Portal de Periódicos da CAPES

Cytostatic activity of coumarin metabolites and derivatives in the B16-F10 murine melanoma cell line

1999; Lippincott Williams & Wilkins; Volume: 9; Issue: 3 Linguagem: Inglês

10.1097/00008390-199906000-00005

1473-5636

Fausto Alejandro Jiménez-Orozco, Juan Molina‐Guarneros, Nicandro Mendoza-Patiño, Fernando León-Cedeño, Blas Flores-Pérez, E. Santos-Santos, J. J. Mandokl,

Beetle Biology and Toxicology Studies

Coumarin has antitumour effects In vivo and cytostatic effects in vitro. Its half-life in humans is short (1–1.5 h) and the monohydroxylated biotransformation products have significantly longer half-lives. One or several of these products may thus be responsible for the antitumoral effects. We have assayed the In vitro cytostatic activity of five monohydroxylated coumarins (3-, 4-, 6-, 7− and 8 monohydroxycoumarin), their acetates and methyl-ethers. Murine melanoma cells (cell line B16-F10) and murine fibroblasts (B82) were exposed to the test compounds at concentrations between 10 and 160μg/ml. The cytostatic effects were estimated by reduction of the tetrazolium dye MTT. In the melanoma cells, some of the compounds inhibited growth after exposure for 1 day. In contrast, coumarin inhibited growth to a smaller extent, and only after exposure for 3 days. The most active compounds (3-acetoxycoumarin, 4-methoxycoumarin and 6-hydroxycoumarin), as well as coumarin, were also assayed in murine fibroblasts. The cytostatic effects of 4-methoxycoumarin and 6-hydroxycoumarin were less pronounced in fibroblasts than in melanoma cells. Our observations suggest that these compounds may have a greater therapeutic margin.