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Cyclic Lipopeptide

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42. Infective Endocarditis in Adults: Diagnosis, Antimicrobial Therapy, and Management of Complications Full Text available with Trip Pro

, perturbations of antibiotic penetration into the vegetation, and unique antibiotic pharmacokinetic/pharmacodynamic (PK/PD) features. Therefore, prolonged, parenteral, bactericidal therapy is required for attempted infection cure. Inoculum Effect The effect of high bacterial densities on antimicrobial activity is called the inoculum effect in which certain groups of antimicrobials commonly used to treat IE such as β-lactams and glycopeptides (and, to a lesser extent, lipopeptides such as daptomycin) are less (...) efficacy as the optimized PD parameters for aminoglycoside, fluoroquinolone, and daptomycin therapy, the AUC 24 /MIC is the optimized PD activity for glycopeptides such as vancomycin, teicoplanin, telavancin, oritavancin, and lipopeptides such as daptomycin. β-Lactam efficacy, in contrast, is best predicted by the percent duration of time that the serum concentration exceeds the MIC. For penicillins and cephalosporins to achieve a bacteriostatic effect in a murine model, the time the free drug must

2016 Infectious Diseases Society of America

43. Colobreathe (colistimethate sodium)

Alanine aminotransferase ANCOVA Analysis of Covariance API Active Pharmaceutical Ingredient AR Assessment report AST Aspartate aminotransferase AUC Area under the concentration-time curve BMI Body mass index BSAC British Society for Antimicrobial Therapy BUN Blood urea nitrogen C Colistin cAMP Cyclic adenosine monophosphate CEP Certificate of Suitability CF Cystic fibrosis CFTR Cystic Fibrosis Transmembrane Conductance Regulator CFQ CFQ – Cystic Fibrosis Questionnaire CFQ-R Cystic Fibrosis (...) be delivered by a multi-dose DPI (Clickhaler, Innovata biomed) but this required administration of 32 doses (each dose 5 mg gentamicin) over 30 minutes. In the current application a novel unit-dose DPI - Turbospin DPI – has been used to deliver 125 mg (equivalent to 1,662,500 IU) colistimethate sodium per dose from gelatine capsules. About the product Polymyxins are a group of lipopeptide antibiotics isolated from the spore-forming soil bacterium Bacillus polymyxa. Five major, chemically distinct members

2012 European Medicines Agency - EPARs

44. Daptomycin: a comparison of two intravenous formulations Full Text available with Trip Pro

Daptomycin: a comparison of two intravenous formulations Daptomycin is a cyclic lipopeptide antibacterial agent with potent bactericidal activity against a broad range of Gram-positive organisms. In 2003, daptomycin for injection received approval from the US Food and Drug Administration (FDA) for the treatment of patients with complicated skin and skin structure infections (cSSSIs); in 2006, it was approved for the treatment of patients with Staphylococcus aureus bacteremia, including those

2018 Drug design, development and therapy

45. Genomic and Genotypic Characterization of Cylindrospermopsis raciborskii: Toward an Intraspecific Phylogenetic Evaluation by Comparative Genomics Full Text available with Trip Pro

by comparing their genomes with sequences from other strains available in public databases. The results obtained by comparing seven C. raciborskii and the Raphidiopsis brookii D9 genomes revealed a set of conserved core genes and a variable set of accessory genes, such as those involved in the biosynthesis of natural products, heterocyte glycolipid formation, and nitrogen fixation. Gene cluster arrangements related to the biosynthesis of the antifungal cyclic glycosylated lipopeptide hassallidin were

2018 Frontiers in microbiology

46. The LuxR Regulators PcoR and RfiA Co-regulate Antimicrobial Peptide and Alginate Production in Pseudomonas corrugata Full Text available with Trip Pro

The LuxR Regulators PcoR and RfiA Co-regulate Antimicrobial Peptide and Alginate Production in Pseudomonas corrugata Cyclic lipopeptides (CLPs) are considered as some of the most important secondary metabolites in different plant-associated bacteria, thanks to their antimicrobial, cytotoxic, and surfactant properties. In this study, our aim was to investigate the role of the Quorum Sensing (QS) system, PcoI/PcoR, and the LuxR-type transcriptional regulator RfiA in CLP production

2018 Frontiers in microbiology

47. Surfactin-based nanoparticles loaded with doxorubicin to overcome multidrug resistance in cancers Full Text available with Trip Pro

Surfactin-based nanoparticles loaded with doxorubicin to overcome multidrug resistance in cancers Multidrug resistance (MDR) is one of the major obstacles to successful cancer chemotherapy. Developing efficient strategies to reverse MDR remains a major challenge. Surfactin (SUR), a cyclic lipopeptide biosurfactant, has been found to display anticancer activity.In this paper, SUR was assembled by solvent-emulsion method to load the anticancer drug doxorubicin (DOX). The cytotoxicity of DOX

