Caerulomycins produced by Streptomyces caeruleus are bipyridinic molecules endowed with antibiotic properties. Caerulomycin A was found to have a strong anti-fungal and anti-amoebic activity, and a mild antibacterial activity.
Notes préparatoires
Caerulomycin A stock solution may be prepared in DMSO or methanol at 1 mg/mL. The stock solution can be further diluted in water to 0.1 mg/mL. Higher concentrations my requrie gentle heating to 40 °C. Dilutions from the stock solution should be freshly prepared.
In order to enable the caerulomyicn biosynthetic study by in vivo gene disruptions, it is crucial to develop a genetic modification system for the producer Actinoalloteichus sp. WH1-2216-6. The spore germination timing and the concentration of MgSO4 in the medium
[reaction: see text] The total synthesis of caerulomycin C is described. Key steps in this synthesis utilize 1,2-, 1,3-, and 1,4-halogen dance reactions for the functionalization of the pyridine ring.
The anti-amoebic action of the bipyridyl antibiotic caerulomycin was assessed in vitro and in vivo using various strains of Entamoeba histolytica from polyxenic, axenic and monoxenic cultures. Minimum inhibition concentrations of caerulomycin (metronidazole) were 7.5 (5), 15.6(1.95) and 60 (2.5)
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