Abstract

3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors, were originally designed to reduce cholesterol biosynthesis and have been extensively used as prevention drugs against hyperlipidemia and cardiovascular conditions. Recently, these compounds have been shown to display chemopreventive activity against cancer. However, the effects of statins on cancer are not completely understood. For this reason, we have studied the cytotoxic effect of rosuvastatin and fluvastatin on three cell tumoral lines: human larynx carcinoma (HEp-2), human nasopharyngeal carcinoma (KB), and human epithelial carcinoma (HeLa). We have found that only fluvastatin has relevant activity against the tumoral cell lines assayed and the capacity to arrest G₁-phase, whereas a significant decline was observed in the S-phase percentage. Fluvastatin IC₅₀ were 2.43±0.56 g/mL (HEp-2), 2.29±0.19 g/mL (KB), and 5.02±1.52 g/mL (HeLa), whereas rosuvastatin showed poor activity. These results indicate that the cytotoxic effect of fluvastatin may not depend directly on HMG-CoA reductase inhibition. The antitumor statins effect needs further investigation.

Key words: Cell cycle, cytotoxicity, statins.