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Potential of Mycochemicals in the Prevention and Control of Microbial Diseases
Published in Mahendra Rai, Chistiane M. Feitosa, Eco-Friendly Biobased Products Used in Microbial Diseases, 2022
Terpenoids are by far the largest class of natural products, but only four are currently approved as antimicrobial drugs (tiamulin, valnemulin, retapamulin and lefamulin), and these are all semisynthetic derivatives of the fungal antibiotic pleuromutilin (Mendes et al. 2016).
High-Performance Liquid Chromatography
Published in Adorjan Aszalos, Modern Analysis of Antibiotics, 2020
Joel J. Kirschbaum, Adorjan Aszalos
Bulk tiamulin, an animal antibiotic, was assayed using an octadecylsilane column with a mobile phase of methanol-acetonitrile-2 M aqueous ammonium chloride-10% ammonia (10 ml 30% ammonium hydroxide solution diluted to 100 ml in water; 700:200:40:80) flowing at 1 ml/min through a 254 nm detector [493]. Responses were linear between 2 and 8 μg/ml. Ammonium acetate can be substituted for ammonium chloride, we found in this laboratory.
Translation
Published in Paul Pumpens, Single-Stranded RNA Phages, 2020
The action mechanism of such a popular translation inhibitor as fusidic acid was clarified finally in the R17 RNA-directed in vitro protein synthesis system (San Millan et al. 1975). The latter was also used by the studies of tiamulin, a semisynthetic pleuromutilin derivative, on the bacterial polypeptide chain initiation (Dornhelm and Högenauer 1978). The cell-free extracts of tiamulin resistant mutants of E. coli exhibited an increased in vitro resistance to tiamulin in the R17 RNA-dependent protein synthesis systems, and it was a property of the 50S subunit (Böck et al. 1982).
Occupational inhalation poisoning with the veterinary antibiotic tiamulin
Published in Clinical Toxicology, 2020
Mojca Dobaja Borak, Lucija Sarc, Darja Gnezda Mugerli, Bor Antolic, Miran Brvar
Pleuromutilins were discovered in 1950 as natural-product antibiotics. They are diterpene compounds with the main structure being an eight-membered carbocyclic ring. Most of them have an antibacterial spectrum that spans the common pathogens involved in respiratory tract and skin infections [1,2] (Figure 1). The clarification of the structure in 1962 led to the development and approval of tiamulin in 1979 for veterinary use [3]. Tiamulin is used for treatment and prophylaxis of dysentery, pneumonia and mycoplasmal infections in pigs and poultry in Europe and USA [4]. As a feed additive, it is also used to increase weight gain in swine. Tiamulin acts by inhibiting protein synthesis at the ribosomal level by binding to the 50 S subunit of ribosomes. It is almost completely absorbed in the gastrointestinal tract with peak blood levels occurring after two to four hours and is rapidly distributed with tissue concentrations several times higher than concentrations found in serum [5].
Emerging antibiotics for community-acquired pneumonia
Published in Expert Opinion on Emerging Drugs, 2019
Adamantia Liapikou, Catia Cilloniz, Andrea Palomeque, Toni Torres
Pleuromutilin antibiotics are semisynthetic derivatives of pleuromutilin, a natural product of the fungi Pleurotus mutilus (now called Clitopilus scyphoides). These function by inhibiting bacterial protein synthesis through binding to the peptidyl transferase site on 23S RNA of the 50S ribosome. Retapamulin was the first agent to be approved by the FDA in 2006, but this was only for topical use in impetigo. Another pleuromutilin, tiamulin, has been used with success as a veterinary drug in Europe and Canada [33]. However, lefamulin is the first pleuromutilin to be developed for oral or intravenous use in humans.
Lefamulin: a promising new pleuromutilin antibiotic in the pipeline
Published in Expert Review of Anti-infective Therapy, 2019
Caroline Dillon, Anthony J. Guarascio, Jordan R. Covvey
Pleuromutilins were discovered as natural agents in 1951. Tiamulin and valnemulin were used in veterinary medicine in poultry and swine [13,14], whereas retapamulin was the first pleuromutilin to be approved for human use, used topically for the short-term treatment of impetigo due to methicillin-susceptible Staphylococcus aureus (MSSA) or Streptococcus pyogenes [13]. Evaluation of structure-activity relationships across a vast array of pleuromutilin analogs eventually led to the discovery of BC-3781, known as lefamulin, which is being evaluated in both an intravenous (IV) and oral (PO) dosage form [15].