title: Cytotoxicity and fluorescence visualization of ergot alkaloids in human cell lines.
abstract: The ergot alkaloids as secondary metabolites from fungi of the genus  Claviceps  are the focus of many investigations because of their pharmacological and toxicological properties. The main effects of ergot alkaloids are referred to an interaction with several receptor systems in the human body. It is well-known that ergot alkaloids are able to isomerize with one isomer being biologically active and one being only weakly active, whereas the activity is restricted to receptor interactions. Latest investigations have proven that ergot alkaloids also show cytotoxic effects and induce apoptosis in human primary cells. These effects seem to correlate with accumulation properties. It was the aim of our current study to determine such effects in cancer cell lines, because ergot derivatives are also used in tumor therapy. Our results confirm the apoptotic effects in two cancer cell lines (HepG2 and HT-29) in a high range, and accumulation measurements show an interesting correlation between the alkaloid concentration in the cell lysate of the receptor-inactive isomers and cytotoxicity. In addition, the strong accumulative effects were first visualized by fluorescence microscopy by taking advantage of the natural fluorescence properties of ergot alkaloids.
authors.affiliation: Northrhine Westphalia (NRW) Graduate School of Chemistry, Westfälische Wilhelms-Universität Münster, Wilhelm-Klemm-Strasse 10, 48149 Münster, Germany.
authors.forename: Dennis
authors.initials: D
authors.lastname: Mulac
authors.forename: Silke
authors.initials: S
authors.lastname: Lepski
authors.forename: Franziska
authors.initials: F
authors.lastname: Ebert
authors.forename: Tanja
authors.initials: T
authors.lastname: Schwerdtle
authors.forename: Hans-Ulrich
authors.initials: HU
authors.lastname: Humpf
mesh_terms: D000970:Antineoplastic Agents / Q000378:metabolism / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001692:Biological Transport; D002277:Carcinoma / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D002470:Cell Survival / Q000187:drug effects; D004876:Ergot Alkaloids / Q000378:metabolism / Q000494:pharmacology*; D019073:HT29 Cells; D056945:Hep G2 Cells; D006801:Humans; D008856:Microscopy, Fluorescence
chemical_list: D000970:Antineoplastic Agents; D004876:Ergot Alkaloids