Sparsomycin

Sparsomycin is a bacterial metabolite and a nucleoside analog of uracil that has been found in S. sparsogenes and has diverse biological activities.^1,2,3 It is active against KB carcinoma cells, Gram-positive and Gram-negative bacteria, and fungi.⁴ Sparsomycin is an inhibitor of peptidyl transferase that interferes with tRNA binding to the A-site of the peptidyl transfer center and increases the binding of peptidyl-tRNA to the P-site.² It inhibits protein synthesis in bacteria, archaea, and eukaryotes.^2,3 Sparsomycin reduces tumor growth in a P388 mouse leukemia model and in a Walker 256 carcinosarcoma rat model.⁵

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1. Ottenheijm, H.C., van den Broek, L.A., Ballesta, J.P., et al. Chemical and biological aspects of sparsomycin, an antibiotic from Streptomyces. Prog. Med. Chem. 23, 219-268 (1986).

2. Wilson, D.N. The A-Z of bacterial translation inhibitors. Crit. Rev. Biochem. Mol. Biol. 44(6), 393-433 (2009).

3. Lazaro, E., Van den Broek, L.A., San Felix, A., et al. Chemical, biochemical and genetic endeavours characterizing the interaction of sparsomycin with the ribosome. Biochimie 73(7-8), 1137-1143 (1991).

4. Owen, S.P., Dietz, A., and Camiener, G.W. Sparsomycin, a new antitumor antibiotic. I. Discovery and biological properties. Antimicrob. Agents Chemother. 1962, 772-779 (1963).

5. Zylicz, Z., Wagener, D.J., van Rennes, H., et al. In vivo antitumor activity of sparsomycin and its analogues in eight murine tumor models. Invest. New Drugs 6(4), 285-292 (1988).