2018 International journal of nanomedicine

48. Developments of Cyanobacteria for Nano-Marine Drugs: Relevance of Nanoformulations in Cancer Therapies Full Text available with Trip Pro

Developments of Cyanobacteria for Nano-Marine Drugs: Relevance of Nanoformulations in Cancer Therapies Current trends in the application of nanomaterials are emerging in the nano-biotechnological sector for development of medicines. Cyanobacteria (blue-green algae) are photosynthetic prokaryotes that have applications to human health and numerous biological activities as dietary supplements. Cyanobacteria produce biologically active and chemically diverse compounds such as cyclic peptides (...) , lipopeptides, fatty acid amides, alkaloids, and saccharides. More than 50% of marine cyanobacteria are potentially exploitable for the extraction of bioactive substances, which are effective in killing cancer cells by inducing apoptotic death. The current review emphasizes that not even 10% of microalgal bioactive components have reached commercialized platforms due to difficulties related to solubility. Considering these factors, they should be considered as a potential source of natural products for drug

2018 Marine drugs

49. Synergistic activity of cosecreted natural products from amoebae-associated bacteria Full Text available with Trip Pro

of this bacterium revealed the presence of two biosynthetic gene clusters that were found adjacent to each other on a contiguous stretch of the bacterial genome. Although one cluster codes for the polyketide synthase producing the known antibiotic mupirocin, the other cluster encodes a nonribosomal peptide synthetase leading to the unreported cyclic lipopeptide jessenipeptin. We describe its complete structure elucidation, as well as its synergistic activity against methicillin-resistant Staphylococcus aureus

2018 Proceedings of the National Academy of Sciences of the United States of America

50. Organization and characterization of genetic regions in Bacillus subtilis subsp. krictiensis ATCC55079 associated with the biosynthesis of iturin and surfactin compounds. Full Text available with Trip Pro

Organization and characterization of genetic regions in Bacillus subtilis subsp. krictiensis ATCC55079 associated with the biosynthesis of iturin and surfactin compounds. Bacillus subtilis subsp. krictiensis ATCC55079 produces the cyclic lipopeptide antibiotics iturin A-F as well as several surfactins. Here, we analyzed and characterized the biosynthetic genes associated with iturin and surfactin production in this strain. We aligned the sequences of each iturin and surfactin synthetase ORF

2017 PLoS ONE

51. Association of daptomycin dosing regimen and mortality in patients with VRE bacteraemia: a review. Full Text available with Trip Pro

Association of daptomycin dosing regimen and mortality in patients with VRE bacteraemia: a review. VRE are associated with ∼1300 deaths per year in the USA. Recent literature suggests that daptomycin, a cyclic lipopeptide antibiotic with concentration-dependent bactericidal activity, is the preferred treatment option for VRE bacteraemia, yet the optimal dosing strategy for this indication has not been established. In vitro evidence suggests that higher-than-labelled doses of daptomycin

2018 Journal of Antimicrobial Chemotherapy

52. High-Frequency Occurrence of Surfactin Monomethyl Isoforms in the Ferment Broth of a Bacillus subtilis Strain Revealed by Ion Trap Mass Spectrometry Full Text available with Trip Pro

High-Frequency Occurrence of Surfactin Monomethyl Isoforms in the Ferment Broth of a Bacillus subtilis Strain Revealed by Ion Trap Mass Spectrometry Surfactins are cyclic lipopeptides consisting of a β-hydroxy fatty acid of various chain length and a peptide ring of seven amino acids linked together by a lactone bridge, forming the cyclic structure of the peptide chain. These compounds are produced mainly by Bacillus species and possess numerous biological effects such as antimicrobial (...) (antiviral, antibacterial, and antifungal) activities. A mixture of surfactins extracted from Bacillus subtilis strain SZMC 6179J was examined by HPLC-ESI-IT-MS technique, enhancing their separation to reveal novel lipopeptide varieties with higher masses and to characterize their structures. During the MS² spectra analyses of their sodiated molecular ions [M + Na]⁺, a previously rarely encountered group of surfactins was detected and two novel types of the group were discovered containing methyl

2018 Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry

53. Antagonistic bacteria disrupt calcium homeostasis and immobilize algal cells Full Text available with Trip Pro

and alters the morphology of the biflagellated green alga Chlamydomonas reinhardtii. This antagonistic effect is decreased in a bacterial mutant lacking orfamides, demonstrating that these secreted cyclic lipopeptides play an important role in the algal-bacterial interaction. Using an aequorin Ca2+-reporter assay, we show that orfamide A triggers an increase in cytosolic Ca2+ in C. reinhardtii and causes deflagellation of algal cells. These effects of orfamide A, which are specific to the algal class (...) of Chlorophyceae and appear to target a Ca2+ channel in the plasma membrane, represent a novel biological activity for cyclic lipopeptides.

