Abstract: The disclosure provides a method for manufacturing an active substance for inducing self-lysis in microalga cells, including: inoculating a bacterial strain belonging to Bacillus into a culturing medium to obtain a bacterial suspension; culturing the bacterial strain belonging to Bacillus at least to a stationary phase to a condition in which the bacterial strain belonging to Bacillus aggregates in the bacterial suspension and the bacterial suspension becomes pellucid; and after the bacterial strain belonging to Bacillus aggregates in the bacterial suspension and the bacterial suspension becomes pellucid, performing a vacuum distillation procedure on the bacterial suspension to obtain an active solution, wherein the active solution contains an active substance for inducing self-lysis in microalga cells.

Abstract: Provided are compounds, the use of the said compounds in treatment, for example treatment of microbial infections, particularly by Gram negative bacteria. The compounds are polymyxin-based and are represented by the formula (I): and pharmaceutically acceptable salts thereof, where X is —NHC(O)—, —C(O)—, —OC(O)—, —CH2— or —SO2—; R5 represents C0-12 alkyl(C4-6 heterocyclyl), or C2-12 alkyl or C0-12 alkyl(C3-8 cycloalkyl). and the alkyl or cycloalkyl bears one, two or three hydroxyl groups, or a —NR6R7 group, or one —NR6R7 group and one or two hydroxyl groups; and R1 to R4 and R6 to R8 are as defined in the description.

Abstract: Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin A. The novel compounds have antibacterial properties against a diverse range of Gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin A. Also provided are antibacterial pharmaceutical compositions containing the novel compounds and novel protected compounds, as well as methods for preparing the antibacterial compounds and protected compounds.

Abstract: Disclosed herein are novel peptides and protected peptides. These compounds can be derived from naturally occurring peptides, such as those selected from colistin, circulin A, polymyxin A, polymyxin B, polymyxin D, octapeptin B, octapeptin C, and [Ile7]polymyxin B1. Also disclosed are pharmaceutical compositions containing the new peptides, as well as methods for preparing the novel peptides and protected peptides.

Abstract: The present invention relates to a polymyxin derivative and to a combination product comprising at least two such derivatives. The invention further relates to a method for treating, alleviating or ameliorating an infection in a subject caused by a Gram-negative bacterium, by administering a therapeutically effective amount of a derivative according to the present invention to said subject; to a method for sensitizing Gram-negative bacteria to an antibacterial agent by administering, simultaneously or sequentially in any order a therapeutically effective amount of said antibacterial agent and a derivative according to the present invention to said subject; to methods for developing novel antibiotics; for reducing the nephrotoxicity, for improving the pharmacokinetic properties of natural polymyxins and octapeptins; and for sensitizing clinically important bacteria to a host defense mechanism complement present in serum. Finally, the invention relates to a process for preparing such polymyxin derivatives.

Abstract: The present invention relates to a polymyxin derivative wherein the derivative has a total of three positive charges at physiological pH and wherein the terminal moiety (D) of the derivative comprises a total of 1 to 5 carbon atoms. The invention also relates to a method of treating a subject for a gram-negative bacterial infection by administering a polymyxin derivative of the invention in combination with a second antibacterial agent. Finally, the invention relates to a process for preparing such polymyxin derivatives.

Abstract: The present invention relates to a polymyxin derivative wherein R1, R2 and R3 are optional and R1, R2, R3, R5, R8 and R9 are cationic or neutral amino acid residues selected so that the total number of positive charges at physiological pH is at least two but no more than three; and to a combination product comprising at least two such derivatives.

Abstract: The present invention relates to immobilized biologically active entities that retain a significant biological activity following manipulation. The invention also comprises a medical substrate comprising a heparin entity bound onto a substrate via at least one heparin molecule, wherein said bound heparin entity is heparinase-1 sensitive.

Abstract: The present invention relates to a polymyxin derivative wherein R1, R2 and R3 are optional and R1, R2, R3, R5, R8 and R9 are cationic or neutral amino acid residues selected so that the total number of positive charges at physiological pH is at least two but no more than three; and to a combination product comprising at least two such derivatives.

Abstract: Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin A. The novel compounds have antibacterial properties against a diverse range of Gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin A. Also provided are antibacterial pharmaceutical compositions containing the novel compounds and novel protected compounds, as well as methods for preparing the antibacterial compounds and protected compounds.

Abstract: The present invention relates to a polymyxin derivative wherein the derivative has a total of three positive charges at physiological pH and wherein the terminal moiety (D) of the derivative comprises a total of 1 to 5 carbon atoms. The invention also relates to a method of treating a subject for a gram-negative bacterial infection by administering a polymyxin derivative of the invention in combination with a second antibacterial agent. Finally, the invention relates to a process for preparing such polymyxin derivatives.

