Ref ID : 4855
M. Bamdad, C.A. Groliere, Janine Dupy-Blanc, and Lucien David; Toxicity of Two Pairs of Epimeric Ionophorous Antibiotics Towards Tetrahymena pyriformis. Structure-Activity Relationship. Arch.Protistenk 144:297-307, 1994
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Structure-activity relationship of four ionophorous antibiotics, nigericin (C29-CH2OH) and grisorixin (C29-CH3) and their respective epimers, epinigericin and epigrisorixin where the methyl is in axial position on C28, was investigated. Toxicity studies of these antibiotics (10 mg/l) were carried out with respect to the population time course of T. pyriformis in the exponential growth phase, and DNA and RNA synthesis. Results showed different durations of cell division inhibition which increased in the following order: epigrisorixin < epinigericin < grisorixin < nigericin. All four antibiotics caused a marked decrease in DNA and RNA synthesis at the beginning of the experiment. For each pair, nigericin and grisorixin were more active than their respective epimers (epinigericin and epigrisorixin). Toxicity differences towards Tetrahymena, between nigericin/grisorixin and between each antibiotic and its epimer, may be due respectively to structural differences at carbons 30 and 28.