utilizes a glutaric dialdehyde method to synthesize the envelope antigen of the aminoglycoside antibiotics and establish the enzyme-linked immunodetection method of the aminoglycoside antibiotics in the animal-derived foods; a polyclonal antibody with the specificity of aminoglycoside cluster is adopted as a detection reagent; gentamicin, neomycin, kanamycin or streptomycin is adopted as a standard substance, the four antibiotics and OVA conjugate are adopted as the envelope antigens, and the establishment of an ELISA method for detecting multi-residue of the aminoglycoside antibiotics provides a detecting means with high speed and high efficiency for the multi-residue detection of the aminoglycoside antibiotics in the animal-derived foods. The invention has the advantages of simple pre-processing, high sensitivity, high precision and the like.

The present invention provides aminoglycosides and pharmaceutical compositions that include the aminoglycosides. The aminogylcosides are useful to treat or prevent infectious diseases (e.g., bacterial infections) in a mammal (e.g., human).

An antibacterial eye medicine containing pranoprofen contains non-steroid antiphlogistic medicine, aminoglycoside-type antibacterial medicine, polyvinyl pyrrolidone, and pharmacologically acceptable carrier. Its preparing process is also disclosed.