Cyclamen Trochopteranthum: Cytotoxic activity and possible adverse interactions including drugs and carcinogens.

Abstract

OBJECTIVE: To examine the effect of water extracts of cyclamen tubers on the expression of main cytochrome P450 (CYP450s) including CYP1A1, CYP1A2 CYP2E1, CYP2B6, CYP2C9 and CYP3A4 that participate in the metabolism of both drugs and carcinogens and cytotoxic activity in human cancer cell lines, namely HepG2 and Caco-2. METHODS: Cyclamen trochopteranthum tubers were extracted with dH(2)O and then lyophilized under vacuum. Infrared spectral study was made for extracts by Fourier transform infrared spectroscopy (FT-IR). Cytotoxic activity of cyclamen was determined by crystal violet staining in HepG2 and Caco-2 cells. CYP expression was determined by reverse transcription polymerase chain reaction (RT-PCR). RESULTS: Cyclamen water extract had moderate cytotoxic activity. It was found that lethal concentration (LC50) value of the cyclamen extract was 50 and 125 ?g/mL in HepG2 and Caco-2 cell lines, respectively. Moreover, it caused induction and suppression of CYP450s mRNA levels in HepG2 and Caco-2 cells. CONCLUSION: Cyclamen may have a potential not only inhibition and/or induction of the metabolism of certain co-administered drugs but also development of toxicity, mutagenesis and malignant transformation due to induction or suppression of the CYP450s dependent drug metabolizing enzymes.