Translation of "Gramicidin" in German

Between 1942 and 1948 he studied peptides of the protein group gramicidin, work later used by Frederick Sanger in determining the structure of insulin.

As polypeptide antibiotics there may be mentioned especially, for example, colistrin, gramicidin S, polymyxin B, virginamycin, tyrothricin, viomycin and vancomycin.

As polypeptide antibiotics, for example colistin, gramicidin S, polymyxin B, virginamycin, tyrothricin, viomycin or vancomycin may in particular be mentioned.

Such cytotoxic substances, which belong to the spectrum of multidrug resistance include for example daunorubicin, doxorubicin, mitoxantrone, et oposid, tenoposid, vinblastine, vincristine, actinomycin D, mitomycin C, taxol (paclitaxel), topotecan, colchicine, emetin, ethidiumbromide, puromycin, gramicidin D, valinomycin and mithramycin.

The basicity and the in some cases insoluble compounds of the cyclic and linear tyrocidine (A-E) and of the linear gramicidin and its cyclic form have greatly restricted the therapeutic use, together with their secondary effects and their non-specific effect only on grampositive pathogens, so that the method described for the effect on grampositive pathogens includes specific gramnegative pathogens; in addition there is no antiviral effect as will be shown below.

Whereas the therapeutical use of these cyclic peptide antibiotics is known, employed analogously mainly as skin and mucous membrane infections, in spite of the use of tyrocidines in the complex with gramicidin D (tyrothricin) in the throat, nose and pharynx, no investigations on the antiviral and molecular-biological effect are known.

For these specifically included active substances, in particular the linear tyrocidine and the cyclic tyrocidine (A-E) as well as the tuftsin and its analogs, gramicidin (D and S) and the polymyxins, in addition typical NMR signals are obtained which are characteristic of the secondary or monomer structure of these cyclic and linear peptides in the hydrophobic micellar core.

In contrast, suitable tyrocidine (A-E) and cyclic gramicidin (S) as well as tuftsin do not effect hemolysis, as has surprisingly been found.

It may be concluded from this that specifically the ionophoric properties of the linear gramicidin (D) are responsible for this undesirable secondary effect.

A relationship to individual pharmacodynamic effects of tyrocidine (A-E) and/or linear gramicidin (D) as regards a molecular-biological action, for example on the transcription and ionophoresis with fungi and yeast is not known and nor is its antiviral effect.

In contrast to gramicidin D it has been found that tyrocidines (A-E), including the linear tyrocidines (see FIG. 4), bonds to (dA+dT)-rich regions of the DNA which through this pharmaceutical formulation has lost the salt-dependence.

It has further been found that the N+ -tensides according to the general formula I and II intensify the antifungal action in combination with the gramicidin or tyrocidine or tyrocidine analogs by their ionophoric character.

Moreover, in this case the active transport, which is inhibited by the ionophoric properties of the claimed peptide analogs, in particular linear formyltyrocidine and linear gramicidin, is intensified by N+ -tensides.

There may be mentioned as polypeptide antibiotics, especially, for example, collistin, gramicidin S, polymyxin B, virginiamycin, tyrothricin, viomycin and vancomycin.

As polypeptide antibiotics, special mention should be made, for example, of colistin, gramicidin S, polymyxin B, virginamycin, tyrothricin, viomycin or vancomycin.

Especially preferred are inhibitors of the cell wall synthesis such as imipenem, meropenem, ertapenem, aztreonam, pencilline, aminpenicillins, acylaminopenicillins, isoxazolylpenicillins, cephalosporins, sultamicillin, fosfomycin, glycopeptide such as vancomycin and teicoplanin, polypetides such as bacitracin, colistin, gramicidin, polymyxin B, tyrothricin and of the protein synthesis at the ribosome such as antibiotics from the group of amino glycosides also called amino glycoside-antibiotics.

Lipophilic antibiotics are preferably benzathin, phenoxymethylpenicillin, chloramphenicol, chlortetracyclin, ciprofloxacin betaine, ciprofloxacin, clarithromycin, clindamycin palmitate hydrochloride, trimethoprim, erythromycin 2-acetate, and the corresponding stearate; erythromycin estolate, erythromycin ethylsuccinate, erythromycin glutamate, erythromycin lactopropionate, erythromycin stearate, fusidinic acid, preferably free fusidinic acid, gramicidin, mupirocin, lipophilic members of the imidazole series, such as econazole, itraconazole, clotrimazole and others, pristinamycin, rifabutin, rifapentin, rifampicin, silver sulfadiazine.

Moreover, proline-rich peptides, in stark contrast to AMPS such as melittin or gramicidin which have a defined secondary structure, seem in vitro to have neither a hemolytic nor a toxic effect on eukaryotic cells.

A suitable molecule with cytotoxic properties against tumors is the biomolecule gramicidin S (GS), a natural antibiotic.

Channels (like gramicidin) form continuous aqueous pores through the bilayer, allowing ions to diffuse through.

Clinical course: Under treatment with propamidine, polymyxin b, neomycin, gramicidin and polyhexidine (topical) as well as fluconazole/ketoconazole (systemic) the diameter of the annular infiltrate became smaller.

Our group investigates the modular pathways biosynthesizing nonribosomal peptides, such as the antibiotics gramicidin S and penicillin or the immunosuppressant cyclosporin.

The patient received local treatment with combined antibacterial and antifungal therapy (Ofloxacin, Polymyxin-B, Neomycin, Gentamycin, Amicacin, Gramicidin, Natamycin, Cetokonazol) due to a circumscribed corneal infiltrate.

The proteins according to the invention can be administered together with antibiotics, for example, from the following group: bacitracin, gramicidin, polymyxin, vancomycin, teichoplanin, aminoglycosides, penicillin, and monobactam.

O2 and not allow their effect on the arachidonic acid metabolism, and satisfy the above mechanism (1-5), with the preparation according to the invention at pH 7.0 and pH 8.0 the radicals are intercepted by the ionophoric nature of the gramicidins and tyrocidines.

Among the polypeptide antibiotics are inter alia polymixins the tyrocidines A-E, the cyclic and linear gramicidins (S and D), bacitracin and amphomycin, as well as capreomycin.

Whereas tyrothrocin consists of a mixture of basic tyrocidines (80% A, 20% B-E) and linear gramicidins (D) which have a neutral pK and are synthesized by Bacillus subtilis, tuftsin is a natural activator of phagocytic cells and is thus of eukaryotic origin.

Among the polypeptide antibiotics are inter alia polymyxins, the tyrocidines A-E, the cyclic and linear gramicidins (S and D), bacitracin and amphomycin, as well as capreomycin.

Whereas tyrothrocin consists of a mixture of basic tyrocidines (80% A, 20% B-E) and linear gramicidins (D) which have a neutral pK and are synthesized by Bacillus subtilis, tuftsin is a natural activator of phagocytic cells and is thus of eucaryotic origin.

In accordance with the invention, use can be made of all known antibiotics, for example beta-lactam, vancomycin, macrolides, tetracyclines, quinolones, fluoroquinolones, nitrated compounds (such as nitroxoline, tilboquinol or nitrofurantoin), aminoglycosides, phenicols, lincosamida, synergistins, fosfomycin, fusidic acid, oxazolidinones, rifamycins, polymixyns, gramicidins, tyrocydines, glycopeptides, sulfonamides or trimethoprims.