Autor: Sarek, J.; Kvasnica, M.; Vlk, M.; Biedermann, D.;
Název práce v češtině: Pentacyclické triterpeny – potenciální léčiva proti rakovině
Název práce v angličtině: Pentacyclic Triterpenes as Promising Agents in Cancer

Klíčová slova v angličtině: triterpenes; cytotoxicity; derivatives

Abstrakt anglicky: Lupane compounds occupy an unique position among cytotoxic triterpenoids. In 1976, the cytotoxiceffect of the extract of Vauquelinia corymbosa against the lymphocytic leukemia cell line P-388 hadalready been described. Betulinic acid was subsequently recognized as an active component of thisextract. A few years later, its cytotoxic activity (IC50 value of approximately 0.5-1.5 _g/mL) on thehuman melanoma cell line MEL-1 was reported. Since then, interest in this acid and its derivatives hasbeen growing, especially within the pharmaceutical industry.Several years after the publication of the article by Pisha, a new work was published on a groupof semisynthetic derivatives of betulin and betulinic acid called betulinines, with significant anticancereffects against a range of tumor cell lines of different histogenetic origin, including multidrug resistantcell types. 3_,28-Diacetoxy-18-oxo-19,20,21,29,30-pentanorlupan-22-oic acid (also known as JS8) hasbecome the most important compound of this group with an IC50 value lower than 0.5 _mol/L. Thisacid induces fast and selective apoptosis of tumor cells, which is comparable to the effect observedwith the conventional anticancer drug paclitaxel. On the basis of further studies, it was found that anew mechanism operates in the effects of JS8, whereas its primary target is located at the mitochondria.In the following years, a lot of core functionalized and derived lupane compounds have beensynthesized and tested against various cancer cell lines. For the modification of the lupane skeleton,positions 1, 2, 18, 19, 20, 21, 22, 29, 30 were mostly used, while derivatization was made mostly atpositions 3 (hydroxyl group) and 28 (carboxylic group). Besides the most abundant lupane triterpenesbetulinic acid and betulin, ot
Jazyk v originále: angličtina

Typ publikace: kapitola v knize
Kód ISBN nebo ISMN: 978-1-60876-973–5
Název nakladatele: Nova Publishers (USA)

Způsob financování: A/CZ 0046/1/0022 of FM EEA NORSKA, Grant Nadace pro výzkum rakoviny