LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 3 of total 3

Search options

  1. Article ; Online: Computational Studies on Selected Macrolides Active against Escherichia coli Combined with the NMR Study of Tylosin A in Deuterated Chloroform

    Biljana Arsic / Jill Barber / Ana Cikos / Manikandan Kadirvel / Emilija Kostic / Andrew J. McBain / Jelena Milicevic / Angela Oates / Andrew Regan

    Molecules, Vol 27, Iss 7280, p

    2022  Volume 7280

    Abstract: Although many antibiotics are active against Gram-positive bacteria, fewer also show activity against Gram-negative bacteria. Here, we present a combination of in silico (electron ion-interaction potential, molecular docking, ADMET), NMR, and ... ...

    Abstract Although many antibiotics are active against Gram-positive bacteria, fewer also show activity against Gram-negative bacteria. Here, we present a combination of in silico (electron ion-interaction potential, molecular docking, ADMET), NMR, and microbiological investigations of selected macrolides (14-membered, 15-membered, and 16-membered), aiming to discover the pattern of design for macrolides active against Gram-negative bacteria. Although the conformational studies of 14-membered and 15-membered macrolides are abundant in the literature, 16-membered macrolides, and their most prominent representative tylosin A, have received relatively little research attention. We therefore report the complete 1 H and 13 C NMR assignment of tylosin A in deuterated chloroform, as well as its 3D solution structure determined through molecular modelling (conformational search) and 2D ROESY NMR. Additionally, due to the degradation of tylosin A in deuterated chloroform, other species were also detected in 1D and 2D NMR spectra. We additionally studied the anti-bacterial activity of tylosin A and B against selected Gram-positive and Gram-negative bacteria.
    Keywords macrolides ; bacteria ; 2D ROESY NMR ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2022-10-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    Full text online

    More links

    Kategorien

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

  2. Article ; Online: Inhibition of aggregation of amyloid-β through covalent modification with benzylpenicillin; potential relevance to Alzheimer's disease

    Izzeddin Alsalahat / Zubida M. Al-Majdoub / Mutasem O. Taha / Jill Barber / Harmesh Aojula / Nigel Hodson / Sally Freeman

    Biochemistry and Biophysics Reports, Vol 26, Iss , Pp 100943- (2021)

    2021  

    Abstract: The pathogenesis of Alzheimer's disease (AD) is correlated with the misfolding and aggregation of amyloid-beta protein (Aβ). Here we report that the antibiotic benzylpenicillin (BP) can specifically bind to Aβ, modulate the process of aggregation and ... ...

    Abstract The pathogenesis of Alzheimer's disease (AD) is correlated with the misfolding and aggregation of amyloid-beta protein (Aβ). Here we report that the antibiotic benzylpenicillin (BP) can specifically bind to Aβ, modulate the process of aggregation and supress its cytotoxic effect, initially via a reversible binding interaction, followed by covalent bonding between specific functional groups (nucleophiles) within the Aβ peptide and the beta-lactam ring. Mass spectrometry and computational docking supported covalent modification of Aβ by BP. BP was found to inhibit aggregation of Aβ as revealed by the Thioflavin T (ThT) fluorescence assay and atomic force microscopy (AFM). In addition, BP treatment was found to have a cytoprotective activity against Aβ-induced cell cytotoxicity as shown by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) cell toxicity assay. The specific interaction of BP with Aβ suggests the possibility of structure-based drug design, leading to the identification of new drug candidates against AD. Moreover, good pharmacokinetics of beta-lactam antibiotics and safety on long-time use make them valuable candidates for drug repurposing towards neurological disorders such as AD.
    Keywords Alzheimer's disease ; Amyloid-beta ; Benzylpenicillin ; Thioflavin T ; Atomic force microscopy ; Mass spectrometry ; Biology (General) ; QH301-705.5 ; Biochemistry ; QD415-436
    Subject code 540
    Language English
    Publishing date 2021-07-01T00:00:00Z
    Publisher Elsevier
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

    Full text online

    More links

    Kategorien

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

  3. Article: 16-Membered Macrolide Antibiotics: a Review

    Arsic, Biljana / Jill Barber / Ana Čikoš / Milan Mladenovic / Nevena Stankovic / Predrag Novak

    International Journal of Antimicrobial Agents. 2017,

    2017  

    Abstract: Mainly used in veterinary medicine, the 16-membered macrolide antibiotics (e.g. tylosin A and josamycin) are much less studied than their 14- and 15-membered erythromycin-based cousins. Even though they share similar antibacterial profile (they are ... ...

    Abstract Mainly used in veterinary medicine, the 16-membered macrolide antibiotics (e.g. tylosin A and josamycin) are much less studied than their 14- and 15-membered erythromycin-based cousins. Even though they share similar antibacterial profile (they are active primarily against Gram-positive and a limited range of Gram-negative organisms), the 16-membered macrolides show some advantages, including better gastrointestinal tolerance, lack of drug-drug interactions and activity against some resistant strains with additional interactions by extending the peptide tunnel reach. In addition to the antibacterial activity, the most famous representative of the class, tylosin A, as well as some derivatives of desmycosin (tylosin B), have been shown to possess anti-malarial activity (also observed in 14-membered macrolide antibiotics, azithromycin, solithromycin and clindamycin), thus providing the opportunity to investigate these drugs as cheap and effective anti-malarials. This is an overview of the latest research on biosynthesis, structure, chemical properties and mode of action of 16-membered macrolides, with special emphasis on their most explored members: tylosin A and josamycin.
    Keywords antibacterial properties ; antimalarials ; azithromycin ; biosynthesis ; clindamycin ; drug interactions ; drugs ; gastrointestinal system ; josamycin ; mechanism of action ; physicochemical properties ; tylosin ; veterinary medicine
    Language English
    Size p. .
    Publishing place Elsevier B.V.
    Document type Article
    Note Pre-press version
    ZDB-ID 1093977-5
    ISSN 1872-7913 ; 0924-8579
    ISSN (online) 1872-7913
    ISSN 0924-8579
    DOI 10.1016/j.ijantimicag.2017.05.020
    Database NAL-Catalogue (AGRICOLA)

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 3368: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)
    Zs.MO 500: Show issues

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

To top