2017 Nature communications

54. Increasing rate of daptomycin non-susceptible strains of Staphylococcus aureus in patients with atopic dermatitis Full Text available with Trip Pro

Increasing rate of daptomycin non-susceptible strains of Staphylococcus aureus in patients with atopic dermatitis Daptomycin is a cyclic lipopeptide that is bactericidal against Staphylococcus aureus, including methicillin-resistant S. aureus (MRSA), vancomycin-intermediate S. aureus (VISA) and vancomycin-resistant S. aureus (VRSA) strains. Daptomycin exerts its antimicrobial effect by a calcium-dependent interaction with the cytoplasmic membrane resulting in depolarization, ion loss and rapid

2017 Advances in Dermatology and Allergology/Postȩpy Dermatologii i Alergologii

55. Surotomycin versus vancomycin in adults with Clostridium difficile infection: primary clinical outcomes from the second pivotal, randomized, double-blind, Phase 3 trial. Full Text available with Trip Pro

Surotomycin versus vancomycin in adults with Clostridium difficile infection: primary clinical outcomes from the second pivotal, randomized, double-blind, Phase 3 trial. The available treatment options for Clostridium difficile infection (CDI) are limited by high recurrence rates. Surotomycin was a novel bactericidal cyclic lipopeptide in development to treat CDI that demonstrated non-inferiority to vancomycin in a Phase 2 trial.To assess surotomycin safety and clinical response (non

2017 Journal of Antimicrobial Chemotherapy Controlled trial quality: predicted high

56. Enteric microbiome profiles during a randomized Phase 2 clinical trial of surotomycin versus vancomycin for the treatment of Clostridium difficile infection. Full Text available with Trip Pro

Enteric microbiome profiles during a randomized Phase 2 clinical trial of surotomycin versus vancomycin for the treatment of Clostridium difficile infection. The effects of surotomycin (CB-183,315, MK-4261), a bactericidal cyclic lipopeptide, and vancomycin, the current standard-of-care for Clostridium difficile infection (CDI), on intestinal pathogens and microbiota were evaluated parallel to a Phase 2 randomized, double-blind clinical trial.The single-centre cohort included 26 patients

2017 Journal of Antimicrobial Chemotherapy Controlled trial quality: uncertain

57. Antimicrobial octapeptin C4 analogues active against <i>Cryptococcus</i> species. Full Text available with Trip Pro

Antimicrobial octapeptin C4 analogues active against Cryptococcus species. Resistance to antimicrobials is a growing problem in both developed and developing countries. In nations where AIDS is most prevalent, the human fungal pathogen Cryptococcus neoformans is a significant contributor to mortality, and its growing resistance to current antifungals is an ever-expanding threat. We investigated octapeptin C4, from the cationic cyclic lipopeptide class of antimicrobials, as a potential

2017 Antimicrobial Agents and Chemotherapy

58. Daptomycin. Full Text available with Trip Pro

Daptomycin. Daptomycin is a cyclic lipopeptide antibiotic used for the treatment of Gram-positive infections including complicated skin and skin structure infections, right-sided infective endocarditis, bacteraemia, meningitis, sepsis and urinary tract infections. Daptomycin has distinct mechanisms of action, disrupting multiple aspects of cell membrane function and inhibiting protein, DNA and RNA synthesis. Although daptomycin resistance in Gram-positive bacteria is uncommon

2017 Journal of Antimicrobial Chemotherapy

59. Pharmacokinetics of surotomycin from phase 1 single and multiple ascending dose studies in healthy volunteers Full Text available with Trip Pro

Pharmacokinetics of surotomycin from phase 1 single and multiple ascending dose studies in healthy volunteers Surotomycin, a novel, orally administered, cyclic, lipopeptide antibacterial in development for the treatment of Clostridium difficile-associated diarrhea, has demonstrated minimal intestinal absorption in animal models.Safety, tolerability, and plasma pharmacokinetics of single and multiple ascending oral doses (SAD/MAD) of surotomycin in healthy volunteers were characterized in two

2017 BMC pharmacology & toxicology Controlled trial quality: predicted high

60. Daptomycin-Induced Acute Eosinophilic Pneumonia: Late Onset and Quick Recovery Full Text available with Trip Pro

Daptomycin-Induced Acute Eosinophilic Pneumonia: Late Onset and Quick Recovery Daptomycin is a cyclic lipopeptide antibiotic that provides great coverage for gram positive cocci. From the early years of daptomycin use, concerns were raised regarding the pulmonary side effects of daptomycin and potential development of acute eosinophilic pneumonia (AEP) secondary to daptomycin therapy.AEP could be idiopathic or induced by drugs or toxins. It is a distinct entity from atopic diseases

2017 Case reports in pulmonology

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