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High-Performance Liquid Chromatography
Published in Adorjan Aszalos, Modern Analysis of Antibiotics, 2020
Joel J. Kirschbaum, Adorjan Aszalos
Novobiocin is an antibiotic produced by Streptomyces. It was quantified in a bovine mastitis product using an octadecylsilane analytical column and pre-column (50 x 2 mm) with a mobile phase of 0.005 M 1-heptanesulfonate, sodium salt-methanol (20:80) flowing at 1 ml/min through a 254 nm detector. Recoveries averaged 101%. Novenamine, hydroxynovobiocin, novobiocic acid, desmethyldescarbamylnovobiocin, dihydronovobiocin, isonovobiocin, descarbamylnovobiocin, and two other unknown impurities can be resolved by this system [464].
Physiology and Growth
Published in Paul Pumpens, Single-Stranded RNA Phages, 2020
Furthermore, novobiocin, the first clinically employed antibiotic that has been shown to inhibit nucleic acid synthesis without direct binding to DNA, blocked replication of the phage MS2 (Smith and Davis 1965). Chromomycin A3, another inhibitor of the host's DNA-dependent RNA-polymerase, reduced the yield of phage MS2 by 90% (Kaziro and Kamiyama 1965; Hasegawa 1966), although purified Qβ replicase was insensitive to the drug (Kaziro and Kamiyama 1967).
Novobiocin
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Novobiocin formerly had a role in the treatment of staphylococcal infections. With the advent of the penicillinase-resistant penicillins and other antistaphylococcal agents, novobiocin is no longer used for this indication, except perhaps as an adjunct to other drugs for the treatment of methicillin-resistant staphylococcal infections. For instance, novobiocin–sodium fusidate and novobiocin–rifampicin combinations have been used successfully to treat staphylococcal infections of this nature (Jensen, 1968). These combinations have been used only to prevent the emergence of further drug resistance among such strains, and there is no evidence that they act synergistically. With the emergence of more resistant staphylococci, there is an increased interest in the drug. It has been used as a prophylactic agent in the prevention of catheter infections in cancer patients (Raad et al., 1998).
A novobiocin derivative, XN4, triggers ferroptosis in gastric cancer cells via the activation of NOX4
Published in Pharmaceutical Biology, 2022
Rongrong Li, Bin Yin, Deyu Zeng, Zhenyang Liu
Novobiocin (Nov) is a type of coumarin antibiotic, which, along with its synthetic derivatives, displays high efficacy in anti-proliferative assays against various cancer cell lines (Lettini et al. 2017). Several reports have demonstrated that Nov acts as a potential anticancer agent by leading to cell death in human cancer cells (Dlugosz and Janecka 2017; Le Bras et al. 2007). In order to explore more efficacious anticancer agents, we synthesised a series of Nov derivatives and found XN4 to be one of the most active agents. In Imatinib-sensitive and -resistant chronic myeloid leukaemia cells, XN4 has been reported to generate reactive oxygen species (ROS), resulting in DNA damage and cell apoptosis (Wu et al. 2015). Although no studies have reported the relationship between XN4 and ferroptosis of cancer cells, increasing evidence suggests that Nov may induce apoptosis and that ferroptosis occurs simultaneously with apoptosis and autophagy (Wu et al. 2008; Hou et al. 2016; Hong et al. 2017). Therefore, XN4 might have potential as a cancer treatment. In this study, we explore the possible effect of XN4 on the ferroptosis of GC cells and determine the potential role of nicotinamide adenine dinucleotide phosphate oxidase 4 (NOX4) in this process.
The war against bacteria, from the past to present and beyond
Published in Expert Review of Anti-infective Therapy, 2022
Lucrezia Bottalico, Ioannis Alexandros Charitos, Maria Assunta Potenza, Monica Montagnani, Luigi Santacroce
Antimicrobial agents that do not belong to the above described groups include, among others, bacitracin, novobiocin, oxazolidinones, and streptogramins. Bacitracin has a similar antimicrobial spectrum to benzylpenicillin and acts by inhibiting the biosynthesis of the cell wall of susceptible bacteria [124]. Novobiocin is a broad-spectrum antimicrobial drug that binds to magnesium ions, which are essential for the stability of the cell wall of susceptible bacteria and causes cell membrane damage, concomitantly interfering with DNA synthesis [125].
Repurposing of Streptomyces antibiotics as adenosine deaminase inhibitors by pharmacophore modeling, docking, molecular dynamics, and in vitro studies
Published in Journal of Receptors and Signal Transduction, 2020
K. G. Arun, C. S. Sharanya, J. Abhithaj, C. Sadasivan
Kinetics of enzyme inhibition by novobiocin was conducted using different concentrations of substrate (10–60 μM) and fixed concentration of inhibitor (50 μM). A Lineweaver–Burk plot was drawn, and Km, K’m (altered Km), and Ki (inhibitor constant) values were determined (Figure 10). The mode of inhibition was found to be competitive, and Ki was determined as 39.28 micromolar. The enzyme kinetics study revealed that the aminocoumarin antibiotics, novobiocin, is a potent inhibitor of ADA through the active site binding.