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Cytotoxic activities of Amaryllidaceae alkaloids against gastrointestinal cancer cells
Authors: Doskočil Ivo | Hošťálková Anna | Šafratová Marcela | Benešová Nina | Havlík Jaroslav | Havelek Radim | Kuneš Jiří | Královec Karel | Chlebek Jakub | Cahlíková Lucie
Year: 2015
Type of publication: článek v odborném periodiku
Name of source: Phytochemistry Letters
Publisher name: Elsevier Science BV
Place: Amsterdam
Page from-to: 394-398
Titles:
Language Name Abstract Keywords
cze Cytotoxická aktivita alkaloidů Amaryllidaceae vůči gastrointestinálním nádorovým buňkám Tato práce popisuje cytotoxicitu třinácti alkaloidů Amaryllidaceae vůči gastrointestinálním nádorovým buňkám s mutovaným proteinem p53. Amaryllidaceae; Haemanthamin; Cytotoxicita; Caco-2; HT-29; FHs 74 Int
eng Cytotoxic activities of Amaryllidaceae alkaloids against gastrointestinal cancer cells The treatment of many diseases is highly dependent on natural products and natural products can also be used as design templates for future anticancer drugs. Thirteen Amaryllidaceae alkaloids possessing alpha-crinane, beta-crinane, galantamine, lycorine and tazettine-type skeleton have been isolated in our laboratory, and their cytotoxicity against p53-mutated gastrointestinal cancer cells were evaluated. At the same time, healthy small intestine cells were used to determine overall toxicity against noncancerous cells. In this study, we demonstrated that haemanthamine, haemanthidine and lycorine showed strong cytotoxicity against p53-mutated Caco-2 and HT-29 colorectal adenocarcinoma cells as quantified in terms of IC50 values. We for the first time observed approximately 20 times higher IC(50)values against normal intestine epithelial cells FHs-74 Int after haemanthamine and lycorine treatment when compared with Caco-2 and HT-29 cancer cells. In conclusion, our data indicate that alpha-C2 bridged haemanthamine may be perspective anticancer drug candidate for further semisynthetic modification and structure-activity relationship study. Amaryllidaceae; Haemanthamine; Cytotoxicity; Caco-2; HT-29; FHs 74 Int

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