Abstract: Provided herein are novel compounds and novel protected compounds that can be derived from polymyxin, including, e.g., polymyxin A. The novel compounds have antibacterial properties against a diverse range of Gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin A. Also provided are antibacterial pharmaceutical compositions containing the novel compounds and novel protected compounds, as well as methods for preparing the antibacterial compounds and protected compounds.

Abstract: The present disclosure defines a method for identifying and/or treating risk and/or occurrence of cardiac defect. As is shown herein, microbiomes are reproducibly and detectably associated with cardiac defect risk factors and changes to the microbiome can directly alter cardiac defect risk. The present disclosure demonstrates that microbial signatures can be used to characterize components of microbiomes that associate with altered risk or occurrence of cardiac defects and to identify treatments to reduce risk or severity of cardiac defects.

Abstract: Provided herein is an antibacterial compound of the following formula: or a pharmaceutically acceptable salt thereof. The antibacterial compound has antibacterial properties against a diverse range of gram negative bacteria and reduced toxicity compared to polymyxins such as polymyxin B. Also provided are antibacterial pharmaceutical compositions containing the antibacterial compound, as well as methods for preparing the antibacterial compound.

Abstract: The present invention provides a new class of polymyxin derivates useful for treating bacterial infections, especially Gram-negative infections, that have reduced renal cytotoxicity.

Abstract: The present invention relates to a polymyxin derivative wherein R1, R2 and R3 are optional and R1, R2, R3, R5, R8 and R9 are cationic or neutral amino acid residues selected so that the total number of positive charges at physiological pH is at least two but no more than three; and to a combination product comprising at least two such derivatives.

Abstract: The present invention relates to a polymyxin derivative wherein the derivative has a total of three positive charges at physiological pH and wherein the terminal moiety (D) of the derivative comprises a total of 1 to 5 carbon atoms The invention also relates to a method of treating a subject for a gram-negative bacterial infection by administering a polymyxin derivative of the invention in combination with a second antibacterial agent. Finally, the invention relates to a process for preparing such polymyxin derivatives.

Abstract: The present invention relates to a polymyxin derivative wherein the derivative has a total of three positive charges at physiological pH and wherein the terminal moiety (D) of the derivative comprises a total of 1 to 5 carbon atoms; and to a combination product comprising at least two such derivatives. The invention further relates to a method for sensitizing Gram-negative bacteria to an antibacterial agent by administering, simultaneously or sequentially in any order a therapeutically effective amount of said antibacterial agent and a derivative according to the present invention to said subject; to methods for developing novel antibiotics; and for sensitizing clinically important bacteria to a host defense mechanism complement present in serum. The invention also relates to a method of treating a subject for a gram-negative bacterial infection by administering a polymyxin derivative of the invention in combination with a second antibacterial agent.

Abstract: The invention is related to the method of polymyxine B recovery from fermentation broth for the purpose of pure substance recovery. The invention mentioned above is obtained by using the method of polymyxine B recovery from fermentation broth according invention, which abstract is characterized by, that the filtrate is obtained from fermentation broth, its pH and color is adjusted and purified on non-ionogenic synthetic adsorbents of polystyrene type with specific surface 500 till 1000 m2·g?1 and fabric size 3 till 30 nm. The polymyxine B is eluated from adsorbent by aqueous solution of organic solvent. The polymyxine B base is coagulated from eluate after adjustment of pH to alcaline area. The polymyxine B base is converted by mineral acid to polymyxine B salt solution, from which is obtained crystal substance by drying.

Abstract: A topical ointment is described for use in the treatment of indolent wounds composed of fat-soluble vitamins, namely, vitamin A, vitamin D, vitamin E, and a subantimicrobial amount of polypeptide antibiotic, which, in turn, acts as a proteinase inhibitor. The active ingredients are combined with a pharmaceutically acceptable topical carrier of lanolin, white petrolatum, mineral oil, and admixtures thereof. In treating these difficult to heal wounds, the selection of the level of the antibiotic at near trace amounts was surprisingly found to be above the proteinase inhibiting threshold and below the wound irritation level. The formulation hereof produced unexpected healing results not found in vitamin-enriched ointments or in antibiotic ointments.

Abstract: An ointment composition for treating decubitus ulcers and methods for its making and its use. The composition includes a skin protestant ointment, a rash cream, an antibiotic ointment, virgin olive oil, and boric acid powder. The skin protestant ointment includes active ingredients petroleum 53.4%, lanolin 15.5%, and inactive ingredients cod liver oil containing vitamin A & vitamin D, a fragrance, light mineral oil, microcrystalline wax, and paraffin. The rash cream includes active ingredients dimethicone 1% and zinc oxide 10%, and inactive ingredients aloe barbadensis extract, benzyl alcohol, coconut oil, cod liver oil containing vitamin A & vitamin D, a fragrance, glycerol oleate, light mineral oil, ozokerite, paraffin, propylene glycol, sorbitol, synthetic beeswax, and water. The antibiotic ointment includes active ingredients polymyxin B sulfate 5,000 units, bacitracin zinc 400 units, and neomycin base (as sulfate) 3.5 mg., and an inactive ingredient white petroleum.

