Antibacterial tryglysin agents
Inventors
Seyedsayamdost, Mohammad R. • Federle, Michael J. • COVINGTON, Brett C. • BUSHIN, Leah B. • RUED, Britta E. • Ambrose, John
Assignees
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Publication Number
US-12630585-B2
Publication Date
2026-05-19
Expiration Date
Abstract
There is currently a high demand for new therapeutic antibiotics with new mechanisms of action. Disclosed are two small molecules, tryglysin A and B, with novel chemical structures and potent antibiotic activity against a narrow spectrum of bacteria. This narrow spectrum of activity indicates the tryglysins could be working through a novel antibiotic mechanism of action. Due to this narrow spectrum, the tryglysins could be used as highly targeted therapeutics to treat or prevent disease without disturbing other important, “beneficial” bacteria within the human microbiome, which is a great improvement over virtually all other clinically used antibiotics that are broad-spectrum. The tryglysins are potent against several streptococcal pathogens, including Streptococcus pneumonia, the leading cause of pneumonia, and Streptococcus mutans, the primary causative agent of tooth decay and gum disease. The tryglycins may allow the development of therapeutics for the treatment and/or prevention of disease caused by these streptococci.
Core Innovation
The disclosed subject matter relates to antibacterial tryglysin A and tryglysin B that are macrocyclic compounds of formula (I), where X is OH or SH. The document describes defined macrocyclic 7-mer peptide sequences containing the tetrahydro[5,6]benzindole motif and indicates targeted activity against streptococcal pathogens including Streptococcus pneumoniae and Streptococcus mutans.
The invention is directed to compositions and methods for treating an infection or disease in a patient caused by at least one streptococcal pathogen, using a tryglysin of formula (I) with X as OH or SH. The document further frames the therapeutic effect as an inhibitory effect that is specific to the streptococcal pathogen(s).
Pharmaceutical and oral-care formulations are described to include the tryglysin with pharmaceutically acceptable carriers, and oral-care examples include mouth wash, oral rinse, and toothpaste with optional oral-care additives such as abrasive agents, flavoring agents, and alcohol. The document also describes recombinant production concepts involving wgkA/wgkB/wgkC expression and isolation/purification, and provides experimental support showing narrow-spectrum growth inhibition against streptococcal pathogens with example inhibitory activity data.
Claims Coverage
The independent claims are two in number and each is centered on administering a tryglysin that is a macrocyclic compound of formula (I) with X being OH or SH, one for a composition use and one for a treatment/prevention method. Across the independent claims, the inventive features are the formula-defined tryglysin and its use to treat or prevent diseases/infections caused by at least one streptococcal pathogen.
Macrocyclic tryglysin for treating streptococcal infection
A composition comprising a tryglysin for use in treating an infection of at least one streptococcal pathogen, the tryglysin being a macrocyclic compound of formula (I) where X is OH or SH.
Administering macrocyclic tryglysin to prevent or treat streptococcal disease
A method for treatment or prevention of a disease in a patient caused by at least one streptococcal pathogen comprising administering to a patient in need of such treatment or prevention an effective amount of a tryglysin, wherein the tryglysin is a macrocyclic compound of formula (I) where X is OH or SH.
The claim coverage centers on a tryglysin defined by macrocyclic formula (I) with X as OH or SH, used either as a composition for treating streptococcal infections or as an administered active for treating or preventing streptococcal-caused diseases. Dependent claims further narrow to particular streptococcal species, quantify dosing/concentration and MIC thresholds, and specify that the inhibitory effect is specific to the targeted streptococcal pathogen(s).
Stated Advantages
Narrow-spectrum growth inhibition against streptococcal pathogens (pathogen-specific inhibitory effect).
Selective inactivity versus non-target bacteria described in the partial content (e.g., L. lactis and E. faecalis).
Documented Applications
Treatment of an infection caused by at least one streptococcal pathogen using a composition comprising a macrocyclic tryglysin of formula (I) where X is OH or SH.
Prevention or treatment of a disease in a patient caused by at least one streptococcal pathogen by administering an effective amount of a macrocyclic tryglysin of formula (I) where X is OH or SH.
Oral-care use via oral care compositions including mouth wash, oral rinse, and toothpaste containing the tryglysin and optionally selected oral-care additives such as abrasive agents, flavoring agents, and alcohol [procedural detail omitted for safety].
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