Autor: Urban, M.; Hodoň, J.; Borková, L.; Pokorný, J.; Krajčovičová, S.; Lišková, B.; Soural, M.; Václavková, J.; Staňková, J.; Holub, D.; Džubák, P.; Hajdúch, M.; Šarek, J.
Název práce v češtině: Cytotoxické triterpeny a terpenické konjugáty využívané pro studium mechanizmu účinku
Název práce v angličtině: Cytotoxic triterpenes and triterpenic conjugates used for Studies of the Mechanism of Action.
Klíčová slova v češtině: triterpeny, cytotoxicita, konjugáty, mechanizmus účinku
Klíčová slova v angličtině:triterpenes, cytotoxicity, conjugates, mechanism of action
Abstrakt česky: Byly zkoumány cytotoxické triterpeny a jejich mechanizmus účinku.
Abstrakt anglicky: Introduction: Triterpenoids are secondary metabolites from plants, fungi, marine invertebrate or other organisms. They often have a variety of biological activities. Betulinic acid, for example, has a strong anti-cancer activity and its hemiesters inhibit maturation of HIV.
Results: In this work, a number of new semisynthetic triterpenoids of various skeletons (such as lupane, oleanane, ursane, taraxastane etc.) were prepared. Their in vitro cytotoxic activity was measured and it was found that the best structures belong to the analogues of lupane with an electronegative substituent at the position C-2 or with a heterocycle condensed to the A-ring. Pharmacological parameters and the influence of the best compounds on cell cycle and on the DNA/RNA synthesis was then studied. The most interesting compounds were then equipped with biotin5 to identify the potential target proteins using pull-down assays and also with a fluorescent label to visualize them in cells. New methodologies for the synthesis of such probes was developed using solid-phase approach.
Conclusion: It was found that the studied compounds easily penetrate to the cells and enter some of the sub-cellular structures. Potential protein targets were found for several active heterocycles. Basic assumptions about SAR, possible pharmacophores and targets will be discussed.
Jazyk v originále: Anglický
Publikace abstraktu: Sborník 20/41
Forma prezentace: Plenární přednáška
Název konference: XIV. Diagnostic, Predictive and Experimental Oncology Days
Místo konání: Olomouc (Czech Republic)
Datum konání: November 19 – 21
Rok konání: 2018
Způsob financování: N/A