Vermiculin derivatives. Part 2: Cytotoxic and mutagenic activities of vermiculin derivatives.

The induction of mutations at the HPRT locus and cytotoxicities of 4 vermiculin derivatives 2-4 and 6 were examined in V79 Chinese hamster cells and compared with those of the parent compound vermiculin (1). Derivatives prepared by hydrogenation were less toxic and mutagenic or non toxic and non mutagenic. The substitution at position 13 affected the evaluated biological effects. The results suggest that in vitro metabolism of vermiculin resulted in decreased cytotoxicity and mutagenicity.