Cytotoxic effects of hyperatomarin, a prenylated phloroglucinol from Hypericum annulatum Moris subsp. annulatum, in a panel of malignant cell lines.
The cytotoxic effects of hyperatomarin - a prenylated phloroglucinol isolated from Hypericum annulatum Moris subsp. annulatum were assessed in a broad spectrum of tumor cell lines originating from leukemias, lymphomas and solid malignancies. The tested compound exerted strong concentration-dependent cytotoxic effects (IC50 values ranging 0.14-15.7 μM), comparable to and even outclassing in some cell lines those of the established anti-cancer drug daunorubicin. Exposure of different human tumor cell lines to hyperatomarin resulted in strong mono- and oligo-nucleosomal fragmentation of genomic DNA, as evidenced by 'Cell death detection' ELISA kit and by DNA-electrophoresis, which unambiguously indicates that the induction of apoptosis is implicated in the cytotoxic mode of action of the tested compound.
Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University-Sofia, Sofia, Bulgaria. gmomekov@gmail.com
G
G
Momekov
D
D
Ferdinandov
D
D
Zheleva-Dimitrova
P
P
Nedialkov
U
U
Girreser
G
G
Kitanov
D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D053938:DNA Fragmentation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020902:Hypericum / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D007938:Leukemia / Q000188:drug therapy / Q000473:pathology; D008223:Lymphoma / Q000188:drug therapy / Q000473:pathology; D010696:Phloroglucinol / Q000031:analogs & derivatives* / Q000494:pharmacology
D000972:Antineoplastic Agents, Phytogenic; C481745:hyperatomarin; D010696:Phloroglucinol