Autor: Urban, M.; Pokorný, J.; Šidová, V.; Hodoň, J.; Gurská, S.; Lišková, B.; Hajdúch, M.; Šarek, J.
Název práce v češtině: Lupanové triterpeny se selektivní cytotoxicitou vůči nádorovým buńkám CCRF-CEM
Název práce v angličtině: Lupane Triterpenes with Selective Cytotoxicity to Leukemia Cells CCRF-CEM
Klíčová slova v češtině: triterpeny, cytotoxicita, leukemie
Klíčová slova v angličtině:triterpenes, cytotoxicity, lekuemia
Abstrakt česky: Byly připraveny triterpeny selektivnně cytotoxické vůči nádorové linii CCRF-CEM a studována jejich další biologické vlastnosti.
Abstrakt anglicky: Pentacyclic triterpenes are natural compounds from plants which have a variety of biological activities. In our research group, we mostly focus on compounds with selective cytotoxic activity on cancer cells.
One of the most cytotoxic compounds prepared earlier was 30-oxobetulinic acid (1), which, however, was too toxic to be developed into anti-cancer drug. The toxicity of 1 is likely caused by the presence of Michael acceptor in the molecule. To replace this reactive moiety, a set of 30 triterpenoids modified at the position C-30 was prepared (such as azines 2 or triazoles 3, fig. 1) and tested in vitro on 8 cancer cell lines and 2 non-cancer fibroblasts. It was found that azines 2 were selectively cytotoxic against t-lymphoblastic leukemia CCRF-CEM while triazoles 3 were inactive. Influence of the most active compounds on cell cycle and on the DNA/RNA synthesis was studied and it showed that compounds cause apoptosis in cancer cells. Synthesis, cytotoxicity, and results of the cell cycle analysis will be shown.
Jazyk v originále: anglický
Publikace abstraktu: Sborník, 140/154
Forma prezentace: Poster
Název konference: 53rd. Advances in Organic, Bioorganic, and Pharmaceutical Chemistry „Liblice 2018“
Místo konání: Lázně Bělohrad (Czech Republic)
Datum konání: November 2 – 4
Rok konání: 2018
Způsob financování: GACR 15-05620S, IGA_PrF_2018_029, IGA_LF_2018_032