Comparative in vitro activity of valnemulin against porcine bacterial pathogens

Aitken, I A; Morgan, J. H.; Dalziel, R.; Burch, David; Ripley, P. H.

doi:10.1136/vr.144.5.128

Cited by 17 publications

(8 citation statements)

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“…In Figure 1 the distribution of tiamulin and valnemulin MICs is presented. A few studies have been made comparing tiamulin and valnemulin MICs for B. hyodysenteriae (Møller et al, 1996;Aitken et al, 1999). Aitken et al studied field isolates from the UK and Møller et al studied Danish isolates.…”

Section: Resultsmentioning

confidence: 99%

Susceptibility to pleuromutilins inBrachyspira(Serpulina)hyodysenteriae

Karlsson

Gunnarsson

Franklin

2001

Anim. Health. Res. Rev.

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The pleuromutilins are the only antimicrobial agents with sufficient minimum inhibitory concentration (MIC) values left to treat swine dysentery in Sweden. Other antimicrobials are either not approved for use against swine dysentery or only partly active against Brachyspira hyodysenteriae. To date, in Sweden two pleuromutilins, tiamulin and valnemulin, are authorized for use in pigs. This study includes a comparison between MICs of tiamulin and valnemulin for Swedish field isolates of B. hyodysenteriae, as determined by broth dilution. For different isolates the MIC of tiamulin was between 0 and 8 times higher than that of valnemulin. No resistance to pleuromutilins was recorded (tiamulin MIC range 0.031–2 μg/ml, valnemulin MIC range ≤0.016–1 μg/ml). In vitro development of tiamulin resistance was also studied. Two B. hyodysenteriae and two B. pilosicoli strains became resistant to tiamulin following reiterated passages on agar containing tiamulin in increasing concentrations. The resistance emerged slowly and three of the strains that went through more than 60 passages increased their tiamulin MICs from 0.031–0.25 to more than 128 μg/ml. The tiamulin MIC for one B. hyodysenteriaestrain that went through 29 passages increased from 0.0125 to 4 μg/ml. One B. pilosicoli strain developed cross-resistance to valnemulin; the MIC increased from 0.25 to more than 64 μg/ml. The valnemulin MIC for one B. hyodysenteriae strain increased from 0.031 μg/ml to 32 μg/ml. Valnemulin MIC was not determined for the B. hyodysenteriae strain that only went through 29 passages. The valnemulin MIC of the other B. pilosicoli strain increased from 0.031 to 4 μg/ml.

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Section: Resultsmentioning

confidence: 99%

Susceptibility to pleuromutilins inBrachyspira(Serpulina)hyodysenteriae

Karlsson

Gunnarsson

Franklin

2001

Anim. Health. Res. Rev.

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“…This led first to the commercialisation of two pleuromutilin-derived antibiotics employed in veterinary field: tiamulin (Sandoz) (Drews et al. 1975) and valnemulin (Novartis) (Aitken et al. 1999), both used on swine and poultry as a treatment and prophylaxis agent for dysentery caused by Gram-positive bacteria and Mycoplasma spp.…”

Section: Medicinal Basidiomycetesmentioning

confidence: 99%

The good, the bad and the tasty: The many roles of mushrooms

Mattos-Shipley¹,

Ford²,

Alberti³

et al. 2016

Studies in Mycology

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Fungi are often inconspicuous in nature and this means it is all too easy to overlook their importance. Often referred to as the “Forgotten Kingdom”, fungi are key components of life on this planet. The phylum Basidiomycota, considered to contain the most complex and evolutionarily advanced members of this Kingdom, includes some of the most iconic fungal species such as the gilled mushrooms, puffballs and bracket fungi. Basidiomycetes inhabit a wide range of ecological niches, carrying out vital ecosystem roles, particularly in carbon cycling and as symbiotic partners with a range of other organisms. Specifically in the context of human use, the basidiomycetes are a highly valuable food source and are increasingly medicinally important. In this review, seven main categories, or ‘roles’, for basidiomycetes have been suggested by the authors: as model species, edible species, toxic species, medicinal basidiomycetes, symbionts, decomposers and pathogens, and two species have been chosen as representatives of each category. Although this is in no way an exhaustive discussion of the importance of basidiomycetes, this review aims to give a broad overview of the importance of these organisms, exploring the various ways they can be exploited to the benefit of human society.

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“…In addition to boronated analogs of the pleuromutilin core, we also obtained or prepared several clinically relevant non-boron analogs as summarized in Figure 1. 18−21…”

Section: Introductionmentioning

confidence: 99%

Boron-Pleuromutilins as Anti-Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis

Jacobs¹,

Lunde²,

Freund³

et al. 2019

J. Med. Chem.

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A series of pleuromutilins modified by introduction of a boron-containing heterocycle on C(14) of the polycyclic core are described. These analogs were found to be potent anti-Wolbachia antibiotics and, as such, may be useful in the treatment of filarial infections caused by Onchocerca volvulus, resulting in Onchocerciasis or river blindness, or Wuchereria bancrofti and Brugia malayi and related parasitic nematodes resulting in lymphatic filariasis. These two important neglected tropical diseases disproportionately impact patients in the developing world. The lead preclinical candidate compound containing 7-fluoro-6-oxybenzoxaborole (15, AN11251) was shown to have good in vitro anti-Wolbachia activity and physicochemical and pharmacokinetic properties providing high exposure in plasma. The lead was effective in reducing the Wolbachia load in filarial worms following oral administration to mice.

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Comparative in vitro activity of valnemulin against porcine bacterial pathogens

Cited by 17 publications

References 0 publications

Susceptibility to pleuromutilins inBrachyspira(Serpulina)hyodysenteriae

Susceptibility to pleuromutilins inBrachyspira(Serpulina)hyodysenteriae

The good, the bad and the tasty: The many roles of mushrooms

Boron-Pleuromutilins as Anti-Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis

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