Introduction

Lantipeptides are compounds synthesized from bacterial ribosomes. Their name comes from the aminoacid lanthionine, which gives conformational stability to the peptide structure. They are compounds characterized by antibacterial activity, antiviral activity, as well as activity against neuropathic and inflammatory pain. However, they are structurally rigid and highly hydrophobic molecules. The purpose of this invention is to provide new, more flexible lantipeptide compounds that can be used in the form of a pharmaceutical product to treat inflammatory and neuropathic pain, oncological pain and pain induced by chemotherapy, migraine and topical and general anesthesia.

Technical features

The main characteristics of the new lantipeptides are: different sequence of amino acids compared to the lantipeptides present in the state of the art, absence of a disulfide bridge, presence of a derivative of the labionine aminoacid, which has never been described before, and the presence of at least one replacement of the tryptophan residue. In particular, the compounds are characterized by a different molecular charge than the known compounds and are characterized by the presence of 22 aminoacids instead of the 18 traditional aminoacids. The absence of a disulfide bridge, as well as the presence of aminoacid residues between positions 11 and 14 not involved in the formation of rings, allows the new compounds to be more flexible and to adopt additional conformational states than known compounds. In addition, disulfide bridges are highly prone to redox reactions, which therefore cannot occur on lantipeptides of new molecular structure. Furthermore, depending on the excipient used, pharmaceutical compounds may be created which, depending on the treatment to be carried out, may be administered orally, topically or parenterally in various dosage forms.

Possible Applications

• Pharmaceutical product for the treatment of inflammatory and neuropathic pain, oncological pain and pain induced by chemotherapy, migraine and topical and general anesthesia.
• Combined therapy for the prevention and treatment of pain together with other active ingredients of analgesic preparations used in human or veterinary medicine

Advantages

• Molecular flexibility with the possibility of adopting additional conformational states
• Absence of redox reactions
• Possibility of creating pharmaceutical compounds with different forms of administration depending on the excipient used