Abstract
Among the growing family of ribosomally synthesized, post-translationally modified peptides, particularly intriguing are class III lanthipeptides containing the triamino acid labionin. In the course of a screening program aimed at finding bacterial cell wall inhibitors, we discovered a new lanthipeptide produced by an Actinoplanes sp. The molecule, designated NAI-112, consists of 22 amino acids and contains an N-terminal labionin and a C-terminal methyl-labionin. Unique among lanthipeptides, it carries a 6-deoxyhexose moiety N-linked to a tryptophan residue. Consistently, the corresponding gene cluster encodes, in addition to the LanKC enzyme characteristic of this lanthipeptide class, a glycosyl transferase. Despite possessing weak antibacterial activity, NAI-112 is effective in experimental models of nociceptive pain, reducing pain symptoms in mice in both the formalin and the chronic constriction injury tests. Thus, NAI-112 represents, after the labyrinthopeptins, the second example of a lanthipeptide effective against nociceptive pain.
Highlights
In the course of a screening program for peptidoglycan inhibitors, we unexpectedly discovered a labionin-containing lanthipeptide, designated NAI-112, which possesses unique structural properties
In the course of a screening program aimed at finding bacterial cell wall inhibitors, we discovered a new lanthipeptide produced by an Actinoplanes sp
Despite possessing weak antibacterial activity, NAI-112 is effective in experimental models of nociceptive pain, reducing pain symptoms in mice in both the formalin and the chronic constriction injury tests
Summary
In the course of a screening program for peptidoglycan inhibitors, we unexpectedly discovered a labionin-containing lanthipeptide, designated NAI-112, which possesses unique structural properties. Since labyrinthopeptins have been reported to exert potent antiallodynic effects in the spinal nerve injury model of neuropathic pain,[11] we assessed whether NAI-112 has antinociceptive/antiallodynic activity in two different experimental models of inflammatory pain
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