Add time:09/05/2019         Source:sciencedirect.com

SPARSOMYCIN (cas 1404-64-4) (Sm) is a known antibiotic derived from Streptomyces. Its potential antitumor activity stimulated the search for a synthetic production method and the development of new derivatives. In a recent screening investigation, three Sm analogues appeared to be more active and considerably less toxic than the parent drug. Sparsomycins became especially interesting when it was shown that Sm potentiates the antitumor activity of cisplatin. In the present study Sm and its three promising analogues: deshydroxy-Sm (dSm), ethyl-deshydroxy-Sm (EdSm) and n-pentyl-Sm (PSm) were studied for their cisplatin potentiating effect. The experiments were performed on CD2F1 mice inoculated with 106 L1210 cells s.c. Sparsomycins were administered i.p. 3 h before cisplatin on days 1, 5 and 9. Three of the drugs, Sm, dSm and PSm, showed no potentiating effect in this tumor model. At a dose of 10 mg/kg, EdSm potentiated cisplatin antitumor activity 2.8 times (P < 0.01) without an increase in weight loss. These results warrant further investigation.

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