Anti-HIV and cytotoxic ruthenium(II) complexes containing flavones: biochemical evaluation in mice

Ru(II) polypyridyl complexes containing 3-hydroxyflavone derivatives as coligands were screened for anti-HIV and cytotoxic activities against eleven tumor cell lines. In order to check the effect of flavones containing Ru(II) complexes in vivo on a mammal, a representative complex Ru(L)2(DMSO)2 x 5H2O (LH-3-Hdroxy-4'-benzyloxyflavone; M5) was orally administered to adult male mice. Its effects on protein content and LDH were studied in different tissues of the animal. The compound got absorbed and retained in the blood between 1-3 hr after feeding. As compared to the normal and DMSO control sets, tissue specific significant reversible changes in the protein content as well as in LDH activity were observed between 1-4 hr of treatment. However, on polyacrylamide gel electrophoresis, except some tissue specific transitory alterations, expression patterns of five LDH isozymes were unchanged after feeding the compound. The present results suggested that in addition to its potent cytotoxic and anti-HIV effects on cell lines in vitro, M5 inhibited LDH activity, but reversibly with a little effect on biosynthetic status of the enzyme in mice.