Abstract: The invention is related to the method of polymyxine B recovery from fermentation broth for the purpose of pure substance recovery. The invention mentioned above is obtained by using the method of polymyxine B recovery from fermentation broth according invention, which abstract is characterized by, that the filtrate is obtained from fermentation broth, its pH and color is adjusted and purified on non-ionogenic synthetic adsorbents of polystyrene type with specific surface 500 till 1000 m2.g?1 and fabric size 3 till 30 nm. The polymyxine B is eluated from adsorbent by aqueous solution of organic solvent. The polymyxine B base is coagulated from eluate after adjustment of pH to alcaline area. The polymyxine B base is converted by mineral acid to polymyxine B salt solution, from which is obtained crystal substance by drying.

Abstract: The present invention relates to a polymyxin derivative wherein the derivative has a total of three positive charges at physiological pH and wherein the terminal moiety (D) of the derivative comprises a total of 1 to 5 carbon atoms; and to a combination product comprising at least two such derivatives. The invention further relates to a method for sensitizing Gram-negative bacteria to an antibacterial agent by administering, simultaneously or sequentially in any order a therapeutically effective amount of said antibacterial agent and a derivative according to the present invention to said subject; to methods for developing novel antibiotics; and for sensitizing clinically important bacteria to a host defense mechanism complement present in serum. The invention also relates to a method of treating a subject for a gram-negative bacterial infection by administering a polymyxin derivative of the invention in combination with a second antibacterial agent.

Abstract: Novel conjugates of bacterial outer membrane binding peptides, preferably having bacterial sensitization activity, and immune cells chemotactic peptides, and pharmaceutical compositions containing same useful in the treatment of bacteremia and/or septicemia following infection by gram negative bacteria administered alone or in combination with conventional antibiotics.

Abstract: Disclosed is a safe and effective hair-growing agent comprising a protein kinase C-specific inhibitor.

Abstract: Provided are compounds of the formula (1): wherein R? is hydrogen, methyl or NH2C(O)CH2—; R? and R?? are independently methyl or hydrogen; R adn Ry are independently hydroxy or hydrogen; R1 is hydroxy, hydrogen, or hydroxysulfonyloxy; R7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy; R2 is a novel acyl side chain. Also provided are novel formulations, methods of inhibiting fungal and parasitic activity, and a process for preparing dideoxy (R?H) forms of the compounds.

Abstract: The present invention provides monoclonal antibodies which are highly specific for Bacillus spores. Also provided are peptides derived from those monoclonal antibodies. Both the antibodies and peptides are highly specific and can discriminate between spores of potentially lethal organisms such as Bacillus anthracis and other harmless but closely related bacilli and provide a very powerful tool in the construction of detection instruments as counter measures.

Abstract: Compositions and methods are described for preventing and treating sepsis in humans and animals. Surgical patients, low birth weight infants, and burn and trauma victims can be treated prophylactically. Methods for treating acute infections are provided with advantages over current therapeutic approaches.

Abstract: A liposome composition comprising small, surface-bound effector molecules is disclosed. The liposomes have a surface layer of hydrophilic polymer chains, for enhanced circulation time in the bloodstream. The effector molecules are attached to the distal ends of the polymer chains. In one embodiment, the effector is polymyxin B, for treatment of septic shock.

Abstract: Disclosed is a safe and effective hair-growing agent comprising a protein kinase C-specific inhibitor.

Abstract: Antimicrobial compounds and compositions and uses thereof, including the treatment and prevention of bacterial infections are described. The compounds and compositions include lantibiotic polypeptides and the nucleic acid sequences encoding the polypeptides. The compounds and compositions are useful as antimicrobials in antibiotic pharmaceutical preparation and as an antimicrobial or antiseptic dentifrice.

Abstract: Disclosed are multibinding compounds which are antibiotics effective against bacterial infections, in particular, Gram-negative bacterial infections. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a polymyxin, circulin or octapeptin antibiotic or other suitable compound which binds to the LPS present in bacteria, in particular, Gram-negative bacteria. The multibinding compounds of this invention are useful for the prophylaxis and treatment of various bacterial infections caused by bacteria.

Abstract: A liposome composition comprising small, surface-bound effector molecules is disclosed. The liposomes have a surface layer of hydrophilic polymer chains, for enhanced circulation time in the bloodstream. The effector molecules are attached to the distal ends of the polymer chains. In one embodiment, the effector is polymyxin B, for treatment of septic shock.

