Biological activities of pargamicin A, a novel cyclic peptide antibiotic from Amycolatopsis sp.

  title={Biological activities of pargamicin A, a novel cyclic peptide antibiotic from Amycolatopsis sp.},
  author={Hideki Hashizume and Hayamitsu Adachi and Masayuki Igarashi and Yoshio Nishimura and Yuzuru Akamatsu},
  journal={The Journal of Antibiotics},
The time-kill studies using pargamicin A against Staphylococcus aureus and Enterococcus faecalis were performed. The effects of the incorporation of radioactive precursors into macromolecules, membrane potential and function using fluorescent dyes were also examined. These studies revealed that rapid bactericidal activity of pargamicin A correlates with the perturbation of bacterial cell membrane potential and membrane function. 

Structure and antibacterial activities of new cyclic peptide antibiotics, pargamicins B, C and D, from Amycolatopsis sp. ML1-hF4

Structure and antibacterial activities of new cyclic peptide antibiotics, pargamicins B, C and D, from Amycolatopsis sp. ML1-hF4

Valgamicin C, a novel cyclic depsipeptide containing the unusual amino acid cleonine, and related valgamicins A, T and V produced by Amycolatopsis sp. ML1-hF4

In the course of optimizing pargamicin A production in Amycolatopsis sp. ML1-hF4, we discovered novel cyclic depsipeptide compounds in the broth and designated them valgamicins A, C, T and V. The

Total Synthesis of Pargamicin A.

This work enables the synthesis of pargamicin congeners for the development of structure-activity relationships and informs strategies for accessing other sterically congested piperazic acid-containing natural products.

Biologically active secondary metabolites from Actinomycetes

The diversity of secondary metabolites produced by actinomycete strains with respect to their chemical structure, biological activity and origin is demonstrated and it is concluded that the discovery of new bioactive compounds will continue to pose a great challenge for scientists.

Tripropeptin C Blocks the Lipid Cycle of Cell Wall Biosynthesis by Complex Formation with Undecaprenyl Pyrophosphate †

TPPC can potentially inhibit C55-PP phosphatase activity, which plays a crucial role in the lipid cycle of peptidoglycan synthesis, and this mode of action is different from that of currently available drugs such as vancomycin, daptomycin, and bacitracin.

Amycolamicin: a novel broad-spectrum antibiotic inhibiting bacterial topoisomerase.

The abuse of antibacterial drugs imposes a selection pressure on bacteria that has driven the evolution of multidrug resistance in many pathogens. Our efforts to discover novel classes of antibiotics

Bacteria Hunt Bacteria through an Intriguing Cyclic Peptide

This review provides an overview of the chemical classification of cyclic AMPs isolated from bacteria, and provides a description of their biological activity and mode of action.

[Studies for the development of novel anti-MRSA/VRE drugs].

  • H. Hashizume
  • Biology, Chemistry
    Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan
  • 2012
Tripropeptin C (TPPC), major component of tripropeptins, is the most promising compound because it is efficacious against MRSA and VRE both in vitro and in a mouse septicemia model, and shows no cross-resistance to available drugs including vancomycin.

Selective, On-Resin N-Methylation of Cyclic Peptides and Implications for the Discovery of Membrane Permeable Scaffolds

2D 1H NMR and H/D exchange studies provide insight into the conformational basis of the regioselectivity of the reaction and provide a rationale for the observation that the partially methylated derivatives are not only significantly more membrane permeable than their nonmethylated precursors, but are also more permeability than the corresponding permethylated species.



Pargamicin A, a Novel Cyclic Peptide Antibiotic from Amycolatopsis sp.

Pargamicin A showed potent antibacterial activity against Staphylococcus aureus strains including MRSA and Enterococcus faecalis/faecium strains including VRE.

Telavancin, a Multifunctional Lipoglycopeptide, Disrupts both Cell Wall Synthesis and Cell Membrane Integrity in Methicillin-Resistant Staphylococcus aureus

It is demonstrated that telavancin's antibacterial activity derives from at least two mechanisms: inhibited late-stage peptidoglycan biosynthesis in a substrate-dependent fashion and bound the cell wall, as it did the lipid II surrogate tripeptide N,N′-diacetyl-l-lysinyl- d-alanyl-d-alanine, with high affinity.

In vitro activity of RP 59500, a semisynthetic injectable pristinamycin, against staphylococci, streptococci, and enterococci

  • R. Fass
  • Medicine, Biology
    Antimicrobial Agents and Chemotherapy
  • 1991
RP 59500 antagonized the bactericidal activities of oxacillin and gentamicin against Staphylococcus aureus and that of ampicillin against E. faecalis ATCC 29212 and has a broad spectrum of in vitro activity against gram-positive cocci; combining it with other drugs is not advantageous.

In Vitro and In Vivo Antibacterial Activities of a Novel Glycylcycline, the 9-t-Butylglycylamido Derivative of Minocycline (GAR-936)

Overall, TBG-MINO shows antibacterial activity against a wide spectrum of gram-positive and gram-negative aerobic and anaerobic bacteria including strains resistant to other chemotherapeutic agents.

Daptomycin Nonsusceptibility in Staphylococcus aureus with Reduced Vancomycin Susceptibility Is Independent of Alterations in MprF

It is reported that among three clinical S. aureus isolates which developed vancomycin heteroresistance, as well as daptomycin nonsusceptibility despite a lack of exposure to this drug, there were no mutations resulting in amino acid substitutions in MprF.

Failures in Clinical Treatment of Staphylococcus aureus Infection with Daptomycin Are Associated with Alterations in Surface Charge, Membrane Phospholipid Asymmetry, and Drug Binding

The cross-resistance to hNP-1 and tPMP-1 may also impact the capacity of these daptomycin-resistant organisms to be cleared from sites of infection, particularly endovascular foci.

Tigecycline Efflux as a Mechanism for Nonsusceptibility in Acinetobacter baumannii

Assessment of tigecycline efflux mediated by the resistance-nodulation-division-type transporter AdeABC indicates that an efflux-based mechanism plays a role in reduced tigecacline susceptibility in Acinetobacter.

Quinupristin-Dalfopristin Resistance among Gram-Positive Bacteria in Taiwan

ABSTRACT To understand quinupristin-dalfopristin resistance among clinical isolates of gram-positive bacteria in Taiwan, where this agent is not yet available for clinical use, we evaluated 1,287

Activities of RPR 106972 (a new oral streptogramin), cefditoren (a new oral cephalosporin), two new oxazolidinones (U-100592 and U-100766), and other oral and parenteral agents against 203 penicillin-susceptible and -resistant pneumococci

The MICs of RPR 106972, cefditoren, two new oxazolidinones, and other oral and parenteral agents for 203 penicillin-susceptible and -resistant pneumococci were determined.