Abstract: The present invention is directed to a novel depsipeptide has been isolated from a new marine strain L-13-ACM2-092 belonging to the family Micromonosporaceae. Its production by aerobic fermentation under controlled conditions of the strain, and the isolation and purification of PM-93135 are described herein. The compound and the fermentation broth demonstrate significant activity against several cancer cell lines. The compound also shows activity against several gram positive bacteria.

Abstract: A liposome composition comprising small, surface-bound effector molecules is disclosed. The liposomes have a surface layer of hydrophilic polymer chains, for enhanced circulation time in the bloodstream. The effector molecules are attached to the distal ends of the polymer chains. In one embodiment, the effector is polymyxin B, for treatment of septic shock.

Abstract: The present invention relates to methods and compositions for treating gram-negative bacterial infections, using BPI protein products. Co-treatment, or concurrent administration, of BPI protein product with an antibiotic in treatment of gram-negative bacterial infections improves the therapeutic effectiveness of the antibiotic, including increasing antibiotic susceptibility of gram-negative bacteria and reversing resistance of the bacteria to antibiotics.

Abstract: The present invention is concerned with methods of potentiating an antibiotic. The invention also includes compositions of an antibiotic and a peptide having units of the formula:(a) (A).sub.n wherein A is Lysine or Arginine and n is an integer with a minimum value of 7.(b) (AB).sub.m wherein A is Lysine or Arginine and B is a hydrophobic amino acid selected from the group consisting of Valine, Leucine, Isoleucine, Tyrosine, Phenylalanine and Tryptophan; m is an integer with a minimum value of 3; and(c) (ABC).sub.p wherein A is a cationic amino acid which is Lysine or Arginine; B and C are hydrophobic amino acids which may be the same or different and are selected from the group consisting of Valine, Leucine, Isoleucine, Tyrosine, Phenylalanine and Tryptophan; p is an integer with a minimum value of 2. The compositions have potentiated antibiotic activity.

Abstract: This invention relates to personal care compositions, and, more specifically, to a composition comprising a pyrithione salt or acid, polymyxin antibiotic, and a suitable carrier. The pyrithione plus the polymyxin provide antimicrobial efficacy to the personal care composition. The personal care composition is useful in a variety of dermatological items, such as soaps, shampoos, and skin care medicaments.

Abstract: Compositions and methods are described for preventing and treating sepsis in humans and other animals. Surgical patients, low birth weight infants, burn and trauma victims, as well as other individuals at risk can be treated prophylactically. Methods for treating acute infections with advantages over current therapeutic approaches are provided. Conjugates and methods of making conjugates for the prevention and treatment of sepsis are described.

Abstract: The present invention relates to methods and compositions for treating gram-negative bacterial infections, using BPI protein products. Co-treatment, or concurrent administration, of BPI protein product with an antibiotic in treatment of gram-negative bacterial infections improves the therapeutic effectiveness of the antibiotic, including increasing antibiotic susceptibility of gram-negative bacteria and reversing resistance of the bacteria to antibiotics.

Abstract: An improved device is provided which may be used, e.g. for immunoassay of lipopolysaccharides or for removing LPS pyrogens from aqueous solutions, or for removing LPS endotoxins from wounds. Such device comprises, in combination, a substrate, e.g. plastic, i.e. polystyrene, polycarbonate, polymethylmethacrylate or polyvinyl chloride, or a woven cloth, i.e. a rayon/polyester cloth or a polyester cloth, or a non-woven cloth, i.e. a rayon/polyester cloth, or a polyester cloth, or paper, which is adapted to receive a sample to be tested, and an oligopeptide, or a hydrophobic polypeptide or a polymyxin, e.g. polymyxin B, polymyxin B.sub.1, polymyxin B.sub.2, polymyxin D.sub.1, polymyxin D.sub.2, or polymyxin E, adhered to the substrate.

Abstract: Novel peptides are disclosed which are based on the formula:R.sub.1 (Lys-Phe-Leu).sub.n --Rwherein n is an integer of from 1-10 and R and R.sub.1 are H or an amino acid residue or a fatty acid residue which are useful in the treatment of septic shock.

Abstract: Polymyxin B carrier conjugates, especially polymyxin B-dextran, are water soluble, have a greater half-life in the bloodstream and are significantly less toxic than native polymyxin B.

Abstract: In vitro results indicate that trimethoprim may be ineffective against S. enteritides. However, in vivo results show that trimethoprim alone and in combination with polymyxin B sulfate is effective on S. enteritidis infections in poultry.

Abstract: Antigens that produce antibodies specific for the lipopolysaccharide or endotoxin are produced and characterized. A method of producing the antigen is disclosed. These specific antibodies may be used as immunodiagnostic agents to detect the presence of and quantity of endotoxin in samples.